Page last updated: 2024-08-02 14:51:14
bibw 2992
Description
afatinib : A quinazoline compound having a 3-chloro-4-fluoroanilino group at the 4-position, a 4-dimethylamino-trans-but-2-enamido group at the 6-position, and an (S)-tetrahydrofuran-3-yloxy group at the 7-position. Used (as its dimaleate salt) for the first-line treatment of patients with metastatic non-small cell lung cancer. [CHeBI]
Cross-References
Synonyms (99)
| Synonym |
|---|
| tovok |
| afatinib , |
| bibw-2992 |
| tomtovok |
| 439081-18-2 |
| afatinibum |
| (2e)-n-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3s)-tetrahydrofuran-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide |
| 850140-72-6 |
| bdbm50322823 |
| (s)-n-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| bibw 2992 |
| bibw2992 |
| chebi:61390 , |
| nsc-750691 |
| CHEMBL1173655 , |
| nsc750691 |
| S1011 , |
| NCGC00185000-01 |
| EX-8656 |
| 2-butenamide, n-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3s)-tetrahydro-3-furanyl)oxy)- 6-quinazolinyl)-4-(dimethylamino)-, (2e)- |
| (2e)-n-(4-(3-chloro-4-fluoroanilino)-7-(((3s)-oxolan-3-yl)oxy)quinoxazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| D09724 |
| afatinib (usan/inn) |
| BCP9000407 |
| A15572 |
| (s,e)-n-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| 2-butenamide, n-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3s)-tetrahydro-3-furanyl)oxy)-6-quinazolinyl)-4-(dimethylamino)-, (2e)- |
| 41ud74l59m , |
| unii-41ud74l59m |
| afatinib [usan:inn] |
| (s,e)-n-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| (s)-n-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| (2e)-n-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3s)-oxolan-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide |
| BCPP000338 |
| bibw2992,afatinib |
| afatinib [mart.] |
| afatinib [vandf] |
| afatinib [mi] |
| afatinib [inn] |
| afatinib [usan] |
| afatinib [who-dd] |
| (r,e)-n-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| AKOS015850681 |
| AKOS015904219 |
| c24h25clfn5o3 |
| (2e)-n-(4-((3-chloro-4-fluorophenyl)amino)-7-(((3s)-tetrahydro-3-furanyl)oxy)-6-quinazolinyl)-4-(dimethylamino)-2-butenamide |
| gtpl5667 |
| BRD-K66175015-001-01-7 |
| DB08916 |
| smr004701084 |
| MLS006010000 |
| 2-butenamide, n-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3s)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2e)- |
| AM808098 |
| (e)-n-[4-(3-chloro-4-fluoro-anilino)-7-[(3s)-tetrahydrofuran-3-yl]oxy-quinazolin-6-yl]-4-(dimethylamino)but-2-enamide |
| J-502300 |
| J-500781 |
| ULXXDDBFHOBEHA-CWDCEQMOSA-N |
| (e)-4-dimethylamino-but-2-enoic acid-(4-(3-chloro-4-fluoro-phenylamino)-7-((s)-tetrahydrofuran-3-yloxy)-quinazolin-6yl)-amide |
| (e)-4-dimethylamino-but-2-enoic acid-[4-(3-chloro-4-fluoro-phenylamino)-7-((s)-tetrahydrofuran-3-yloxy)-quinazolin-6-yl]-amide |
| (e)-4-dimethylamino-but-2-enoic acid-(4-(3-chloro-4-fluoro-phenylamino)-7-((s)-tetrahydrofuran-3-yloxy)-quinazolin-6-yl)-amide |
| afatinib (bibw2992) , |
| AKOS025149636 |
| AC-27018 |
| AC-26079 |
| AB01565886_02 |
| (e)-n-[4-(3-chloro-4-fluoroanilino)-7-[(3s)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide |
| EX-A065 |
| sr-01000941576 |
| SR-01000941576-1 |
| CHEBI:94698 |
| SW219248-1 |
| DTXSID20893451 , |
| Q4688818 |
| (s,e)-n-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide. |
| 850140-72-6 (free base) |
| afatinib free base |
| mfcd12407405 |
| DS-14172 |
| afatinib, free base |
| afatinib(cis-trans isomerismtautomers) |
| BCP01779 |
| CCG-264776 |
| bibw2992 (tovok) |
| nsc799327 |
| nsc-799327 |
| EN300-6487482 |
| afatinib- bio-x |
| BA164141 |
| AS-80916 |
| CS-0020030 |
| (e/z)-afatinib |
| (2e)-n-(4-((3-chloro-4-fluorophenyl)amino)-7-((3s)-tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide |
| l01xe13 |
| afatinib (mart.) |
| dtxcid301323466 |
| EN300-19625328 |
| n-{4-[(3-chloro-4-fluorophenyl)amino]-7-[(3s)-oxolan-3-yloxy]quinazolin-6-yl}-4-(dimethylamino)but-2-enamide |
| HY-10261B |
| Z2568727518 |
Roles (2)
Drug Classes (8)
| Class | Description |
|---|
| quinazolines | Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. |
| furans | Compounds containing at least one furan ring. |
| organofluorine compound | An organofluorine compound is a compound containing at least one carbon-fluorine bond. |
| enamide | An alpha,beta-unsaturated carboxylic acid amide of general formula R(1)R(2)C=CR(3)-C(=O)NR(4)R(5) in which the amide C=O function is conjugated to a C=C double bond at the alpha,beta position. |
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
| monochlorobenzenes | Any member of the class of chlorobenzenes containing a mono- or poly-substituted benzene ring in which only one substituent is chlorine. |
| secondary carboxamide | A carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1). |
Pathways (6)
bibw 2992 is involved in 6 pathway(s), involving a total of 1567 unique proteins and 280 unique compounds
Protein Targets (485)
Potency Measurements
Inhibition Measurements
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|
| Leukotriene C4 synthase | Cavia porcellus (domestic guinea pig) | Kd | 10.0000 | AID625128 |
| Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 20.0000 | AID1424922; AID624825 |
| Membrane-associated progesterone receptor component 1 | Homo sapiens (human) | Kd | 30.0000 | AID1425109 |
| Cell division cycle 7-related protein kinase | Homo sapiens (human) | Kd | 30.0000 | AID1424936 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Homo sapiens (human) | Kd | 10.0000 | AID624974 |
| Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 20.0000 | AID1425121; AID625076 |
| Serine/threonine-protein kinase 25 | Homo sapiens (human) | Kd | 10.0000 | AID625059 |
| ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | AID1424975 |
| Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta | Homo sapiens (human) | Kd | 10.0000 | AID624877 |
| Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | AID1425106 |
| Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 16.4500 | AID1424954; AID625065 |
| Serine/threonine-protein kinase RIO3 | Homo sapiens (human) | Kd | 10.0000 | AID624926 |
| Dual specificity mitogen-activated protein kinase kinase 7 | Homo sapiens (human) | Kd | 10.0000 | AID624722 |
| Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 20.0000 | AID1424953; AID624831 |
| Inhibitor of nuclear factor kappa-B kinase subunit beta | Homo sapiens (human) | Kd | 10.0000 | AID624836 |
| Peripheral plasma membrane protein CASK | Homo sapiens (human) | Kd | 10.0000 | AID624749 |
| Aurora kinase A | Homo sapiens (human) | Kd | 20.0000 | AID1424917; AID624919 |
| Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 0.6430 | AID1425009; AID1595619; AID625012 |
| Serine/threonine-protein kinase DCLK1 | Homo sapiens (human) | Kd | 10.0000 | AID624966 |
| Inhibitor of nuclear factor kappa-B kinase subunit alpha | Homo sapiens (human) | Kd | 10.0000 | AID624832 |
| Muscle, skeletal receptor tyrosine-protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID625022 |
| Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 16.5500 | AID1424995; AID624957 |
| Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | AID1424896 |
| Mitogen-activated protein kinase 13 | Homo sapiens (human) | Kd | 10.0000 | AID624892 |
| 3-phosphoinositide-dependent protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID624876 |
| Mitogen-activated protein kinase kinase kinase 13 | Homo sapiens (human) | Kd | 10.0000 | AID624965 |
| Death-associated protein kinase 3 | Homo sapiens (human) | Kd | 10.0000 | AID624834 |
| Mitogen-activated protein kinase kinase kinase 7 | Homo sapiens (human) | Kd | 10.0000 | AID624724 |
| Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 16.3500 | AID1425155; AID624925 |
| Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | AID1424926 |
| NUAK family SNF1-like kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID625088 |
| Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1425097 |
| Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma | Homo sapiens (human) | Kd | 10.0000 | AID624751 |
| Tyrosine-protein kinase JAK2 | Homo sapiens (human) | Kd | 20.0000 | AID1425031; AID624973 |
| Rho-associated protein kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425158; AID624969 |
| Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 20.0000 | AID1425208; AID624916 |
| Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 20.0000 | AID1424997; AID624835 |
| Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 16.6667 | AID1425162; AID624736; AID624967 |
| U5 small nuclear ribonucleoprotein 200 kDa helicase | Homo sapiens (human) | Kd | 30.0000 | AID1425174 |
| Ribosomal protein S6 kinase alpha-4 | Homo sapiens (human) | Kd | 16.6667 | AID1425161; AID624806; AID624927 |
| Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 20.0000 | AID1425179; AID624775 |
| Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit gamma | Homo sapiens (human) | Kd | 10.0000 | AID624958 |
| Serine/threonine-protein kinase PAK 3 | Homo sapiens (human) | Kd | 10.0000 | AID624873 |
| Cyclin-dependent kinase-like 5 | Homo sapiens (human) | Kd | 10.0000 | AID624905 |
| Serine/threonine-protein kinase 17B | Homo sapiens (human) | Kd | 10.0000 | AID624942 |
| Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 17.1500 | AID1425177; AID625030 |
| Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 20.0000 | AID1425137; AID625024 |
| Cyclin-dependent kinase 14 | Homo sapiens (human) | Kd | 10.0000 | AID625070 |
| Structural maintenance of chromosomes protein 2 | Homo sapiens (human) | Kd | 30.0000 | AID1425173 |
| Mitogen-activated protein kinase kinase kinase 6 | Homo sapiens (human) | Kd | 20.0000 | AID1425050; AID624962 |
| Serine/threonine-protein kinase OSR1 | Homo sapiens (human) | Kd | 10.0000 | AID624977 |
| Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 20.0000 | AID1425054; AID624756 |
| Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 20.0000 | AID1425033; AID624963 |
| Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 23.3333 | AID1425100; AID624811 |
| Serine/threonine-protein kinase Chk2 | Homo sapiens (human) | Kd | 10.0000 | AID624803 |
| Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 2.7762 | AID1424890; AID624978; AID624979; AID624980; AID624981; AID624982; AID624983; AID624984; AID624985; AID624986; AID624987; AID624988; AID624989; AID624990; AID624991; AID624992 |
| Epidermal growth factor receptor | Homo sapiens (human) | EC50 | 0.0216 | AID1807693; AID1807694; AID1880122; AID1880123 |
| Epidermal growth factor receptor | Homo sapiens (human) | Kd | 0.0004 | AID1424983; AID1595618; AID624996; AID624997; AID624998; AID624999; AID625000; AID625001; AID625002; AID625003; AID625004; AID625005; AID625006; AID625007 |
| RAF proto-oncogene serine/threonine-protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624897 |
| Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | EC50 | 0.0030 | AID1880133 |
| Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | Kd | 0.0050 | AID624804 |
| High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 20.0000 | AID1425094; AID624808 |
| Guanine nucleotide-binding protein G(i) subunit alpha-2 | Homo sapiens (human) | Kd | 30.0000 | AID1425011 |
| ADP/ATP translocase 2 | Homo sapiens (human) | Kd | 30.0000 | AID1425169 |
| Protein kinase C beta type | Homo sapiens (human) | Kd | 30.0000 | AID1425130 |
| Insulin receptor | Homo sapiens (human) | Kd | 23.3333 | AID1425026; AID624784 |
| Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 15.2850 | AID1425034; AID625013 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 20.0000 | AID1425008; AID624727 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424937 |
| Glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 30.0000 | AID1425146 |
| Tyrosine-protein kinase Fes/Fps | Homo sapiens (human) | Kd | 20.0000 | AID1425003; AID624852 |
| Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) | Kd | 10.0000 | AID624995 |
| Adenine phosphoribosyltransferase | Homo sapiens (human) | Kd | 30.0000 | AID1424914 |
| Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 20.0000 | AID1425212; AID625018 |
| Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 20.0000 | AID1425037; AID624862 |
| Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 14.0000 | AID1425154; AID625121; AID625122; AID625123; AID625124 |
| Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 20.0000 | AID1425022; AID624800 |
| Signal recognition particle receptor subunit alpha | Homo sapiens (human) | Kd | 30.0000 | AID1425176 |
| Cytochrome c1, heme protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1424969 |
| Hepatocyte growth factor receptor | Homo sapiens (human) | Kd | 2.7393 | AID1425076; AID624794; AID624795; AID624796 |
| Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 16.1000 | AID1425017; AID624857 |
| Proto-oncogene tyrosine-protein kinase ROS | Homo sapiens (human) | Kd | 10.0000 | AID624899 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 20.0000 | AID1425104; AID624875 |
| Tyrosine-protein kinase Fgr | Homo sapiens (human) | Kd | 20.0000 | AID1425005; AID625011 |
| Wee1-like protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID624746 |
| Uncharacterized serine/threonine-protein kinase SBK3 | Homo sapiens (human) | Kd | 10.0000 | AID624747 |
| Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | AID1424915 |
| Mast/stem cell growth factor receptor Kit | Homo sapiens (human) | Kd | 10.0000 | AID624786; AID624787; AID624788; AID624789; AID624790; AID624791; AID624792; AID624793 |
| Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | AID1425145 |
| Breakpoint cluster region protein | Homo sapiens (human) | Kd | 30.0000 | AID1424919 |
| Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Kd | 20.0000 | AID1425111; AID624878 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425004; AID625132 |
| DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | AID1425202 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 16.6667 | AID1424946; AID624780; AID624781 |
| ADP/ATP translocase 3 | Homo sapiens (human) | Kd | 30.0000 | AID1425170 |
| Inosine-5'-monophosphate dehydrogenase 2 | Homo sapiens (human) | Kd | 30.0000 | AID1425025 |
| Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | Kd | 16.4000 | AID1425175; AID625016 |
| cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | AID1425128 |
| Insulin receptor-related protein | Homo sapiens (human) | Kd | 10.0000 | AID625075 |
| Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 16.6667 | AID1424924; AID624946; AID624947 |
| Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 1.9270 | AID1425110; AID624797 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 30.0000 | AID1425093 |
| Platelet-derived growth factor receptor alpha | Homo sapiens (human) | Kd | 10.0000 | AID625034 |
| Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 20.0000 | AID1425002; AID625010 |
| Protein kinase C alpha type | Homo sapiens (human) | Kd | 30.0000 | AID1425129 |
| cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 20.0000 | AID1425123; AID624881 |
| Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | Kd | 10.0000 | AID624853 |
| General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | AID1424996 |
| Interferon-induced, double-stranded RNA-activated protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624896 |
| Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 20.0000 | AID1424968; AID624849 |
| Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | AID1425150 |
| Serine/threonine-protein kinase MAK | Homo sapiens (human) | Kd | 10.0000 | AID625025 |
| Cyclin-dependent kinase 11B | Homo sapiens (human) | Kd | 10.0000 | AID624708 |
| Ephrin type-A receptor 1 | Homo sapiens (human) | Kd | 10.0000 | AID625008 |
| Fibroblast growth factor receptor 2 | Homo sapiens (human) | Kd | 10.0000 | AID625131 |
| Receptor tyrosine-protein kinase erbB-3 | Homo sapiens (human) | Kd | 4.5000 | AID624851 |
| Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | AID1425098 |
| Fibroblast growth factor receptor 4 | Homo sapiens (human) | Kd | 10.0000 | AID625130 |
| Fibroblast growth factor receptor 3 | Homo sapiens (human) | Kd | 10.0000 | AID624782; AID624783 |
| cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | Kd | 30.0000 | AID1425125 |
| cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | Kd | 20.0000 | AID1425124; AID624882 |
| Ferrochelatase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1425001 |
| Ribosomal protein S6 kinase beta-1 | Homo sapiens (human) | Kd | 20.0000 | AID1425164; AID624906 |
| Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 16.6667 | AID1425030; AID624858; AID624859 |
| Protein kinase C eta type | Homo sapiens (human) | Kd | 10.0000 | AID625049 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1424944; AID624844 |
| Beta-adrenergic receptor kinase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424908 |
| Probable ATP-dependent RNA helicase DDX6 | Homo sapiens (human) | Kd | 30.0000 | AID1424977 |
| Activin receptor type-2A | Homo sapiens (human) | Kd | 10.0000 | AID624838 |
| Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425061; AID624885 |
| MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425069; AID624863 |
| Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | AID1424970 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425056; AID624713 |
| Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 23.3333 | AID1424988; AID624951 |
| Ephrin type-A receptor 3 | Homo sapiens (human) | Kd | 10.0000 | AID625009 |
| Ephrin type-A receptor 8 | Homo sapiens (human) | Kd | 10.0000 | AID625120 |
| Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 20.0000 | AID1424992; AID625105 |
| Leukocyte tyrosine kinase receptor | Homo sapiens (human) | Kd | 10.0000 | AID624743 |
| Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 16.6667 | AID1425207; AID624912; AID624913 |
| Phosphatidylethanolamine-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | AID1425107 |
| Wee1-like protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1425210; AID624914 |
| Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | AID1425018 |
| Tyrosine-protein kinase receptor UFO | Homo sapiens (human) | Kd | 5.3000 | AID624840 |
| Mitogen-activated protein kinase 4 | Homo sapiens (human) | Kd | 10.0000 | AID624886 |
| S-adenosylmethionine synthase isoform type-2 | Homo sapiens (human) | Kd | 30.0000 | AID1425071 |
| DnaJ homolog subfamily A member 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424980 |
| RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1424910; AID624994 |
| RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1424911; AID624839 |
| G protein-coupled receptor kinase 4 | Homo sapiens (human) | Kd | 10.0000 | AID624739 |
| Dual specificity protein kinase TTK | Homo sapiens (human) | Kd | 20.0000 | AID1425205; AID624910 |
| DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | AID1425072 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | Kd | 10.0000 | AID625141 |
| Myosin-10 | Homo sapiens (human) | Kd | 30.0000 | AID1425079 |
| Tyrosine-protein kinase receptor Tie-1 | Homo sapiens (human) | Kd | 10.0000 | AID625017 |
| Vascular endothelial growth factor receptor 3 | Homo sapiens (human) | Kd | 10.0000 | AID624854 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | Kd | 10.0000 | AID624860 |
| Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425039; AID625137 |
| Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 9.9250 | AID1425006; AID624934; AID624935; AID624936; AID624937; AID624938; AID624939; AID624940 |
| Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 20.0000 | AID1424921; AID624945 |
| Activin receptor type-1B | Homo sapiens (human) | Kd | 20.0000 | AID1424901; AID624943 |
| TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 20.0000 | AID1425196; AID624961 |
| Serine/threonine-protein kinase receptor R3 | Homo sapiens (human) | Kd | 10.0000 | AID624778 |
| TGF-beta receptor type-2 | Homo sapiens (human) | Kd | 20.0000 | AID1425197; AID624909 |
| Electron transfer flavoprotein subunit beta | Homo sapiens (human) | Kd | 30.0000 | AID1424999 |
| Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 20.0000 | AID1424960; AID624948 |
| Glycine--tRNA ligase | Homo sapiens (human) | Kd | 30.0000 | AID1425010 |
| Protein kinase C iota type | Homo sapiens (human) | Kd | 20.0000 | AID1425133; AID624883 |
| Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | AID1425168 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Homo sapiens (human) | Kd | 10.0000 | AID625036; AID625037; AID625038; AID625039; AID625040; AID625041; AID625042; AID625043; AID625044; AID625045 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | Homo sapiens (human) | Kd | 10.0000 | AID625046 |
| Serine/threonine-protein kinase mTOR | Homo sapiens (human) | Kd | 10.0000 | AID624972 |
| Megakaryocyte-associated tyrosine-protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624864 |
| Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 20.0000 | AID1425193; AID624908 |
| Tyrosine-protein kinase TXK | Homo sapiens (human) | Kd | 3.1000 | AID624911 |
| Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 20.0000 | AID1424891; AID624993 |
| Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 15.7000 | AID1425007; AID624855 |
| Tyrosine-protein kinase ZAP-70 | Homo sapiens (human) | Kd | 10.0000 | AID624744 |
| Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 20.0000 | AID1425188; AID624907 |
| 26S proteasome regulatory subunit 6B | Homo sapiens (human) | Kd | 30.0000 | AID1425141 |
| Mitogen-activated protein kinase 8 | Homo sapiens (human) | Kd | 20.0000 | AID1425063; AID624889 |
| Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 2.3215 | AID1425064; AID624717 |
| Dual specificity mitogen-activated protein kinase kinase 4 | Homo sapiens (human) | Kd | 10.0000 | AID624902 |
| Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425040; AID624894 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Homo sapiens (human) | Kd | 30.0000 | AID1425113 |
| Casein kinase I isoform alpha | Homo sapiens (human) | Kd | 20.0000 | AID1424961; AID624846 |
| Casein kinase I isoform delta | Homo sapiens (human) | Kd | 20.0000 | AID1424962; AID624716 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Homo sapiens (human) | Kd | 10.0000 | AID624879 |
| MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 5.4085 | AID1425065; AID624703 |
| Cyclin-dependent kinase 8 | Homo sapiens (human) | Kd | 10.0000 | AID624829 |
| Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1425206 |
| Choline-phosphate cytidylyltransferase A | Homo sapiens (human) | Kd | 30.0000 | AID1425103 |
| Cysteine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | AID1424932 |
| Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 15.6500 | AID1424963; AID624847 |
| Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1424894 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 20.0000 | AID1424955; AID624764 |
| Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 20.0000 | AID1424956; AID624932 |
| Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 20.0000 | AID1424957; AID624931 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 20.0000 | AID1425013; AID625114 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 20.0000 | AID1425014; AID624856 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 20.0000 | AID1424949; AID624845 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 20.0000 | AID1424950; AID624830 |
| Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | AID1425149 |
| Tyrosine-protein kinase Blk | Homo sapiens (human) | Kd | 0.2200 | AID624841 |
| Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 15.1200 | AID1425027; AID624837 |
| Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 20.0000 | AID1425160; AID624960 |
| Cytoplasmic tyrosine-protein kinase BMX | Homo sapiens (human) | Kd | 10.0000 | AID624842 |
| cAMP-dependent protein kinase catalytic subunit PRKX | Homo sapiens (human) | Kd | 10.0000 | AID624976 |
| Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 20.0000 | AID1425086; AID624869 |
| Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 20.0000 | AID1425087; AID624870 |
| Serine/threonine-protein kinase Nek4 | Homo sapiens (human) | Kd | 10.0000 | AID624904 |
| Tyrosine-protein kinase JAK3 | Homo sapiens (human) | Kd | 10.0000 | AID624785 |
| Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 20.0000 | AID1425043; AID624895 |
| Serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Kd | 20.0000 | AID1425120; AID624975 |
| Death-associated protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID624971 |
| LIM domain kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425035; AID624861 |
| LIM domain kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425036; AID625021 |
| Mitogen-activated protein kinase 12 | Homo sapiens (human) | Kd | 10.0000 | AID624766 |
| Mitogen-activated protein kinase 10 | Homo sapiens (human) | Kd | 16.0000 | AID1425057; AID624891 |
| Tyrosine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | AID1425211 |
| 5'-AMP-activated protein kinase subunit gamma-1 | Homo sapiens (human) | Kd | 30.0000 | AID1425126 |
| 5'-AMP-activated protein kinase catalytic subunit alpha-2 | Homo sapiens (human) | Kd | 10.0000 | AID625047 |
| Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 20.0000 | AID1424993; AID624955 |
| Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 20.0000 | AID1424990; AID624737 |
| Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 20.0000 | AID1424994; AID624956 |
| Ephrin type-B receptor 1 | Homo sapiens (human) | Kd | 10.0000 | AID624954 |
| Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 20.0000 | AID1424989; AID624952 |
| Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | AID1424909 |
| Adenosine kinase | Homo sapiens (human) | Kd | 3.4930 | AID1424907 |
| Hormonally up-regulated neu tumor-associated kinase | Homo sapiens (human) | Kd | 10.0000 | AID625084 |
| Serine/threonine-protein kinase SIK1 | Homo sapiens (human) | Kd | 10.0000 | AID624733 |
| Receptor-interacting serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 10.0000 | AID624763 |
| Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | AID1425148 |
| Cell division control protein 2 homolog | Plasmodium falciparum 3D7 | Kd | 10.0000 | AID624760 |
| Actin-related protein 3 | Homo sapiens (human) | Kd | 30.0000 | AID1424899 |
| Actin-related protein 2 | Homo sapiens (human) | Kd | 30.0000 | AID1424898 |
| Calcium-dependent protein kinase 1 | Plasmodium falciparum 3D7 | Kd | 10.0000 | AID624759 |
| GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | AID1425153 |
| Casein kinase II subunit alpha | Homo sapiens (human) | Kd | 10.0000 | AID624848 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 beta | Homo sapiens (human) | Kd | 10.0000 | AID624915 |
| SRSF protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID624768 |
| Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 20.0000 | AID1424965; AID624833 |
| Mitogen-activated protein kinase kinase kinase 9 | Homo sapiens (human) | Kd | 10.0000 | AID624706 |
| Serine/threonine-protein kinase PknB | Mycobacterium tuberculosis H37Rv | Kd | 10.0000 | AID624753 |
| Cyclin-dependent kinase 3 | Homo sapiens (human) | Kd | 23.3333 | AID1424945; AID624828 |
| Cyclin-dependent kinase-like 1 | Homo sapiens (human) | Kd | 10.0000 | AID624941 |
| Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 30.0000 | AID1424948 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 20.0000 | AID1424947; AID624970 |
| Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 20.0000 | AID1424941; AID625033 |
| Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 20.0000 | AID1424942; AID624776 |
| Protein kinase C epsilon type | Homo sapiens (human) | Kd | 10.0000 | AID625014 |
| Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425038; AID624893 |
| Angiopoietin-1 receptor | Homo sapiens (human) | Kd | 10.0000 | AID624799 |
| Mitogen-activated protein kinase kinase kinase 10 | Homo sapiens (human) | Kd | 10.0000 | AID624867 |
| DNA topoisomerase 2-beta | Homo sapiens (human) | Kd | 30.0000 | AID1425203 |
| Protein kinase C theta type | Homo sapiens (human) | Kd | 20.0000 | AID1425134; AID625051 |
| Activin receptor type-1 | Homo sapiens (human) | Kd | 20.0000 | AID1424900; AID624819 |
| Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 20.0000 | AID1425078; AID624868 |
| Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425142; AID624729 |
| Protein kinase C zeta type | Homo sapiens (human) | Kd | 30.0000 | AID1425135 |
| Protein kinase C delta type | Homo sapiens (human) | Kd | 20.0000 | AID1425131; AID625048 |
| Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 23.3333 | AID1424925; AID624779 |
| Tyrosine-protein kinase receptor TYRO3 | Homo sapiens (human) | Kd | 10.0000 | AID625057 |
| Cyclin-dependent kinase 18 | Homo sapiens (human) | Kd | 10.0000 | AID624874 |
| Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425201; AID624807 |
| Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 20.0000 | AID1424972; AID624850 |
| Tyrosine-protein kinase ITK/TSK | Homo sapiens (human) | Kd | 10.0000 | AID625020 |
| Myotonin-protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624950 |
| Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425052; AID624959 |
| Mitogen-activated protein kinase kinase kinase 12 | Homo sapiens (human) | Kd | 10.0000 | AID624762 |
| Tyrosine-protein kinase Mer | Homo sapiens (human) | Kd | 10.0000 | AID624767 |
| Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 20.0000 | AID1425185; AID625055 |
| 5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 20.0000 | AID1425122; AID624773 |
| Serine/threonine-protein kinase PAK 1 | Homo sapiens (human) | Kd | 10.0000 | AID624871 |
| Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 15.6500 | AID1425042; AID624721 |
| Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 20.0000 | AID1425062; AID624888 |
| Serine/threonine-protein kinase PAK 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425099; AID624872 |
| Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425182; AID625054 |
| Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425044; AID625026 |
| cGMP-dependent protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID625053 |
| Integrin-linked protein kinase | Homo sapiens (human) | Kd | 30.0000 | AID1425024 |
| Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425157; AID625015 |
| Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 20.0000 | AID1425200; AID624930 |
| Serine/threonine-protein kinase PRP4 homolog | Homo sapiens (human) | Kd | 10.0000 | AID624750 |
| Receptor-interacting serine/threonine-protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID624924 |
| Calcium/calmodulin-dependent protein kinase type II subunit beta | Homo sapiens (human) | Kd | 10.0000 | AID624827 |
| Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 20.0000 | AID1424929; AID624731 |
| Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 20.0000 | AID1424928; AID624770 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 15.4850 | AID1424981; AID624712 |
| Activin receptor type-2B | Homo sapiens (human) | Kd | 20.0000 | AID1424902; AID624820 |
| Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 20.0000 | AID1424923; AID624826 |
| Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 20.0000 | AID1425144; AID625029 |
| cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425138; AID625052 |
| Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 20.0000 | AID1424940; AID624761 |
| Calcium/calmodulin-dependent protein kinase type 1 | Homo sapiens (human) | Kd | 10.0000 | AID624922 |
| Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 20.0000 | AID1425023; AID625074 |
| Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 20.0000 | AID1425143; AID624732 |
| Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 20.0000 | AID1425074; AID625087 |
| Chromodomain-helicase-DNA-binding protein 4 | Homo sapiens (human) | Kd | 30.0000 | AID1424952 |
| Peroxisomal acyl-coenzyme A oxidase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424895 |
| Serine/threonine-protein kinase D1 | Homo sapiens (human) | Kd | 10.0000 | AID624884 |
| Serine/threonine-protein kinase 38 | Homo sapiens (human) | Kd | 10.0000 | AID625067 |
| Receptor tyrosine-protein kinase erbB-4 | Homo sapiens (human) | Kd | 0.0063 | AID624815 |
| Ribosomal protein S6 kinase alpha-2 | Homo sapiens (human) | Kd | 10.0000 | AID624805; AID625127 |
| Ephrin type-A receptor 7 | Homo sapiens (human) | Kd | 10.0000 | AID624953 |
| Delta(24)-sterol reductase | Homo sapiens (human) | Kd | 30.0000 | AID1424978 |
| Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | Kd | 16.6667 | AID1425159; AID624900; AID624901 |
| Dual specificity testis-specific protein kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425194; AID625056 |
| Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 20.7995 | AID1425081; AID624709 |
| Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 6.4055 | AID1425058; AID624890 |
| Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 20.0000 | AID1425178; AID624798 |
| Rhodopsin kinase GRK1 | Homo sapiens (human) | Kd | 10.0000 | AID624898 |
| NT-3 growth factor receptor | Homo sapiens (human) | Kd | 10.0000 | AID624765 |
| Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 20.0000 | AID1425117; AID624745 |
| Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 20.0000 | AID1425118; AID625050 |
| Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 1.1735 | AID1425059; AID624714 |
| Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 20.0000 | AID1424930; AID624843 |
| Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 20.0000 | AID1425045; AID624866 |
| BDNF/NT-3 growth factors receptor | Homo sapiens (human) | Kd | 10.0000 | AID625032 |
| MAP kinase-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | AID1425066 |
| Mitogen-activated protein kinase 6 | Homo sapiens (human) | Kd | 10.0000 | AID624887 |
| Phosphorylase b kinase gamma catalytic chain, skeletal muscle/heart isoform | Homo sapiens (human) | Kd | 1.3000 | AID625035 |
| Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 20.0000 | AID1424973; AID624777 |
| AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1424889; AID625089 |
| Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425082; AID624738 |
| Uncharacterized aarF domain-containing protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | AID1424906 |
| Serine/threonine-protein kinase SBK1 | Homo sapiens (human) | Kd | 4.8000 | AID624812 |
| Mitogen-activated protein kinase kinase kinase 19 | Homo sapiens (human) | Kd | 10.0000 | AID625136 |
| Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | AID1425019 |
| Serine/threonine-protein kinase TNNI3K | Homo sapiens (human) | Kd | 10.0000 | AID625097 |
| Rab-like protein 3 | Homo sapiens (human) | Kd | 30.0000 | AID1425151 |
| Leucine-rich repeat serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID624740; AID624741 |
| Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 20.0000 | AID1424933; AID624920 |
| Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 20.0000 | AID1424935; AID625107 |
| Acyl-CoA dehydrogenase family member 10 | Homo sapiens (human) | Kd | 30.0000 | AID1424892 |
| Serine/threonine-protein kinase Nek5 | Homo sapiens (human) | Kd | 10.0000 | AID624742 |
| Serine/threonine-protein kinase N3 | Homo sapiens (human) | Kd | 30.0000 | AID1425119 |
| Serine/threonine-protein kinase ULK3 | Homo sapiens (human) | Kd | 23.3333 | AID1425209; AID624818 |
| Dual serine/threonine and tyrosine protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624758 |
| Mitogen-activated protein kinase kinase kinase 15 | Homo sapiens (human) | Kd | 10.0000 | AID624801 |
| Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 30.0000 | AID1425147 |
| Acyl-CoA dehydrogenase family member 11 | Homo sapiens (human) | Kd | 30.0000 | AID1424893 |
| Serine/threonine-protein kinase/endoribonuclease IRE2 | Homo sapiens (human) | Kd | 30.0000 | AID1424998 |
| Serine/threonine-protein kinase MARK2 | Homo sapiens (human) | Kd | 20.0000 | AID1425068; AID625106 |
| ATP-dependent RNA helicase DHX30 | Homo sapiens (human) | Kd | 30.0000 | AID1424979 |
| Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 20.0000 | AID1425189; AID625126 |
| STE20-related kinase adapter protein alpha | Homo sapiens (human) | Kd | 30.0000 | AID1425186 |
| Myosin-14 | Homo sapiens (human) | Kd | 30.0000 | AID1425080 |
| AarF domain-containing protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424904 |
| Serine/threonine-protein kinase tousled-like 2 | Homo sapiens (human) | Kd | 10.0000 | AID624771 |
| Serine/threonine-protein kinase 32C | Homo sapiens (human) | Kd | 10.0000 | AID624734 |
| Serine/threonine-protein kinase pim-3 | Homo sapiens (human) | Kd | 10.0000 | AID624802 |
| ATP-dependent RNA helicase DDX42 | Homo sapiens (human) | Kd | 30.0000 | AID1424976 |
| Serine/threonine-protein kinase VRK2 | Homo sapiens (human) | Kd | 10.0000 | AID625058 |
| Myosin light chain kinase family member 4 | Homo sapiens (human) | Kd | 10.0000 | AID624809 |
| Homeodomain-interacting protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID624726 |
| Calcium/calmodulin-dependent protein kinase type 1D | Homo sapiens (human) | Kd | 10.0000 | AID625118 |
| Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425053; AID624921 |
| Cyclin-dependent kinase-like 3 | Homo sapiens (human) | Kd | 10.0000 | AID624822 |
| MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 20.0000 | AID1425067; AID624923 |
| Serine/threonine-protein kinase BRSK2 | Homo sapiens (human) | Kd | 10.0000 | AID624929 |
| Serine/threonine-protein kinase NIM1 | Homo sapiens (human) | Kd | 10.0000 | AID624728 |
| Eukaryotic peptide chain release factor GTP-binding subunit ERF3B | Homo sapiens (human) | Kd | 30.0000 | AID1425015 |
| Serine/threonine-protein kinase ULK2 | Homo sapiens (human) | Kd | 10.0000 | AID625085 |
| Misshapen-like kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1425077; AID624813 |
| Serine/threonine-protein kinase DCLK2 | Homo sapiens (human) | Kd | 10.0000 | AID624814 |
| Calcium/calmodulin-dependent protein kinase kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID625143 |
| Casein kinase I isoform alpha-like | Homo sapiens (human) | Kd | 10.0000 | AID624723 |
| Homeodomain-interacting protein kinase 4 | Homo sapiens (human) | Kd | 0.3600 | AID624720 |
| Myosin-IIIa | Homo sapiens (human) | Kd | 10.0000 | AID625104 |
| Ankyrin repeat and protein kinase domain-containing protein 1 | Homo sapiens (human) | Kd | 10.0000 | AID624735 |
| Serine/threonine-protein kinase Nek11 | Homo sapiens (human) | Kd | 10.0000 | AID624725 |
| Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 20.0000 | AID1424905; AID625116 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 23.3333 | AID1425115; AID625134 |
| Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 20.0000 | AID1425060; AID624715 |
| Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 20.0000 | AID1425089; AID624704 |
| Serine/threonine-protein kinase BRSK1 | Homo sapiens (human) | Kd | 10.0000 | AID624702 |
| Serine/threonine-protein kinase 35 | Homo sapiens (human) | Kd | 10.0000 | AID624711 |
| Serine/threonine-protein kinase Nek7 | Homo sapiens (human) | Kd | 20.0000 | AID1425088; AID624754 |
| Rhodopsin kinase GRK7 | Homo sapiens (human) | Kd | 10.0000 | AID624719 |
| Serine/threonine-protein kinase 32A | Homo sapiens (human) | Kd | 10.0000 | AID624821 |
| Myosin-IIIb | Homo sapiens (human) | Kd | 10.0000 | AID624817 |
| ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | AID1424974 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 2 | Homo sapiens (human) | Kd | 1.8000 | AID624918 |
| Cyclin-dependent kinase-like 2 | Homo sapiens (human) | Kd | 10.0000 | AID624928 |
| Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 23.3333 | AID1425051; AID624816 |
| Serine/threonine-protein kinase Sgk3 | Homo sapiens (human) | Kd | 10.0000 | AID625073 |
| Atypical kinase COQ8B, mitochondrial | Homo sapiens (human) | Kd | 10.0000 | AID625135 |
| Aurora kinase B | Homo sapiens (human) | Kd | 20.0000 | AID1424918; AID624772 |
| MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 20.0000 | AID1425070; AID625140 |
| Calcium/calmodulin-dependent protein kinase type 1G | Homo sapiens (human) | Kd | 10.0000 | AID625119 |
| Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 20.0000 | AID1425085; AID625068 |
| Cyclin-dependent kinase 15 | Homo sapiens (human) | Kd | 10.0000 | AID624718 |
| PAS domain-containing serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | AID1425102 |
| Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1424931; AID625060 |
| EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | AID1425204 |
| SRSF protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID624903 |
| Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 20.0000 | AID1425116; AID624757 |
| Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 20.0000 | AID1425049; AID625028 |
| Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha | Homo sapiens (human) | Kd | 10.0000 | AID624824 |
| Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 20.0000 | AID1425047; AID624865 |
| Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 20.0000 | AID1424984; AID625080 |
| Serine/threonine-protein kinase RIO1 | Homo sapiens (human) | Kd | 10.0000 | AID625141 |
| MAP kinase-interacting serine/threonine-protein kinase 1 | Homo sapiens (human) | Kd | 1.8000 | AID624823 |
| Serine/threonine-protein kinase RIO2 | Homo sapiens (human) | Kd | 10.0000 | AID625111 |
| Cyclin-dependent kinase 19 | Homo sapiens (human) | Kd | 10.0000 | AID625094 |
| Transient receptor potential cation channel subfamily M member 6 | Homo sapiens (human) | Kd | 10.0000 | AID625110 |
| Testis-specific serine/threonine-protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID625142 |
| Serine/threonine-protein kinase 33 | Homo sapiens (human) | Kd | 10.0000 | AID625138 |
| Nucleolar GTP-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | AID1425016 |
| Serine/threonine-protein kinase D2 | Homo sapiens (human) | Kd | 20.0000 | AID1425136; AID625102 |
| Serine/threonine-protein kinase DCLK3 | Homo sapiens (human) | Kd | 10.0000 | AID624707 |
| NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425095; AID625139 |
| RNA cytidine acetyltransferase | Homo sapiens (human) | Kd | 30.0000 | AID1425083 |
| Serine/threonine-protein kinase SIK2 | Homo sapiens (human) | Kd | 20.0000 | AID1425166; AID625095 |
| Myosin light chain kinase 2, skeletal/cardiac muscle | Homo sapiens (human) | Kd | 10.0000 | AID624705 |
| STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 16.8500 | AID1425171; AID625086 |
| Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 20.0000 | AID1425191; AID625101 |
| Homeodomain-interacting protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID625129 |
| Tyrosine-protein kinase Srms | Homo sapiens (human) | Kd | 10.0000 | AID624710 |
| Homeodomain-interacting protein kinase 3 | Homo sapiens (human) | Kd | 10.0000 | AID625023 |
| Serine/threonine-protein kinase PLK3 | Homo sapiens (human) | Kd | 10.0000 | AID624933 |
| dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1424971 |
| Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 20.0000 | AID1424958; AID625125 |
| MAP kinase-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 1.6000 | AID625108 |
| Serine/threonine-protein kinase Nek6 | Homo sapiens (human) | Kd | 10.0000 | AID625079 |
| Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 20.0000 | AID1424964; AID625128 |
| Serine/threonine-protein kinase PAK 6 | Homo sapiens (human) | Kd | 10.0000 | AID625115 |
| SNF-related serine/threonine-protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID624752 |
| Serine/threonine-protein kinase LATS2 | Homo sapiens (human) | Kd | 10.0000 | AID625083 |
| Serine/threonine-protein kinase 36 | Homo sapiens (human) | Kd | 10.0000 | AID625096 |
| Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | AID1425000 |
| BMP-2-inducible protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1424920; AID625109 |
| Obg-like ATPase 1 | Homo sapiens (human) | Kd | 30.0000 | AID1425096 |
| Midasin | Homo sapiens (human) | Kd | 30.0000 | AID1425073 |
| Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 20.0000 | AID1425029; AID625098 |
| Serine/threonine-protein kinase 32B | Homo sapiens (human) | Kd | 10.0000 | AID625112 |
| Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 23.3333 | AID1425213; AID624755 |
| Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | AID1424939 |
| Serine/threonine-protein kinase PLK2 | Homo sapiens (human) | Kd | 10.0000 | AID625063 |
| NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 | Homo sapiens (human) | Kd | 30.0000 | AID1425084 |
| Serine/threonine-protein kinase MARK1 | Homo sapiens (human) | Kd | 10.0000 | AID625113 |
| Serine/threonine-protein kinase pim-2 | Homo sapiens (human) | Kd | 20.0000 | AID1425112; AID625064 |
| Serine/threonine-protein kinase PAK 5 | Homo sapiens (human) | Kd | 10.0000 | AID625117 |
| Serine/threonine-protein kinase 26 | Homo sapiens (human) | Kd | 20.0000 | AID1425181; AID625103 |
| eIF-2-alpha kinase GCN2 | Homo sapiens (human) | Kd | 10.0000 | AID624810 |
| Serine/threonine-protein kinase NLK | Homo sapiens (human) | Kd | 20.0000 | AID1425090; AID625100 |
| Phosphatidylinositol 4-kinase beta | Homo sapiens (human) | Kd | 10.0000 | AID624880 |
| Serine/threonine-protein kinase 17A | Homo sapiens (human) | Kd | 2.3000 | AID624968 |
| STE20/SPS1-related proline-alanine-rich protein kinase | Homo sapiens (human) | Kd | 10.0000 | AID625071 |
| Ephrin type-A receptor 6 | Homo sapiens (human) | Kd | 0.3400 | AID624748 |
| 5'-AMP-activated protein kinase subunit gamma-2 | Homo sapiens (human) | Kd | 30.0000 | AID1425127 |
| Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | Kd | 20.0000 | AID1425192; AID625072 |
| Septin-9 | Homo sapiens (human) | Kd | 30.0000 | AID1425165 |
| Death-associated protein kinase 2 | Homo sapiens (human) | Kd | 10.0000 | AID625077 |
| Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 14.3667 | AID1425163; AID625081; AID625082 |
| TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1425199; AID625093 |
| Serine/threonine-protein kinase tousled-like 1 | Homo sapiens (human) | Kd | 10.0000 | AID625069 |
| Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 20.0000 | AID1425190; AID625099 |
| Long-chain-fatty-acid--CoA ligase 5 | Homo sapiens (human) | Kd | 30.0000 | AID1424897 |
| ALK tyrosine kinase receptor | Homo sapiens (human) | Kd | 10.0000 | AID624944 |
| SRSF protein kinase 3 | Homo sapiens (human) | Kd | 10.0000 | AID625078 |
| Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 20.0000 | AID1425021; AID625090 |
| Cyclin-dependent kinase 11A | Homo sapiens (human) | Kd | 10.0000 | AID625133 |
| Aurora kinase C | Homo sapiens (human) | Kd | 10.0000 | AID624769 |
| Calcium/calmodulin-dependent protein kinase type II subunit alpha | Homo sapiens (human) | Kd | 10.0000 | AID624730 |
| RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 20.0000 | AID1424912; AID625019 |
| Serine/threonine-protein kinase 38-like | Homo sapiens (human) | Kd | 10.0000 | AID625092 |
| Microtubule-associated serine/threonine-protein kinase 1 | Homo sapiens (human) | Kd | 10.0000 | AID625091 |
| Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 20.0000 | AID1425167; AID624774 |
| Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 20.0000 | AID1425046; AID625062 |
| Thyroid hormone receptor-associated protein 3 | Homo sapiens (human) | Kd | 30.0000 | AID1425198 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Homo sapiens (human) | Kd | 2.8000 | AID624964 |
| Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 20.0000 | AID1425055; AID625061 |
| Receptor-interacting serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | AID1425156 |
| Serine/threonine-protein kinase MRCK beta | Homo sapiens (human) | Kd | 20.0000 | AID1424934; AID625031 |
| Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 23.3333 | AID1425028; AID625066 |
| Serine/threonine-protein kinase 24 | Homo sapiens (human) | Kd | 10.0000 | AID624917 |
| Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 20.0000 | AID1424966; AID624949 |
| Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 20.0000 | AID1425048; AID625027 |
Bioassays (1092)
| Assay ID | Title | Year | Journal | Article |
|---|
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425010 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425087 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904505 | Antiproliferative activity against human BT-474 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321123 | Antitumor activity against human NCI-H1975 cells xenografted in Foxn1 nude mouse assessed as reduction in tumor volume at 25 mg/kg, po qd for 5 days relative to untreated control | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ISSN: 1520-4804 | Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants |
| AID1425146 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1616615 | Oral bioavailability in rat at 20 mg/kg | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID1250288 | Elimination half-life in Sprague-Dawley rat at 1 mg/kg, iv incubated for 24 hrs by LC/MS/MS method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102ISSN: 1768-3254 | Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250263 | Inhibition of EGFR (unknown origin) by ELISA method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102ISSN: 1768-3254 | Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors. |
| AID1616606 | Clearance in rat at 5 mg/kg, iv | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID1424993 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1822762 | Inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
ISSN: 1520-4804 | |
| AID1616607 | Volume of distribution at steady state in rat at 5 mg/kg, iv | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID492109 | Inhibition of GST-tagged EGFR expressed in Escherichia coli | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
ISSN: 1520-4804 | Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. |
| AID1445476 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
ISSN: 1520-4804 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1673921 | Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
ISSN: 1520-4804 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| AID1425105 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID410943 | Inhibition of EGFR by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
ISSN: 1464-3405 | Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. |
| AID1368036 | Inhibition of recombinant EGFR (unknown origin) T790M/L858R double mutant preincubated for 30 mins followed by poly (Glu-Tyr) biotinylated peptide substrate addition measured after 30 mins in presence of ATP by ELISA | 2017 | Bioorganic & medicinal chemistry, 12-15, Volume: 25, Issue:24
ISSN: 1464-3391 | Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant. |
| AID1128590 | Irreversible inhibition of EGFR (unknown origin) using 5-FAM-EEPLYWSFPAKKK-CONH2 peptide as substrate assessed as decrease in enzyme activity at 100 times IC50 preincubated for 30 mins followed by 100 fold dilution with ATP/substrate measured for 2 hrs | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425073 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1420983 | Antiproliferative activity against human MDA231 cells by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | |
| AID1894151 | Inhibition of human wild type EGFR using pEY (4:1) as substrate | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214ISSN: 1768-3254 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID718822 | Inhibition of ERBB2 at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
ISSN: 1464-3405 | Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
| AID1425064 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID708781 | Toxicity in human NCI-H1975 cells xenografted BALB/c mouse assessed as body weight loss at 20 mg/kg, po qd | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1425196 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1425106 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425171 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1813989 | Induction of apoptosis in human DLD-1 cells harboring KRAS G13D mutant assessed as cleaved-PRAP at 100 nM measured after 24 to 48 hrs | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425165 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425043 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1610894 | Antiproliferative activity against human H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
ISSN: 1464-3391 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425159 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676511 | Inhibiton of EGFR L858R/T790M mutant (unknown origin) expressed in human NCI-H1975 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID719887 | Inhibition of ErbB2 | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676518 | Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells assessed as ratio of Kinact to Ki using TK as substrate measured up to 2 to 40 mins by fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1807692 | Inhibition of wild type EGFR (unknown origin) preincubated for 60 mins followed by substrate addition and further incubated for 60 mins in presence of ATP by IMAP-FP assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52ISSN: 1464-3405 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1724454 | Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID410944 | Inhibition of ERBb2 by HTRF assay | 2009 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 19, Issue:1
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| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1301838 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425163 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676519 | Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells assessed as Kinact using TK as substrate measured up to 2 to 40 mins by fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1301834 | Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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| AID1171451 | Apparent volume of distribution in BALB/c mouse at 10 mg/kg, po after 24 hrs by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424940 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1425059 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424963 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421405 | Inhibition of recombinant human PDGFRbeta at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425176 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1167145 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 10 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ISSN: 1520-4804 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1909872 | Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
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| AID1616594 | Toxicity in athymic NU-Fox1nu nude mouse xenografted with human HCC827 cells assessed as induction of body weight loss at 20 mg/kg, po dosed via gavage for 5 days/week for 2 consecutive weeks | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425056 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1301839 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137584 | Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1891051 | Inhibition of recombinant human N-terminal His-tagged EGFR (676 to 1255 residues) expressed in Sf21 insect cells using kinase substrate 22 incubated for 30 mins in presence of ATP | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67ISSN: 1464-3405 | Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1616617 | Half life in rat at 20 mg/kg, po | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1365585 | Inhibition of EGFR L858R mutant (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
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| AID1279101 | Inhibition of EGFR (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by addition of substrate by mobility shift assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
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| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424907 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424935 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904501 | Antiproliferative activity against human NCI-H1650 cells expressing PTEN assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424890 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421403 | Inhibition of recombinant human VEGFR1 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425021 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425160 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID718821 | Inhibition of ERBB4 at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
ISSN: 1464-3405 | Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
| AID1301836 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904470 | Inhibition of c-Kit (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1128565 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) expressed in baculovirus expression system using Poly(Glu:Tyr)4:1 substrate after 60 mins by ELISA | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
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ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904496 | Antiproliferative activity against human NCI-H1975 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1814379 | Inhibition of EGFR (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1565417 | Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425117 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1822765 | Selectivity ratio of IC50 for inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA to IC50 for inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
ISSN: 1520-4804 | |
| AID1424933 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424909 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1279099 | Cytotoxicity against human HeLa cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
ISSN: 1464-3391 | Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors. |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1171456 | Ratio of drug level in brain to plasma in BALB/c mouse at 30 mg/kg, po after 6 hrs by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1909897 | Antitumor activity against patient derived CUTO17 cells harboring EGFR-H773_V774insNPH mutant xenografted in BALB/c mouse assessed as reduction in tumor shrinkage at 20 mg/kg, po measured after 21 days | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
ISSN: 1520-4804 | Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. |
| AID1137582 | Inhibition of recombinant INSR (unknown origin) using fluorescent dye-labelled KKSRGDYMTMQIG peptide peptide as substrate after 1 hr by IMAP assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1424898 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676506 | Intrinsic clearance in human liver microsomes at 3 uM measured up to 50 mins by LC-MS analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1424964 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424998 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1545468 | Cytotoxicity against human EC1 cells assessed as reduction in cell growth at 2 nM incubated for 48 and 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1425144 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1478518 | Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo assay | 2017 | Bioorganic & medicinal chemistry, 06-01, Volume: 25, Issue:11
ISSN: 1464-3391 | Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B. |
| AID1425063 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1610895 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
ISSN: 1464-3391 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
| AID1425009 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904495 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425077 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425148 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1057934 | Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1719559 | Inhibition of recombinant wild type EGFR T790M/L858R mutant (696 to C terminal end) (unknown origin) using poly (Glu-Tyr) as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 03-15, Volume: 34ISSN: 1464-3391 | |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904489 | Inhibition of ABL (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1616555 | Inhibition of GST-tagged human EGFR kinase domain (696 to 1022 residues) using poly(Glu, Tyr) 4:1 substrate incubated for 60 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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| AID1167180 | Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 7.5 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1464-3391 | Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1867213 | Inhibition of human EGFR in human HCC1937 cells at 10 uM incubated for 48 hrs by ELISA | 2022 | Bioorganic & medicinal chemistry, 05-01, Volume: 61ISSN: 1464-3391 | Synthesis of novel dual target inhibitors of PARP and EGFR and their antitumor activities in triple negative breast cancers. |
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ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1520-4804 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1409092 | Inhibition of human ErbB4 at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
ISSN: 1464-3391 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1520-4804 | Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1595616 | Antiproliferative activity against human UCH1 cells measured after 72 hrs by alamar blue assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
ISSN: 1520-4804 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
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| AID1880123 | Inhibition of EGFR T790M mutant phosphorylation in human NCI-H1975 cells incubated for 2 hrs by ELISA | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
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ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1558401 | Irreversible inhibition of HER2 (unknown origin) | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
ISSN: 1520-4804 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID1171420 | Inhibition of wild type EGFR T790M mutant (unknown origin) incubated for 5 mins by HTRF assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321125 | Toxicity in human NCI-H1975 cells xenografted Foxn1 nude mouse assessed as change in body weight at 25 mg/kg, po qd for 5 days (Rvb = 3.9%) | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ISSN: 1520-4804 | Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants |
| AID1279098 | Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Apr-01, Volume: 24, Issue:7
ISSN: 1464-3391 | Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425138 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1445470 | Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 20 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
ISSN: 1520-4804 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
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| AID1724452 | Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676510 | Solubility of compound in aqueous buffer at pH 7.4 after 120 mins by turbidometric assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424919 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250367 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in MDCK2-MDR1 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425188 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425206 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1452381 | Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
ISSN: 1464-3391 | Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425155 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424962 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1171460 | Growth inhibition of human SW620 cells at 5 uM | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID729978 | Inhibition of ERBB2 (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61ISSN: 1768-3254 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425153 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID770082 | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
ISSN: 1520-4804 | Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904513 | Antiproliferative activity against human SW-620 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1625325 | Inhibition of human wild type GST-tagged EGFR kinase domain expressed in insect Sf9 cells using pEY (4:1)/biotinylated pEY as substrate after 30 mins by ELISA | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ISSN: 1520-4804 | Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. |
| AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904507 | Antiproliferative activity against human SK-OV-3 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1822764 | Inhibition of GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hrs by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
ISSN: 1520-4804 | |
| AID1425145 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904511 | Antiproliferative activity against human MCF7 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1565419 | Antiproliferative activity against human CL68 cells harbouring EGFR delE746-A750/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
| AID1535502 | Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
| AID1171438 | Intrinsic clearance in dog liver microsomes assessed per mg protein at 1 uM in presence of NADPH after 0.5 to 30 mins by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1171453 | Oral bioavailability in BALB/c mouse at 10 mg/kg after 24 hrs by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID1425199 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424978 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1137579 | Inhibition of recombinant EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1904484 | Inhibition of HER2 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1676520 | Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate measured up to 2 to 40 mins by fluorescence assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1425111 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425193 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425045 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904485 | Inhibition of HER4 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1137586 | Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424974 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425039 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425049 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1891055 | Antiproliferative activity against human NCI-H1781 cells expressing HER G776V mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67ISSN: 1464-3405 | Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1167158 | Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ISSN: 1520-4804 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
| AID1904492 | Inhibition of RET (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1424957 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1458980 | Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
ISSN: 1520-4804 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
| AID1171455 | Ratio of drug level in lung to plasma in BALB/c mouse at 30 mg/kg, po after 6 hrs by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID1421413 | Inhibition of recombinant human Erbb4 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425182 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425098 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1574932 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by EZ-Cytox assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
ISSN: 1464-3405 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1425121 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250291 | Bioavailability in Sprague-Dawley rat at 1 mg/kg, iv incubated for 24 hrs by LC/MS/MS method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102ISSN: 1768-3254 | Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137587 | Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1617959 | Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669-1210 AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187ISSN: 1768-3254 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID1167178 | Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 20 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ISSN: 1520-4804 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
| AID1676512 | Inhibiton of EGFR (unknown origin) expressed in human A431 cells assessed as reduction in EGFR induced cell viability after 96 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904487 | Inhibition of EPH-A2 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1574929 | Inhibition of human N-terminal GST-tagged EGFR kinase domain (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
ISSN: 1464-3405 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1535511 | Antitumor activity against human NCI-H1975 cells harboring EGFR T790M mutant xenografted in BALB/c mouse assessed as tumor growth inhibition at 20 mg/kg, po administered daily via gavage for 14 days measured at 7 days post last dose relative to control | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321122 | Time duration during which free plasma concentration stays above in-vitro IC50 level in human NCI-H1975 cells xenografted Foxn1 nude mouse at 25 mg/kg, po qd for 5 days | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ISSN: 1520-4804 | Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425055 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424924 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424928 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425036 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421411 | Inhibition of recombinant human Erbb2 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425016 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425175 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1535501 | Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
| AID1171461 | Antitumor activity against human NCI-H1975 cells xenografted in nude mouse assessed as reduction in tumor growth at 30 mg/kg/day, ig relative to untreated control | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425170 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425070 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904478 | Inhibition of recombinant human EGFR L858R/T790M double mutant using GGMEDIYFEFMGG as substrate in presence of ATP by radiometric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1616593 | Antitumor activity against human HCC827 cells xenografted in athymic NU-Fox1nu nude mouse assessed as inhibition of tumor growth at 20 mg/kg, po dosed via gavage for 5 days/week for 2 consecutive weeks relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424980 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424958 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425037 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425143 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425210 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250370 | Fraction unbound in Han Wistar rat blood at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1708303 | Antiproliferative activity against human RPC9 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
| AID1574931 | Inhibition of human C-terminal His6-tagged ERBB2 (676 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
ISSN: 1464-3405 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1738670 | Inhibition of N-terminal GST-fused human EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate incubated for 20 mins by Mobility shift assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199ISSN: 1768-3254 | Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676529 | Inhibition of HER2-G776delinsVC mutant (unknown origin) expressed in human H1781 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1616605 | Half life in rat at 5 mg/kg, iv | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904490 | Inhibition of FGFR1 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424926 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425067 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425027 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1176840 | Inhibition of EGFR (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
ISSN: 1464-3405 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1595619 | Binding affinity to wild-type human partial length GAK (G13 to Y338 residues) expressed in bacterial expression system by Kinomescan method | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
ISSN: 1520-4804 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
| AID1535503 | Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425085 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676528 | Inhibition of HER2-A775_G776insYVMA mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in HER2 induced cell viability after 96 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1617960 | Inhibition of N-terminal GST-tagged human EGFR (d746-750AA) expressed in baculovirus using FAM-labelled peptide as substrate pre-incubated for 10 mins followed by substrate addition by mobility shift assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187ISSN: 1768-3254 | Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904503 | Antiproliferative activity against human SK-BR-3 cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1814381 | Inhibition of ERBB4 (unknown origin) at 100 uM incubated for 60 min by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
ISSN: 1520-4804 | Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| AID1425116 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1167177 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 20 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ISSN: 1520-4804 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
| AID1676530 | Inhibition of C-terminal His6-tagged HER2-A775_G776insYVMA mutant (703 to 1029 residues) (unknown origin) expressed in Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 40 mins in presence of | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID729594 | Inhibition of ERBB4 (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61ISSN: 1768-3254 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421419 | Inhibition of recombinant human IGF1R at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676509 | Kinetic solubility of compound in HEPES buffer a pH 7.4 at 500 uM after 90 mins | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1757411 | Inhibition of ERBB4 (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. |
| AID1420986 | Antiproliferative activity against human Caco2 cells by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1738671 | Inhibition of N-terminal GST-fused human wild type EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using 5-FAM-EEPLYWSFPAKKK-CONH2 as substrate incubated for 20 mins by Mobility shift assay | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199ISSN: 1768-3254 | Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1616556 | Inhibition of GST-tagged human EGFR kinase domain I858R/T790M mutant (696 to 1022 residues) using EGFR L858R/T790M substrate peptide incubated for 120 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421409 | Inhibition of recombinant human EGFR at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425202 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1894154 | Inhibition of HER2 (unknown origin) using pEY (4:1) as substrate | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214ISSN: 1768-3254 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904504 | Antiproliferative activity against human BT-474 cells expressing EGFR assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425060 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676503 | Ratio of apparent permeability across basolateral to apical over apical to basolateral side in human Caco2 cells at 5 uM after 2 hrs by transwell assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425014 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425040 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425167 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425083 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424912 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1610890 | Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
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| AID1715789 | Inhibition of recombinant human N-terminal GST tagged EGFR L858R/T790M double mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by T | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
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| AID1545478 | Inhibition of human recombinant GST-tagged EGFR L858R/T790M mutant using pEY as substrate incubated for 30 mins by ELISA | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1724451 | Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
ISSN: 1464-3391 | Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR |
| AID1708231 | Antiproliferative activity against human PC-9 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212ISSN: 1768-3254 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425130 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904493 | Antiproliferative activity against human A-431 cells expressing EGFR assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1250372 | Ratio of unbound AUC (0 to 24 hrs) in brain to blood of Han Wistar rat at 20 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1574935 | Antiproliferative activity against HER2-dependant human SKBR3 cells after 72 hrs by EZ-Cytox assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
ISSN: 1464-3405 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1424889 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424996 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424904 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904488 | Inhibition of IGF1R (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425023 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904491 | Inhibition of Flt-1 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1250368 | Permeability from apical to basolateral side in BCRP transfected MDCK2 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425174 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1137602 | Induction of apoptosis in human NCI-H1993 cells at 1 uM after 24 hrs using propidium iodide by flow cytometry | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1545492 | Cytotoxicity against human HKESC1 cells assessed as reduction in cell growth at 2 nM incubated for 48 and 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1610893 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
ISSN: 1464-3391 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
| AID1904499 | Antiproliferative activity against human A549 cells expressing RAS assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1484893 | Inhibition of ErbB4 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135ISSN: 1768-3254 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425002 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425066 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425122 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425123 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1321118 | Glutathione reactivity in human liver microsomes assessed as GSH adduct formation in presence of NADPH and GSH incubated for 1 hr | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
ISSN: 1520-4804 | Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1813986 | Anticancer activity against human DLD-1 cells xenografted rat model assessed as tumor growth inhibition at 50 mg/kg measured | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
ISSN: 1520-4804 | One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS. |
| AID1425013 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904469 | Inhibition of PDGFR-beta (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425028 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425209 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425213 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1301835 | Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1880129 | Inhibition of EGFR L858R/T790M mutant phosphorylation (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
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| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1595617 | Antiproliferative activity against human UCH2 cells measured after 72 hrs by alamar blue assay | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
ISSN: 1520-4804 | Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. |
| AID1715790 | Inhibition of recombinant human N-terminal GST tagged EGFR d746-750 mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET ass | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
ISSN: 1464-3391 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1420985 | Antiproliferative activity against human HCT116 cells by MTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | |
| AID1425051 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1891054 | Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67ISSN: 1464-3405 | Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors. |
| AID1171436 | Intrinsic clearance in rat liver microsomes assessed per mg protein at 1 uM in presence of NADPH after 0.5 to 30 mins by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421415 | Inhibition of recombinant human c-SRC at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1250287 | Mean residence time in Sprague-Dawley rat at 1 mg/kg, iv incubated for 24 hrs by LC/MS/MS method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102ISSN: 1768-3254 | Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425149 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250366 | Permeability from apical to basolateral side in MDCK2-MDR1 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
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ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1627111 | Antitumor activity against human A431 cells xenografted in BALB/c mouse assessed as inhibition of tumor growth at 25 mg/kg, po qd for 14 consecutive days | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15
ISSN: 1520-4804 | Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation. |
| AID1909873 | Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1175324 | Inhibition of EGFR (unknown origin) at 100 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
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ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1137585 | Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
ISSN: 1948-5875 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424989 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1167156 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 5 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
ISSN: 1520-4804 | Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. |
| AID1595618 | Binding affinity to wild-type human partial length EGFR (R669 to V1011 residues) expressed in bacterial expression system by Kinomescan method | 2019 | Journal of medicinal chemistry, 05-09, Volume: 62, Issue:9
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| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1558402 | Drug excretion in human urine at 15 mg, po administered as single dose and measured after 96 hrs by HPLC method | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
ISSN: 1520-4804 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID1425208 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425052 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425158 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425099 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425178 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1880122 | Inhibition of EGF-stimulated wild-type EGFR phosphorylation in human A-431 cells incubated for 2 hrs by ELISA | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
ISSN: 1520-4804 | The Ascension of Targeted Covalent Inhibitors. |
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| AID1424955 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1616598 | Toxicity in nude BALB/c mouse xenografted with human NCI-H1975 cells assessed as drug tolerability at 15 mg/kg, po QD for 15 days relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID770080 | Selectivity ratio of IC50 for wild type EGFR phosphorylation in human LoVo cells over IC50 for EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
ISSN: 1520-4804 | Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
| AID1421417 | Inhibition of recombinant human ABL at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158ISSN: 1768-3254 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425033 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1807693 | Inhibition of EGF-induced phosphorylation of EGFR T790M/L858R double mutant in human NCI-H1975 cells preincubated for 120 mins followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52ISSN: 1464-3405 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
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ISSN: 1464-3391 | Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1545467 | Inhibition of HER2 (unknown origin) using pEY as substrate incubated for 30 mins by ELISA | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1250371 | Fraction unbound in Han Wistar rat brain at 5 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
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| AID1458982 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18
ISSN: 1520-4804 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
| AID1171435 | Intrinsic clearance in human liver microsomes assessed per mg protein at 1 uM in presence of NADPH after 0.5 to 30 mins by LC/MS/MS method | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1535504 | Inhibition of recombinant human GST-tagged EGFR catalytic domain (668 to 1210 residues) expressed in baculovirus expression system using TK-biotin peptide as substrate measured after 10 mins by HTRF assay | 2019 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
ISSN: 1464-3405 | Discovery of new quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors and their anticancer activities - Part 1. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425000 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1128567 | Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as growth inhibition after 72 hrs by SRB assay | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
| AID1880133 | Inhibition of wild-type HER2 phosphorylation in human BT-474 cells | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
ISSN: 1520-4804 | The Ascension of Targeted Covalent Inhibitors. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425109 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
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| AID1545495 | Cytotoxicity against human SLMT1 cells assessed as reduction in cell growth at 2 nM incubated for 48 and 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1301837 | Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
ISSN: 1520-4804 | Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
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ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID1676508 | Stability of compound in human plasma assessed as parent compound remaining at 5 uM measured for 1 hr by LC-MS analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
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ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1616609 | Cmax in rat at 20 mg/kg, po | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1616587 | Toxicity in ICR mouse assessed as induction of fur loss in nose and abdomen area at 100 mg/kg, po QD for 2 weeks | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22
ISSN: 1520-4804 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
| AID1724474 | Inhibition of recombinant human EGFR T790M/L858R mutant expressed in baculovirus insect cell expression system in presence of ATP preincubated 5 mins measured for 30 mins by detection reagent based HTRF analysis | 2020 | Bioorganic & medicinal chemistry, 10-01, Volume: 28, Issue:19
ISSN: 1464-3391 | Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFR |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1610891 | Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
ISSN: 1464-3391 | Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1545518 | Cytotoxicity against human Embryonic stem cells assessed as reduction in cell growth at 2 nM incubated for 48 and 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1425181 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID719885 | Inhibition of EGFR | 2012 | Journal of medicinal chemistry, Jul-26, Volume: 55, Issue:14
ISSN: 1520-4804 | Irreversible protein kinase inhibitors: balancing the benefits and risks. |
| AID1425135 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904506 | Antiproliferative activity against human SK-OV-3 cells expressing EGFR assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1176841 | Inhibition of ErbB4 (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
ISSN: 1464-3405 | Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1894152 | Inhibition of EGFR L858R mutant (unknown origin) using pEY (4:1) as substrate | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214ISSN: 1768-3254 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424960 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1673922 | Growth inhibition of human LoVo cells harboring wild type EGFR | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
ISSN: 1520-4804 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| AID1822763 | Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
ISSN: 1520-4804 | |
| AID1452378 | Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
ISSN: 1464-3391 | Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors. |
| AID1904486 | Inhibition of VEGFR2 (unknown origin) | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1545494 | Cytotoxicity against human KYSE10 cells assessed as reduction in cell growth at 2 nM incubated for 48 and 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170ISSN: 1768-3254 | Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. |
| AID1409093 | Inhibition of human EGFR at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
ISSN: 1464-3391 | Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1807691 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) preincubated for 60 mins followed by substrate addition and further incubated for 60 mins in presence of ATP by IMAP-FP assay | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52ISSN: 1464-3405 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
| AID1425168 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1574933 | Antiproliferative activity against human PC9 cells harboring EGFR exon-19 del mutant after 72 hrs by EZ-Cytox assay | 2019 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
ISSN: 1464-3405 | Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors. |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1057928 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant after 72 hrs by SRB assay | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor. |
| AID1599557 | Inhibition of cathepsin C (unknown origin) | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
ISSN: 1520-4804 | Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1484891 | Inhibition of ErbB2 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA relative to control | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135ISSN: 1768-3254 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1904509 | Antiproliferative activity against human T47D cells expressing ERBB2 assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676504 | Apparent permeability across apical side to basolateral side in human Caco-2 cells at 5 uM after 2 hrs by transwell assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1478517 | Cytotoxicity against human Ramos cells assessed as decrease in cell viability after 24 hrs by CellTiter-Glo assay | 2017 | Bioorganic & medicinal chemistry, 06-01, Volume: 25, Issue:11
ISSN: 1464-3391 | Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID770078 | Inhibition of wild type human EGFR after 50 mins by HTRF assay | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
ISSN: 1520-4804 | Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). |
| AID1424921 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1891048 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in Sf21 insect cells at 200 uM using kinase substrate 22 incubated for 30 mins in presence of ATP relative to control | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67ISSN: 1464-3405 | Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors. |
| AID1424992 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424911 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1171419 | Inhibition of wild type EGFR (unknown origin) incubated for 5 mins by HTRF assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID1424914 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676507 | Stability of compound in mouse plasma assessed as parent compound remaining at 5 uM measured for 1 hr by LC-MS analysis | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424905 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676514 | Inhibition of human N-terminal GST-tagged EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus infected Sf9 insect cells using TK as substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by HTRF assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1425203 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425164 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425090 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904508 | Antiproliferative activity against human T47D cells expressing EGFR assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1452380 | Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
ISSN: 1464-3391 | Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1171418 | Antiproliferative activity against human NCI-H1975 cells after 48 hrs by Celltiter-Glo assay | 2014 | Journal of medicinal chemistry, Dec-11, Volume: 57, Issue:23
ISSN: 1520-4804 | A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. |
| AID1822766 | Selectivity ratio of IC50 for human EGFR expressed in baculovirus expression system using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA to IC50 for inhibition of human BTK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | 2022 | Journal of medicinal chemistry, 02-10, Volume: 65, Issue:3
ISSN: 1520-4804 | |
| AID1128589 | Reversible inhibition of EGFR (unknown origin) using 5-FAM-EEPLYWSFPAKKK-CONH2 peptide as substrate assessed as enzyme activity at 100 times IC50 preincubated for 30 mins followed by 100 fold dilution with ATP/substrate measured for 2 hrs | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
ISSN: 1464-3391 | Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors. |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1757410 | Inhibition of ERBB2 (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216ISSN: 1768-3254 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1535439 | Inhibition of human GST-fused HER2 kinase domain expressed in baculovirus expression system measured after 30 mins by ELISA | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
ISSN: 1464-3391 | The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton. |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425127 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1894153 | Inhibition of human GST-tagged EGFR L858R/T790M double mutant using pEY (4:1) as substrate | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214ISSN: 1768-3254 | FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1535438 | Inhibition of human GST-fused EGFR kinase domain expressed in baculovirus expression system measured after 30 mins by ELISA | 2019 | Bioorganic & medicinal chemistry, 02-01, Volume: 27, Issue:3
ISSN: 1464-3391 | The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton. |
| AID1425071 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1250373 | Ratio of unbound AUC (0 to 24 hrs) in CSF to blood of Han Wistar rat at 20 mg/kg, po by LC-MS/MS analysis | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1425003 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1676533 | Apparent permeability across basolateral side to apical side in human Caco-2 cells at 5 uM after 2 hrs by transwell assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
ISSN: 1520-4804 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
| AID1886715 | Covalent inhibition of human EGFR L858R/T790M double mutant expressed in baculovirus infected Sf21 cells assessed as ratio of Kinact/Ki | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
ISSN: 1520-4804 | |
| AID1425025 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1880128 | Inhibition of wild-type EGFR phosphorylation (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8
ISSN: 1520-4804 | The Ascension of Targeted Covalent Inhibitors. |
| AID1424946 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424929 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1424939 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1724046 | Inhibition of EGFR (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18
ISSN: 1464-3391 | Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1558400 | Irreversible inhibition of wild type EGFR (unknown origin) | 2020 | Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2
ISSN: 1520-4804 | The Exploration of Chirality for Improved Druggability within the Human Kinome. |
| AID729977 | Inhibition of EGFR (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61ISSN: 1768-3254 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID1424915 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
ISSN: 1095-9203 | The target landscape of clinical kinase drugs. |
| AID1715791 | Inhibition of recombinant human N-terminal GST tagged EGFR L858R mutant (669 to 1210 residues) expressed in insect expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
ISSN: 1464-3391 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
| AID1891050 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in Sf21 insect cells using kinase substrate 22 incubated for 30 mins in presence of ATP | 2022 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 67ISSN: 1464-3405 | Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors. |
| AID1250369 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in BCRP transfected MDCK2 cells | 2015 | Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
ISSN: 1520-4804 | Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. |
| AID1904500 | Antiproliferative activity against human NCI-H1650 cells expressing EGFR assessed as growth inhibition by SRB colorimetric assay | 2022 | European journal of medicinal chemistry, Apr-05, Volume: 233ISSN: 1768-3254 | Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. |
| AID1565418 | Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182ISSN: 1768-3254 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2010 | Journal of medicinal chemistry, Jul-08, Volume: 53, Issue:13
ISSN: 1520-4804 | Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. |
| AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
ISSN: 1546-1696 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1345653 | Human erb-b2 receptor tyrosine kinase 2 (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2008 | Oncogene, Aug-07, Volume: 27, Issue:34
ISSN: 1476-5594 | BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. |
| AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2008 | Oncogene, Aug-07, Volume: 27, Issue:34
ISSN: 1476-5594 | BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. |
Research
Studies (1,029)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (0.97) | 29.6817 |
| 2010's | 687 (66.76) | 24.3611 |
| 2020's | 332 (32.26) | 2.80 |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|
| Trials | 147 (14.08%) | 5.53% |
| Reviews | 136 (13.03%) | 6.00% |
| Case Studies | 169 (16.19%) | 4.05% |
| Observational | 22 (2.11%) | 0.25% |
| Other | 570 (54.60%) | 84.16% |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| rtki cpd | | aromatic ether;
monochlorobenzenes;
quinazolines | antineoplastic agent;
antiviral agent;
epidermal growth factor receptor antagonist;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alfuzosin | | monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bunazosin | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cgs 15943 | | aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline | adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cl 387785 | | bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxazosin | | aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines | alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| whi p97 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ketanserin | | aromatic ketone;
organofluorine compound;
piperidines;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
cardiovascular drug;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metolazone | | organochlorine compound;
quinazolines;
sulfonamide | antihypertensive agent;
diuretic;
ion transport inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 153035 | | aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd168393 | | acrylamides;
bromobenzenes;
quinazolines;
secondary carboxamide;
substituted aniline | epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prazosin | | aromatic ether;
furans;
monocarboxylic acid amide;
piperazines;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| terazosin | | furans;
piperazines;
primary amino compound;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methaqualone | | quinazolines | GABA agonist;
sedative | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinethazone | | quinazolines | antihypertensive agent;
diuretic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinazolines | | azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines | | 2007 | 2023 | 8.7 | medium | 85 | 0 | 0 | 15 | 463 | 12 |
| mecloqualone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinelorane | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| halofuginone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glycosine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| febrifugine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3-trimethylene-4-quinazolone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenquizone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenazaquin | | quinazolines | acaricide;
mitochondrial NADH:ubiquinone reductase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluquinconazole | | conazole fungicide;
dichlorobenzene;
organofluorine compound;
quinazolines;
triazole fungicide;
triazoles | antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2008 | 2023 | 6.4 | low | 18 | 0 | 0 | 3 | 149 | 41 |
| cyclazosin | | aromatic amide;
aromatic ether;
furans;
monocarboxylic acid amide;
quinazolines;
quinoxaline derivative | adenosine A2A receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyantrypine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| canertinib | | monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erlotinib | | aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound | antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2023 | 7.9 | low | 2 | 0 | 0 | 1 | 28 | 4 |
| (5-amino-3-triazolo[1,5-a]quinazolinyl)-(4-morpholinyl)methanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mrs 1220 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-deoxyvasicine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-benzylquinazolin-4-amine | | benzenes;
quinazolines;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-hydroxy-3-methoxyphenyl)-3-(2-methoxyphenyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(cyclohexylmethyl)-5,6,7,8-tetrahydrotetrazolo[5,1-b]quinazolin-9-amine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-pyridinylmethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[5,1-b]quinazolin-9-amine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-methyl-4-oxo-3-(phenylmethyl)-7-(1-piperidinyl)-6-quinazolinyl]-3-pyridinecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(6-ethoxy-1,3-benzothiazol-2-yl)-2-[[3-(2-furanylmethyl)-4-oxo-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-pyridin-4-yl-2,3-dihydro-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(trifluoromethyl)phenyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-cyclohexyl-4-quinazolinyl)thio]-N-(4-methyl-1,2,5-oxadiazol-3-yl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[[[3-[(4-chlorophenyl)methyl]-2-methyl-4-oxo-6-quinazolinyl]amino]-oxomethyl]amino]propanoic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-(3,4-dihydro-2H-quinolin-1-yl)-2-oxoethyl]thio]-3-ethyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(3-ethyl-4-oxo-2-quinazolinyl)thio]acetic acid cyclohexyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-thiophen-2-yl-2,3-dihydro-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(pyridin-4-yl)-4-(pyrrolidin-1-yl)quinazoline | | pyridines;
pyrrolidines;
quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methyl-6-pyridin-4-yl-6H-benzimidazolo[1,2-c]quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-[(2-methoxy-2-oxoethyl)thio]-4-oxo-3-quinazolinyl]oxy]acetic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(1,3-benzoxazol-2-ylamino)-5-spiro[1,6,7,8-tetrahydroquinazoline-4,1'-cyclopentane]one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-methoxy-2-(3-pyridinylmethylthio)-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5,5-trimethyl-2-sulfanylidene-1,6-dihydrobenzo[h]quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N1-(6-bromo-4-quinazolinyl)-N4,N4-dimethylbenzene-1,4-diamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-fluorophenyl)-2-(pyridin-4-yl)quinazolin-4-amine | | aromatic amine;
monofluorobenzenes;
pyridines;
quinazolines;
secondary amino compound;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-methyl-2-[2-(4-methyl-5-thiazolyl)ethylthio]-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(4-oxo-3-quinazolinyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-bromo-3-phenyl-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-methyl-2-(4-methylphenyl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine | | piperidines;
quinazolines;
tertiary amino compound;
toluenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-furanyl)-3-(6-methyl-2-pyridinyl)-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-methoxyphenyl)-3-(3-pyridinyl)-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-phenyl-1H-quinazoline-4-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(ethylthio)-[1,3,4]thiadiazolo[2,3-b]quinazolin-5-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(3-methyl-4-oxo-2-quinazolinyl)thio]-N-phenylacetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,3-dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-3-phenyl-1H-quinazoline-2,4-dione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxy-4-methyl-2-[(2-methylphenyl)methylthio]quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-chlorophenyl)-4-propan-2-yloxyquinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-bromo-1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3-methoxyphenyl)-4-propan-2-yloxyquinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-(5-methyl-2-thiophenyl)-2-oxoethyl]thio]-3-phenyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(phenylmethyl)-2-[[4-(trifluoromethyl)-5,6-dihydrobenzo[h]quinazolin-2-yl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(6-amino-2-methyl-4-oxo-3-quinazolinyl)-N-(2-methylphenyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-amino-3-[(2-chlorophenyl)methyl]-2-propyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-chlorophenyl)-N-[2-(4-morpholinyl)ethyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-ethoxycarbonylanilino)-2-quinazolinecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-anilinoanilino)-2-quinazolinecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-(3,4-dihydro-1H-isoquinolin-2-yl)-2-oxoethyl]thio]-3-phenyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,4-dimethoxyphenyl)-2-(1-pyrrolidinyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-oxo-3-quinazolinyl)-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)propanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methoxy-N-[2-[(4-nitrophenyl)methylthio]-4-oxo-3-quinazolinyl]benzamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methoxyphenyl)-2-(3-nitrophenyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-tert-butyl-4-quinazolinyl)thio]-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-[[2-(phenylmethyl)-4-quinazolinyl]thio]ethanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-propyl-4-quinazolinyl)thio]-N-(4,5,6,7-tetrahydro-1,3-benzothiazol-2-yl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3,4-dihydro-1H-isoquinolin-2-yl)-2-[(2-propyl-4-quinazolinyl)thio]ethanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(5-methyl-3-isoxazolyl)-2-[(2-propan-2-yl-4-quinazolinyl)thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| Src Inhibitor-1 | | aromatic ether;
polyether;
quinazolines;
secondary amino compound | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-N-[(4-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-methyl-5,6,7,8-tetrahydrotetrazolo[5,1-b]quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2,4-dichlorophenyl)methylthio]-6,7-dimethoxy-3-(thiophen-2-ylmethyl)-4-quinazolinimine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-chloro-N-(2-furanylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methoxy-N-(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)benzamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| SMER 28 | | organobromine compound;
quinazolines;
secondary amino compound | autophagy inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methoxy-2-(4-propoxyphenyl)quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-butoxy-3-phenyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N,N-dibutyl-2-(pyridin-4-yl)quinazolin-4-amine | | pyridines;
quinazolines;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloro-N-(8-methyl-[1,3]dioxolo[4,5-g]quinazolin-6-yl)benzamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromophenyl)-5-[(7-nitro-4-quinazolinyl)oxymethyl]-1,3,4-oxadiazole | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[4-(2-benzofuranyl)-2-thiazolyl]methyl]-2-[(dimethylamino)methyl]-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(benzenesulfonyl)-N-(3-methylphenyl)-5-triazolo[1,5-a]quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[2-[[3-(4-methylphenyl)-5-triazolo[1,5-a]quinazolinyl]amino]ethyl]benzenesulfonamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-bromo-3-[4-nitro-3-(trifluoromethyl)phenyl]-2-propyl-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 12-oxo-N-(4-phenyl-2-thiazolyl)-7,8,9,10-tetrahydro-6H-azepino[2,1-b]quinazoline-3-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4,5-dimethyl-2-[[1-oxo-2-(4-quinazolinyloxy)ethyl]amino]-3-thiophenecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-[(6,8-dichloro-4-quinazolinyl)oxymethyl]-5-thiazolo[3,2-a]pyrimidinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,3-dihydro-1H-inden-5-yl)-2-[[3-(2-fluorophenyl)-4-oxo-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[3-(2,4-difluorophenyl)-4-oxo-2-quinazolinyl]thio]-N-(2,3-dihydro-1H-inden-5-yl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[3-[(4-fluorophenyl)methyl]-4-oxo-2-quinazolinyl]thio]-N-(thiophen-2-ylmethyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-furanylmethyl)-4-oxo-N,N-dipropyl-2-sulfanylidene-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-(4-quinazolinyloxymethyl)-5-thiazolo[3,2-a]pyrimidinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N'-(4-quinazolinyl)acetohydrazide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methyl-N'-(4-quinazolinyl)benzohydrazide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-{3-[(2-phenylquinazolin-4-yl)amino]phenyl}acetamide | | acetamide;
aromatic amine;
quinazolines;
secondary amino compound;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,3-dihydro-1H-inden-5-yl)-2-[(4-oxo-3-phenyl-2-quinazolinyl)thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(3-butyl-4-oxo-2-quinazolinyl)thio]-N-cyclopropylacetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4-(5-Fluoro-4-imino-3,4-dihydroquinazolin-3-yl)isonicotinamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(4-chlorophenyl)methyl]-4-(prop-2-enylthio)quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-nitrophenyl)-N-(2-oxolanylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-chloro-2-methyl-3-(4-pyridylmethyl)-3,4-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(7-chloro-4-quinazolinyl)oxy]-1-(2,3-dihydro-1,4-benzodioxin-6-yl)ethanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3-dimethyl-1-[[9-(methylthio)-5,6-dihydrothieno[3,4-h]quinazolin-2-yl]thio]-2-butanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4,6,7-Trimethyl-2-quinazolinyl)guanidine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LSM-19241 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LSM-19663 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[7-(2-furanyl)-5-oxo-7,8-dihydro-6H-quinazolin-2-yl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2,4-dichlorophenyl)-3-(phenylmethyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(3-methoxyphenyl)-3,4,5,6-tetrahydro-1H-benzo[h]quinazoline-2-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[3-[2-(1-cyclohexenyl)ethyl]-4-oxo-2-sulfanylidene-1H-quinazolin-7-yl]-oxomethyl]-1-piperazinecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3-nitrophenyl)-N-(phenylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-furanylmethyl)-2-phenyl-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LSM-19894 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| importazole | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(1,3-benzothiazol-2-ylamino)-5-spiro[1,6,7,8-tetrahydroquinazoline-4,1'-cyclopentane]one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-3-(2-oxolanylmethyl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(6-quinolinyl)-1,3,4,6,7,8-hexahydroquinazoline-2,5-dione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-phenyl-1,5,6,7,8,9-hexahydro-[1,2,4]triazolo[5,1-b]quinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(3-butan-2-yl-4-oxo-2-quinazolinyl)thio]propanenitrile | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| altanserin | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tandutinib | | aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zd 6474 | | aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3,5-dimethyl-1-[(4-methylphenyl)methyl]-4-pyrazolyl]-2-[[4-(trifluoromethyl)-5,6-dihydrobenzo[h]quinazolin-2-yl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(methylthio)-6-phenyl-6,7-dihydro-5H-[1,2,4]triazolo[5,1-b]quinazolin-8-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N'-[2-[(2-cyclohexyl-4-quinazolinyl)thio]-1-oxoethyl]-2-methylpropanehydrazide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3,5-dimethyl-1-piperidinyl)-2-[[2-(thiophen-2-ylmethyl)-4-quinazolinyl]thio]ethanone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ml106 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-(2-furanylmethyl)-N-methyl-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-furanylmethyl)-6-(3-methoxyphenyl)-N-methyl-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-[(3-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2-chlorophenyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-furanyl)-N-[(3-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-pyridinyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-furanyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methoxyphenyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2-chlorophenyl)-N-(2-furanylmethyl)-N-methyl-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methoxyphenyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-furanyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(3-methylphenyl)methyl]-6-(3-pyridinyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[5-[[2-(3-methoxypropylamino)-2-oxoethyl]thio]-3-oxo-2H-imidazo[1,2-c]quinazolin-2-yl]-N-(phenylmethyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[6-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-6-oxohexyl]-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[2-[butyl(methyl)amino]ethyl]-6-(4-morpholinyl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-chlorophenyl)-2-[6,7-dimethoxy-2,4-dioxo-3-(2-oxolanylmethyl)-1-quinazolinyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4-dioxo-3-pentyl-N-[3-(1-piperidinyl)propyl]-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(3-oxo-2-propan-2-yl-2H-imidazo[1,2-c]quinazolin-5-yl)thio]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(6-benzimidazolo[1,2-c]quinazolinylthio)-N-(2-furanylmethyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3-methylanilino)-[1,3,4]thiadiazolo[2,3-b]quinazolin-5-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[4-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-4-oxobutyl]-6,7-diethoxy-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5a,6,7,8,9,10-hexahydro-5H-azepino[2,1-b]quinazolin-12-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-3-cyclopentyl-2,4-dioxo-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-diethoxy-3-[3-(2-oxo-1-pyrrolidinyl)propyl]-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(1,3-benzodioxol-5-yl)-3-hydroxy-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(6,7-diethoxy-4-oxo-2-sulfanylidene-1H-quinazolin-3-yl)-N-(2-furanylmethyl)pentanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-chloro-3-[2-(diethylamino)ethyl]-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4-dioxo-3-(2-oxolanylmethyl)-N-pentyl-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[1,3-dioxo-3-[(12-oxo-7,8,9,10-tetrahydro-6H-azepino[2,1-b]quinazolin-2-yl)amino]propyl]-1-piperazinecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-butyl-2-[[6-(4-morpholinyl)-4-oxo-3-(2-phenylethyl)-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-diethoxy-3-(3-methoxypropyl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| savirin | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[(6,7-diethoxy-2,4-dioxo-1H-quinazolin-3-yl)methyl]-N-(3-methoxypropyl)-1-cyclohexanecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-4-(2-oxolanylmethylamino)-1H-quinazoline-2-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(5-methyl-1H-pyrazol-3-yl)-2-[[3-oxo-2-(phenylmethyl)-2H-imidazo[1,2-c]quinazolin-5-yl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-chlorophenyl)-2-(1-pyrrolidinyl)-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[2,4-dioxo-3-(phenylmethyl)-1-quinazolinyl]-N-(5-methyl-3-isoxazolyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-methylanilino)-[1,3,4]thiadiazolo[2,3-b]quinazolin-5-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[4-oxo-2-[[2-oxo-2-[(phenylmethyl)amino]ethyl]thio]-3-quinazolinyl]-1-piperidinecarboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-hydroxy-2-(2-hydroxy-3-methoxyphenyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(12-oxo-7,8,9,10-tetrahydro-6H-azepino[2,1-b]quinazolin-2-yl)-3-(3-pyridinylmethyl)thiourea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[3-(N-ethylanilino)propyl]-6-(4-morpholinyl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-methylene-7-(phenylmethyl)-5H-[1,3]dioxolo[4,5-g]quinazoline-6-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[4-methoxy-3-(4-morpholinylmethyl)phenyl]-3-(phenylmethyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-oxo-2-phenyl-1,2-dihydroquinazolin-3-yl)benzenesulfonamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-[(3-nitrophenyl)methylthio]-4-oxo-3-quinazolinyl]benzamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-chloro-3-hydroxy-2-[3-(trifluoromethyl)phenyl]-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-diethyl-2-(3-hydroxypropylamino)-5-methyl-6H-benzo[h]quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-methoxyphenyl)-2-methyl-4-oxo-1H-quinazoline-2-carboxylic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-butyl-1-methyl-3-(12-oxo-7,8,9,10-tetrahydro-6H-azepino[2,1-b]quinazolin-2-yl)thiourea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N,N-diethyl-2-[[7-[(4-methoxyphenyl)methyl]-8-oxo-[1,3]dioxolo[4,5-g]quinazolin-6-yl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(4-morpholinyl)-3-(2-phenylethyl)-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-[6-(4-morpholinyl)-4-oxo-2-sulfanylidene-1H-quinazolin-3-yl]hexanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-oxo-2-(2-pyridinyl)-1,2-dihydroquinazolin-3-yl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(1-azepanylsulfonyl)-4-methylphenyl]-2-(4-quinazolinylthio)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-fluorophenyl)-4-oxo-2-sulfanylidene-1H-quinazoline-7-carboxylic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromophenyl)-3-[3-(4-morpholinyl)propyl]-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch 79797 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-diethyl-2-(2-hydroxyethylamino)-5-methyl-6H-benzo[h]quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-(5-bromo-1h-indol-3-yl)ethyl)-3-(1-methylethoxyphenyl)-4-(3h)-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-[4-(dimethylamino)phenyl]-4-oxo-1,2-dihydroquinazolin-3-yl]carbamic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-morpholinyl)-10-pyridazino[6,1-b]quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-ethylphenyl)-2-[[3-[3-(4-methyl-1-piperidinyl)propyl]-4-oxo-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-{[2-(2-fluorophenyl)quinazolin-4-yl]amino}phenyl)acetamide | | acetamide;
aromatic amine;
monofluorobenzenes;
quinazolines;
secondary amino compound;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-cyclohexyl-3-(12-oxo-7,8,9,10-tetrahydro-6H-azepino[2,1-b]quinazolin-2-yl)thiourea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-methoxyethyl)-4-oxo-3-[3-(2-oxo-1-pyrrolidinyl)propyl]-2-sulfanylidene-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-propan-2-ylphenyl)-3,4,5,6-tetrahydro-1H-benzo[h]quinazolin-2-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(6-bromo-4-oxo-2-sulfanylidene-1H-quinazolin-3-yl)-N-[2-(4-sulfamoylphenyl)ethyl]hexanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-methoxyphenyl)-2-[(4-oxo-3-propyl-2-quinazolinyl)thio]-2-phenylacetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-thiophen-2-yl-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1-benzylpiperidin-4-yl)-2-(pyridin-3-yl)quinazolin-4-amine | | aromatic amine;
piperidines;
pyridines;
quinazolines;
secondary amino compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-oxo-3-quinazolinyl)-N-[3-(1-piperidinylsulfonyl)phenyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-(4-methoxyphenyl)-4-oxo-1,2-dihydroquinazolin-3-yl]carbamic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-chloro-3-[2-(1-cyclohexenyl)ethyl]-2-sulfanylidene-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[2-[[2-[(5-methyl-1H-pyrazol-3-yl)amino]-2-oxoethyl]thio]-4-oxo-3-quinazolinyl]-N-(phenylmethyl)butanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[3-butyl-6-(4-morpholinyl)-4-oxo-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(3,4-dimethoxyphenyl)-3,4,5,6-tetrahydro-1H-benzo[h]quinazoline-2-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[3-(1-benzotriazolylmethyl)-4-methoxyphenyl]-3-(4-methoxyphenyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-cycloheptyl-3-(2-methoxyethyl)-2,4-dioxo-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cb676475 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,5-dioxo-2,4-dihydropyrrolo[1,2-a]quinazoline-3-carboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| GSK3-XIII | | aromatic amine;
pyrazoles;
quinazolines;
secondary amino compound | EC 2.7.11.26 (tau-protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(1,3-benzoxazol-2-ylamino)-7,7-dimethyl-4-(2-pyridinyl)-1,4,6,8-tetrahydroquinazolin-5-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-(2-fluorophenyl)ethyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[5,1-b]quinazolin-9-amine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-chloro-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(4-morpholinyl)propyl]-2,4-dioxo-3-(2-phenylethyl)-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-methoxyethyl)-2,4-dioxo-N-pentyl-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(1-amino-1-oxopropan-2-yl)thio]-3-butyl-4-oxo-7-quinazolinecarboxylic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ic 87114 | | 6-aminopurines;
biaryl;
quinazolines | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zm 447439 | | aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| linagliptin | | aminopiperidine;
quinazolines | EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sotrastaurin | | indoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines | anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| saracatinib | | aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| luotonin a | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PDGF receptor tyrosine kinase inhibitor III | | aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
quinazolines;
tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erastin | | aromatic ether;
diether;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
quinazolines;
tertiary carboxamide | antineoplastic agent;
ferroptosis inducer;
voltage-dependent anion channel inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 8931 | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152 | | anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 00299804 | | enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lapatinib ditosylate | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| idelalisib | | aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-methoxyethyl)-2-[[3-[(4-methoxyphenyl)methyl]-6-(4-morpholinyl)-4-oxo-2-quinazolinyl]thio]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[(2-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)hydrazo]-4-oxo-N-propan-2-ylbutanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-butyl-N-methyl-4-[(2-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)hydrazo]-4-oxobutanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[4-[1-[(2-fluorophenyl)methyl]-2,4-dioxo-3-quinazolinyl]phenyl]-N-(2-oxolanylmethyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[6,7-dimethoxy-3-(3-methoxyphenyl)-2,4-dioxo-1-quinazolinyl]-N-(5-methyl-1H-pyrazol-3-yl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-butyl-3-[1-[(2,5-dimethylphenyl)methyl]-2,4-dioxo-3-quinazolinyl]propanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(4-methylphenyl)methyl]-2,4-dioxo-N-(phenylmethyl)-3-prop-2-enyl-7-quinazolinecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[(4-methoxyphenyl)methyl]-N-(3-methoxypropyl)-2,4-dioxo-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[1-(4-bromophenoxy)butyl]-8,9-dimethoxy-3H-[1,2,4]triazolo[1,5-c]quinazoline-5-thione | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152-hqpa | | anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(diethylamino)propyl]-4-[(2-methyl-[1,2,4]triazolo[1,5-c]quinazolin-5-yl)hydrazo]-4-oxobutanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chaetominine | | indole alkaloid;
lactam;
organic heterotetracyclic compound;
quinazolines | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(1-azepanyl)propyl]-3-[(4-methoxyphenyl)methyl]-2,4-dioxo-1H-quinazoline-7-carboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[6-(4-morpholinyl)-4-oxo-3-(2-phenylethyl)-2-quinazolinyl]thio]-N-(2-oxolanylmethyl)acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-[2-(1-piperidinyl)ethyl]-[1,2,4]triazolo[1,5-c]quinazolin-5-yl]thio]-N-[2-(4-sulfamoylphenyl)ethyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-methylphenyl)-5-oxo-N-propyl-8-thiazolo[2,3-b]quinazolinecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-methylphenyl)-5-oxo-8-thiazolo[2,3-b]quinazolinecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zm323881 | | aromatic ether;
benzyl ether;
fluorophenol;
halophenol;
monofluorobenzenes;
organic cation;
quinazolines;
secondary amino compound;
substituted aniline | vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,5-dimethyl-4-isoxazolyl)-N-[(3-methoxyphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,5-dimethyl-4-isoxazolyl)-N-[(2-ethoxyphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[[6-(3,5-dimethyl-4-isoxazolyl)-4-quinazolinyl]amino]methyl]phenyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,5-dimethyl-4-isoxazolyl)-N-[(1-methyl-2-piperidinyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,5-dimethyl-4-isoxazolyl)-N-[1-(2-furanyl)ethyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,5-dimethyl-4-isoxazolyl)-N-[(3-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[2-[(6-chloro-4-quinazolinyl)amino]ethyl]phenol | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ast 1306 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-(phenoxymethyl)-4-quinazolinyl]thio]acetic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| poziotinib | | acrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[5-[5-hydroxy-4-oxo-3-(phenylmethyl)-1,2-dihydroquinazolin-2-yl]-2-methoxyphenyl]methoxy]phenyl]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-furanylmethyl)-N-methyl-6-(1-methyl-5-indolyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2-chlorophenyl)-N-[(3-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methoxyphenyl)-N-[(3-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-[(3-methylphenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2-chlorophenyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-chlorophenyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-pyridinyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methylphenyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1-methyl-5-indolyl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-(2,3-dihydro-1,4-benzodioxin-6-yl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-[(3-fluorophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-chlorophenyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methylphenyl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-(3-pyridinylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-(2-chlorophenyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-(3-pyridinyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-6-(3-furanyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2-chlorophenyl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-chlorophenyl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-methoxyphenyl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(4-methyl-2-thiophenyl)methyl]-6-(3-pyridinyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(2,3-dihydro-1,4-benzodioxin-6-yl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3-furanyl)-N-[(4-methyl-2-thiophenyl)methyl]-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[5-(3-hydroxy-4-oxo-1,2-dihydroquinazolin-2-yl)-2-furanyl]benzonitrile | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[5-(2-fluorophenyl)-2-furanyl]-3-hydroxy-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-hydroxy-2-(5-thiophen-2-yl-2-furanyl)-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[5-(3-fluorophenyl)-2-furanyl]-3-hydroxy-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-hydroxy-2-[5-[4-(trifluoromethyl)phenyl]-2-furanyl]-1,2-dihydroquinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(1,3-benzodioxol-5-yl)-N-methyl-N-(thiophen-2-ylmethyl)-4-quinazolinamine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cp 466722 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| [5-[4-[(5-methyl-2-furanyl)methylamino]-6-quinazolinyl]-2-furanyl]methanol | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| unc 0638 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| unc 0321 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML240 | | aromatic amine;
aromatic ether;
benzimidazoles;
primary amino compound;
quinazolines;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ncgc00242364 | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide | | aromatic ether;
methylpyridines;
olefinic compound;
quinazolines;
secondary amino compound;
secondary carboxamide;
toluenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(3-chloro-4-fluoroanilino)-7-[[(3S)-3-oxolanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(3-chloro-4-fluoroanilino)-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methoxy-n-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nu 1025 | | phenols;
quinazolines | EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[amino-[(6-methoxy-4-methyl-2-quinazolinyl)amino]methylidene]-3-phenylurea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-oxo-2-(trifluoromethyl)-1H-quinazoline-6-carboxylic acid ethyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hydroxyquinazoline | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3,4-dihydro-1H-isoquinolin-2-ylmethyl)-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-methyl-2,3-dihydroindol-1-yl)methyl]-4-oxo-1H-quinazoline-7-carboxylic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[[5,7-bis(ethylamino)-[1,2,4]triazolo[4,3-a][1,3,5]triazin-3-yl]thio]methyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-oxo-1H-quinazolin-2-yl)propanoic acid (3,5-dimethyl-4-isoxazolyl)methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-3-methoxy-N-[(4-oxo-1H-quinazolin-2-yl)methyl]benzamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-cyclopentyl-1-[(4-oxo-1H-quinazolin-2-yl)methyl]-3-(phenylmethyl)urea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,8-dibromo-2-[[[4-(difluoromethoxy)phenyl]methyl-methylamino]methyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(5'-chloro-2'-phosphoryloxyphenyl)-6-chloro-4-(3h)-quinazolinone | | aryl phosphate;
monochlorobenzenes;
quinazolines | fluorochrome | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glycosminine | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(4-oxo-1H-quinazolin-2-yl)methyl]-N-(2-phenylethyl)butanamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-methoxyphenyl)-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(7-methoxy-4-methyl-2-quinazolinyl)amino]-5,6-dimethyl-1H-pyrimidin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-2-[(1H-1,2,4-triazol-5-ylthio)methyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(dimethylamino)methyl]-4-spiro[1,6-dihydrobenzo[h]quinazoline-5,1'-cyclohexane]one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(diethylaminomethyl)-4-spiro[1,6-dihydrobenzo[h]quinazoline-5,1'-cyclohexane]one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[5-(3-chlorophenyl)-2-furanyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(6-ethyl-4-methyl-2-quinazolinyl)amino]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-pyridinylthio)methyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,5-diethyl-2-(2-hydroxyethylamino)-1,6-dihydrobenzo[h]quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(7-chloro-4-oxo-1H-quinazolin-2-yl)methyl]-4-piperidinecarboxamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-ethyl-2-[(4-oxo-1H-quinazolin-2-yl)methylthio]-4-quinazolinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,7-dimethoxy-2-[[methyl-[(4-oxo-1H-quinazolin-2-yl)methyl]amino]methyl]-1H-quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(6-ethyl-4-methyl-2-quinazolinyl)amino]-6-(methoxymethyl)-1H-pyrimidin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,5-diethyl-2-hydrazinyl-1,6-dihydrobenzo[h]quinazolin-4-one | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(3-ethoxypropyl)-1-[(4-oxo-1H-quinazolin-2-yl)methyl]-1-(phenylmethyl)thiourea | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chrysogine | | cyclic amide;
quinazoline alkaloid;
quinazolines;
secondary alcohol;
secondary amide | Aspergillus metabolite;
biological pigment;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(cyclohexylamino)-oxomethyl]-2-[ethyl-[(4-oxo-1H-quinazolin-2-yl)methyl]amino]acetamide | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-[[ethyl-[(4-oxo-1H-quinazolin-2-yl)methyl]amino]methyl]-5-thiazolo[3,2-a]pyrimidinone | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[(6-ethyl-4-oxo-3-prop-2-enyl-2-thieno[2,3-d]pyrimidinyl)thio]methyl]-4-oxo-1H-quinazoline-7-carboxylic acid methyl ester | | quinazolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ARS-1620 | | quinazolines | antineoplastic agent;
antiviral agent;
inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furosemide | | chlorobenzoic acid;
furans;
sulfonamide | environmental contaminant;
loop diuretic;
xenobiotic | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| kinetin | | 6-aminopurines;
furans | cytokinin;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| resmethrin | | cyclopropanecarboxylate ester;
furans | agrochemical;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole | | aromatic primary alcohol;
furans;
indazoles | antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furfuryl alcohol | | furans;
primary alcohol | Maillard reaction product | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furaldehyde | | aldehyde;
furans | Maillard reaction product;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| maleic anhydride | | cyclic dicarboxylic anhydride;
furans | allergen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furan | | furans;
mancude organic heteromonocyclic parent;
monocyclic heteroarene | carcinogenic agent;
hepatotoxic agent;
Maillard reaction product | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methylfuran | | furans;
volatile organic compound | flavouring agent;
fuel;
hepatotoxic agent;
human urinary metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methyl-2-furfural | | aldehyde;
furans | EC 2.2.1.6 (acetolactate synthase) inhibitor;
flavouring agent;
human metabolite;
Maillard reaction product | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-dimethylfuran | | furans | antifungal agent;
bacterial metabolite;
fuel;
fumigant;
human urinary metabolite;
Maillard reaction product;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-nitro-2-furaldehyde | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-methylfuran | | furans;
volatile organic compound | Aspergillus metabolite;
environmental contaminant;
fungal metabolite;
Penicillium metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-acetylfuran | | aromatic ketone;
furans;
methyl ketone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-ethylfuran | | furans;
volatile organic compound | bacterial metabolite;
fragrance;
Maillard reaction product;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furaneol | | cyclic ketone;
enol;
furans | flavouring agent;
fragrance;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diloxanide furoate | | carboxylic ester;
furans;
organochlorine compound;
tertiary carboxamide | antiamoebic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-pentylfuran | | furans | Aspergillus metabolite;
bacterial metabolite;
flavouring agent;
human urinary metabolite;
insect repellent;
plant growth stimulator;
volatile oil component | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fuberidazole | | benzimidazole fungicide;
benzimidazoles;
furans | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furoylglycine | | furans;
N-acylglycine | human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-methyl-1,1-dioxo-1,4-thiazinan-4-yl)-1-(5-nitro-2-furanyl)methanimine | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hydroxy-2-ethyl-5-methyl-3(2h)-furanone | | cyclic ketone;
enol;
furans | Saccharomyces cerevisiae metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| furalaxyl | | alanine derivative;
aromatic amide;
carboxamide;
furans;
methyl ester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-Amino-5-(5-nitro-2-furyl)-1,3,4-thiadiazole | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perillene | | furans;
monoterpenoid | fragrance;
metabolite;
semiochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-diformylfuran | | arenecarbaldehyde;
dialdehyde;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-bis(hydroxymethyl)furan | | diol;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-furandicarboxylic acid | | dicarboxylic acid;
furans | human urinary metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cafestol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nimbin | | acetate ester;
cyclic terpene ketone;
enone;
furans;
limonoid;
methyl ester;
tetracyclic triterpenoid | pesticide;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kahweol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bioresmethrin | | furans;
resmethrin | pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| limonin | | epoxide;
furans;
hexacyclic triterpenoid;
lactone;
limonoid;
organic heterohexacyclic compound | inhibitor;
metabolite;
volatile oil component | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-hydroxymethylfurfural | | arenecarbaldehyde;
furans;
primary alcohol | indicator;
Maillard reaction product | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[[2-furanyl(oxo)methyl]amino]phenyl]-1-isoquinolinecarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2,5-diethoxy-4-[[2-(3-methoxyphenyl)-1-oxoethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[oxo-(2-pyridinylamino)methyl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2,5-dimethoxy-4-[[oxo(thiophen-2-yl)methyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-methoxy-4-[(2-methyl-1-oxopropyl)amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-methoxy-4-[[2-[(3-methyl-4-oxo-2-quinazolinyl)thio]-1-oxoethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-[2-[2-(4-methoxyanilino)-2-oxoethyl]-5-tetrazolyl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-chloro-4-(4-morpholinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(7-methyl-2-oxo-1H-quinolin-3-yl)methyl]-N-phenyl-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-cyclohexyl-3-furan-2-yl-(1,2,4)triazolo(3,4-b)(1,3,4)thiadiazole | | furans;
triazolothiadiazole | Wnt signalling inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3-chlorophenyl)-N-[2-methyl-5-(3-methyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-6-yl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(diethylamino)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[2-benzofuranyl(oxo)methyl]amino]benzoic acid ethyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,4-dichlorophenyl)-N-(2-methylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[2-furanyl(oxo)methyl]amino]benzoic acid propan-2-yl ester | | aromatic amide;
furans;
isopropyl ester;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,5-dimethylphenyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methoxyphenyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-(2,4-dichlorophenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-chloro-4-(1-pyrrolidinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxy-5-[[(5-methyl-2-furanyl)-oxomethyl]amino]benzoic acid | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[[2-furanyl(oxo)methyl]amino]phenyl]-5-nitro-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[(2,5-dimethyl-3-furanyl)-oxomethyl]amino]benzoic acid | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-(4-propan-2-ylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(6-methyl-2-pyridinyl)-5-nitro-2-furancarboxamide | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-bromo-2-fluorophenyl)-2-methyl-3-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[(5-bromo-2-furanyl)-oxomethyl]amino]benzoic acid | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methyl-2-pyridinyl)-5-nitro-2-furancarboxamide | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-chlorophenyl)-5-nitro-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-hydroxyphenyl)-5-methyl-3-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[(1,3-dioxo-5-isoindolyl)oxy]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-N-(2,4,6-trimethylphenyl)-3-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[(5-bromo-2-furanyl)-oxomethyl]amino]-2-methylbenzoic acid | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[oxo-(3-pyridinylmethylamino)methyl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-chloro-N-[4-[(3,4-dimethyl-5-isoxazolyl)sulfamoyl]phenyl]-3-methyl-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methoxyphenyl)-N-thiophen-2-ylsulfonyl-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(2,4-dichlorophenoxy)methyl]-N-(2-fluorophenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-bromophenyl)-N-(2-methoxyphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-[4-(4-methyl-1-piperazinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[2-furanyl(oxo)methyl]amino]phenyl]-1,3-benzodioxole-5-carboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-nitro-N-[4-(2-oxazolo[4,5-b]pyridinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[[[oxo(thiophen-2-yl)methyl]amino]-sulfanylidenemethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-chloro-4-[[2-furanyl(oxo)methyl]amino]phenyl]-2,3-dihydro-1,4-benzodioxin-6-carboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2,5-diethoxy-4-[[(2-methylpropylamino)-sulfanylidenemethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2,5-diethoxy-4-[[(2-furanylmethylamino)-sulfanylidenemethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-[3-chloro-2-(1-pyrrolidinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methyl-N-[2-(methylthio)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propanoic acid [4-[[2-furanyl(oxo)methyl]amino]phenyl] ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[4-(1-oxopropyl)-1-piperazinyl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[[2-(2-bromo-4,6-dimethylphenoxy)-1-oxoethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2-chlorophenyl)-N-phenyl-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(4-morpholinyl)phenyl]-5-(2-nitrophenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-tert-butyl-N-[2-(cyclopentylamino)-2-oxoethyl]-N-(2,5-dimethylphenyl)-3-methyl-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-chlorophenyl)-N-[4-(4-methyl-1-piperazinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[(1-oxohexylamino)-sulfanylidenemethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-furanyl(oxo)methyl]amino]benzoic acid [2-(cyclohexylmethylamino)-2-oxoethyl] ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-acetylphenyl)-5-[(phenylthio)methyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methoxyphenyl)-5-(phenoxymethyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[(2-methyl-3-furanyl)-oxomethyl]amino]benzoic acid butyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[[5-[(4-chloro-3,5-dimethyl-1-pyrazolyl)methyl]-2-furanyl]-oxomethyl]amino]benzoic acid propan-2-yl ester | | aromatic amide;
furans;
isopropyl ester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-N-(2,3,4,5,6-pentafluorophenyl)-3-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-(2-phenylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-[4-[(4-chlorophenyl)-oxomethyl]-1-piperazinyl]phenyl]-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[[2-(2,6-dimethylphenoxy)-1-oxoethyl]amino]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-[2-(4-methyl-1-piperazinyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[(2-methyl-3-furanyl)-oxomethyl]amino]benzoic acid | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[[5-(3-chlorophenyl)-2-furanyl]-oxomethyl]amino]benzoic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-cyano-4,5-bis(4-methoxyphenyl)-2-furanyl]acetamide | | furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-furanyl(oxo)methyl]amino]-4,5-dimethoxybenzoic acid [2-[(3,5-dichloro-2-pyridinyl)amino]-2-oxoethyl] ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-chloro-2-fluorophenyl)-3-(methoxymethyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[2-[[2-[[2-furanyl(oxo)methyl]amino]phenyl]-oxomethoxy]-1-oxoethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid ethyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[5-[anilino(oxo)methyl]-2-furanyl]-2-thiophenecarboxylic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-morpholinylsulfonyl)-N-[4-(trifluoromethoxy)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[[[5-(2-chlorophenyl)-2-(trifluoromethyl)-3-furanyl]-oxomethyl]amino]-2-(4-morpholinyl)benzoic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-morpholinyl)-5-[[oxo-[2-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]-3-furanyl]methyl]amino]benzoic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[[[5-(4-chlorophenyl)-2-(trifluoromethyl)-3-furanyl]-oxomethyl]amino]-2-(4-morpholinyl)benzoic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[(5-tert-butyl-2-methyl-3-furanyl)-oxomethyl]amino]-4,5-dimethoxybenzoic acid methyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| S-[5-(trifluoromethyl)-4H-1,2,4-triazol-3-yl] 5-(phenylethynyl)furan-2-carbothioate | | acetylenic compound;
furans;
organofluorine compound;
thioester;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methyl-2-nitrophenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-hydroxy-5-methylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alanyl-alanyl-alanyl-alanine, (d-ala-l-ala-l-ala-l-ala)-isomer | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[[4-(4-methoxyphenyl)-4-oxanyl]methylamino]-oxomethyl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(4-acetyl-1-piperazinyl)-3-chlorophenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[[[2-[[2-furanyl(oxo)methyl]amino]phenyl]-oxomethoxy]methyl]-3-methyl-1H-pyrrole-2,4-dicarboxylic acid diethyl ester | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ranitidine | | C-nitro compound;
furans;
organic sulfide;
tertiary amino compound | anti-ulcer drug;
drug allergen;
environmental contaminant;
H2-receptor antagonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-deacetylgedunin | | cyclic terpene ketone;
delta-lactone;
enone;
epoxide;
furans;
limonoid;
pentacyclic triterpenoid | anti-inflammatory agent;
antimalarial;
metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-methyl-5-nitro-N-(phenylmethyl)-2-furancarboxamide | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[5,6-bis(4-methoxyphenyl)-4-furo[2,3-d]pyrimidinyl]amino]-1-propanol | | furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-Butan-2-ylphenyl)-N-[2-(cyclopentylamino)-2-oxo-1-pyridin-3-ylethyl]furan-2-carboxamide | | aromatic amide;
furans | anticoronaviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-(Cyclopentylamino)-2-oxo-1-pyridin-3-ylethyl]-N-(4-propan-2-ylphenyl)furan-2-carboxamide | | aromatic amide;
furans | anticoronaviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,4-dimethoxyphenyl)-3-[[2-(2-methoxyphenoxy)-1-oxoethyl]amino]-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,4-dimethoxyphenyl)-3-[[2-furanyl(oxo)methyl]amino]-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[5-[(2-methylphenoxy)methyl]-1,2,4-oxadiazol-3-yl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-chlorophenyl)-5-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylsulfonyl)-3-methyl-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[2-furanyl(oxo)methyl]amino]-N-(4-methoxyphenyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-chlorophenyl)-5-(1,4-dioxa-8-azaspiro[4.5]decan-8-ylsulfonyl)-3-methyl-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,3-dimethylphenyl)-3-methyl-5-(4-morpholinylsulfonyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3,4-dimethylphenyl)-3-methyl-5-(4-morpholinylsulfonyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-amino-7-methyl-4-(5-nitro-2-furanyl)-5-oxo-4H-pyrano[3,2-c]pyran-3-carbonitrile | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nefurthiazole | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,4-dimethylphenyl)-3-methyl-5-(4-morpholinylsulfonyl)-2-benzofurancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2-chlorophenyl)-N-(4-methoxyphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hydroxy-5-methyl-3(2h)-furanone | | cyclic ketone;
enol;
furans | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-bromo-N-[4-[5-(2-methylphenyl)-1,2,4-oxadiazol-3-yl]phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-methoxyphenyl)-5-[2-(trifluoromethyl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| atractylodin | | furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cefuroxime | | 3-(carbamoyloxymethyl)cephalosporin;
furans;
oxime O-ether | drug allergen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-methyl-1-naphthalenyl)-N-phenyl-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nitrovin | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dihydroxymethylfuratrizine | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nifurpirinol | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salannin | | acetate ester;
furans;
limonoid;
methyl ester;
organic heteropentacyclic compound | antifeedant;
insect growth regulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nidroxyzone | | C-nitro compound;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-deacetylnimbin | | cyclic terpene ketone;
diester;
enone;
furans;
limonoid;
methyl ester;
tetracyclic triterpenoid | antifeedant;
insect growth regulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azadirone | | acetate ester;
cyclic terpene ketone;
furans;
limonoid;
tetracyclic triterpenoid | antineoplastic agent;
antiplasmodial drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gedunin | | acetate ester;
enone;
epoxide;
furans;
lactone;
limonoid;
organic heteropentacyclic compound;
pentacyclic triterpenoid | antimalarial;
antineoplastic agent;
Hsp90 inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azadiradione | | acetate ester;
cyclic terpene ketone;
furans;
limonoid;
tetracyclic triterpenoid | anti-inflammatory agent;
antimycobacterial drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvileucalin b | | bridged compound;
diterpenoid;
furans;
gamma-lactone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,5-difluorophenyl)-N-(2,6-dimethylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,5-dichlorophenyl)-N-(2,6-dimethoxyphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,5-dichlorophenyl)-N-[2,6-di(propan-2-yl)phenyl]-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,5-dichlorophenyl)-N-(2,6-diethylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2,6-dimethylphenyl)-5-(4-methyl-3-thiophenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(1R)-2-(tert-butylamino)-2-oxo-1-(3-pyridinyl)ethyl]-N-(4-tert-butylphenyl)-2-furancarboxamide | | aromatic amide;
furans | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epoxyazadiradione | | acetate ester;
cyclic terpene ketone;
epoxide;
furans;
limonoid;
pentacyclic triterpenoid | anti-inflammatory agent;
insecticide;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wilforgine | | acetate ester;
dihydroagarofuran sesquiterpenoid;
furans;
macrocyclic lactone;
organic heteropentacyclic compound;
pyridine alkaloid | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benefin | | C-nitro compound;
organofluorine compound;
substituted aniline;
tertiary amino compound | agrochemical;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| celecoxib | | organofluorine compound;
pyrazoles;
sulfonamide;
toluenes | cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| cgs 12066 | | N-arylpiperazine;
organofluorine compound;
pyrroloquinoxaline | serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| citalopram | | 2-benzofurans;
cyclic ether;
nitrile;
organofluorine compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflunisal | | monohydroxybenzoic acid;
organofluorine compound | non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| droperidol | | aromatic ketone;
benzimidazoles;
organofluorine compound | anaesthesia adjuvant;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enflurane | | ether;
organochlorine compound;
organofluorine compound | anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carbonyl cyanide p-trifluoromethoxyphenylhydrazone | | aromatic ether;
hydrazone;
nitrile;
organofluorine compound | ATP synthase inhibitor;
geroprotector;
ionophore | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flecainide | | aromatic ether;
monocarboxylic acid amide;
organofluorine compound;
piperidines | anti-arrhythmia drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flucytosine | | aminopyrimidine;
nucleoside analogue;
organofluorine compound;
pyrimidine antifungal drug;
pyrimidone | prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fludiazepam | | 1,4-benzodiazepinone;
organochlorine compound;
organofluorine compound | anxiolytic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flufenamic acid | | aromatic amino acid;
organofluorine compound | antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluphenazine | | N-alkylpiperazine;
organofluorine compound;
phenothiazines | anticoronaviral agent;
dopaminergic antagonist;
phenothiazine antipsychotic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flumazenil | | ethyl ester;
imidazobenzodiazepine;
organofluorine compound | antidote to benzodiazepine poisoning;
GABA antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flumequine | | 3-oxo monocarboxylic acid;
organofluorine compound;
pyridoquinoline;
quinolone antibiotic | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluorouracil | | nucleobase analogue;
organofluorine compound | antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic | 2010 | 2023 | 7.6 | low | 1 | 0 | 0 | 1 | 4 | 2 |
| fluphenazine depot | | decanoate ester;
N-alkylpiperazine;
organofluorine compound;
phenothiazines | dopaminergic antagonist;
phenothiazine antipsychotic drug;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vanoxerine | | ether;
N-alkylpiperazine;
organofluorine compound;
tertiary amino compound | dopamine uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| haloperidol | | aromatic ketone;
hydroxypiperidine;
monochlorobenzenes;
organofluorine compound;
tertiary alcohol | antidyskinesia agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| halothane | | haloalkane;
organobromine compound;
organochlorine compound;
organofluorine compound | inhalation anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoflurane | | organofluorine compound | inhalation anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mefloquine hydrochloride | | organofluorine compound;
piperidines;
quinolines;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxyflurane | | ether;
organochlorine compound;
organofluorine compound | hepatotoxic agent;
inhalation anaesthetic;
nephrotoxic agent;
non-narcotic analgesic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ofloxacin | | 3-oxo monocarboxylic acid;
N-arylpiperazine;
N-methylpiperazine;
organofluorine compound;
oxazinoquinoline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pantoprazole | | aromatic ether;
benzimidazoles;
organofluorine compound;
pyridines;
sulfoxide | anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pipamperone | | aromatic ketone;
bipiperidines;
monocarboxylic acid amide;
organofluorine compound;
tertiary amino compound | dopaminergic antagonist;
first generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| risperidone | | 1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine | alpha-adrenergic antagonist;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
H1-receptor antagonist;
psychotropic drug;
second generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ritanserin | | organofluorine compound;
piperidines;
thiazolopyrimidine | antidepressant;
antipsychotic agent;
anxiolytic drug;
dopaminergic antagonist;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sb 220025 | | aminopyrimidine;
imidazoles;
organofluorine compound;
piperidines | angiogenesis inhibitor;
anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sb 202190 | | imidazoles;
organofluorine compound;
phenols;
pyridines | apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sevoflurane | | ether;
organofluorine compound | central nervous system depressant;
inhalation anaesthetic;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoroacetic acid | | haloacetic acid;
organofluorine compound | EC 4.2.1.3 (aconitate hydratase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiperone | | aromatic ketone;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound | alpha-adrenergic antagonist;
antipsychotic agent;
dopaminergic antagonist;
psychotropic drug;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gatifloxacin | | N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone | antiinfective agent;
antimicrobial agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tosufloxacin | | 1,8-naphthyridine derivative;
amino acid;
aminopyrrolidine;
monocarboxylic acid;
organofluorine compound;
primary amino compound;
quinolone antibiotic;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifluoperazine | | N-alkylpiperazine;
N-methylpiperazine;
organofluorine compound;
phenothiazines | antiemetic;
calmodulin antagonist;
dopaminergic antagonist;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor;
phenothiazine antipsychotic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triflupromazine | | organofluorine compound;
phenothiazines;
tertiary amine | anticoronaviral agent;
antiemetic;
dopaminergic antagonist;
first generation antipsychotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zardaverine | | organofluorine compound;
pyridazinone | anti-asthmatic drug;
bronchodilator agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
peripheral nervous system drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| floxuridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifluridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
EC 2.1.1.45 (thymidylate synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dinitrofluorobenzene | | C-nitro compound;
organofluorine compound | agrochemical;
allergen;
chromatographic reagent;
EC 2.7.3.2 (creatine kinase) inhibitor;
protein-sequencing agent;
spectrophotometric reagent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,1-difluoroethylene | | olefinic compound;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,1,1-trifluoro-2-chloroethane | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chloropentafluoroethane | | organochlorine compound;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-fluoroadenosine | | adenosines;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perfluorotributylamine | | organofluorine compound | blood substitute;
greenhouse gas;
solvent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluorouridine | | organofluorine compound;
uridines | mutagen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluorotryptophan | | non-proteinogenic alpha-amino acid;
organofluorine compound;
tryptophan derivative | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromochlorodifluoromethane | | one-carbon compound;
organobromine compound;
organochlorine compound;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| difluoroacetic acid | | monocarboxylic acid;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluroxene | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3,4,5,6-pentafluorobenzyl alcohol | | benzyl alcohols;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-fluoroadenine | | organofluorine compound;
purines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-dichlorofluoromethylthio-n',n'-dimethyl-n-p-tolylsulfamide | | organochlorine compound;
organofluorine compound;
phenylsulfamide fungicide;
sulfamides | antifungal agrochemical;
genotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hexafluoroisopropanol | | organofluorine compound;
secondary alcohol | drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dichlofluanid | | organochlorine compound;
organofluorine compound;
phenylsulfamide fungicide;
sulfamides | acaricide;
antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pimozide | | benzimidazoles;
heteroarylpiperidine;
organofluorine compound | antidyskinesia agent;
dopaminergic antagonist;
first generation antipsychotic;
H1-receptor antagonist;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluorocytidine | | cytidines;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxifluridine | | organofluorine compound;
pyrimidine 5'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fludarabine phosphate | | nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate | antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flubendazole | | aromatic ketone;
benzimidazoles;
carbamate ester;
organofluorine compound | antinematodal drug;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flunixin | | aminopyridine;
organofluorine compound;
pyridinemonocarboxylic acid | antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| desflurane | | organofluorine compound | inhalation anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| paroxetine | | aromatic ether;
benzodioxoles;
organofluorine compound;
piperidines | antidepressant;
anxiolytic drug;
hepatotoxic agent;
P450 inhibitor;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acifluorfen | | aromatic ether;
benzoic acids;
C-nitro compound;
monocarboxylic acid;
organochlorine compound;
organofluorine compound | agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triflumuron | | aromatic ether;
benzoylurea insecticide;
monochlorobenzenes;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4,5-amino-3,5-dichloro-6-fluoro-2-pyridinyloxyacetic acid | | aminopyridine;
aromatic ether;
monocarboxylic acid;
organochlorine compound;
organofluorine compound | environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| haloxyfop | | aromatic ether;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
pyridines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluazifop-butyl | | aromatic ether;
carboxylic ester;
organofluorine compound;
pyridines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fomesafen | | aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-sulfonylcarboxamide;
organofluorine compound;
phenols | agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| temafloxacin | | amino acid;
monocarboxylic acid;
N-arylpiperazine;
organofluorine compound;
quinolone antibiotic;
quinolone;
secondary amino compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sertindole | | heteroarylpiperidine;
imidazolidinone;
organochlorine compound;
organofluorine compound;
phenylindole | alpha-adrenergic antagonist;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemcitabine hydrochloride | | hydrochloride;
organofluorine compound | anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemcitabine | | organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic | 2013 | 2023 | 6.6 | low | 6 | 0 | 0 | 0 | 13 | 3 |
| emtricitabine | | monothioacetal;
nucleoside analogue;
organofluorine compound;
pyrimidone | antiviral drug;
HIV-1 reverse transcriptase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| capecitabine | | carbamate ester;
cytidines;
organofluorine compound | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-fluorofentanyl | | monocarboxylic acid amide;
organofluorine compound;
piperidines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| efavirenz | | acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound | antiviral drug;
HIV-1 reverse transcriptase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| heptafluorobutyric anhydride | | acyclic carboxylic anhydride;
organofluorine compound | chromatographic reagent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perfluorotripropylamine | | organofluorine compound | blood substitute | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-fluoropyruvate | | 2-oxo monocarboxylic acid;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiramide | | aromatic ether;
azaspiro compound;
organofluorine compound;
piperidines;
tertiary amino compound | dopaminergic antagonist;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flunoxaprofen | | 1,3-benzoxazoles;
monocarboxylic acid;
organofluorine compound | antirheumatic drug;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
protein kinase C agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| halopropane | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enrofloxacin | | cyclopropanes;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone | antibacterial agent;
antimicrobial agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flurithromycin | | cyclic ketone;
erythromycin derivative;
organofluorine compound;
semisynthetic derivative | antibacterial drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nebivolol | | chromanes;
diol;
organofluorine compound;
secondary alcohol;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hp 873 | | 1,2-benzoxazoles;
aromatic ether;
aromatic ketone;
methyl ketone;
monoamine;
organofluorine compound;
piperidines;
tertiary amino compound | dopaminergic antagonist;
second generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluphenacur | | aromatic ether;
benzoylurea insecticide;
dichlorobenzene;
N-acylurea;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nucleocidin | | 6-aminopurines;
adenosines;
diol;
organofluorine compound;
sulfamate ester | antibacterial agent;
bacterial metabolite;
nucleoside antibiotic;
protein synthesis inhibitor;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoroacetaldehyde | | aldehyde;
organofluorine compound | cardiotoxic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fc 75 | | alkyltetrahydrofuran;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetraconazole | | dichlorobenzene;
ether;
organofluorine compound;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hei 712 | | organofluorine compound;
quinolone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2,4-dichloro-5-(4-(difluoromethyl)-4,5-dihydro-3-methyl-5-oxo-1h-1,2,4-triazol-1-yl)phenyl)methanesulfonamide | | dichlorobenzene;
organofluorine compound;
sulfonamide;
triazoles | agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thifluzamide | | 1,3-thiazoles;
anilide fungicide;
aromatic amide;
aromatic ether;
dibromobenzene;
organofluorine compound | antifungal agrochemical;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fludioxonil | | benzodioxoles;
nitrile;
organofluorine compound;
pyrroles | androgen antagonist;
antifungal agrochemical;
estrogen receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cloransulam-methyl | | methyl ester;
monochlorobenzenes;
organofluorine compound;
sulfonamide;
triazolopyrimidines | agrochemical;
EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluazifop | | aromatic ether;
monocarboxylic acid;
organofluorine compound;
pyridines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dithiopyr | | organofluorine compound;
pyridines;
thioester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s 53482 | | benzoxazine;
dicarboximide;
organofluorine compound;
terminal acetylenic compound | agrochemical;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clodinafop-propargyl | | aromatic ether;
carboxylic ester;
organochlorine compound;
organofluorine compound;
propyzamide;
pyridines | agrochemical;
EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triflusulfuron-methyl | | 1,3,5-triazines;
aromatic ether;
benzoate ester;
methyl ester;
N-sulfonylurea;
organofluorine compound;
tertiary amino compound | agrochemical;
EC 2.2.1.6 (acetolactate synthase) inhibitor;
proherbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| novaluron | | aromatic ether;
benzoylurea insecticide;
monochlorobenzenes;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fulvestrant | | 17beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide | antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyfluthrin | | aromatic ether;
cyclopropanecarboxylate ester;
nitrile;
organochlorine compound;
organofluorine compound | agrochemical;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoromethyl 2,2-difluoro-1-(trifluoromethyl)vinyl ether | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| florfenicol | | organochlorine compound;
organofluorine compound;
secondary alcohol;
secondary carboxamide;
sulfone | antimicrobial agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| paliperidone | | 1,2-benzoxazoles;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 58125 | | organofluorine compound;
pyrazoles;
sulfone | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofarabine | | adenosines;
organofluorine compound | antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluoromethylornithine | | organofluorine compound;
ornithine derivative | EC 2.6.1.13 (ornithine aminotransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nitroflurbiprofen | | biphenyls;
carboxylic ester;
nitrate ester;
organofluorine compound | cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
geroprotector;
non-steroidal anti-inflammatory drug;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ezogabine | | carbamate ester;
organofluorine compound;
secondary amino compound;
substituted aniline | anticonvulsant;
potassium channel modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| garenoxacin | | aromatic ether;
cyclopropanes;
isoindoles;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone antibiotic | antibacterial drug;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluorowillardiine | | L-alanine derivative;
non-proteinogenic L-alpha-amino acid;
organofluorine compound | AMPA receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perfluoro-n-methyldecahydroisoquinoline | | organofluorine compound | blood substitute | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fc 80 | | alkyltetrahydrofuran;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ezetimibe | | azetidines;
beta-lactam;
organofluorine compound | anticholesteremic drug;
antilipemic drug;
antimetabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluorouridine 5'-phosphate | | organofluorine compound;
pyrimidine ribonucleoside 5'-monophosphate | drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cox 189 | | amino acid;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
secondary amino compound | cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jte 522 | | 1,3-oxazoles;
organofluorine compound;
sulfonamide | cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifluoromethionine | | L-methionine derivative;
non-proteinogenic L-alpha-amino acid;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cimicoxib | | aromatic ether;
imidazoles;
organochlorine compound;
organofluorine compound;
sulfonamide | cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflomotecan | | epsilon-lactone;
organic heteropentacyclic compound;
organofluorine compound;
organonitrogen heterocyclic compound;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5',5',5'-trifluoroleucine | | leucine derivative;
non-proteinogenic alpha-amino acid;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sorbinil | | azaspiro compound;
chromanes;
imidazolidinone;
organofluorine compound;
oxaspiro compound | antioxidant;
EC 1.1.1.21 (aldehyde reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| linezolid | | acetamides;
morpholines;
organofluorine compound;
oxazolidinone | antibacterial drug;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2'-deoxy-2-fluoroadenosine | | adenosines;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | | 6-aminopurines;
acetylenic compound;
methoxybenzenes;
monochlorobenzenes;
organofluorine compound | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| roflumilast | | aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound | anti-asthmatic drug;
phosphodiesterase IV inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| posaconazole | | aromatic ether;
conazole antifungal drug;
N-arylpiperazine;
organofluorine compound;
oxolanes;
triazole antifungal drug;
triazoles | trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| efinaconazole | | conazole antifungal drug;
olefinic compound;
organofluorine compound;
piperidines;
tertiary alcohol;
tertiary amino compound;
triazole antifungal drug | EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| favipiravir | | hydroxypyrazine;
organofluorine compound;
primary carboxamide | anticoronaviral agent;
antiviral drug;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ck-0944666 | | benzamides;
indoles;
organofluorine compound | actin polymerisation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3-Chloro-2-fluorophenyl)-2,3-dihydroisothiazol-3-one | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[(3-fluorophenyl)methyl-(3-pyridinylmethyl)amino]-4-oxobutanoic acid | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| transfluthrin | | carboxylic ester;
cyclopropanes;
organochlorine compound;
organofluorine compound | pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-fluorophenyl)-3H-thiazole-2-thione | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-chlorophenyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(4-fluorophenyl)methyl]-2-thiophen-2-ylacetamide | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(cycloheptylideneamino)-3-(4-fluorophenyl)thiourea | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-fluorophenyl)-5-phenyl-4-thieno[2,3-d][1,3]oxazinone | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac | | monocarboxylic acid;
organofluorine compound;
sulfoxide | analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-cyano-N'-(2-fluorophenyl)carbamimidothioic acid [2-(tert-butylamino)-2-oxoethyl] ester | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-fluorobenzyl)urea | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N1-(3-chloro-4-fluorophenyl)-2-(methylthio)acetamide | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethyl 1-[4-(4-chlorobenzenesulfonamido)phenyl]-5-(trifluoromethyl)pyrazole-4-carboxylate | | ethyl ester;
monochlorobenzenes;
organofluorine compound;
pyrazoles;
sulfonamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[1-(4-fluorophenyl)ethyl]-3-thiophen-2-yl-1H-1,2,4-triazole-5-thione | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(4-fluorophenyl)-1-cyclopentanecarboxylic acid [2-(2,6-dimethyl-4-morpholinyl)-2-oxoethyl] ester | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deracoxib | | organofluorine compound;
pyrazoles;
sulfonamide | cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline | | organic heterotricyclic compound;
organofluorine compound;
pyridines;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(4-fluorophenyl)-N-methyl-3,4-dihydro-1H-pyrrolo[1,2-a]pyrazine-2-carbothioamide | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-[3-(4-fluorophenyl)-5-thiophen-2-yl-3,4-dihydropyrazol-2-yl]-2-oxoethyl]thio]acetic acid butyl ester | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 560 | | aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(2-fluorophenyl)methyl]-4-pyrazolamine | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[2,2-dichloro-1-(3-fluoro-4-methylphenyl)ethyl]-1,1-bis(phenylmethyl)urea | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 60-0175 | | indoles;
organochlorine compound;
organofluorine compound;
primary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jtk-303 | | aromatic ether;
monochlorobenzenes;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone | HIV-1 integrase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arachidonyltrifluoromethane | | fatty acid derivative;
ketone;
olefinic compound;
organofluorine compound | EC 3.1.1.4 (phospholipase A2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyhalothrin | | aromatic ether;
cyclopropanecarboxylate ester;
nitrile;
organochlorine compound;
organofluorine compound | agrochemical;
pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac sulfide | | aryl sulfide;
monocarboxylic acid;
organofluorine compound | antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bw b70c | | aromatic ether;
hydroxamic acid;
organofluorine compound;
ureas | EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid | | dihydroxy monocarboxylic acid;
indoles;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac sulfone | | monocarboxylic acid;
organofluorine compound;
sulfone | apoptosis inducer;
cyclooxygenase 2 inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clodinafop | | aromatic ether;
monocarboxylic acid;
organochlorine compound;
organofluorine compound;
pyridines | EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor;
phenoxy herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | | organic heterotetracyclic compound;
organofluorine compound | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| z-val-ala-asp(ome)-fluoromethylketone | | carbamate ester;
organofluorine compound;
tripeptide | apoptosis inhibitor;
protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| robenacoxib | | aromatic amino acid;
monocarboxylic acid;
organofluorine compound;
phenylacetic acids;
secondary amino compound | cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acrinathrin | | cyclopropanecarboxylate ester;
organofluorine compound | pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bifenthrin | | carboxylic ester;
cyclopropanecarboxylate ester;
cyclopropanes;
organochlorine compound;
organofluorine compound | pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| netupitant | | aminopyridine;
monocarboxylic acid amide;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
toluenes | antiemetic;
neurokinin-1 receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flibanserin | | benzimidazoles;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound | antidepressant;
serotonergic agonist;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ru 58668 | | 17beta-hydroxy steroid;
3-hydroxy steroid;
aromatic ether;
organofluorine compound;
sulfone | anti-estrogen;
antineoplastic agent;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nepicastat | | 1,3-dihydroimidazole-2-thiones;
organofluorine compound;
primary amino compound;
tetralins | EC 1.14.17.1 (dopamine beta-monooxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gw 501516 | | 1,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound | carcinogenic agent;
PPARbeta/delta agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| noviflumuron | | aromatic ether;
benzoylurea insecticide;
dichlorobenzene;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flonicamid | | nitrile;
organofluorine compound;
pyridinecarboxamide | environmental contaminant;
insecticide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide | | organofluorine compound;
pyrazoles;
sulfonamide | cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| paliperidone palmitate | | 1,2-benzoxazoles;
fatty acid ester;
heteroarylpiperidine;
organofluorine compound;
pyridopyrimidine | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cangrelor | | adenosine 5'-phosphate;
aryl sulfide;
nucleoside triphosphate analogue;
organochlorine compound;
organofluorine compound;
secondary amino compound | P2Y12 receptor antagonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tafluprost | | isopropyl ester;
organofluorine compound;
prostaglandins Falpha | prostaglandin receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ticagrelor | | aryl sulfide;
hydroxyether;
organofluorine compound;
secondary amino compound;
triazolopyrimidines | P2Y12 receptor antagonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| am 694 | | aromatic ketone;
indoles;
organofluorine compound;
organoiodine compound;
synthetic cannabinoid | cannabinoid receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rucaparib | | azepinoindole;
caprolactams;
organofluorine compound;
secondary amino compound | antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| NNC 55-0396 (free base) | | benzimidazoles;
cyclopropanecarboxylate ester;
organofluorine compound;
tertiary amino compound;
tetralins | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osu 03012 | | antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vorapaxar | | carbamate ester;
lactone;
naphthofuran;
organofluorine compound;
pyridines | cardiovascular drug;
platelet aggregation inhibitor;
protease-activated receptor-1 antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 6244 | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rolapitant | | azaspiro compound;
ether;
organofluorine compound;
piperidines;
pyrrolidin-2-ones | antiemetic;
neurokinin-1 receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| r-138727 | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoxastrobin | | aromatic ether;
dioxazine;
monochlorobenzenes;
organofluorine compound;
oxime O-ether;
pyrimidines;
strobilurin antifungal agent | antifungal agrochemical;
mitochondrial cytochrome-bc1 complex inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flumorph | | aromatic ether;
enamide;
morpholines;
organofluorine compound;
tertiary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluopicolide | | benzamide fungicide;
benzamides;
dichlorobenzene;
monochloropyridine;
organofluorine compound | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gamendazole | | alpha,beta-unsaturated monocarboxylic acid;
dichlorobenzene;
indazoles;
olefinic compound;
organofluorine compound | antispermatogenic agent;
eukaryotic translation elongation factor 1alpha 1 inhibitor;
Hsp90 inhibitor;
synthetic oral contraceptive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tedizolid | | carbamate ester;
organofluorine compound;
oxazolidinone;
primary alcohol;
pyridines;
tetrazoles | antimicrobial agent;
drug metabolite;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rx-3117 | | organofluorine compound;
primary allylic alcohol;
triol | antimetabolite;
antineoplastic agent;
apoptosis inducer;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| picoxystrobin | | aromatic ether;
enoate ester;
enol ether;
methoxyacrylate strobilurin antifungal agent;
organofluorine compound;
pyridines | antifungal agrochemical;
mitochondrial cytochrome-bc1 complex inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bay 63-2521 | | aminopyrimidine;
carbamate ester;
organofluorine compound;
pyrazolopyridine | antihypertensive agent;
soluble guanylate cyclase activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| penthiopyrad | | aromatic amide;
organofluorine compound;
pyrazoles;
thiophenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tedizolid phosphate | | carbamate ester;
organofluorine compound;
oxazolidinone;
phosphate monoester;
pyridines;
tetrazoles | antimicrobial agent;
prodrug;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tavaborole | | benzoxaborole;
organofluorine compound | antifungal agent;
EC 6.1.1.4 (leucine--tRNA ligase) inhibitor;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tembotrione | | aromatic ketone;
beta-triketone;
cyclic ketone;
ether;
monochlorobenzenes;
organofluorine compound;
sulfone | agrochemical;
carotenoid biosynthesis inhibitor;
EC 1.13.11.27 (4-hydroxyphenylpyruvate dioxygenase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| finafloxacin | | cyclopropanes;
monocarboxylic acid;
nitrile;
organofluorine compound;
quinolone;
secondary amino compound;
tertiary amino compound | antibacterial drug;
antimicrobial agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | | aminopyridine;
aromatic ether;
dichlorobenzene;
organofluorine compound;
pyrazolylpiperidine;
racemate | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zstk474 | | benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifloxystrobin | | methoxyiminoacetate strobilurin antifungal agent;
methyl ester;
organofluorine compound;
oxime O-ether | antifungal agrochemical;
mitochondrial cytochrome-bc1 complex inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-fluoro-1,3-dimethyl-N-[2-(4-methylpentan-2-yl)phenyl]pyrazole-4-carboxamide | | aromatic amide;
organofluorine compound;
pyrazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2-(1,1'-bicyclopropyl)-2-ylphenyl)-3-(difluoromethyl)-1-methyl-1h-pyrazole-4-carboxamide | | aromatic amide;
cyclopropanes;
organofluorine compound;
pyrazoles;
ring assembly | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trametinib | | acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| butafenacil | | benzoate ester;
diester;
monochlorobenzenes;
olefinic compound;
organofluorine compound | EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bgt226 | | aromatic ether;
imidazoquinoline;
N-arylpiperazine;
organofluorine compound;
pyridines | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| buparlisib | | aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lumacaftor | | aromatic amide;
benzodioxoles;
benzoic acids;
cyclopropanes;
organofluorine compound;
pyridines | CFTR potentiator;
orphan drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro5126766 | | aryloxypyrimidine;
coumarins;
organofluorine compound;
pyridines;
sulfamides | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulfoxaflor | | nitrile;
organofluorine compound;
pyridines;
sulfoximide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 7545 | | benzamides;
monochlorobenzenes;
organofluorine compound;
secondary carboxamide;
sulfone;
tertiary alcohol;
tertiary carboxamide | EC 2.7.11.2 - [pyruvate dehydrogenase (acetyl-transferring)] kinase inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ph 797804 | | aromatic ether;
benzamides;
organobromine compound;
organofluorine compound;
pyridone | anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lde225 | | aminopyridine;
aromatic ether;
benzamides;
biphenyls;
morpholines;
organofluorine compound;
tertiary amino compound | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dafadine D | | aromatic amide;
aromatic ether;
isoxazoles;
N-acylpiperidine;
organofluorine compound;
pyridines | P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| canagliflozin | | C-glycosyl compound;
organofluorine compound;
thiophenes | hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| florbetapir f 18 | | (18)F radiopharmaceutical;
aromatic ether;
organofluorine compound;
pyridines;
substituted aniline | radioactive imaging agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| navitoclax | | aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dcc-2036 | | organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cabozantinib | | aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pexidartinib | | aminopyridine;
organochlorine compound;
organofluorine compound;
pyrrolopyridine;
secondary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| TAK-580 | | 1,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dabrafenib | | 1,3-thiazoles;
aminopyrimidine;
organofluorine compound;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sofosbuvir | | isopropyl ester;
L-alanyl ester;
nucleotide conjugate;
organofluorine compound;
phosphoramidate ester | antiviral drug;
hepatitis C protease inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| [5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid | | organofluorine compound | non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 1 | | N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 4929097 | | dibenzoazepine;
dicarboxylic acid diamide;
lactam;
organofluorine compound | EC 3.4.23.46 (memapsin 2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 2 | | aminopyridine;
organofluorine compound;
primary amino compound;
pyridoquinoline | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2656157 | | biaryl;
indoles;
methylpyridines;
organofluorine compound;
pyrrolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
PERK inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl]-3-(difluoromethyl)-1-methylpyrazole-4-carboxamide | | aromatic amide;
bridged compound;
olefinic compound;
organochlorine compound;
organofluorine compound;
pyrazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vericiguat | | aminopyrimidine;
carbamate ester;
organofluorine compound;
pyrazolopyridine | antihypertensive agent;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pacific blue succinimidyl ester | | hydroxycoumarin;
N-hydroxysuccinimide ester;
organofluorine compound | fluorochrome | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(difluoromethyl)-N-methoxy-1-methyl-N-[1-(2,4,6-trichlorophenyl)propan-2-yl]pyrazole-4-carboxamide | | aromatic amide;
monocarboxylic acid amide;
organofluorine compound;
pyrazoles;
trichlorobenzene | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxathiapiprolin | | 1,3-thiazoles;
isoxazoline;
N-acylpiperidine;
organofluorine compound;
pyrazoles;
tertiary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[[5-(4-fluoro-2-hydroxyphenyl)-2-furanyl]methylidene]thiazolidine-2,4-dione | | halophenol;
organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LimKi 3 | | 1,3-thiazoles;
dichlorobenzene;
organofluorine compound;
pyrazoles;
secondary carboxamide | LIM kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ledipasvir | | azaspiro compound;
benzimidazole;
bridged compound;
carbamate ester;
carboxamide;
fluorenes;
imidazoles;
L-valine derivative;
N-acylpyrrolidine;
organofluorine compound | antiviral drug;
hepatitis C protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ivosidenib | | cyanopyridine;
monochlorobenzenes;
organofluorine compound;
pyrrolidin-2-ones;
secondary carboxamide;
tertiary carboxamide | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| as 1842856 | | organofluorine compound;
primary amino compound;
quinolinemonocarboxylic acid;
quinolone;
secondary amino compound;
tertiary amino compound | anti-obesity agent;
antineoplastic agent;
apoptosis inducer;
autophagy inhibitor;
forkhead box protein O1 inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| praliciguat | | aminopyrimidine;
isoxazoles;
monofluorobenzenes;
organofluorine compound;
pyrazoles;
secondary amino compound;
tertiary alcohol | anti-inflammatory agent;
antihypertensive agent;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enasidenib | | 1,3,5-triazines;
aminopyridine;
aromatic amine;
organofluorine compound;
secondary amino compound;
tertiary alcohol | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MMP-9-IN-1 | | aromatic compound;
organic sulfide;
organofluorine compound;
pyrimidone;
secondary carboxamide | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2,5-difluorophenyl)-N-(2-oxolanylmethyl)-6H-1,3,4-thiadiazin-2-amine | | organofluorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nirmatrelvir | | azabicyclohexane;
nitrile;
organofluorine compound;
pyrrolidin-2-ones;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide | anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| crotamiton | | enamide;
tertiary carboxamide | antipruritic drug;
scabicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carboxin | | anilide fungicide;
anilide;
enamide;
organosulfur heterocyclic compound;
oxacycle;
secondary carboxamide | antifungal agrochemical;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ag-490 | | catechols;
enamide;
monocarboxylic acid amide;
nitrile;
secondary carboxamide | anti-inflammatory agent;
antioxidant;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector;
STAT3 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pipercallosidine | | alkaloid;
benzodioxoles;
enamide;
secondary carboxamide | apoptosis inducer;
metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| streptogramin a | | 1,3-oxazoles;
cyclic ketone;
enamide;
lactam;
macrolide antibiotic;
macrolide;
pyrroline;
secondary alcohol;
secondary carboxamide;
tertiary carboxamide | antibacterial drug;
Mycoplasma genitalium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dimethomorph | | aromatic ether;
enamide;
monochlorobenzenes;
morpholine fungicide;
tertiary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| su 1498 | | enamide;
monocarboxylic acid amide;
nitrile;
phenols;
secondary carboxamide | vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tyrphostin ag825 | | aromatic ether;
benzothiazoles;
enamide;
nitrile;
organic sulfide;
phenols;
primary carboxamide | epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s 1006 | | 1,3-thiazoles;
carbamate ester;
carboxylic acid;
cephalosporin;
enamide;
secondary carboxamide | antibacterial drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manumycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asukamycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| SIS3 free base | | aromatic ether;
enamide;
isoquinolines;
monocarboxylic acid amide;
pyrrolopyridine;
tertiary carboxamide | Smad3 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bl1521 | | enamide;
hydroxamic acid;
monocarboxylic acid amide | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pha 665752 | | dichlorobenzene;
enamide;
indolones;
N-acylpyrrolidine;
pyrrolecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lfm a13 | | aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teriflunomide | | (trifluoromethyl)benzenes;
aromatic amide;
enamide;
enol;
nitrile;
secondary carboxamide | drug metabolite;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| THZ531 | | aminopyrimidine;
enamide;
indoles;
N-acylpiperidine;
organochlorine compound;
secondary amino compound;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinacrine | | acridines;
aromatic ether;
organochlorine compound;
tertiary amino compound | antimalarial;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vanilmandelic acid | | 2-hydroxy monocarboxylic acid;
aromatic ether;
phenols | human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(2,4-dichlorophenoxy)butyric acid | | aromatic ether;
monocarboxylic acid;
organochlorine compound | agrochemical;
phenoxy herbicide;
synthetic auxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| win 52035 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| win 52084 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(nonyloxy)tryptamine | | aromatic ether;
primary amino compound;
tryptamines | serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methylbufotenin | | aromatic ether;
tertiary amino compound;
tryptamine alkaloid | hallucinogen;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methoxytryptamine | | aromatic ether;
primary amino compound;
tryptamines | 5-hydroxytryptamine 2A receptor agonist;
5-hydroxytryptamine 2B receptor agonist;
5-hydroxytryptamine 2C receptor agonist;
antioxidant;
cardioprotective agent;
human metabolite;
mouse metabolite;
neuroprotective agent;
radiation protective agent;
serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 48-8071 | | aromatic ether;
aromatic ketone;
bromobenzenes;
monofluorobenzenes;
olefinic compound;
tertiary amino compound | antineoplastic agent;
EC 5.4.99.7 (lanosterol synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amsacrine | | acridines;
aromatic ether;
sulfonamide | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aristolochic acid i | | aristolochic acids;
aromatic ether;
C-nitro compound;
cyclic acetal;
monocarboxylic acid;
organic heterotetracyclic compound | carcinogenic agent;
metabolite;
mutagen;
nephrotoxin;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4-dihydroxy-7-methoxy-1,4-benzoxazin-3-one | | aromatic ether;
benzoxazine;
cyclic hydroxamic acid;
lactol | allelochemical;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bufetolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bufexamac | | aromatic ether;
hydroxamic acid | antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bunitrolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bupranolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| verapamil | | aromatic ether;
nitrile;
polyether;
tertiary amino compound | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cgp 12177 | | aromatic ether;
benzimidazoles;
secondary alcohol;
secondary amino compound | beta-adrenergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ciglitazone | | aromatic ether;
thiazolidinone | antineoplastic agent;
insulin-sensitizing drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cirazoline | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofibrate | | aromatic ether;
ethyl ester;
monochlorobenzenes | anticholesteremic drug;
antilipemic drug;
geroprotector;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofibric acid | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| colchicine, (+-)-isomer | | acetamides;
alkaloid;
aromatic ether;
carbotricyclic compound | microtubule-destabilising agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| croconazole | | aromatic ether;
conazole antifungal drug;
imidazole antifungal drug;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cypermethrin | | aromatic ether;
cyclopropanecarboxylate ester;
nitrile;
organochlorine compound | agrochemical;
molluscicide;
pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| racemethorphan | | aromatic ether;
morphinane alkaloid;
morphinane-like compound;
organic heterotetracyclic compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dibucaine | | aromatic ether;
monocarboxylic acid amide;
tertiary amino compound | topical anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dilacor xr | | acetate ester;
aromatic ether;
benzothiazepine;
lactam;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| domiphen | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| donepezil | | aromatic ether;
indanones;
piperidines;
racemate | EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
nootropic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epirizole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethacrynic acid | | aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ethoxyquin | | aromatic ether;
quinolines | antifungal agrochemical;
food antioxidant;
genotoxin;
geroprotector;
herbicide;
Hsp90 inhibitor;
neuroprotective agent;
UDP-glucuronosyltransferase activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethoxzolamide | | aromatic ether;
benzothiazoles;
sulfonamide | antiglaucoma drug;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hexyloxybenzamide | | aromatic ether;
benzamides | antifungal agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenofibrate | | aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes | antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenvalerate | | aromatic ether;
carboxylic ester;
monochlorobenzenes | pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoxetine | | (trifluoromethyl)benzenes;
aromatic ether;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gallamine triethiodide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemfibrozil | | aromatic ether | antilipemic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| haloprogin | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| indomethacin | | aromatic ether;
indole-3-acetic acids;
monochlorobenzenes;
N-acylindole | analgesic;
drug metabolite;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
gout suppressant;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ipriflavone | | aromatic ether;
isoflavones | bone density conservation agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly 171883 | | acetophenones;
aromatic ether;
phenols;
tetrazoles | anti-asthmatic drug;
leukotriene antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mephenesin | | aromatic ether;
glycerol ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methocarbamol | | aromatic ether;
carbamate ester;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoctramine | | aromatic ether;
tetramine | muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxsalen | | aromatic ether;
psoralens | antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metoprolol | | aromatic ether;
propanolamine;
secondary alcohol;
secondary amino compound | antihypertensive agent;
beta-adrenergic antagonist;
environmental contaminant;
geroprotector;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mexiletine | | aromatic ether;
primary amino compound | anti-arrhythmia drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| midodrine | | amino acid amide;
aromatic ether;
secondary alcohol | alpha-adrenergic agonist;
prodrug;
sympathomimetic agent;
vasoconstrictor agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clorgyline | | aromatic ether;
dichlorobenzene;
terminal acetylenic compound;
tertiary amino compound | antidepressant;
EC 1.4.3.4 (monoamine oxidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nefazodone | | aromatic ether;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazoles | alpha-adrenergic antagonist;
analgesic;
antidepressant;
serotonergic antagonist;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nimesulide | | aromatic ether;
C-nitro compound;
sulfonamide | cyclooxygenase 2 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nisoxetine | | aromatic ether;
secondary amino compound | adrenergic uptake inhibitor;
antidepressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | | aromatic ether;
C-nitro compound;
sulfonamide | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| omeprazole | | aromatic ether;
benzimidazoles;
pyridines;
sulfoxide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxprenolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pentamidine | | aromatic ether;
carboxamidine;
diether | anti-inflammatory agent;
antifungal agent;
calmodulin antagonist;
chemokine receptor 5 antagonist;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
NMDA receptor antagonist;
S100 calcium-binding protein B inhibitor;
trypanocidal drug;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenacetin | | acetamides;
aromatic ether | cyclooxygenase 3 inhibitor;
non-narcotic analgesic;
peripheral nervous system drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pioglitazone | | aromatic ether;
pyridines;
thiazolidinediones | antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| piretanide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pramoxine | | aromatic ether;
morpholines | local anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| primaquine | | aminoquinoline;
aromatic ether;
N-substituted diamine | antimalarial | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| proglumetacin | | aromatic ether;
benzamides;
carboxylic ester;
monochlorobenzenes;
N-acylindole;
N-alkylpiperazine | antipyretic;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
lipoxygenase inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propoxur | | aromatic ether;
carbamate ester | acaricide;
agrochemical;
carbamate insecticide;
EC 3.1.1.7 (acetylcholinesterase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrilamine | | aromatic ether;
ethylenediamine derivative | H1-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulfadimethoxine | | aromatic ether;
pyrimidines;
substituted aniline;
sulfonamide antibiotic;
sulfonamide | antiinfective agent;
antimicrobial agent;
drug allergen;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetrahydropapaverine | | aromatic ether;
benzylisoquinoline alkaloid;
benzyltetrahydroisoquinoline;
polyether;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tilorone | | aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound | anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ultram | | aromatic ether;
tertiary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triclosan | | aromatic ether;
dichlorobenzene;
monochlorobenzenes;
phenols | antibacterial agent;
antimalarial;
drug allergen;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
fungicide;
persistent organic pollutant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| viloxazine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wb 4101 | | aromatic ether;
benzodioxine;
secondary amino compound | alpha-adrenergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3',5-triiodothyropropionic acid | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methacetin | | acetamides;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mestranol | | 17beta-hydroxy steroid;
aromatic ether;
terminal acetylenic compound | prodrug;
xenoestrogen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| visnagin | | aromatic ether;
furanochromone;
polyketide | anti-inflammatory agent;
antihypertensive agent;
EC 1.1.1.37 (malate dehydrogenase) inhibitor;
phytotoxin;
plant metabolite;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-tert-butyl-4-hydroxyanisole | | aromatic ether;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mecoprop | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenetidine | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-4-chlorophenoxy gamma-butyric acid | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | environmental contaminant;
phenoxy herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-bromophenyl phenyl ether | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| di-(4-aminophenyl)ether | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenyl ether | | aromatic ether | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diglycidyl resorcinol ether | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenetole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| scoparone | | aromatic ether;
coumarins | anti-allergic agent;
anti-inflammatory agent;
antihypertensive agent;
antilipemic drug;
immunosuppressive agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dimethoxyphenylethylamine | | alkaloid;
aromatic ether;
phenylethylamine | allergen;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dichlorprop | | aromatic ether;
dichlorobenzene;
monocarboxylic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-tert-butyl-4-hydroxyanisole | | aromatic ether;
phenols | antioxidant;
human xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethyl vanillin | | aromatic ether;
benzaldehydes;
phenols | antioxidant;
flavouring agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzethonium chloride | | aromatic ether;
chloride salt;
quaternary ammonium salt | antibacterial agent;
antifungal agent;
antiseptic drug;
antiviral agent;
disinfectant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| peucedanin | | aromatic ether;
furanocoumarin;
lactone | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenetidine | | aromatic ether;
primary amino compound;
substituted aniline | drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxybenzoxazolinone | | aromatic ether;
benzoxazole | antibacterial agent;
anticonvulsant;
antifungal agent;
muscle relaxant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-anisidine | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| domiphen bromide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dibrompropamidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-Ethoxyphenol | | aromatic ether;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bulbocapnine | | aporphine alkaloid;
aromatic ether;
oxacycle;
phenols | EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor;
EC 1.4.3.22 (diamine oxidase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzydamine | | aromatic ether;
indazoles;
tertiary amino compound | analgesic;
central nervous system stimulant;
hallucinogen;
local anaesthetic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xylocholine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-methoxycatechol | | aromatic ether;
catechols | G-protein-coupled receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-phenoxypropanoic acid | | aromatic ether;
carboxylic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxyquinoline | | aromatic ether;
quinolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metaxalone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| heliamine | | aromatic ether;
diether;
isoquinoline alkaloid;
isoquinolines | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4,6-trichlorophenyl 4-nitrophenyl ether | | aromatic ether;
C-nitro compound;
chlorobenzenes | EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etridiazol | | aromatic ether;
organochlorine compound;
thiadiazole antifungal agent;
thiadiazoles | antifungal agrochemical;
nitrification inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toliprolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methoxyindoleacetic acid | | aromatic ether;
indole-3-acetic acids | antibacterial agent;
Brassica napus metabolite;
carcinogenic agent;
human urinary metabolite;
marine xenobiotic metabolite;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| iproclozide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenoxyacetic acid | | aromatic ether;
monocarboxylic acid | allergen;
Aspergillus metabolite;
human xenobiotic metabolite;
plant growth retardant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nafenopin | | aromatic ether;
monocarboxylic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyl vanillate | | aromatic ether;
benzoate ester;
phenols | antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methoxyindole-2-carboxylic acid | | aromatic ether;
indolecarboxylic acid | EC 1.8.1.4 (dihydrolipoyl dehydrogenase) inhibitor;
hypoglycemic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-isopropoxyphenol | | aromatic ether;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dehydroemetine | | aromatic ether;
isoquinolines;
pyridoisoquinoline | antileishmanial agent;
antimalarial;
antiprotozoal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,2-epoxy-3-(p-nitrophenoxy)propane | | aromatic ether;
C-nitro compound;
epoxide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| laurolitsine | | aporphine alkaloid;
aromatic ether;
phenols | HIV-1 integrase inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metocurine iodide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ac 45594 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-phenoxybenzylalcohol | | aromatic ether;
benzyl alcohols | marine xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| devrinol | | aromatic ether;
monocarboxylic acid amide;
naphthalenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluorodifen | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acridine half-mustard | | aminoacridines;
aromatic ether;
organochlorine compound;
secondary amino compound | mutagen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| precocene i | | aromatic ether;
chromenes | plant metabolite;
precocenes | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxadiazon | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lofexidine | | aromatic ether;
carboxamidine;
dichlorobenzene;
imidazoles | alpha-adrenergic agonist;
antihypertensive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alclofenac | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | drug allergen;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenylglycidyl ether | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenoxyethanol | | aromatic ether;
glycol ether;
primary alcohol | antiinfective agent;
central nervous system depressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metipranolol | | acetate ester;
aromatic ether;
propanolamine;
secondary amino compound | anti-arrhythmia drug;
antiglaucoma drug;
antihypertensive agent;
beta-adrenergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| silybin | | aromatic ether;
benzodioxine;
flavonolignan;
polyphenol;
secondary alpha-hydroxy ketone | antineoplastic agent;
antioxidant;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxamethacin | | aromatic ether;
hydroxamic acid;
N-acylindole;
organochlorine compound | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| canadine | | aromatic ether;
berberine alkaloid;
organic heteropentacyclic compound;
oxacycle | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-ethoxycoumarin | | aromatic ether;
coumarins | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| medifoxamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlormethoxynil | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| climbazole | | aromatic ether;
hemiaminal ether;
imidazoles;
ketone;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hexyloxyaniline | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ticrynafen | | aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid;
thiophenes | antihypertensive agent;
hepatotoxic agent;
loop diuretic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-(2,4-dichlorophenoxy)phenoxy)propionic acid | | aromatic ether;
dichlorobenzene;
diether;
monocarboxylic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bezafibrate | | aromatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes | antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxyfluorofen | | aromatic ether | EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triadimefon | | aromatic ether;
hemiaminal ether;
ketone;
monochlorobenzenes;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| levobunolol | | aromatic ether;
cyclic ketone;
propanolamine | antiglaucoma drug;
beta-adrenergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dichlorfop-methyl | | aromatic ether;
dichlorobenzene;
diether;
methyl ester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| decamethrin | | aromatic ether;
cyclopropanecarboxylate ester;
nitrile;
organobromine compound | agrochemical;
antifeedant;
calcium channel agonist;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triadimenol | | aromatic ether;
conazole fungicide;
hemiaminal ether;
monochlorobenzenes;
secondary alcohol;
triazole fungicide | antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor;
xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triclopyr | | aromatic ether;
chloropyridine;
monocarboxylic acid | agrochemical;
environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prenalterol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| st 1059 | | aromatic ether;
primary amino compound;
secondary alcohol | alpha-adrenergic agonist;
sympathomimetic agent;
vasoconstrictor agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bopindolol | | aromatic ether;
benzoate ester;
methylindole;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenpropathrin, (+-)-isomer | | aromatic ether;
cyclopropanecarboxylate ester | agrochemical;
pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flutolanil | | (trifluoromethyl)benzenes;
aromatic ether;
benzamides;
benzanilide fungicide | antifungal agrochemical;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenoxaprop ethyl | | aromatic ether | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| triclabendazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluvalinate | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
nitrile;
organochlorine acaricide;
organochlorine insecticide;
organofluorine acaricide;
organofluorine insecticide | agrochemical;
pyrethroid ester acaricide;
pyrethroid ester insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenoxycarb | | aromatic ether;
carbamate ester | environmental contaminant;
insecticide;
juvenile hormone mimic;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quizalofop-ethyl | | aromatic ether;
ethyl ester;
organochlorine compound;
quinoxaline derivative | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cetamolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| atomoxetine | | aromatic ether;
secondary amino compound;
toluenes | adrenergic uptake inhibitor;
antidepressant;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyl bensulfuron | | aromatic ether;
methyl ester;
N-sulfonylurea;
pyrimidines | agrochemical;
EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| itraconazole | | aromatic ether;
conazole antifungal drug;
cyclic ketal;
dichlorobenzene;
dioxolane;
N-arylpiperazine;
triazole antifungal drug;
triazoles | EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
Hedgehog signaling pathway inhibitor;
P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| loxtidine | | aromatic ether;
piperidines;
primary alcohol;
triazoles | H2-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| disoxaril | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorimuron ethyl | | aromatic ether;
ethyl ester;
N-sulfonylurea;
organochlorine pesticide;
pyrimidines;
sulfamoylbenzoate | agrochemical;
EC 2.2.1.6 (acetolactate synthase) inhibitor;
proherbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tepoxalin | | aromatic ether;
hydroxamic acid;
monochlorobenzenes;
pyrazoles | antipyretic;
apoptosis inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
immunomodulator;
lipoxygenase inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| esmolol | | aromatic ether;
ethanolamines;
methyl ester;
secondary alcohol;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pioglitazone hydrochloride | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aripiprazole | | aromatic ether;
delta-lactam;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
quinolone | drug metabolite;
H1-receptor antagonist;
second generation antipsychotic;
serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulfametrole | | aromatic ether;
substituted aniline;
sulfonamide antibiotic;
thiadiazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propamidine | | aromatic ether;
guanidines;
polyether | antimicrobial agent;
antiseptic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hexamidine | | aromatic ether;
guanidines;
polyether | antimicrobial agent;
antiseptic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| o-4-methylthymine | | aromatic ether;
methylthymine | human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenclofenac | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetraiodothyroacetic acid | | 2-halophenol;
aromatic ether;
iodophenol;
monocarboxylic acid | apoptosis inducer;
human metabolite;
thyroid hormone | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluazuron | | aromatic ether;
chloropyridine;
monochlorobenzenes;
N-acylurea;
organochlorine acaricide;
organofluorine acaricide;
phenylureas | acaricide;
mite growth regulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etiroxate | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etofamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| d 888 | | aromatic ether;
nitrile;
tertiary amino compound | anti-arrhythmia drug;
calcium channel blocker;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| esreboxetine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| guaethol | | aromatic ether;
phenols;
volatile organic compound | flavouring agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5'-nitro-2'-propoxyacetanilide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| suberosin | | aromatic ether;
coumarins | anticoagulant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methoxyestradiol | | 17beta-hydroxy steroid;
3-hydroxy steroid;
aromatic ether;
phenols | estrogen;
human metabolite;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toltrazuril | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plafibride | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cinitapride | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoscopoletin | | aromatic ether;
hydroxycoumarin | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethofenprox | | aromatic ether | pyrethroid ether insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uk 68798 | | aromatic ether;
sulfonamide;
tertiary amino compound | anti-arrhythmia drug;
potassium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenoxypropazine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amezinium | | aromatic ether;
primary arylamine;
pyridazinium ion | adrenergic uptake inhibitor;
antihypotensive agent;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
sympathomimetic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubrofusarin | | aromatic ether;
benzochromenone;
phenols;
polyketide | biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triasulfuron | | 1,3,5-triazines;
aromatic ether;
N-sulfonylurea;
organochlorine compound | agrochemical;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dauricine | | aromatic ether;
bisbenzylisoquinoline alkaloid;
isoquinolines;
phenols;
tertiary amino compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uvaretin | | aromatic ether;
dihydrochalcones;
polyketide;
resorcinol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fangchinoline | | aromatic ether;
bisbenzylisoquinoline alkaloid;
macrocycle | anti-HIV-1 agent;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prochloraz | | amide fungicide;
aromatic ether;
conazole fungicide;
imidazole fungicide;
imidazoles;
trichlorobenzene;
ureas | antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stictic acid | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pramoxine hydrochloride | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methoxybenzylamine | | aralkylamino compound;
aromatic ether;
primary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xanthurenic acid 8-methyl ether | | aromatic ether;
monohydroxyquinoline;
quinolinemonocarboxylic acid | carcinogenic agent;
metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| adriamycinol | | aminoglycoside;
anthracycline antibiotic;
aromatic ether;
deoxy hexoside;
p-quinones;
phenols;
polyol;
tetracenequinones | cardiotoxic agent;
drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| difenoconazole | | aromatic ether;
conazole fungicide;
cyclic ketal;
dioxolane;
triazole fungicide;
triazoles | antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| a 8947 | | aromatic ether;
biaryl;
N-sulfonylurea;
pyrazole pesticide;
tetrazoles | EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethylhydrocupreine | | aromatic ether;
cinchona alkaloid | EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7,8-dihydromethysticin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4,5-dimethoxy-2-nitrobenzaldehyde | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bisphenol f diglycidyl ether | | aromatic ether;
diarylmethane;
epoxide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oryzemate | | 1,2-benzisothiazole;
aromatic ether;
benzothiazole fungicide;
sulfone | antifungal agrochemical;
plant activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bitertanol | | aromatic ether;
biphenyls;
secondary alcohol;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflufenican | | (trifluoromethyl)benzenes;
aromatic ether;
pyridinecarboxamide | carotenoid biosynthesis inhibitor;
environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hexafluoron | | aromatic ether;
benzoylurea insecticide;
dichlorobenzene;
N-acylurea;
organochlorine insecticide;
organofluorine insecticide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diethofencarb | | aromatic ether;
carbamate ester;
carbanilate fungicide | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyriproxyfen | | aromatic ether;
pyridines | juvenile hormone mimic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyl 2-(((((4-ethoxy-6-(methylamino)-1,3,5-triazin-2-yl)amino)carbonyl)amino)sulfonyl)benzoate | | aromatic ether;
benzoate ester;
diamino-1,3,5-triazine;
methyl ester;
N-sulfonylurea | EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dpx e9636 | | aromatic ether;
N-sulfonylurea;
pyridines;
pyrimidines;
sulfone | environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aclonifen | | aromatic ether;
C-nitro compound;
monochlorobenzenes;
primary amino compound;
substituted aniline | agrochemical;
carotenoid biosynthesis inhibitor;
EC 1.3.3.4 (protoporphyrinogen oxidase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cinosulfuron | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vestitol | | aromatic ether;
hydroxyisoflavans;
methoxyisoflavan | anti-inflammatory agent;
phytoalexin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| laudanine | | aromatic ether;
benzylisoquinoline alkaloid;
benzyltetrahydroisoquinoline;
phenols;
racemate | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cryptopleurine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | antineoplastic agent;
antiviral agent;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-hydroxymethylmexiletine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hydroxymexiletine | | aromatic ether;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cloquintocet-mexyl | | aromatic ether;
carboxylic ester;
organochlorine compound;
quinolines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bursehernin | | aromatic ether;
benzodioxoles;
butan-4-olide;
lignan | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2',4,4'-tetrabromodiphenyl ether | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| allocryptopine | | aromatic ether;
cyclic acetal;
cyclic ketone;
dibenzazecine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sporidesmin | | aromatic ether;
cyclic ketone;
diketone;
organic disulfide;
organic heteropentacyclic compound;
organochlorine compound;
secondary alcohol;
tertiary alcohol;
tertiary amino compound | mycotoxin;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| syringaresinol | | aromatic ether;
furofuran;
lignan;
polyether;
polyphenol | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| p-methoxy-n-methylphenethylamine | | aromatic ether;
secondary amino compound | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aflatoxin q1 | | aflatoxin;
aromatic ether;
aromatic ketone | carcinogenic agent;
human xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| u 73122 | | aromatic ether;
aza-steroid;
maleimides | EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| norverapamil | | aromatic ether;
nitrile;
polyether;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fumitremorgin a | | aromatic ether;
diol;
indole alkaloid;
organic heterohexacyclic compound;
organic peroxide | mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deguelin | | aromatic ether;
diether;
organic heteropentacyclic compound;
rotenones | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
mitochondrial NADH:ubiquinone reductase inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aristolochic acid ii | | aristolochic acids;
aromatic ether;
C-nitro compound;
cyclic acetal;
monocarboxylic acid;
organic heterotetracyclic compound | carcinogenic agent;
metabolite;
mutagen;
nephrotoxin;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tephrosin | | aromatic ether;
cyclic ketone;
organic heteropentacyclic compound;
rotenones | antineoplastic agent;
metabolite;
pesticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alpha-hydroxymetoprolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(tetradecyloxy)-2-furancarboxylic acid | | aromatic ether;
furoic acid | antineoplastic agent;
apoptosis inducer;
EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tafenoquine | | (trifluoromethyl)benzenes;
aminoquinoline;
aromatic ether;
primary amino compound;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-hydroxymethylomeprazole | | aromatic ether;
benzimidazoles;
pyridines;
sulfoxide | drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mosapride | | aromatic ether;
benzamides;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
secondary carboxamide;
substituted aniline;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ym 12617 | | aromatic ether;
secondary amino compound;
sulfonamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cgp 28392 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sodium-binding benzofuran isophthalate | | 1-benzofurans;
aromatic ether;
crown compound;
tetracarboxylic acid | fluorochrome | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ay 25545 | | acetate ester;
aromatic ether;
C-glycosyl compound;
naphthoisochromene;
olefinic compound;
phenols;
tertiary amine | antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| reboxetine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| b 823-08 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ivabradine | | aromatic ether;
benzazepine;
carbobicyclic compound;
tertiary amino compound | cardiotonic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| febuxostat | | 1,3-thiazolemonocarboxylic acid;
aromatic ether;
nitrile | EC 1.17.3.2 (xanthine oxidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marsupsin | | 1-benzofurans;
aromatic ether;
polyphenol | antilipemic drug;
hypoglycemic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6,6'-bieckol | | aromatic ether;
oxacycle;
phlorotannin | anti-HIV-1 agent;
metabolite;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xibenolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cicloprolol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chs 828 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-methoxyphenoxy)propanoic acid | | aromatic ether;
carboxylic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| moxifloxacin | | aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone | antibacterial drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rp 73401 | | aromatic ether;
benzamides;
chloropyridine;
monocarboxylic acid amide | anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
phosphodiesterase IV inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2',4,4',5,5'-hexabrominated diphenyl ether | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| varespladib | | aromatic ether;
benzenes;
dicarboxylic acid monoamide;
indoles;
monocarboxylic acid;
primary carboxamide | anti-inflammatory drug;
antidote;
EC 3.1.1.4 (phospholipase A2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| birb 796 | | aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas | EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| schizandrin b | | aromatic ether;
cyclic acetal;
organic heterotetracyclic compound;
oxacycle;
tannin | anti-asthmatic agent;
anti-inflammatory agent;
antilipemic drug;
antioxidant;
apoptosis inhibitor;
hepatoprotective agent;
nephroprotective agent;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s 23121 | | aromatic ether;
dicarboximide;
monochlorobenzenes;
monofluorobenzenes;
pyrroline;
terminal acetylenic compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acrovestone | | acetophenones;
aromatic ether;
olefinic compound;
polyphenol | antioxidant;
EC 1.14.18.1 (tyrosinase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| corytuberine | | aporphine alkaloid;
aromatic ether;
organic heterotetracyclic compound;
polyphenol;
tertiary amino compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| actinodaphine | | aporphine alkaloid;
aromatic ether;
organic heteropentacyclic compound;
phenols;
secondary amino compound | antibacterial agent;
antifungal agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite;
platelet aggregation inhibitor;
topoisomerase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isohomovanillic acid | | aromatic ether;
phenols;
phenylacetic acids | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-diiodothyropropionic acid | | aromatic ether;
monocarboxylic acid;
organoiodine compound;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7,8-dihydro-5,6-dehydrokawain | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-amino-2-methoxypyrimidine | | aminopyrimidine;
aromatic ether;
methylcytosine | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aristolochic acid D | | aristolochic acids;
aromatic ether;
C-nitro compound;
cyclic acetal;
monocarboxylic acid;
organic heterotetracyclic compound | carcinogenic agent;
metabolite;
nephrotoxin;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| myricanone | | aromatic ether;
cyclic ketone;
diarylheptanoid;
methoxybenzenes;
phenols | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pannarin | | aldehyde;
aromatic ether;
depsidones;
organic heterotricyclic compound;
organochlorine compound;
phenols | antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lichen metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminopotentidine | | aromatic ether;
benzamides;
guanidines;
nitrile;
piperidines;
substituted aniline | H2-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aristolochic acid c | | aristolochic acids;
aromatic ether;
C-nitro compound;
cyclic acetal;
monocarboxylic acid;
organic heterotetracyclic compound | carcinogenic agent;
metabolite;
mutagen;
nephrotoxin;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pluviatolide | | aromatic ether;
benzodioxoles;
butan-4-olide;
lignan;
phenols | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erysodine | | aromatic ether;
diether;
Erythrina alkaloid;
organic heterotetracyclic compound;
phenols | antiparasitic agent;
nicotinic antagonist;
phytogenic insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubrofusarin B | | aromatic ether;
benzochromenone;
naphtho-gamma-pyrone;
phenols;
polyketide | Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly 293111 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enrasentan | | aromatic ether;
benzodioxoles;
indanes;
monocarboxylic acid;
monomethoxybenzene;
primary alcohol | antihypertensive agent;
endothelin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quizalofop | | aromatic ether;
monocarboxylic acid;
organochlorine compound;
quinoxaline derivative | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyhalofop-butyl | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyperin | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aflatoxin b1 | | aflatoxin;
aromatic ether;
aromatic ketone | carcinogenic agent;
human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etravirine | | aminopyrimidine;
aromatic ether;
dinitrile;
organobromine compound | antiviral agent;
HIV-1 reverse transcriptase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-o-methyllicoricidin | | aromatic ether;
hydroxyisoflavans;
methoxyisoflavan | antibacterial agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pronuciferine | | aromatic ether;
cyclic ketone;
isoquinoline alkaloid;
isoquinolines;
organic heterotetracyclic compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dronedarone | | 1-benzofurans;
aromatic ether;
aromatic ketone;
sulfonamide;
tertiary amino compound | anti-arrhythmia drug;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| famoxadone | | aromatic ether;
carbohydrazide;
oxazolidinone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2014 | 2022 | 6.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| dabuzalgron | | aromatic ether;
imidazoles;
monochlorobenzenes;
sulfonamide | alpha-adrenergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fonsecin | | aromatic ether;
cyclic hemiketal;
heptaketide;
naphtho-gamma-pyrone;
phenols | Aspergillus metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lasofoxifene | | aromatic ether;
N-alkylpyrrolidine;
naphthols;
tetralins | antineoplastic agent;
bone density conservation agent;
cardioprotective agent;
estrogen receptor agonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (+-)-Dihydromethysticin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[2-[2-(2-aminophenoxy)ethoxy]ethoxy]aniline | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chondocurine (1beta)-(+-)-isomer | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-methyl-4-prop-2-enoxy-2-pyrimidinone | | aromatic ether;
pyrimidone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| noscapine | | aromatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound | antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[4-(3-methyl-4-nitrophenoxy)butoxy]benzonitrile | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lariciresinol | | aromatic ether;
lignan;
oxolanes;
phenols;
primary alcohol | antifungal agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tryptoquivaline | | aromatic ether;
indole alkaloid;
organic heteropentacyclic compound | breast cancer resistance protein inhibitor;
mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methoxyestrone | | 17-oxo steroid;
3-hydroxy steroid;
alicyclic ketone;
aromatic ether;
phenolic steroid;
phenols | human metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| win 54954 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| silychristin | | 1-benzofurans;
aromatic ether;
flavonolignan;
polyphenol;
secondary alpha-hydroxy ketone | lipoxygenase inhibitor;
metabolite;
prostaglandin antagonist;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cleomiscosin a | | aromatic ether;
delta-lactone;
organic heterotricyclic compound;
phenols;
primary alcohol | anti-inflammatory agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bispyribac | | aromatic ether;
benzoic acids;
monocarboxylic acid;
pyrimidines | herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| petunidin-3-glucoside | | anthocyanin cation;
aromatic ether;
beta-D-glucoside | antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| malvidin-3-glucoside | | anthocyanin cation;
aromatic ether;
beta-D-glucoside | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dioncophylline c | | aromatic ether;
biaryl;
isoquinoline alkaloid;
isoquinolines;
methoxynaphthalene;
methylnaphthalenes;
naphthols | antimalarial;
antiplasmodial drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stigmatellin | | aromatic ether;
chromones;
olefinic compound;
phenols | bacterial metabolite;
quinol oxidation site inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teniposide | | aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prinomastat | | aromatic ether;
hydroxamic acid;
pyridines;
sulfonamide;
thiomorpholines | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gancaonin I | | 1-benzofurans;
aromatic ether;
resorcinols | antibacterial agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glycyrin | | aromatic ether;
coumarins;
hydroxyisoflavans | antibacterial agent;
metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyasperin D | | aromatic ether;
hydroxyisoflavans;
methoxyisoflavan | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| licoricidin | | aromatic ether;
hydroxyisoflavans;
methoxyisoflavan | antibacterial agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| egonol | | 1-benzofurans;
aromatic ether;
benzodioxoles;
primary alcohol | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-ethylharmine | | aromatic ether;
beta-carbolines;
semisynthetic derivative | anti-HIV agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 1163a | | aromatic ether;
lactam;
macrolide antibiotic;
secondary alcohol | antifungal agent;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 1163b | | aromatic ether;
lactam;
macrolide antibiotic | antifungal agent;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| licocoumarone | | 1-benzofurans;
aromatic ether;
resorcinols | antibacterial agent;
apoptosis inducer;
EC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-chloro-2-methylphenoxy)-n-hydroxybutanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LSM-22807 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-(3-methylphenoxy)ethyl]-1H-1,2,4-triazole-5-carboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| piperlactam s | | alkaloid;
aromatic ether;
gamma-lactam;
organic heterotetracyclic compound;
phenols | anti-inflammatory agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,5-dioxo-1-(4-phenoxyphenyl)-3a,4,6,6a-tetrahydro-3H-thieno[3,4-b]pyrrol-2-one | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antofine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | angiogenesis inhibitor;
anti-inflammatory agent;
antimicrobial agent;
antineoplastic agent;
antiviral agent;
phytotoxin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xanthohumol | | aromatic ether;
chalcones;
polyphenol | anti-HIV-1 agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.3.1.20 (diacylglycerol O-acyltransferase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-phenoxy-N-(2-pyridinyl)butanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-amino-4-(2-ethoxyphenyl)-3-propyl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile | | aromatic ether;
pyranopyrazole | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[4-[[1-oxo-2-(1-pyrrolidinyl)ethyl]amino]phenoxy]phenyl]-2-(1-pyrrolidinyl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(3,4-diethoxyphenyl)-5-(2-furanyl)-1,3,4-oxadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[5-(phenoxymethyl)-4-(2-phenylethyl)-1,2,4-triazol-3-yl]thio]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(8-methyl-2,5,11,14-tetraoxa-8-azabicyclo[13.4.0]nonadeca-1(15),16,18-trien-17-yl)ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[2-(3-phenoxypropyl)-5-tetrazolyl]pyridine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-cyclohexyl-5-(2-phenoxyethylthio)tetrazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-[[5-[(3-methylphenoxy)methyl]-1,3,4-oxadiazol-2-yl]thio]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-amino-4-[3-ethoxy-4-[2-(4-morpholinyl)ethoxy]phenyl]-3-ethyl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile | | aromatic ether;
pyranopyrazole | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[5-[(2,3-dimethylphenoxy)methyl]-4-methyl-1,2,4-triazol-3-yl]thio]-1-thiophen-2-ylethanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (1-methyl-2-imidazolyl)-(4-phenylmethoxyphenyl)methanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3-butoxyphenyl)-1,3,4-thiadiazol-2-amine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2-ethoxy-6-methyl-3-pyridinyl)-5-(2-pyridinyl)-1,2,4-oxadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(3,4,5-triethoxyphenyl)-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole | | aromatic ether;
triazolothiadiazole | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(1-benzotriazolyl)-5-(2-methoxyphenoxy)benzene-1,2-dicarbonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-cyclohexyl-3-[(3-methylphenoxy)methyl]-1H-1,2,4-triazole-5-thione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-ethoxy-9-nitro-5H-benzo[b][1,4]benzoxazepin-6-one | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[4-(2-quinoxalinyl)phenoxy]benzene-1,2-dicarbonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(4-amino-1,2,5-oxadiazol-3-yl)-5-(phenoxymethyl)-4-triazolecarboxylic acid ethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-ethylphenoxy)-N-(1H-1,2,4-triazol-5-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-chloro-3-methylphenoxy)-N-(1H-1,2,4-triazol-5-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(4-ethylphenoxy)methyl]-N-(2-pyridinylmethyl)-2-furancarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-methoxy-3,5-dimethyl-2-thiazolo[4,5-d]pyrimidinethione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(4-ethylphenyl)-2-thiazolyl]carbamic acid phenyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromo-4-methylphenoxy)-N-(2-pyridinylmethyl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[[3-(4-chlorophenoxy)phenyl]methyl]-4-ethylpiperazine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methoxy-4-[(4-methyl-1,4-diazepan-1-yl)methyl]-6-nitrophenol | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[4-(ethylamino)-6-(methylthio)-1,3,5-triazin-2-yl]oxy]benzoic acid ethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-ethyl-3-[[4-(2-methylpropoxy)phenyl]methylthio]-1H-1,2,4-triazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| [4-[(2-fluorophenyl)methoxy]phenyl]-(1-pyrrolidinyl)methanethione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(2-chlorophenoxy)methyl]-3-pyridin-4-yl-1,2,4-oxadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-phenylmethoxyphenyl)thiadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-methyl-2-[[4-methyl-5-[(4-nitrophenoxy)methyl]-1,2,4-triazol-3-yl]thio]acetamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[5-(4-ethoxyphenyl)-1,3,4-oxadiazol-2-yl]thio]-1-(4-morpholinyl)ethanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(3-pyridinyloxy)benzene-1,2-dicarbonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-tert-butyl-2-(4-chloro-3-methylphenoxy)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(2-furanylmethyl)-3-(4-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(2-methylpropyl)-3-(4-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-cyclopentyl-3-(4-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(4-ethoxyphenoxy)methyl]-N-(3-pyridinyl)-2-furancarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2,3-dimethylphenoxy)-N-pyridin-4-ylacetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(2-chlorophenoxy)methyl]-N-(2-thiazolyl)-2-furancarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[5-[(4-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-2-furancarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4,5-dihydrothiazol-2-yl)-2-(2-methylphenoxy)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2-fluorophenoxy)-1-methyl-3-nitro-1,2,4-triazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-methyl-5-(1-naphthalenyloxy)-4-nitroimidazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| curcumin | | aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| 1-(3,4-dimethoxyphenyl)-3-(2-methoxy-5-nitrophenyl)urea | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-cyclopentyl-3-(2-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1-ethyl-2-benzimidazolyl)-5-[(4-methyl-2-nitrophenoxy)methyl]-2-furancarboxamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-chloro-12-(4-methoxyphenyl)sulfonylquinoxalino[2,3-b][1,4]benzoxazine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-methoxy-5-nitrophenyl)-3-(4-methylphenyl)urea | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromo-4-chlorophenoxy)-N-cyclohexyl-N-methylacetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-furanyl-[4-(4-phenoxyphenyl)sulfonyl-1-piperazinyl]methanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(2-methoxyphenoxy)-N-(3-pyridinyl)benzenesulfonamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-chlorophenyl)-3-(2-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[2-(1-azepanyl)-4,5-dicyanophenoxy]phenyl]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-dimethoxy-N-(4-phenoxyphenyl)benzenesulfonamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[4-(dimethylamino)-6-(4-morpholinyl)-1,3,5-triazin-2-yl]oxy]benzoic acid methyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[5-[(4-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-5-methyl-3-phenyl-4-isoxazolecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[4-[[4-(2-chloro-6-nitrophenoxy)phenyl]methoxy]phenyl]ethanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-[[2-(4-hydroxyphenyl)-1,3-dioxo-5-isoindolyl]oxy]phenyl]-2,2-dimethylpropanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[[4-(4-chlorophenoxy)anilino]-sulfanylidenemethyl]benzamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-fluorophenoxy)-N-(5-pyridin-4-yl-1,3,4-thiadiazol-2-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[3-chloro-5-(trifluoromethyl)-2-pyridinyl]oxy]-N-propan-2-ylbenzenesulfonamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-tert-butylphenoxy)-5-methoxy-2-phenylpyrimidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-phenoxy-2-phenyl-5-pyrimidinecarboxylic acid ethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2,5-dioxo-6-(4-phenoxyphenyl)-3-pyrano[3,2-c]pyridinyl]benzamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-chlorophenoxy)-4-(dimethylamino)-3-pyridinecarbonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methyl-5-[2-(2-methylphenoxy)ethyl]-2-sulfanylidene-1H-pyrimidin-4-one | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-chlorophenoxy)-1-(4-morpholinyl)-1-butanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4-ethyl-6-[2-(4-methylphenoxy)ethylthio]-N2-propan-2-yl-1,3,5-triazine-2,4-diamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(phenylmethyl)-3-[2-(4-propoxyphenyl)ethyl]-1H-1,2,4-triazole-5-thione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[[1-oxo-3-(4-propan-2-yloxyphenyl)propyl]amino]-3-(phenylmethyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(3-methylphenoxy)-5-nitrophenyl]-2-(3-nitro-1,2,4-triazol-1-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-bis(2-fluorophenoxy)phosphoryl-3,4-dimethylaniline | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(2-ethoxyanilino)-6-(4-ethoxyanilino)-2-pyrimidinyl]methylidene]propanedinitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methyl-3-[(4-pentoxyphenyl)methylthio]-1H-1,2,4-triazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4,5-dichloro-1-[2-(4-chlorophenoxy)ethyl]imidazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-butyl-3-(4-phenoxyphenyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-cyano-2-thiophenyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenoxy]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromophenyl)-5-[(2-chlorophenoxy)methyl]-1,3,4-oxadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-ethoxyphenyl)-N-(3,4,5,6-tetrahydro-2H-azepin-7-yl)-1,3,4-oxadiazol-2-amine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-chloro-2-methylphenoxy)-1-(4-morpholinyl)-1-butanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N9-(4-butoxyphenyl)-6,8,10-triazaspiro[4.5]deca-6,9-diene-7,9-diamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[2-(4-chlorophenoxy)ethylthio]pyrimidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3-phenoxypropyl)-3-(3-pyridinyl)-1,2,4-oxadiazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(3-ethoxy-2-prop-2-enoxyphenyl)methyl]-2-thiazolamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-bromophenoxy)-N-(2-pyridinylmethyl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[2-[(4-chlorophenyl)thio]ethoxy]-3-ethoxybenzaldehyde | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-fluorophenyl)-4-(4-hydroxy-3-methoxy-5-nitrophenyl)-4H-pyridine-3,5-dicarboxylic acid diethyl ester | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2-ethoxyphenyl)-3H-1,3,4-oxadiazole-2-thione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-tert-butyl-4-(2-fluorophenoxy)-1-butanamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-butyl-4-phenoxy-1-butanamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-[[diethylamino(sulfanylidene)methyl]thio]-1-oxopropyl]carbamic acid (4-methylphenyl) ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,3-dimethyl-5-[[2-[2-(4-nitrophenoxy)ethoxy]phenyl]methylidene]-1,3-diazinane-2,4,6-trione | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[2-[2-(4-bromo-2-chlorophenoxy)ethoxy]ethyl]morpholine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[2-(3-ethylphenoxy)ethyl]propanedioic acid diethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3-dihydro-1,4-dioxin-5-carboxylic acid [2-[4-[4-(2-methylbutan-2-yl)phenoxy]anilino]-2-oxoethyl] ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[3-(2-bromo-4-chlorophenoxy)propyl]-4-methylpiperidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4-(2-methoxyphenyl)benzene-1,4-diamine | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(1H-benzimidazol-2-ylthio)butanoic acid [2-oxo-2-(4-phenoxyanilino)ethyl] ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-phenoxybenzoic acid [2-(2-furanylmethylamino)-2-oxoethyl] ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[2,5-dimethyl-1-(phenylmethyl)-3-pyrrolyl]-2-[4-(1,3,4-oxadiazol-2-yl)phenoxy]ethanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[6-amino-1-(2-methylpropyl)-2,4-dioxo-5-pyrimidinyl]-2-(2-methylphenoxy)-N-(2-methylpropyl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[6-[(2-methyl-5-thieno[2,3-e][1,3]benzothiazolyl)oxy]-3-pyridinyl]sulfonyl]morpholine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3-fluorophenoxy)-8-nitroisoquinoline | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[4-(2-prop-2-enylphenoxy)butyl]pyrrolidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2,4-dibromophenoxy)-N-[oxo-(propan-2-ylamino)methyl]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-phenoxyphenyl 4-hydroxypiperidine-1-carboxylate | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N'-benzoyl-5-(3,5-dichlorophenoxy)-2-furancarbohydrazide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[2-[(4-chlorophenoxy)methyl]-4-thiazolyl]ethanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(benzyloxy)-2-(hydroxymethyl)-1,4-dihydropyridin-4-one | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-aminophenoxy)isophthalonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N5-(2-chloro-6-phenoxybenzyl)-1H-1,2,4-triazole-3,5-diamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2-chloro-6-phenoxyphenyl)methyl]benzenesulfonamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[5-(tert-butyl)-3-isoxazolyl]-N'-[2-(trifluoromethoxy)phenyl]urea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-(4-methoxyphenoxy)-2-imidazo[1,2-b]pyridazinecarboxylic acid ethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-fluoro-N-[2,2,2-trichloro-1-[[(4-methoxy-2-nitroanilino)-sulfanylidenemethyl]amino]ethyl]acetamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-amino-4-(4,5-dimethoxy-2-nitrophenyl)-7,7-dimethyl-5-oxo-6,8-dihydro-4H-1-benzopyran-3-carbonitrile | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4-dichloro-N-[2,2,2-trichloro-1-[[(4-methoxy-2-nitroanilino)-sulfanylidenemethyl]amino]ethyl]benzamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-anilino-3-[4-(3-anilino-2-hydroxypropoxy)phenoxy]-2-propanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[4-(3-ethoxyphenoxy)butyl]imidazole | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[5-[(4-chlorophenoxy)methyl]-1,3,4-thiadiazol-2-yl]-2-oxolanecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[[2-(2,4-difluorophenoxy)-1-oxopropyl]amino]-3-(2-oxolanylmethyl)thiourea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[[(5-bromo-6-methyl-2-pyridinyl)amino]-sulfanylidenemethyl]-2-(2-chlorophenoxy)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(4-chlorophenyl)sulfonyl-methylamino]-N-(4-methoxy-2-nitrophenyl)acetamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-oxido-3-(4-phenoxyphenyl)-4a,5,6,7,8,8a-hexahydroquinoxalin-1-ium 1-oxide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(2-fluorophenyl)-3-(4-methoxy-2-nitrophenyl)urea | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[5-[(2-fluorophenoxy)methyl]-4-prop-2-enyl-1,2,4-triazol-3-yl]thio]-N-[(2-furanylmethylamino)-oxomethyl]acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyclopropanecarboxylic acid [2-oxo-2-(4-phenoxyanilino)ethyl] ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toremifene | | aromatic ether;
organochlorine compound;
tertiary amine | antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dieckol | | aromatic ether;
oxacycle;
phlorotannin | anticoagulant;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
hepatoprotective agent;
metabolite;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naproxol | | aromatic ether | antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamoxifen n-oxide | | aromatic ether;
tertiary amine oxide | anti-estrogen;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diafenthiuron | | aromatic ether;
thiourea acaricide;
thiourea insecticide | oxidative phosphorylation inhibitor;
proinsecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ospemifene | | aromatic ether;
organochlorine compound;
primary alcohol | anti-inflammatory agent;
antineoplastic agent;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| adefovir | | aromatic ether;
aromatic ketone;
biaryl;
cyclic ketone;
naphtho-gamma-pyrone;
organooxygen heterocyclic antibiotic;
polyphenol | antimalarial;
Aspergillus metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chloro-N-[2,2,2-trichloro-1-[[(4-methoxy-2-nitroanilino)-sulfanylidenemethyl]amino]ethyl]benzamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-hydroxyethyl)-4-[2-nitro-4-(trifluoromethyl)phenoxy]benzamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N'-[2-[(4-amino-5-cyano-2-pyrimidinyl)thio]-1-oxoethyl]-2-(4-methylphenoxy)acetohydrazide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2-methyl-4-thiazolyl)methyl]-4-phenoxybenzenesulfonamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-amino-4-(2-ethoxy-4-hydroxyphenyl)-3-propyl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile | | aromatic ether;
pyranopyrazole | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(2-ethoxyphenyl)methyl]-3-thiophen-2-ylurea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinoxyfen | | aromatic ether;
monofluorobenzenes;
organochlorine compound;
quinolines | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nafadotride | | aromatic ether;
naphthalenecarboxamide;
nitrile;
pyrrolidines;
tertiary amino compound | dopaminergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(1-naphthalenyl)-3-[[2-(2-nitrophenoxy)-1-oxoethyl]amino]urea | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-1,3-bis(phenylmethoxy)benzene | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[(4-ethylphenoxy)methyl]-4-(6-methylheptan-2-yl)-1H-1,2,4-triazole-5-thione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-chloro-N-(2-methyl-6-oxo-5H-benzo[b][1,4]benzoxazepin-8-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(benzenesulfonyl)-4-(2,6-dimethylphenoxy)-2-phenylpyrimidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(2-methylphenoxy)-6-phenylfuro[2,3-d]pyrimidine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[4-(2-chlorophenoxy)butyl]imidazole | | aromatic ether;
imidazoles;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-chlorophenyl)-4-[[(2-methoxy-4-nitroanilino)-sulfanylidenemethyl]hydrazo]-4-oxobutanamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-methoxy-4-nitrophenyl)-2-[(1-methyl-2-imidazolyl)thio]acetamide | | aromatic ether;
C-nitro compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(phenoxymethyl)-2-thiazolyl]-1-adamantanecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxypioglitazone | | aromatic ether;
pyridines;
thiazolidinediones | human xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc-19220 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methyl-4-(3-phenoxyphenyl)-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-6-carboxylic acid ethyl ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-[4-(4-fluorophenoxy)-3-nitrophenyl]-7-(2-hydroxyethyl)-3-(phenylmethyl)purine-2,6-dione | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-phenoxybenzoic acid [2-oxo-2-(propan-2-ylamino)ethyl] ester | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-bromophenoxy)-N'-[2-[(4-methyl-1,2,4-triazol-3-yl)thio]-1-oxoethyl]acetohydrazide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2-methoxyanilino)-2-(2-phenylmethoxyphenyl)acetonitrile | | aromatic ether;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(4-phenoxyphenyl)-2-(1,2,3,4-tetrahydroisoquinolin-1-yl)acetamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3,4-dimethoxyphenyl)-3-(2-furanylmethyl)-4-imino-5H-[1]benzopyrano[2,3-d]pyrimidin-8-ol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3-dimethyl-1,5-dinitro-6-phenoxy-3-azoniabicyclo[3.3.1]non-6-ene | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fraxin | | aromatic ether;
beta-D-glucoside;
hydroxycoumarin | anti-inflammatory agent;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fraxetin | | aromatic ether;
hydroxycoumarin | anti-inflammatory agent;
antibacterial agent;
antimicrobial agent;
antioxidant;
apoptosis inducer;
apoptosis inhibitor;
Arabidopsis thaliana metabolite;
hepatoprotective agent;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,6-dehydrokawain | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| coniferin | | aromatic ether;
cinnamyl alcohol beta-D-glucoside;
monosaccharide derivative | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| daphnoretin | | aromatic ether;
hydroxycoumarin | antineoplastic agent;
antiviral agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kavain | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methysticin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| yangonin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hinokiflavone | | aromatic ether;
biflavonoid;
hydroxyflavone | antineoplastic agent;
metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gentiacaulein | | aromatic ether;
polyphenol;
xanthones | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gentisin | | aromatic ether;
polyphenol;
xanthones | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isogentisin | | aromatic ether;
polyphenol;
xanthones | EC 1.4.3.4 (monoamine oxidase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mangostin | | aromatic ether;
phenols;
xanthones | antimicrobial agent;
antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,8-dihydroxy-3,7-dimethoxyxanthone | | aromatic ether;
polyphenol;
xanthones | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| swerchirin | | aromatic ether;
phenols;
xanthones | hypoglycemic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,2,8-trihydroxy-6-methoxyxanthone | | aromatic ether;
polyphenol;
xanthones | antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wedelolactone | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sofalcone | | aromatic ether;
chalcones;
monocarboxylic acid | anti-ulcer drug;
antibacterial agent;
gastrointestinal drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neticonazole | | aromatic ether;
benzenes;
conazole antifungal drug;
enamine;
imidazole antifungal drug;
imidazoles;
methyl sulfide | antifungal drug;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pibutidine | | aromatic ether;
cyclobutenones;
olefinic compound;
piperidines;
primary amino compound;
pyridines;
secondary amino compound | anti-ulcer drug;
H2-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| purmorphamine | | aromatic ether;
morpholines;
purines;
secondary amino compound | osteogenesis regulator;
SMO receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-(2-chlorophenyl)-3-(4-ethoxyphenyl)-6-oxo-2,4,7,8-tetrahydropyrido[2,1-b][1,3,5]thiadiazine-9-carbonitrile | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 41-5253 | | aromatic ether;
benzoic acids;
sulfone;
thiochromane | apoptosis inducer;
retinoic acid receptor alpha antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glycycoumarin | | aromatic ether;
coumarins;
resorcinols | antispasmodic drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoginkgetin | | aromatic ether;
biflavonoid | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neoglycyrol | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhamnazin | | aromatic ether;
dimethoxyflavone;
phenols;
trihydroxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bosutinib | | aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lichexanthone | | aromatic ether;
phenols;
xanthones | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alternariol monomethyl ether | | aromatic ether;
benzochromenone | antifungal agent;
fungal metabolite;
mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| decussatin | | aromatic ether;
phenols;
xanthones | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bedaquiline | | aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound | antitubercular agent;
ATP synthase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benanomicin b | | aromatic ether;
disaccharide derivative;
L-alanine derivative;
polyketide;
polyphenol;
pradimicin;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pradimicin b | | aromatic ether;
L-alanine derivative;
monosaccharide derivative;
polyketide;
polyphenol;
pradimicin;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,7-dihydroxy-4-methoxyxanthone | | aromatic ether;
phenols;
xanthones | metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pradimicin a | | aromatic ether;
carboxylic acid;
disaccharide derivative;
L-alanine derivative;
p-quinones;
polyphenol;
pradimicin;
secondary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ici 118551 | | aromatic ether;
indanes;
secondary alcohol;
secondary amino compound | beta-adrenergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ochnaflavone | | aromatic ether;
biflavonoid;
hydroxyflavone | anti-inflammatory agent;
antiatherogenic agent;
antibacterial agent;
EC 3.1.1.4 (phospholipase A2) inhibitor;
leukotriene antagonist;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-fluorophenoxy)-6-methoxy-2-(4-methoxyphenyl)-1-benzothiophene 1-oxide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flavasperone | | aromatic ether;
naphtho-gamma-pyrone;
phenols | acyl-CoA:cholesterol acyltransferase 2 inhibitor;
antiviral agent;
Aspergillus metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-hydroxycordoin | | aromatic ether;
chalcones;
polyphenol | anti-inflammatory agent;
antibacterial agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-feruloylserotonin | | aromatic ether;
cinnamamides;
hydroxyindoles;
phenols;
secondary carboxamide | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kresoxim-methyl | | aromatic ether;
methoxyiminoacetate strobilurin antifungal agent;
methyl ester;
oxime O-ether | antifungal agrochemical;
environmental contaminant;
mitochondrial cytochrome-bc1 complex inhibitor;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-methoxy-3,6-diphenyl-1,2,4-triazine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrachlostrobin | | aromatic ether;
carbamate ester;
carbanilate fungicide;
methoxycarbanilate strobilurin antifungal agent;
monochlorobenzenes;
pyrazoles | antifungal agrochemical;
environmental contaminant;
mitochondrial cytochrome-bc1 complex inhibitor;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| piericidin a | | aromatic ether;
methylpyridines;
monohydroxypyridine;
secondary allylic alcohol | antimicrobial agent;
bacterial metabolite;
EC 1.6.5.3 [NADH:ubiquinone reductase (H(+)-translocating)] inhibitor;
mitochondrial respiratory-chain inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metrafenone | | aromatic ether;
aryl phenyl ketone fungicide;
benzophenones;
organobromine compound | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-fluoro-3-(trifluoromethyl)phenoxy)-n-(phenylmethyl)butanamide | | (trifluoromethyl)benzenes;
aromatic ether;
monocarboxylic acid amide;
monofluorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| b 43 | | aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(4-phenylbutoxy)psoralen | | aromatic ether;
benzenes;
psoralens | geroprotector;
immunosuppressive agent;
potassium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-ia-85380 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| yunaconitine | | acetate ester;
aromatic ether;
benzoate ester;
bridged compound;
diterpene alkaloid;
organic heteropolycyclic compound;
polyether;
secondary alcohol;
tertiary alcohol;
tertiary amino compound | antifeedant;
human urinary metabolite;
phytotoxin;
plant metabolite;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| altenusin | | aromatic ether;
carboxybiphenyl;
catechols;
hydroxybiphenyls;
polyphenol | antifungal agent;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bay 58-2667 | | aromatic ether;
benzoic acids;
dicarboxylic acid;
tertiary amino compound | antihypertensive agent;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| camostat | | aromatic ether;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lenvatinib | | aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc 716970 | | aromatic amine;
aromatic ether;
indolecarboxamide;
organochlorine compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lobeglitazone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etomoxir | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fr 148083 | | aromatic ether;
macrolide;
phenols;
secondary alcohol;
secondary alpha-hydroxy ketone | antibacterial agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-methoxycanthin-6-one | | aromatic ether;
indole alkaloid;
organic heterotetracyclic compound | antineoplastic agent;
antiplasmodial drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sb 3ct compound | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| varespladib methyl | | aromatic ether;
benzenes;
indoles;
methyl ester;
primary carboxamide | anti-inflammatory drug;
antidote;
EC 3.1.1.4 (phospholipase A2) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dapagliflozin | | aromatic ether;
C-glycosyl compound;
monochlorobenzenes | hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naveglitazar | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tivozanib | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ustiloxin b | | aromatic ether;
heterodetic cyclic peptide;
macrocycle;
phenols;
secondary alcohol;
secondary carboxamide;
sulfoxide | Aspergillus metabolite;
microtubule-destabilising agent;
mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hypothemycin | | aromatic ether;
diol;
enone;
epoxide;
macrolide;
phenols;
polyketide;
secondary alpha-hydroxy ketone | antifungal agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tryprostatin a | | aromatic ether;
dipeptide;
indole alkaloid;
indoles;
pyrrolopyrazine | breast cancer resistance protein inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cediranib | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-iodothyronamine | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n,n-dipropyl-2-(4-methoxy-3-(2-phenylethoxy)phenyl)ethylamine monohydrochloride | | aromatic ether;
hydrochloride;
methoxybenzenes;
tertiary amino compound | antipsychotic agent;
receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubraxanthone | | aromatic ether;
polyphenol;
xanthones | antibacterial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7,8-Dihydroyangonin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch 51344 | | aromatic amine;
aromatic ether;
primary alcohol;
pyrazoloquinoline;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ancistroealaine a | | aromatic ether;
biaryl;
isoquinoline alkaloid;
isoquinolines;
methoxynaphthalene;
methylnaphthalenes | antileishmanial agent;
antiplasmodial drug;
metabolite;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pimavanserin | | aromatic ether;
monofluorobenzenes;
piperidines;
tertiary amino compound;
ureas | 5-hydroxytryptamine 2A receptor inverse agonist;
antipsychotic agent;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tolfenpyrad | | aromatic amide;
aromatic ether;
organochlorine compound;
pyrazole insecticide | agrochemical;
antifungal agent;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor;
mitochondrial NADH:ubiquinone reductase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| apixaban | | aromatic ether;
lactam;
piperidones;
pyrazolopyridine | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dihydrokavain | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| troglitazone sulfate | | aromatic ether;
thiazolidinone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arisugacin | | aromatic ether;
delta-lactone;
enone;
organic heterotetracyclic compound;
tertiary alcohol | antimicrobial agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fonsecinone a | | aromatic ether;
aromatic ketone;
biaryl;
cyclic ketone;
naphtho-gamma-pyrone;
polyphenol | antibacterial agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| crenolanib | | aminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aiphanol | | aromatic ether;
benzodioxine;
lignan;
stilbenoid | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nigerloxin | | aromatic ether;
benzamides;
benzoic acids;
phenols;
styrenes | antioxidant;
Aspergillus metabolite;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
lipoxygenase inhibitor;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| msdc-0160 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dihydroxanthohumol | | aromatic ether;
dihydrochalcones;
polyphenol | EC 1.14.13.39 (nitric oxide synthase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PB28 | | aromatic ether;
piperazines;
tetralins | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-phloroeckol | | aromatic ether;
phlorotannin | antioxidant;
EC 3.1.1.3 (triacylglycerol lipase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-dimethoxy-4-hydroxybenzyl alcohol-4-O-beta-D-glucopyranoside | | aromatic ether;
benzyl alcohols;
beta-D-glucoside;
monosaccharide derivative;
primary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brivanib | | aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fg-4592 | | aromatic ether;
isoquinolines;
N-acylglycine | EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor;
EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cenicriviroc | | aromatic ether;
benzazocine;
diether;
imidazoles;
secondary carboxamide;
sulfoxide | anti-HIV agent;
anti-inflammatory agent;
antirheumatic drug;
chemokine receptor 2 antagonist;
chemokine receptor 5 antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mandipropamid | | aromatic ether;
monocarboxylic acid amide;
monochlorobenzenes;
terminal acetylenic compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyceryl ferulate | | 1-monoglyceride;
aromatic ether;
enoate ester;
phenols | antioxidant;
plant metabolite;
ultraviolet filter | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ki 8751 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ceratamine a | | alkaloid;
aromatic ether;
cyclic ketone;
organic heterobicyclic compound;
organobromine compound;
secondary amino compound;
tertiary amine | antimitotic;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bay94 9172 | | (18)F radiopharmaceutical;
aromatic ether;
polyether;
secondary amino compound;
stilbenoid;
substituted aniline | radioactive imaging agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| olodaterol | | aromatic ether;
benzoxazine;
phenols;
secondary alcohol;
secondary amino compound | beta-adrenergic agonist;
bronchodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dorsomorphin | | aromatic ether;
piperidines;
pyrazolopyrimidine;
pyridines | bone morphogenetic protein receptor antagonist;
EC 2.7.11.31 {[hydroxymethylglutaryl-CoA reductase (NADPH)] kinase} inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cj-042794 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hu 308 | | aromatic ether;
bridged compound;
carbobicyclic compound;
primary allylic alcohol;
synthetic cannabinoid | anti-inflammatory agent;
antihypertensive agent;
apoptosis inhibitor;
bone density conservation agent;
CB2 receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ki11502 | | aromatic ether;
benzamides;
quinolines;
thioureas | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| apremilast | | aromatic ether;
N-acetylarylamine;
phthalimides;
sulfone | non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PF-00835231 | | aromatic ether;
indolecarboxamide;
L-leucine derivative;
primary alcohol;
pyrrolidin-2-ones;
secondary carboxamide | anticoronaviral agent;
drug metabolite;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chir-265 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminocandin | | aromatic ether;
echinocandin;
homodetic cyclic peptide | antiinfective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zk 756326 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bay 60-6583 | | aminopyridine;
aromatic ether;
aryl sulfide;
cyanopyridine;
cyclopropanes;
monocarboxylic acid amide | adenosine A2B receptor agonist;
anti-inflammatory agent;
cardioprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| empagliflozin | | aromatic ether;
C-glycosyl compound;
monochlorobenzenes;
tetrahydrofuryl ether | hypoglycemic agent;
sodium-glucose transport protein subtype 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[5-(4-ethoxyphenyl)-3-isoxazolyl]-N-[(4-methylphenyl)methyl]butanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-desmethylrosiglitazone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(5-methyl-3-nitro-1-pyrazolyl)-N-[3-(4-methylphenoxy)-5-nitrophenyl]butanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| verruculogen | | aromatic ether;
diol;
indole alkaloid;
organic heterohexacyclic compound;
organic peroxide | Aspergillus metabolite;
GABA modulator;
mycotoxin;
Penicillium metabolite;
potassium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-O-feruloyl-beta-D-glucose | | aromatic ether;
beta-D-glucoside;
cinnamate ester;
phenols | antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2',4,5'-tetrabromodiphenyl ether | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hexabromodiphenyl ether 154 | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bde 183 | | aromatic ether;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l-798106 | | aromatic ether;
bromobenzenes;
N-sulfonylcarboxamide | prostaglandin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aflatoxin m1 | | aflatoxin;
aromatic ether;
aromatic ketone;
tertiary alcohol | Aspergillus metabolite;
human xenobiotic metabolite;
mammalian metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| macitentan | | aromatic ether;
organobromine compound;
pyrimidines;
ring assembly;
sulfamides | antihypertensive agent;
endothelin receptor antagonist;
orphan drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| CDN1163 | | aromatic ether;
quinolines;
secondary carboxamide | SERCA activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| e 7050 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(5-chloro-2-thiophenyl)methyl]-5-[(2,6-difluorophenoxy)methyl]-3-isoxazolecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dafadine C | | aromatic amide;
aromatic ether;
difluorobenzene;
isoxazoles;
N-acylpiperidine;
pyridines | P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dafadine B | | aromatic amide;
aromatic ether;
isoxazoles;
monochlorobenzenes;
monofluorobenzenes;
N-acylpiperidine;
pyridines | P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[5-(5-methyl-2-thiophenyl)-1,3,4-oxadiazol-2-yl]-N-[2-(3-pyridinyloxy)propyl]propanamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| violaceol II | | aromatic ether;
catechols;
resorcinols | mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pamapimod | | aromatic amine;
aromatic ether;
difluorobenzene;
diol;
primary alcohol;
pyridopyrimidine;
secondary amino compound | antirheumatic drug;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk690693 | | 1,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cnf 2024 | | 2-aminopurines;
aromatic ether;
organochlorine compound;
pyridines | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uk 453,061 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-{1-[4-(dimethylamino)phenyl]-3-(pyrrolidin-1-yl)propyl}-5,7-dimethoxy-4-pentyl-2H-chromen-2-one | | aromatic ether;
coumarins;
pyrrolidines;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| compound w | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-[2-[(2-methylpropan-2-yl)oxy]anilino]-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| interiotherin b | | aromatic ether;
fatty acid ester;
lignan;
organic heteropentacyclic compound;
oxacycle | anti-HIV agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7-dihydroxy-3-(3-hydroxy-4-methoxybenzyl)-6-methoxychroman-4-one | | aromatic ether;
homoisoflavonoid;
polyphenol | angiogenesis modulating agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diorcinol | | aromatic ether;
phenols | fungal metabolite;
marine metabolite;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(2-phenoxyanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(1-pyrrolidinyl)-6-[2-(trifluoromethoxy)anilino]-1,3,5-triazin-2-yl]amino]ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(5-chloro-2-ethoxyanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(5-chloro-2-propan-2-yloxyanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mk 5108 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-azepanyl-[5-[(4-chloro-3,5-dimethylphenoxy)methyl]-3-isoxazolyl]methanone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(1-((5-((2,6-dimethylphenoxy)methyl)-3-isoxazolyl)carbonyl)-4-piperidinyl)pyridine | | aromatic amide;
aromatic ether;
isoxazoles;
N-acylpiperidine;
pyridines | geroprotector;
P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(1-ethyl-3-methyl-4-pyrazolyl)methyl]-N-[4-(2-fluorophenoxy)phenyl]-4-piperidinecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dafadine O | | aromatic amide;
aromatic ether;
isoxazoles;
N-acylpiperidine;
pyridines;
ring assembly | P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[(3,4-dimethylphenoxy)methyl]-N-methyl-N-(4-oxanylmethyl)-3-isoxazolecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pci 32765 | | acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AMG-208 | | aromatic ether;
quinolines;
triazolopyridazine | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxyspirotryprostatin b | | aromatic ether;
azaspiro compound;
indole alkaloid;
indolones | antineoplastic agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lucitanib | | aromatic ether;
cyclopropanes;
naphthalenecarboxamide;
primary amino compound;
quinolines | antineoplastic agent;
fibroblast growth factor receptor antagonist;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| act-132577 | | aromatic ether;
organobromine compound;
pyrimidines;
sulfamides | antihypertensive agent;
drug metabolite;
endothelin receptor antagonist;
xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk 2126458 | | aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk 1363089 | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(2S,3S)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-2-[[methyl(methylsulfonyl)amino]methyl]-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-8-yl]-3-propan-2-ylurea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[(2S,3S)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-2-[[methyl(methylsulfonyl)amino]methyl]-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-10-yl]-3-propan-2-ylurea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-cyclohexyl-1-[[(2S,3S)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-8-[[oxo-(propan-2-ylamino)methyl]amino]-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-1-methylurea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-cyclohexyl-1-[[(2S,3R)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-10-[[oxo-(propan-2-ylamino)methyl]amino]-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-1-methylurea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2S,3S)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-2-[[methyl-[(4-phenoxyphenyl)methyl]amino]methyl]-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-10-yl]-4-pyridinecarboxamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3,5-dimethyl-4-isoxazolyl)-3-[(2R,3R)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-2-(methylaminomethyl)-6-oxo-2,3,4,7-tetrahydro-1,5-benzoxazonin-9-yl]urea | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monepantel | | (trifluoromethyl)benzenes;
aromatic ether;
aryl sulfide;
nitrile;
secondary carboxamide | anthelminthic drug;
nematicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| an2728 | | aromatic ether;
benzoxaborole;
nitrile | antipsoriatic;
non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| grazoprevir | | aromatic ether;
azamacrocycle;
carbamate ester;
cyclopropanes;
lactam;
N-sulfonylcarboxamide;
quinoxaline derivative | antiviral drug;
hepatitis C protease inhibitor;
hepatoprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hordatine a | | aromatic ether;
benzofurans;
dicarboxylic acid diamide;
guanidines;
phenols | adrenergic antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kavain | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy)-3-pyridazinone | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tak-632 | | (trifluoromethyl)benzenes;
aromatic ether;
benzothiazoles;
cyclopropylcarboxamide;
monofluorobenzenes;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
necroptosis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lrrk2-in1 | | aromatic amine;
aromatic ether;
N-acylpiperidine;
N-alkylpiperazine;
pyrimidobenzodiazepine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quinolobactin | | aromatic ether;
monohydroxyquinoline;
phenols;
quinolinemonocarboxylic acid | bacterial metabolite;
siderophore | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AZD1979 | | aromatic ether;
azaspiro compound;
carboxamide;
N-acylazetidine;
oxadiazole;
oxaspiro compound;
oxetanes | melanin-concentrating hormone receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aripiprazole lauroxil | | aromatic ether;
delta-lactam;
dichlorobenzene;
dodecanoate ester;
N-alkylpiperazine;
N-arylpiperazine;
quinolone | H1-receptor antagonist;
prodrug;
second generation antipsychotic;
serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-199 | | aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xl765 | | aromatic amine;
aromatic ether;
benzamides;
quinoxaline derivative;
sulfonamide | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| DMH1 | | aromatic ether;
pyrazolopyrimidine;
quinolines | antineoplastic agent;
bone morphogenetic protein receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 4800567 | | aromatic ether;
monochlorobenzenes;
oxanes;
pyrazolopyrimidine | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propenylphosphonic acid | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-333 | | aromatic ether;
naphthalenes;
pyrimidone;
sulfonamide | antiviral drug;
nonnucleoside hepatitis C virus polymerase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naloxegol | | aromatic ether;
organic heteropentacyclic compound;
phenols;
polyether;
tertiary alcohol | cathartic;
mu-opioid receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ceritinib | | aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MK-8353 | | aromatic ether;
dihydropyridine;
indazoles;
methyl sulfide;
N-alkylpyrrolidine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| HG-10-102-01 | | aminopyrimidine;
aromatic ether;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
secondary amino compound | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(5-methyl-2-furanyl)methylideneamino]-2-phenoxybenzamide | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| saroglitazar | | aromatic ether;
methyl sulfide;
monocarboxylic acid;
pyrroles | hypoglycemic agent;
PPARalpha agonist;
PPARgamma agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fertaric acid | | aromatic ether;
cinnamate ester;
dicarboxylic acid;
phenols;
tetraric acid derivative | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[4-(4-chlorophenoxy)-2-(trifluoromethyl)phenyl]-1-(1H-1,2,4-triazol-1-yl)propan-2-ol | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
tertiary alcohol;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf-06463922 | | aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| DDR1-IN-1 | | (trifluoromethyl)benzenes;
aromatic ether;
benzamides;
N-alkylpiperazine;
oxindoles;
secondary carboxamide | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ldc4297 | | aromatic ether;
piperidines;
pyrazoles;
pyrazolotriazine;
secondary amino compound | antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MLI-2 | | aromatic ether;
cyclopropanes;
indazoles;
morpholines;
pyrimidines;
tertiary amino compound | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ap20187 | | aromatic ether;
carboxylic ester;
N-acylpiperidine;
tertiary amino compound | ligand | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methysticin | | 2-pyranones;
aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| biliatresone | | aromatic ether;
aromatic ketone;
benzodioxoles;
enone;
phenols | plant metabolite;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tak 491 | | 1,2,4-oxadiazole;
aromatic ether;
benzimidazoles;
carboxylic ester;
cyclic carbonate ester;
dioxolane | angiotensin receptor antagonist;
antihypertensive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azilsartan | | 1,2,4-oxadiazole;
aromatic ether;
benzimidazolecarboxylic acid | angiotensin receptor antagonist;
antihypertensive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydrazinocurcumin | | aromatic ether;
olefinic compound;
polyphenol;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mirodenafil | | aromatic ether;
N-alkylpiperazine;
primary alcohol;
pyrrolopyrimidine;
sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cerulomycin | | aldoxime;
aromatic ether;
bipyridines;
pyridine alkaloid | antineoplastic agent;
bacterial metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| undecylprodigiosin | | alkaloid;
aromatic ether;
tripyrrole | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
biological pigment;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sb-590885 | | aromatic ether;
imidazoles;
ketoxime;
pyridines;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(trifluoromethoxy)phenyl]methylthio]-1,5,6,7-tetrahydrocyclopenta[d]pyrimidin-4-one | | aromatic ether | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PF-07304814 | | aromatic ether;
indolecarboxamide;
L-leucine derivative;
phosphate monoester;
pyrrolidin-2-ones;
secondary carboxamide | anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | | phenols;
tertiary amino compound;
tetralins | serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sk&f 77434 | | benzazepine;
catechols;
tertiary amino compound | dopamine agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 173074 | | aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethylisopropylamiloride | | aromatic amine;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines;
tertiary amino compound | anti-arrhythmia drug;
neuroprotective agent;
sodium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amiodarone | | 1-benzofurans;
aromatic ketone;
organoiodine compound;
tertiary amino compound | cardiovascular drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amodiaquine | | aminoquinoline;
organochlorine compound;
phenols;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antimalarial;
drug allergen;
EC 2.1.1.8 (histamine N-methyltransferase) inhibitor;
non-steroidal anti-inflammatory drug;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antazoline | | aromatic amine;
imidazolines;
tertiary amino compound | cholinergic antagonist;
H1-receptor antagonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azelastine | | monochlorobenzenes;
phthalazines;
tertiary amino compound | anti-allergic agent;
anti-asthmatic drug;
bronchodilator agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
H1-receptor antagonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| biperiden | | piperidines;
tertiary alcohol;
tertiary amino compound | antidote to sarin poisoning;
antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist;
parasympatholytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromhexine | | organobromine compound;
substituted aniline;
tertiary amino compound | mucolytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromodiphenhydramine | | organobromine compound;
tertiary amino compound | antimicrobial agent;
H1-receptor antagonist;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bupivacaine | | aromatic amide;
piperidinecarboxamide;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carbinoxamine | | monochlorobenzenes;
pyridines;
tertiary amino compound | anti-allergic agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorambucil | | aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound | alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chloroquine | | aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorpheniramine | | monochlorobenzenes;
pyridines;
tertiary amino compound | anti-allergic agent;
antidepressant;
antipruritic drug;
H1-receptor antagonist;
histamine antagonist;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofedanol | | diarylmethane;
tertiary amino compound | antitussive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyclopentolate | | carboxylic ester;
tertiary alcohol;
tertiary amino compound | diagnostic agent;
muscarinic antagonist;
mydriatic agent;
parasympatholytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cycrimine | | piperidines;
tertiary alcohol;
tertiary amino compound | antidyskinesia agent;
antiparkinson drug;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diphenhydramine | | ether;
tertiary amino compound | anti-allergic agent;
antidyskinesia agent;
antiemetic;
antiparkinson drug;
antipruritic drug;
antitussive;
H1-receptor antagonist;
local anaesthetic;
muscarinic antagonist;
oneirogen;
sedative | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dipyridamole | | piperidines;
pyrimidopyrimidine;
tertiary amino compound;
tetrol | adenosine phosphodiesterase inhibitor;
EC 3.5.4.4 (adenosine deaminase) inhibitor;
platelet aggregation inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| disopyramide | | monocarboxylic acid amide;
pyridines;
tertiary amino compound | anti-arrhythmia drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-phenyl-2-palmitoylamino-3-morpholino-1-propanol | | benzyl alcohols;
fatty amide;
morpholines;
secondary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxepin | | dibenzooxepine;
tertiary amino compound | antidepressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| profenamine | | phenothiazines;
tertiary amino compound | adrenergic antagonist;
antidyskinesia agent;
antiparkinson drug;
histamine antagonist;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flavoxate | | carboxylic ester;
flavones;
piperidines;
tertiary amino compound | antispasmodic drug;
muscarinic antagonist;
parasympatholytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flurazepam | | 1,4-benzodiazepinone;
monofluorobenzenes;
organochlorine compound;
tertiary amino compound | anticonvulsant;
anxiolytic drug;
GABAA receptor agonist;
sedative | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gbr 12935 | | ether;
N-alkylpiperazine;
tertiary amino compound | dopamine uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxychloroquine | | aminoquinoline;
organochlorine compound;
primary alcohol;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antimalarial;
antirheumatic drug;
dermatologic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lidocaine | | benzenes;
monocarboxylic acid amide;
tertiary amino compound | anti-arrhythmia drug;
drug allergen;
environmental contaminant;
local anaesthetic;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isothipendyl | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ketotifen | | cyclic ketone;
olefinic compound;
organic heterotricyclic compound;
organosulfur heterocyclic compound;
piperidines;
tertiary amino compound | anti-asthmatic drug;
H1-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lofepramine | | aromatic ketone;
dibenzoazepine;
monochlorobenzenes;
tertiary amino compound | antidepressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | | benzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| meperidine | | ethyl ester;
piperidinecarboxylate ester;
tertiary amino compound | antispasmodic drug;
kappa-opioid receptor agonist;
mu-opioid receptor agonist;
opioid analgesic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mesoridazine | | phenothiazines;
sulfoxide;
tertiary amino compound | dopaminergic antagonist;
first generation antipsychotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methadone | | benzenes;
diarylmethane;
ketone;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methiothepin | | aryl sulfide;
dibenzothiepine;
N-alkylpiperazine;
tertiary amino compound | antipsychotic agent;
dopaminergic antagonist;
geroprotector;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metoclopramide | | benzamides;
monochlorobenzenes;
substituted aniline;
tertiary amino compound | antiemetic;
dopaminergic antagonist;
environmental contaminant;
gastrointestinal drug;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| minoxidil | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monodansylcadaverine | | aminonaphthalene;
primary amino compound;
sulfonamide;
tertiary amino compound | EC 2.3.2.13 (protein-glutamine gamma-glutamyltransferase) inhibitor;
fluorochrome;
protective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mosapramine | | azaspiro compound;
dibenzoazepine;
organochlorine compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nefopam | | benzoxazocine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nicardipine | | benzenes;
C-nitro compound;
diester;
dihydropyridine;
methyl ester;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nizatidine | | 1,3-thiazoles;
C-nitro compound;
carboxamidine;
organic sulfide;
tertiary amino compound | anti-ulcer drug;
cholinergic drug;
H2-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| orphenadrine | | ether;
tertiary amino compound | antidyskinesia agent;
antiparkinson drug;
H1-receptor antagonist;
muscarinic antagonist;
muscle relaxant;
NMDA receptor antagonist;
parasympatholytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benoxinate | | amino acid ester;
benzoate ester;
substituted aniline;
tertiary amino compound | drug allergen;
local anaesthetic;
topical anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxybutynin | | acetylenic compound;
carboxylic ester;
racemate;
tertiary alcohol;
tertiary amino compound | antispasmodic drug;
calcium channel blocker;
local anaesthetic;
muscarinic antagonist;
muscle relaxant;
parasympatholytic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pheniramine | | pyridines;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| piromidic acid | | monocarboxylic acid;
pyridopyrimidine;
pyrrolidines;
quinolone antibiotic;
tertiary amino compound | antibacterial drug;
DNA synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pj-34 | | phenanthridines;
secondary carboxamide;
tertiary amino compound | angiogenesis inhibitor;
anti-inflammatory agent;
antiatherosclerotic agent;
antineoplastic agent;
apoptosis inducer;
cardioprotective agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| procaine | | benzoate ester;
substituted aniline;
tertiary amino compound | central nervous system depressant;
drug allergen;
local anaesthetic;
peripheral nervous system drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propiomazine | | aromatic ketone;
phenothiazines;
tertiary amino compound | dopaminergic antagonist;
histamine antagonist;
muscarinic antagonist;
phenothiazine antipsychotic drug;
sedative;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| psilocin | | hydroxyindoles;
phenols;
tertiary amino compound;
tryptamine alkaloid | drug metabolite;
fungal metabolite;
hallucinogen;
human xenobiotic metabolite;
serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol | | benzazepine;
organochlorine compound;
tertiary amino compound | dopaminergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| setiptiline | | tertiary amino compound;
tetracyclic antidepressant | alpha-adrenergic antagonist;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sibutramine | | organochlorine compound;
tertiary amino compound | anti-obesity agent;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetracaine | | benzoate ester;
tertiary amino compound | local anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n,n,n',n'-tetrakis(2-pyridylmethyl)ethylenediamine | | N-substituted diamine;
pyridines;
tertiary amino compound | apoptosis inducer;
chelator;
copper chelator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trimethobenzamide | | benzamides;
tertiary amino compound | antiemetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trimipramine | | dibenzoazepine;
tertiary amino compound | antidepressant;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| venlafaxine | | cyclohexanols;
monomethoxybenzene;
tertiary alcohol;
tertiary amino compound | adrenergic uptake inhibitor;
analgesic;
antidepressant;
dopamine uptake inhibitor;
environmental contaminant;
serotonin uptake inhibitor;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zotepine | | dibenzothiepine;
tertiary amino compound | alpha-adrenergic drug;
second generation antipsychotic;
serotonergic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phentolamine | | imidazoles;
phenols;
substituted aniline;
tertiary amino compound | alpha-adrenergic antagonist;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincristine | | acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminopyrine | | pyrazolone;
tertiary amino compound | antipyretic;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetrabenazine | | benzoquinolizine;
cyclic ketone;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acepromazine | | aromatic ketone;
methyl ketone;
phenothiazines;
tertiary amino compound | phenothiazine antipsychotic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| egtazic acid | | diether;
tertiary amino compound;
tetracarboxylic acid | chelator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gramine | | aminoalkylindole;
indole alkaloid;
tertiary amino compound | antibacterial agent;
antiviral agent;
plant metabolite;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thenyldiamine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(dimethylamino)benzaldehyde | | benzaldehydes;
substituted aniline;
tertiary amino compound | chromogenic compound | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-diethylaminoethanol | | ethanolamines;
primary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triethanolamine | | amino alcohol;
tertiary amino compound;
triol | buffer;
surfactant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-nitrosodimethylaniline | | dimethylaniline;
nitroso compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triethylenediamine | | bridged compound;
diamine;
saturated organic heterobicyclic parent;
tertiary amino compound | antioxidant;
catalyst;
reagent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| galantamine | | benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
organic heterotetracyclic compound;
tertiary amino compound | antidote to curare poisoning;
cholinergic drug;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-erythroidine | | delta-lactone;
indole alkaloid;
organic heterotetracyclic compound;
tertiary amino compound | muscle relaxant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| psilocybin | | organic phosphate;
tertiary amino compound;
tryptamine alkaloid | fungal metabolite;
hallucinogen;
prodrug;
serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neutral red base | | aromatic amine;
phenazines;
primary amino compound;
tertiary amino compound | acid-base indicator;
dye;
two-colour indicator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-dimethylaminopyridine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prothipendyl | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dymanthine | | tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azaperone | | aminopyridine;
aromatic ketone;
monofluorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
tertiary amino compound | antipsychotic agent;
dopaminergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glaucine | | aporphine alkaloid;
organic heterotetracyclic compound;
polyether;
tertiary amino compound | antibacterial agent;
antineoplastic agent;
antitussive;
muscle relaxant;
NF-kappaB inhibitor;
plant metabolite;
platelet aggregation inhibitor;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyphosphine | | glycine derivative;
phosphonic acids;
tertiary amino compound | plant growth retardant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| c.i. solvent yellow 56 | | azobenzenes;
substituted aniline;
tertiary amino compound | dye;
mutagen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-dimethylaminophenol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethyl 4-dimethylaminobenzoate | | benzoate ester;
ethyl ester;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mopidamol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thenalidine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oryzalin | | aromatic amine;
C-nitro compound;
sulfonamide;
tertiary amino compound | agrochemical;
antimitotic;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pirimicarb | | aminopyrimidine;
carbamate ester;
tertiary amino compound | agrochemical;
carbamate insecticide;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
environmental contaminant;
insecticide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dihydro-beta-erythroidine | | delta-lactone;
organic heterotetracyclic compound;
tertiary amino compound | nicotinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propamocarb | | carbamate ester;
carbamate fungicide;
tertiary amino compound | antifungal agrochemical;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tridemorph | | morpholines;
tertiary amino compound | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amitraz | | formamidines;
tertiary amino compound | acaricide;
environmental contaminant;
insecticide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| butaclamol | | amino alcohol;
organic heteropentacyclic compound;
tertiary alcohol;
tertiary amino compound | dopaminergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline | | isoquinolinol;
tertiary amino compound | human metabolite;
neurotoxin;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vx | | organic thiophosphate;
tertiary amino compound | EC 3.1.1.7 (acetylcholinesterase) inhibitor;
neurotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vindesine | | methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
primary carboxamide;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| miglustat | | piperidines;
tertiary amino compound | anti-HIV agent;
EC 2.4.1.80 (ceramide glucosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| loceryl | | morpholine antifungal drug;
tertiary amino compound | EC 1.14.13.132 (squalene monooxygenase) inhibitor;
EC 1.3.1.70 (Delta(14)-sterol reductase) inhibitor;
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mifepristone | | 3-oxo-Delta(4) steroid;
acetylenic compound;
tertiary amino compound | abortifacient;
contraceptive drug;
hormone antagonist;
synthetic oral contraceptive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carmoxirole | | indolecarboxylic acid;
tertiary amino compound;
tetrahydropyridine | antihypertensive agent;
dopamine agonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naxagolide | | organic heterotricyclic compound;
phenols;
tertiary amino compound | anticonvulsant;
antiparkinson drug;
dopamine agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tiagabine | | beta-amino acid;
piperidinemonocarboxylic acid;
tertiary amino compound;
thiophenes | anticonvulsant;
GABA reuptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eliprodil | | monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| irinotecan | | carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| carfentanil | | methyl ester;
piperidines;
tertiary amino compound;
tertiary carboxamide | mu-opioid receptor agonist;
opioid analgesic;
tranquilizing drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acridine orange | | aminoacridines;
aromatic amine;
tertiary amino compound | fluorochrome;
histological dye | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tenocyclidine | | piperidines;
tertiary amino compound;
thiophenes | central nervous system stimulant;
hallucinogen;
neuroprotective agent;
NMDA receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nelfinavir | | aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound | antineoplastic agent;
HIV protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plerixafor | | azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound | anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nile red | | aromatic amine;
cyclic ketone;
organic heterotetracyclic compound;
tertiary amino compound | fluorochrome;
histological dye | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cephalotaxine | | benzazepine alkaloid fundamental parent;
benzazepine alkaloid;
cyclic acetal;
enol ether;
organic heteropentacyclic compound;
secondary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(diethylamino)benzaldehyde | | aromatic amine;
benzaldehydes;
tertiary amino compound | EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| propildazine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tubulosine | | beta-carbolines;
isoquinoline alkaloid;
isoquinolines;
phenols;
secondary amino compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| voacamine | | alkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rivastigmine | | carbamate ester;
tertiary amino compound | cholinergic drug;
EC 3.1.1.8 (cholinesterase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dimethylformamide-dimethylacetal | | acetal;
tertiary amino compound | chromatographic reagent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(3-(dimethylamino)propyl)methacrylamide | | tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n,n-diisopropylethylamine | | tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiroxamine | | dioxolane;
spiroketal;
tertiary amino compound | antifungal agrochemical;
environmental contaminant;
sterol biosynthesis inhibitor;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mor-14 | | hydroxypiperidine;
piperidine alkaloid;
tertiary amino compound | anti-HIV agent;
cardioprotective agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ecgonine methyl ester | | methyl ester;
tertiary amino compound;
tropane alkaloid | analgesic;
central nervous system depressant;
metabolite;
mouse metabolite;
opioid analgesic;
peripheral nervous system drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ecteinascidin 743 | | acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound | alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aporphine | | aporphine alkaloid;
isoquinoline alkaloid fundamental parent;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| efonidipine | | C-nitro compound;
carboxylic ester;
dihydropyridine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(4-(7-diethylamino-4-methylcoumarin-3-yl)phenyl)maleimide | | benzenes;
coumarins;
maleimides;
tertiary amino compound | fluorescent dye | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lofentanil | | methyl ester;
piperidines;
tertiary amino compound;
tertiary carboxamide | mu-opioid receptor agonist;
opioid analgesic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | | 1-benzothiophenes;
piperidines;
tertiary amino compound | dopamine uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| desvenlafaxine | | cyclohexanols;
phenols;
tertiary amino compound | antidepressant;
drug metabolite;
marine xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xaliproden | | (trifluoromethyl)benzenes;
naphthalenes;
tertiary amino compound;
tetrahydropyridine | serotonergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ulipristal acetate | | 20-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester;
tertiary amino compound | contraceptive drug;
progesterone receptor modulator;
progestin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sr 57227a | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,8-dinitroimipramine | | C-nitro compound;
dibenzoazepine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sk&f 83959 | | benzazepine;
catechols;
organochlorine compound;
tertiary amino compound | dopamine agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,6-didehydrosparteine | | organic heterotetracyclic compound;
quinolizidine alkaloid;
tertiary amino compound | human xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stephenanthrine | | cyclic acetal;
organic heterotetracyclic compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydromethylthionine | | aromatic amine;
phenothiazines;
tertiary amino compound | bacterial xenobiotic metabolite;
fluorochrome;
mouse metabolite;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nbi 27914 | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| top 53 | | furonaphthodioxole;
gamma-lactone;
organic heterotetracyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antalarmin | | pyrrolopyrimidine;
tertiary amino compound | corticotropin-releasing factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alpha-putrescinylthymine | | N-substituted putrescine;
pyrimidine nucleobase;
pyrimidone;
secondary amino compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-morpholinoanilino)-6-cyclohexylaminopurine | | morpholines;
purines;
secondary amino compound;
tertiary amino compound | adenosine A3 receptor antagonist;
antineoplastic agent;
Aurora kinase inhibitor;
cell dedifferentiation agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 778,123 | | imidazoles;
monochlorobenzenes;
nitrile;
piperazinone;
tertiary amino compound | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincaleukoblastine | | acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azaleucine | | alanine derivative;
leucine derivative;
non-proteinogenic alpha-amino acid;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc 23766 | | aminopyrimidine;
aminoquinoline;
primary amino compound;
secondary amino compound;
tertiary amino compound | antiviral agent;
apoptosis inducer;
EC 3.6.5.2 (small monomeric GTPase) inhibitor;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gant 61 | | aminal;
dialkylarylamine;
pyridines;
substituted aniline;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
glioma-associated oncogene inhibitor;
Hedgehog signaling pathway inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| conessine | | steroid alkaloid;
tertiary amino compound | antibacterial agent;
antimalarial;
H3-receptor antagonist;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rocuronium | | 3alpha-hydroxy steroid;
acetate ester;
androstane;
morpholines;
quaternary ammonium ion;
tertiary amino compound | drug allergen;
muscle relaxant;
neuromuscular agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deltaline | | acetate ester;
cyclic acetal;
diterpene alkaloid;
organic polycyclic compound;
tertiary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxyacanthine | | bisbenzylisoquinoline alkaloid;
isoquinolines;
macrocycle;
phenols;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ergonovine | | ergot alkaloid;
monocarboxylic acid amide;
organic heterotetracyclic compound;
primary alcohol;
secondary amino compound;
tertiary amino compound | diagnostic agent;
fungal metabolite;
oxytocic;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| colforsin daropate | | acetate ester;
carboxylic ester;
cyclic ketone;
diol;
organic heterotricyclic compound;
tertiary amino compound | adenylate cyclase agonist;
antihypertensive agent;
cardiotonic drug;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cocaine | | benzoate ester;
methyl ester;
tertiary amino compound;
tropane alkaloid | adrenergic uptake inhibitor;
central nervous system stimulant;
dopamine uptake inhibitor;
environmental contaminant;
local anaesthetic;
mouse metabolite;
plant metabolite;
serotonin uptake inhibitor;
sodium channel blocker;
sympathomimetic agent;
vasoconstrictor agent;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| afimoxifene | | phenols;
tertiary amino compound | antineoplastic agent;
estrogen receptor antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-nonyl-1-deoxynojirimycin | | hydroxypiperidine;
tertiary amino compound | antiviral agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
EC 3.2.1.45 (glucosylceramidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-chlorophenyl)-6-(1-pyrrolidinyl)-1,2,4,5-tetrazine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-methylproline | | L-alpha-amino acid zwitterion;
L-proline derivative;
tertiary amino compound | human metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-[3-(dimethylamino)phenyl]-N-methyl-1,3,4-thiadiazol-2-amine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4-(2-furanylmethyl)-N2-(3-methylphenyl)-6-(4-morpholinyl)-1,3,5-triazine-2,4-diamine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-(2-methyl-2,3-dihydroindol-1-yl)-3-(phenylmethyl)triazolo[4,5-d]pyrimidine | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tiamulin | | carbotricyclic compound;
carboxylic ester;
cyclic ketone;
organic sulfide;
secondary alcohol;
semisynthetic derivative;
tertiary amino compound;
tetracyclic diterpenoid | antibacterial drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-amino-4-(cyanomethyl)-6-(N-methylanilino)pyridine-3,5-dicarbonitrile | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[4-(diethylamino)phenyl]-N'-phenylurea | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-bromo-2-phenyl-5-(1-piperidinyl)-3-pyridazinone | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4,N4-dimethyl-N1-(4-nitro-1,1-dioxo-2,5-dihydrothiophen-3-yl)benzene-1,4-diamine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(2,3-dihydro-1H-indol-1-yl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[methyl-(4-thiophen-2-yl-2-thiazolyl)amino]phenol | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[4-bromo-5-(4-morpholinyl)-2-furanyl]methylideneamino]phenol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloro-5-(dimethylamino)-2-(4-methylphenyl)-3-pyridazinone | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[5-(4-chlorophenyl)-1,3,5-dithiazinan-2-ylidene]-2-diethoxyphosphorylacetonitrile | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(4-chloroanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(2,4-dioxo-1H-pyrimidin-6-yl)-N-[2-(4-morpholinyl)ethyl]acetamide | | morpholines;
pyrimidone;
secondary carboxamide;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-chloro-N-[4-(N-propan-2-ylanilino)phenyl]acetamide | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamoxifen | | stilbenoid;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(1-pyrrolidinyl)-5-(trifluoromethyl)pyridine-2-carbothioamide | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wiskostatin | | carbazoles;
organobromine compound;
secondary alcohol;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-oxo-2-[4-[5-(trifluoromethyl)-2-pyridinyl]-1,4-diazepan-1-yl]ethyl]thio]acetic acid | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(4-ethyl-1-piperazinyl)-5-methylpyridazino[3,4-b][1,4]benzoxazine | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(5,6-diphenyl-1,2,4-triazin-3-yl)morpholine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[[5,5-dimethyl-3-(4-morpholinyl)-1-cyclohex-2-enylidene]amino]-N,N-dimethylaniline | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stenusin | | piperidine alkaloid;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dasatinib | | 1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2016 | 2022 | 5.4 | low | 1 | 0 | 0 | 0 | 6 | 2 |
| noribogaine | | monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
secondary amino compound;
tertiary amino compound | kappa-opioid receptor agonist;
NMDA receptor antagonist;
psychotropic drug;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(3-methylanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(N-ethylanilino)-4-thieno[3,2-d][1,3]thiazinone | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(N-ethylanilino)propyl]-2,4-dimethyl-6-oxo-3-pyrancarboxamide | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(1-azepanyl)-1,3,4-thiadiazol-2-amine | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(5-chloro-2-methylphenyl)-6-(2,6-dimethyl-4-morpholinyl)-1H-pyrimidine-2,4-dione | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N4-ethyl-N6,1,2-trimethyl-N4-phenylpyrimidin-1-ium-4,6-diamine | | aromatic amine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clopidogrel carboxylic acid | | monocarboxylic acid;
monochlorobenzenes;
tertiary amino compound;
thienopyridine | drug metabolite;
marine xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| LY-310762 | | aromatic ketone;
monofluorobenzenes;
oxindoles;
piperidines;
tertiary amino compound | receptor modulator;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly 367265 | | dihydropyridine;
fluoroindole;
tertiary amino compound;
thiadiazoloquinoline | antidepressant;
geroprotector;
serotonergic antagonist;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[4-(dimethylamino)phenyl]-N-methyl-5-(4-methylphenyl)-3,4-dihydropyrazole-2-carbothioamide | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mycophenolate mofetil | | carboxylic ester;
ether;
gamma-lactone;
phenols;
tertiary amino compound | anticoronaviral agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cassaine | | enoate ester;
organic hydroxy compound;
tertiary amino compound;
tricyclic diterpenoid | antihypertensive agent;
cardiotonic drug;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
local anaesthetic;
plant metabolite;
poison | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| josamycin | | acetate ester;
aldehyde;
disaccharide derivative;
glycoside;
macrolide antibiotic;
tertiary alcohol;
tertiary amino compound | antibacterial drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acetylspiramycin | | acetate ester;
aldehyde;
disaccharide derivative;
ether;
macrolide;
tertiary amino compound | antibacterial drug;
antimicrobial agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n,n-dimethylsphingenine | | aminodiol;
sphingoid;
tertiary amino compound | EC 2.7.1.91 (sphingosine kinase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alvocidib | | dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound | antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin | | 1,4-benzoquinones;
ansamycin;
carbamate ester;
secondary amino compound;
tertiary amino compound | Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| morphine | | morphinane alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | anaesthetic;
drug allergen;
environmental contaminant;
geroprotector;
mu-opioid receptor agonist;
opioid analgesic;
plant metabolite;
vasodilator agent;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kn 93 | | monochlorobenzenes;
monomethoxybenzene;
primary alcohol;
sulfonamide;
tertiary amino compound | EC 2.7.11.17 (Ca(2+)/calmodulin-dependent protein kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| su 11652 | | olefinic compound;
organochlorine compound;
oxindoles;
pyrrolecarboxamide;
tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| palbociclib | | aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| catharanthine | | alkaloid ester;
bridged compound;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oripavine | | ether;
morphinane alkaloid;
organic heteropentacyclic compound;
organic hydroxy compound;
tertiary amino compound | bacterial xenobiotic metabolite;
opioid analgesic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cinanserin | | aryl sulfide;
cinnamamides;
secondary carboxamide;
tertiary amino compound | anticoronaviral agent;
antiviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| DPI2 | | benzenes;
morpholines;
secondary carboxamide;
tertiary amino compound;
thiazolidinone | ferroptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7-hydroxy-2-(n-n-propyl-n-(3-iodo-2'-propenyl)-amino)tetralin | | organoiodine compound;
phenols;
tertiary amino compound;
tetralins | dopamine agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sdz eaa 494 | | monocarboxylic acid;
olefinic compound;
phosphonic acids;
piperazinecarboxylic acid;
tertiary amino compound | anticonvulsant;
neuroprotective agent;
NMDA receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| demycarosylturimycin h | | aldehyde;
disaccharide derivative;
ether;
macrolide;
tertiary amino compound | antibacterial drug;
antimicrobial agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 25-6981 | | benzenes;
phenols;
piperidines;
secondary alcohol;
tertiary amino compound | anticonvulsant;
antidepressant;
neuroprotective agent;
NMDA receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eaa-090 | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prasugrel | | acetate ester;
cyclopropanes;
ketone;
monofluorobenzenes;
tertiary amino compound;
thienopyridine | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| muromonab-cd3 | | alkaloid;
macrocycle;
organic heteropentacyclic compound;
organonitrogen heterocyclic compound;
oxacycle;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
IP3 receptor antagonist;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| px-866 | | acetate ester;
delta-lactone;
organic heterotetracyclic compound;
tertiary amino compound | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pi103 | | aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| selexipag | | aromatic amine;
ether;
monocarboxylic acid amide;
N-sulfonylcarboxamide;
pyrazines;
tertiary amino compound | orphan drug;
platelet aggregation inhibitor;
prodrug;
prostacyclin receptor agonist;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tofacitinib | | N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound | antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mre 269 | | aromatic amine;
ether;
monocarboxylic acid;
pyrazines;
sulfonamide;
tertiary amino compound | drug metabolite;
orphan drug;
platelet aggregation inhibitor;
prostacyclin receptor agonist;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pateamine a | | 1,3-thiazoles;
macrodiolide;
olefinic compound;
primary amino compound;
tertiary amino compound | antineoplastic agent;
antiviral agent;
eukaryotic initiation factor 4F inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| edoxaban | | chloropyridine;
monocarboxylic acid amide;
tertiary amino compound;
thiazolopyridine | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| akuammicine | | methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-737 | | aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound | anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sarpagine | | indole alkaloid;
phenols;
primary alcohol;
secondary amino compound;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-one | | alkaloid;
chromones;
hydroxypiperidine;
resorcinols;
tertiary amino compound | anti-inflammatory agent;
anti-ulcer drug;
anticholesteremic drug;
antileishmanial agent;
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
fungal metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ku 0063794 | | benzyl alcohols;
monomethoxybenzene;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flupyradifurone | | butenolide;
enamine;
monochloropyridine;
organofluorine insecticide;
tertiary amino compound | insecticide;
nicotinic acetylcholine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alcaftadine | | aldehyde;
imidazobenzazepine;
piperidines;
tertiary amino compound | anti-allergic agent;
H1-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzoylaconine | | benzoate ester;
bridged compound;
diterpene alkaloid;
organic heteropolycyclic compound;
polyether;
secondary alcohol;
tertiary alcohol;
tertiary amino compound;
tetrol | phytotoxin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deoxyaconitine | | acetate ester;
benzoate ester;
bridged compound;
diol;
diterpene alkaloid;
organic heteropolycyclic compound;
polyether;
secondary alcohol;
tertiary amino compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(4-methylanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(2-chloroanilino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]ethanol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[4-(2-hydroxyethylamino)-6-(1-pyrrolidinyl)-1,3,5-triazin-2-yl]amino]phenol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vindolinine | | methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tenovin-6 | | monocarboxylic acid amide;
tertiary amino compound;
thioureas | antineoplastic agent;
p53 activator;
Sir2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzoylmesaconine | | benzoate ester;
bridged compound;
diterpene alkaloid;
organic heteropolycyclic compound;
polyether;
secondary alcohol;
tertiary alcohol;
tertiary amino compound;
tetrol | analgesic;
antiinfective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch772984 | | biaryl;
indazoles;
N-acylpiperazine;
N-alkylpyrrolidine;
N-arylpiperazine;
pyridines;
pyrimidines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary amino compound;
tertiary carboxamide | analgesic;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | | aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound | anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | | benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[[(2R,3S)-10-(dimethylamino)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-N-methylmethanesulfonamide | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S,3R)-8-(dimethylamino)-5-[(2S)-1-hydroxypropan-2-yl]-3-methyl-2-[[methyl(pyridin-4-ylmethyl)amino]methyl]-3,4-dihydro-2H-1,5-benzoxazocin-6-one | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[[(2S,3S)-10-(dimethylamino)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-N,3,5-trimethyl-4-isoxazolesulfonamide | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S,3S)-10-(dimethylamino)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-2-[[methyl(pyridin-4-ylmethyl)amino]methyl]-3,4-dihydro-2H-1,5-benzoxazocin-6-one | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-cyclohexyl-1-[[(2S,3S)-10-(dimethylamino)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-1-methylurea | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[[(2S,3S)-10-(dimethylamino)-5-[(2R)-1-hydroxypropan-2-yl]-3-methyl-6-oxo-3,4-dihydro-2H-1,5-benzoxazocin-2-yl]methyl]-1-methyl-3-propan-2-ylurea | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cblc137 | | aromatic ketone;
carbazoles;
methyl ketone;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
NF-kappaB inhibitor;
p53 activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-[3-[(5-bromo-2-pyridinyl)-butylamino]propyl]-3-[3-(1H-imidazol-5-yl)propyl]thiourea | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tubastatin a | | hydroxamic acid;
pyridoindole;
tertiary amino compound | EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pracinostat | | benzimidazole;
hydroxamic acid;
olefinic compound;
tertiary amino compound | antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| delgocitinib | | azaspiro compound;
N-acylazetidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound;
tertiary carboxamide | anti-inflammatory drug;
antipsoriatic;
antiseborrheic;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 956980 | | N-acylpiperidine;
N-acylpyrrolidine;
pyrrolopyrimidine;
tertiary amino compound | EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AZD3463 | | aminopiperidine;
aminopyrimidine;
indoles;
monomethoxybenzene;
organochlorine compound;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2879552 | | benzenes;
benzoic acids;
cyclopropanes;
monocarboxylic acid;
piperidines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osimertinib | | acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| BDA-366 | | anthraquinone;
epoxide;
secondary alcohol;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(2-chloro-6-fluorobenzyl)-6-methyl-2-morpholinopyrimidin-4-ol | | dialkylarylamine;
tertiary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | | hydroxyindoles;
morpholines;
nitrile;
pyridines;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
tau aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sotorasib | | acrylamides;
methylpyridines;
monofluorobenzenes;
N-acylpiperazine;
phenols;
pyridopyrimidine;
tertiary amino compound;
tertiary carboxamide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dinitrochlorobenzene | | C-nitro compound;
monochlorobenzenes | allergen;
epitope;
sensitiser | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bupropion | | aromatic ketone;
monochlorobenzenes;
secondary amino compound | antidepressant;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pk 11195 | | aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-chlorophenyl)biguanide | | biguanides;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-chlorophenyl)piperazine | | monochlorobenzenes;
N-arylpiperazine | drug metabolite;
environmental contaminant;
serotonergic agonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorocresol | | hydroxytoluene;
monochlorobenzenes | antimicrobial agent;
disinfectant;
ryanodine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| win 53338 | | isoxazoles;
monochlorobenzenes | antiviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acemetacin | | carboxylic ester;
indol-3-yl carboxylic acid;
monocarboxylic acid;
monochlorobenzenes;
N-acylindole | EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amlodipine | | dihydropyridine;
ethyl ester;
methyl ester;
monochlorobenzenes;
primary amino compound | antihypertensive agent;
calcium channel blocker;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azosemide | | monochlorobenzenes;
sulfonamide;
tetrazoles;
thiophenes | loop diuretic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| baclofen | | amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid;
monochlorobenzenes;
primary amino compound | central nervous system depressant;
GABA agonist;
muscle relaxant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carbonyl cyanide m-chlorophenyl hydrazone | | hydrazone;
monochlorobenzenes;
nitrile | antibacterial agent;
geroprotector;
ionophore | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cetirizine | | ether;
monocarboxylic acid;
monochlorobenzenes;
piperazines | anti-allergic agent;
environmental contaminant;
H1-receptor antagonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorhexidine | | biguanides;
monochlorobenzenes | antibacterial agent;
antiinfective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlormezanone | | 1,3-thiazine;
lactam;
monochlorobenzenes;
sulfone | antipsychotic agent;
anxiolytic drug;
muscle relaxant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chloroxylenol | | monochlorobenzenes;
phenols | antiseptic drug;
disinfectant;
molluscicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorphenesin carbamate | | carbamate ester;
monochlorobenzenes;
secondary alcohol | muscle relaxant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorpropamide | | monochlorobenzenes;
N-sulfonylurea | hypoglycemic agent;
insulin secretagogue | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorpropham | | benzenes;
carbamate ester;
monochlorobenzenes | herbicide;
plant growth retardant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorthalidone | | isoindoles;
monochlorobenzenes;
sulfonamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clemizole | | benzimidazoles;
monochlorobenzenes;
pyrrolidines | histamine antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofazimine | | monochlorobenzenes;
phenazines | dye;
leprostatic drug;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clonazepam | | 1,4-benzodiazepinone;
monochlorobenzenes | anticonvulsant;
anxiolytic drug;
GABA modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clorprenaline | | ethanolamines;
monochlorobenzenes;
secondary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clotrimazole | | conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes | antiinfective agent;
environmental contaminant;
xenobiotic | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dichlorodiphenyl dichloroethylene | | chlorophenylethylene;
monochlorobenzenes | human xenobiotic metabolite;
persistent organic pollutant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ddt | | benzenoid aromatic compound;
chlorophenylethane;
monochlorobenzenes;
organochlorine insecticide | bridged diphenyl acaricide;
carcinogenic agent;
endocrine disruptor;
persistent organic pollutant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| econazole | | dichlorobenzene;
ether;
imidazoles;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyburide | | monochlorobenzenes;
N-sulfonylurea | anti-arrhythmia drug;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxyzine | | hydroxyether;
monochlorobenzenes;
N-alkylpiperazine | anticoronaviral agent;
antipruritic drug;
anxiolytic drug;
dermatologic drug;
H1-receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ketamine | | cyclohexanones;
monochlorobenzenes;
secondary amino compound | analgesic;
environmental contaminant;
intravenous anaesthetic;
neurotoxin;
NMDA receptor antagonist;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| loperamide | | monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol | anticoronaviral agent;
antidiarrhoeal drug;
mu-opioid receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| moclobemide | | benzamides;
monochlorobenzenes;
morpholines | antidepressant;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nemonapride | | benzamides;
monochlorobenzenes;
monomethoxybenzene;
N-alkylpyrrolidine;
secondary amino compound;
secondary carboxamide;
substituted aniline | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| niclosamide | | benzamides;
C-nitro compound;
monochlorobenzenes;
salicylanilides;
secondary carboxamide | anthelminthic drug;
anticoronaviral agent;
antiparasitic agent;
apoptosis inducer;
molluscicide;
piscicide;
STAT3 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ag 1879 | | aromatic amine;
monochlorobenzenes;
pyrazolopyrimidine | beta-adrenergic antagonist;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrimethamine | | aminopyrimidine;
monochlorobenzenes | antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulconazole | | dichlorobenzene;
imidazoles;
monochlorobenzenes;
organic sulfide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ticlopidine | | monochlorobenzenes;
thienopyridine | anticoagulant;
fibrin modulating drug;
hematologic agent;
P2Y12 receptor antagonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trazodone | | monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
triazolopyridine | adrenergic antagonist;
antidepressant;
anxiolytic drug;
H1-receptor antagonist;
sedative;
serotonin uptake inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zomepirac | | aromatic ketone;
monocarboxylic acid;
monochlorobenzenes;
pyrroles | cardiovascular drug;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dichlorodiphenyldichloroethane | | chlorophenylethane;
monochlorobenzenes;
organochlorine insecticide | xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| systhane | | monochlorobenzenes;
nitrile;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| buclizine | | monochlorobenzenes;
N-alkylpiperazine | antiemetic;
central nervous system depressant;
cholinergic antagonist;
histamine antagonist;
local anaesthetic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bis(p-chlorophenyl)acetic acid | | monocarboxylic acid;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-chloro-2-nitrobenzene | | C-nitro compound;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| picryl chloride | | C-nitro compound;
monochlorobenzenes | allergen;
epitope;
explosive;
hapten | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3'-dichlorobenzidine | | biphenyls;
monochlorobenzenes;
organochlorine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methyl-4-chlorophenoxyacetic acid | | chlorophenoxyacetic acid;
monochlorobenzenes | environmental contaminant;
phenoxy herbicide;
synthetic auxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chloro-4-methylaniline | | chloroaniline;
monochlorobenzenes | avicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloro-1,2-diaminobenzene | | monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fentichlor | | aryl sulfide;
bridged diphenyl antifungal drug;
monochlorobenzenes;
polyphenol | antiinfective agent;
drug allergen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dyrene | | monochlorobenzenes;
organochlorine pesticide;
secondary amino compound;
triazines | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triclocarban | | dichlorobenzene;
monochlorobenzenes;
phenylureas | antimicrobial agent;
antiseptic drug;
disinfectant;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| barban | | acetylenic compound;
carbamate ester;
monochlorobenzenes | herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorphenesin | | glycol;
monochlorobenzenes;
propane-1,2-diols | antibacterial drug;
antifungal drug;
muscle relaxant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorotoluene | | monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloroaniline | | chloroaniline;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorobenzene | | monochlorobenzenes | solvent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dicofol | | monochlorobenzenes;
organochlorine acaricide;
tertiary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetradifon | | monochlorobenzenes;
organochlorine acaricide;
sulfone;
trichlorobenzene | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chloroprocaine | | benzoate ester;
monochlorobenzenes | central nervous system depressant;
local anaesthetic;
peripheral nervous system drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monuron | | 3-(3,4-substituted-phenyl)-1,1-dimethylurea;
monochlorobenzenes | environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-chlorosalicylic acid | | chlorobenzoic acid;
monochlorobenzenes;
monohydroxybenzoic acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cloflucarban | | monochlorobenzenes;
phenylureas | antibacterial agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloroacetanilide | | acetamides;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrrolnitrin | | alkaloid;
C-nitro compound;
monochlorobenzenes;
pyrroles | antifungal drug;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloro-2-cresol | | monochlorobenzenes;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorophenylacetic acid | | monocarboxylic acid;
monochlorobenzenes | xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4,4'-dichlorobiphenyl | | dichlorobiphenyl;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorocatechol | | chlorocatechol;
monochlorobenzenes | bacterial xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-chloro-4-aminobenzoic acid | | aminobenzoic acid;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ddms | | chlorophenylethane;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-bromo-2-chlorophenol | | halophenol;
monochlorobenzenes;
organobromine compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chlorocatechol | | chlorocatechol;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorophenoxyacetic acid | | chlorophenoxyacetic acid;
monochlorobenzenes | phenoxy herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clemastine | | monochlorobenzenes;
N-alkylpyrrolidine | anti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlortoluron | | monochlorobenzenes;
phenylureas | agrochemical;
environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxuron | | 3-(3,4-substituted-phenyl)-1,1-dimethylurea;
monochlorobenzenes;
monomethoxybenzene | agrochemical;
environmental contaminant;
herbicide;
photosystem-II inhibitor;
plant growth regulator;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benthiocarb | | monochlorobenzenes;
monothiocarbamic ester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,4'-dichlorobiphenyl | | dichlorobiphenyl;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflubenzuron | | benzoylurea insecticide;
monochlorobenzenes | insect sterilant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| profenofos | | monochlorobenzenes;
organic thiophosphate;
organochlorine insecticide;
organophosphate insecticide | acaricide;
agrochemical;
EC 3.1.1.7 (acetylcholinesterase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benoxaprofen | | 1,3-benzoxazoles;
monocarboxylic acid;
monochlorobenzenes | antipsoriatic;
antipyretic;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
hepatotoxic agent;
nephrotoxin;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
protein kinase C agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| closantel | | aromatic amide;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile;
organoiodine compound;
phenols | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenarimol | | monochlorobenzenes;
pyrimidines;
tertiary alcohol | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| butoconazole | | aryl sulfide;
conazole antifungal drug;
dichlorobenzene;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorsulfuron | | methoxy-1,3,5-triazine;
monochlorobenzenes;
N-sulfonylurea | agrochemical;
EC 2.2.1.6 (acetolactate synthase) inhibitor;
herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3,4,4'5-pentachlorobiphenyl | | monochlorobenzenes;
pentachlorobiphenyl;
tetrachlorobenzene | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clomazone | | isoxazolidinone;
monochlorobenzenes | agrochemical;
carotenoid biosynthesis inhibitor;
environmental contaminant;
herbicide;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clopidogrel | | methyl ester;
monochlorobenzenes;
thienopyridine | anticoagulant;
P2Y12 receptor antagonist;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flucofuron | | (trifluoromethyl)benzenes;
monochlorobenzenes;
organochlorine pesticide;
organofluorine pesticide;
phenylureas | epitope | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lonazolac | | monocarboxylic acid;
monochlorobenzenes;
pyrazoles | antineoplastic agent;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chloroperbenzoic acid | | monochlorobenzenes;
peroxy acid | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofentezine | | monochlorobenzenes;
organochlorine acaricide;
tetrazine | mite growth regulator;
tetrazine acaricide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tebuconazole | | monochlorobenzenes;
tertiary alcohol;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyproconazole | | cyclopropanes;
monochlorobenzenes;
tertiary alcohol;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(4-chlorophenyl)-2-phenyl-2-(1,2,4-triazol-1-ylmethyl)butanenitrile | | monochlorobenzenes;
nitrile;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| metconazole | | conazole fungicide;
cyclopentanols;
monochlorobenzenes;
tertiary alcohol;
triazole fungicide;
triazoles | antifungal agrochemical;
EC 1.14.13.70 (sterol 14alpha-demethylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-amino-5-chlorophenol | | monochlorobenzenes;
phenols;
primary amino compound | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pencycuron | | monochlorobenzenes;
phenylureas | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluazinam | | (trifluoromethyl)benzenes;
aminopyridine;
C-nitro compound;
chloropyridine;
monochlorobenzenes;
secondary amino compound | allergen;
antifungal agrochemical;
apoptosis inducer;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flufenoxuron | | (trifluoromethyl)benzenes;
benzoylurea insecticide;
difluorobenzene;
monochlorobenzenes;
monofluorobenzenes | mite growth regulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorfenapyr | | hemiaminal ether;
monochlorobenzenes;
nitrile;
organochlorine acaricide;
organochlorine insecticide;
organofluorine acaricide;
organofluorine insecticide;
pyrroles | proacaricide;
proinsecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyraclofos | | monochlorobenzenes;
organic thiophosphate;
organochlorine insecticide;
organosulfur compound;
organothiophosphate insecticide;
pyrazoles | agrochemical;
EC 3.1.1.7 (acetylcholinesterase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sr141716 | | amidopiperidine;
carbohydrazide;
dichlorobenzene;
monochlorobenzenes;
pyrazoles | anti-obesity agent;
appetite depressant;
CB1 receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chloro-L-tyrosine | | chloroamino acid;
L-alpha-amino acid zwitterion;
L-tyrosine derivative;
monochlorobenzenes;
non-proteinogenic L-alpha-amino acid | biomarker;
human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rh-0345 | | bisacylhydrazine insecticide;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-chloro-4-hydroxyphenylacetic acid | | hydroxy monocarboxylic acid;
monochlorobenzenes;
phenols | mammalian metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vatalanib | | monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carpropamid | | amide fungicide;
cyclopropylcarboxamide;
monochlorobenzenes | antifungal agrochemical;
EC 4.2.1.94 (scytalone dehydratase) inhibitor;
melanin synthesis inhibitor;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tipifarnib | | imidazoles;
monochlorobenzenes;
primary amino compound;
quinolone | antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1h-pyrrole-3-carbonitrile | | monochlorobenzenes;
nitrile;
organobromine compound;
organochlorine acaricide;
organochlorine insecticide;
organofluorine acaricide;
organofluorine insecticide;
pyrroles | acaricide;
antifouling biocide;
insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-chloro-n-(4-chlorobiphenyl-2-yl)nicotinamide | | anilide fungicide;
biphenyls;
monochlorobenzenes;
pyridinecarboxamide | antifungal agrochemical;
EC 1.3.5.1 [succinate dehydrogenase (quinone)] inhibitor;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(3-tert-butyl-1-methylpyrazol-5-yl)-3-(4-chlorophenyl)urea | | monochlorobenzenes;
phenylureas;
pyrazoles | EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorocinnamic acid | | monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oncrasin-1 | | arenecarbaldehyde;
indoles;
monochlorobenzenes | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-amino-1-(4-chlorophenyl)-2-oxo-4-(1,2,4-triazol-1-ylmethyl)-5-pyrimidinecarbonitrile | | monochlorobenzenes;
nitrile;
pyrimidone;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(4-chlorophenyl)methyl]-2-(2,4-dioxo-1H-pyrimidin-6-yl)acetamide | | monochlorobenzenes;
pyrimidone;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| capsazepine | | benzazepine;
catechols;
monochlorobenzenes;
thioureas | capsaicin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-(4-chlorophenyl)-3-[4-methyl-2-(thiophen-2-yl)-1,3-thiazol-5-yl]urea | | 1,3-thiazoles;
monochlorobenzenes;
phenylureas;
thiophenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(3-chloro-4-methylphenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide | | anilide fungicide;
monocarboxylic acid amide;
monochlorobenzenes;
organosulfur compound;
thiadiazoles | antifungal agrochemical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sr 144528 | | bridged compound;
monochlorobenzenes;
pyrazoles;
secondary carboxamide | CB2 receptor antagonist;
EC 2.3.1.26 (sterol O-acyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorobenzoyl coenzyme a | | chlorobenzoyl-CoA;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epoxiconazole | | epoxide;
monochlorobenzenes;
monofluorobenzenes;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 663536 | | aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes | antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brl 15572 | | monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
secondary alcohol | geroprotector;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML162 | | monochlorobenzenes;
monomethoxybenzene;
organochlorine compound;
secondary carboxamide;
tertiary carboxamide;
thiophenes | EC 1.11.1.9 (glutathione peroxidase) inhibitor;
ferroptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sb 415286 | | C-nitro compound;
maleimides;
monochlorobenzenes;
phenols;
secondary amino compound;
substituted aniline | antioxidant;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ver-49009 | | aromatic amide;
monochlorobenzenes;
monomethoxybenzene;
pyrazoles;
resorcinols | Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-(3-chlorostyryl)caffeine | | monochlorobenzenes;
trimethylxanthine | adenosine A2A receptor antagonist;
EC 1.4.3.4 (monoamine oxidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chlorochalcone | | chalcones;
monochlorobenzenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cinidon-ethyl | | ethyl ester;
isoindoles;
monochlorobenzenes | herbicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| proguanil | | biguanides;
monochlorobenzenes | antimalarial;
antiprotozoal drug;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monorden | | cyclic ketone;
enone;
epoxide;
macrolide antibiotic;
monochlorobenzenes;
phenols | antifungal agent;
metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clovoxamine | | 5-methoxyvalerophenone O-(2-aminoethyl)oxime;
monochlorobenzenes | antidepressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascofuranone | | dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid;
tetrahydrofuranone | angiogenesis inhibitor;
antilipemic drug;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uniconazole | | monochlorobenzenes;
secondary alcohol;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lumefantrine | | fluorenes;
monochlorobenzenes;
secondary alcohol;
tertiary amine | antimalarial | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| strobilurin b | | enoate ester;
enol ether;
methoxyacrylate strobilurin antifungal agent;
monochlorobenzenes;
monomethoxybenzene | antifungal agent;
fungal metabolite;
mitochondrial cytochrome-bc1 complex inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ekb 569 | | aminoquinoline;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile | protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prothioconazole | | cyclopropanes;
monochlorobenzenes;
tertiary alcohol;
thiocarbonyl compound;
triazoles | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminopurvalanol a | | monochlorobenzenes;
purvalanol | protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorhexidine | | biguanides;
monochlorobenzenes | antibacterial agent;
antiinfective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-demethylloperamide | | monocarboxylic acid amide;
monochlorobenzenes;
piperidines;
tertiary alcohol | drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sd 0006 | | monochlorobenzenes;
N-acylpiperidine;
primary alcohol;
pyrazoles;
pyrimidines | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| solabegron | | carboxybiphenyl;
monochlorobenzenes;
secondary alcohol;
secondary amino compound;
substituted aniline | beta-adrenergic agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ki16425 | | carbamate ester;
isoxazoles;
monocarboxylic acid;
monochlorobenzenes;
organic sulfide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7867 | | monochlorobenzenes;
piperidines;
pyrazoles | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzobicyclon | | aromatic ketone;
carbobicyclic compound;
cyclic ketone;
monochlorobenzenes;
organic sulfide;
sulfone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascochlorin | | cyclohexanones;
dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid | angiogenesis inhibitor;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorantranilipole | | monochlorobenzenes;
organobromine compound;
pyrazole insecticide;
pyrazoles;
pyridines;
secondary carboxamide | ryanodine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MI-63 | | azaspiro compound;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
oxindoles;
pyrrolidines;
secondary carboxamide | apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 0348292 | | monochlorobenzenes;
monofluorobenzenes;
pyridone;
pyrrolidines;
secondary carboxamide;
ureas | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor;
serine protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methampicillin | | monochlorobenzenes;
tertiary alcohol;
triazoles | brassinosteroid biosynthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gdc 0449 | | benzamides;
monochlorobenzenes;
pyridines;
sulfone | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone | | 1,3-thiazoles;
hydrazone;
monochlorobenzenes | EC 2.3.1.48 (histone acetyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plx4032 | | aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ulixacaltamide | | benzamides;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
secondary carboxamide | non-narcotic analgesic;
T-type calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluazaindolizine | | aromatic amide;
imidazopyridine;
monocarboxylic acid amide;
monochlorobenzenes;
monomethoxybenzene;
N-sulfonylcarboxamide;
organofluorine pesticide | agrochemical;
nematicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML-210 | | C-nitro compound;
diarylmethane;
isoxazoles;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
tertiary carboxamide | antineoplastic agent;
EC 1.11.1.9 (glutathione peroxidase) inhibitor;
ferroptosis inducer;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pelabresib | | monochlorobenzenes;
organic heterotricyclic compound;
primary carboxamide | antineoplastic agent;
bromodomain-containing protein 4 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MS-417 | | methyl ester;
monochlorobenzenes;
thienotriazolodiazepine | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| liproxstatin-1 | | azaspiro compound;
monochlorobenzenes;
organic heterotricyclic compound;
secondary amino compound | antioxidant;
cardioprotective agent;
ferroptosis inhibitor;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| butoctamide succinate | | dicarboxylic acid monoester;
hemisuccinate;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| iodipamide | | benzoic acids;
organoiodine compound;
secondary carboxamide | radioopaque medium | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pilsicainide | | organic heterobicyclic compound;
secondary carboxamide | anti-arrhythmia drug;
sodium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| opc 12759 | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| suramin | | naphthalenesulfonic acid;
phenylureas;
secondary carboxamide | angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[3-(3,4-dimethoxyphenyl)-1-oxoprop-2-enyl]amino]benzoic acid | | amidobenzoic acid;
cinnamamides;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acedapsone | | acetamides;
anilide;
secondary carboxamide;
sulfone | antimalarial;
antimicrobial drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salicylurate | | N-acylglycine;
secondary carboxamide | human xenobiotic metabolite;
uremic toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monoacetyldapsone | | acetamides;
anilide;
secondary carboxamide;
sulfone | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-methylolacrylamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| win 18446 | | organochlorine compound;
secondary carboxamide | EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tromantadine | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aureothricin | | dithiolopyrrolone antibiotic;
secondary carboxamide | angiogenesis inhibitor;
antibacterial agent;
bacterial metabolite;
EC 2.7.7.6 (RNA polymerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| morphazinamide | | morpholines;
pyrazines;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amperozide | | diarylmethane;
monofluorobenzenes;
N-alkylpiperazine;
secondary carboxamide;
ureas | anxiolytic drug;
dopamine uptake inhibitor;
geroprotector;
second generation antipsychotic;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-acetyltryptophanamide | | acetamides;
L-tryptophan derivative;
primary carboxamide;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gamma-glutamyltyrosine | | dicarboxylic acid;
dipeptide;
phenols;
primary amino compound;
secondary carboxamide | human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-acetyldopamine | | acetamides;
catechols;
N-(fatty acyl)-dopamine;
secondary carboxamide | human urinary metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-acetylcytidine | | acetamides;
cytidines;
secondary carboxamide | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marimastat | | hydroxamic acid;
secondary carboxamide | antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(3-oxohexanoyl)-3-aminodihydro-2(3h)-furanone | | N-acyl homoserine lactone;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| benzyloxycarbonylphenylalanylphenylalanine diazomethyl ketone | | carboxylic ester;
diazo compound;
L-phenylalanine derivative;
secondary carboxamide | cathepsin L (EC 3.4.22.15) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| yh 439 | | aromatic amide;
isopropyl ester;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyc 682 | | nitrile;
nucleoside analogue;
secondary carboxamide | antimetabolite;
antineoplastic agent;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sceptrin | | pyrroles;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n(beta)-alanyldopamine | | catechols;
primary amino compound;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monoacetylcadaverine | | acetamides;
N-substituted cadaverine;
primary amino compound;
secondary carboxamide | human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1-phenylethyl)acetamide | | acetamides;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2,2-trifluoro-N-[2-(1H-indol-3-yl)ethyl]acetamide | | indoles;
secondary carboxamide;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xv 638 | | 1,3-thiazoles;
benzamides;
diazepanone;
diol;
secondary alcohol;
secondary carboxamide;
ureas | HIV protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vibriobactin | | 1,3-oxazoles;
secondary carboxamide | siderophore | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 195614 | | benzoic acids;
quinolines;
secondary carboxamide | retinoic acid receptor alpha antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tempace | | aminoxyls;
piperidinecarboxamide;
secondary carboxamide | radiation protective agent;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dimethyloxalylglycine | | glycine derivative;
methyl ester;
secondary carboxamide | EC 1.14.11.29 (hypoxia-inducible factor-proline dioxygenase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-methyl-2-[[oxo-(4-pentoxyphenyl)methyl]amino]butanoic acid | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cinromide | | cinnamamides;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2,2-trifluoro-N-(2-methyl-8-quinolinyl)acetamide | | quinolines;
secondary carboxamide;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(3-carbamoyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)-2-pyrazinecarboxamide | | primary carboxamide;
pyrazines;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[oxo(thiophen-2-yl)methyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxylic acid propan-2-yl ester | | aromatic amide;
isopropyl ester;
secondary carboxamide;
thiophenes | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[1-[(4-chlorophenyl)methyl]-4-pyrazolyl]-2-pyrazinecarboxamide | | pyrazines;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-[[(4-bromo-2-ethyl-3-pyrazolyl)-oxomethyl]amino]benzoic acid propan-2-yl ester | | aromatic amide;
isopropyl ester;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S)-2-[[(2-chlorophenyl)-oxomethyl]amino]-3-methylbutanoic acid (6-nitro-4H-1,3-benzodioxin-8-yl)methyl ester | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2S)-1-(1H-benzimidazol-2-ylamino)-3-methyl-1-oxobutan-2-yl]-3,5-dimethoxybenzamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2S)-1-(1H-benzimidazol-2-ylamino)-3-methyl-1-oxobutan-2-yl]-3-methylbenzamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2,2-trifluoro-N-(5-oxo-1-phenyl-4H-pyrazol-3-yl)acetamide | | pyrazoles;
secondary carboxamide;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(2-anilino-2-oxoethyl)-2-methoxybenzamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[5-[(2,6-dichlorophenyl)methylthio]-1,3,4-thiadiazol-2-yl]-5-methyl-2-pyrazinecarboxamide | | pyrazines;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S)-3-methyl-2-[[(3-methylphenyl)-oxomethyl]amino]butanoic acid (4-oxo-2-pyrimido[2,1-b][1,3]benzothiazolyl)methyl ester | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyl)iodoacetamide | | aminoxyls;
organoiodine compound;
piperidinecarboxamide;
secondary carboxamide | radical scavenger;
spin label | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ANA-12 | | 1-benzothiophenes;
caprolactams;
secondary carboxamide | antidepressant;
anxiolytic drug;
tropomyosin-related kinase B receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-([biphenyl]-2-yl)-3-cyclopentylpropanamide | | biphenyls;
cyclopentanes;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 387032 | | 1,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-(1,3-benzodioxol-5-ylmethyl)-N-[2-(cyclohexylamino)-2-oxo-1-pyridin-4-ylethyl]-2,2,2-trifluoroacetamide | | benzodioxoles;
pyridines;
secondary carboxamide;
tertiary carboxamide;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[2-(cyclohexylamino)-2-oxo-1-thiophen-2-ylethyl]-2,2,2-trifluoro-N-(4-methylphenyl)acetamide | | secondary carboxamide;
tertiary carboxamide;
thiophenes;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[3-(N-(2-chloro-1-oxoethyl)-4-nitroanilino)propyl]-2,2,2-trifluoroacetamide | | C-nitro compound;
secondary carboxamide;
tertiary carboxamide;
trifluoroacetamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-[[2-(3,4-dimethoxyanilino)-2-oxoethyl]thio]-3-pyridinecarboxylic acid propan-2-yl ester | | dimethoxybenzene;
isopropyl ester;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fagaramide | | cinnamamides;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arachidonyl dopamine | | catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-oleoyldopamine | | catechols;
fatty amide;
N-(fatty acyl)-dopamine;
secondary carboxamide | TRPV1 agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tranilast | | amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide | anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arachidonyl-2-chloroethylamide | | fatty amide;
organochlorine compound;
secondary carboxamide;
synthetic cannabinoid | CB1 receptor agonist;
CB2 receptor agonist;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l796778 | | benzenes;
C-nitro compound;
L-lysine derivative;
L-phenylalanine derivative;
methyl ester;
oligopeptide;
secondary carboxamide;
ureas | somatostatin receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l803087 | | benzenes;
fluoroindole;
guanidines;
L-arginine derivative;
methyl ester;
phenylindole;
secondary carboxamide | somatostatin receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-cinnamoyltyramine | | cinnamamides;
phenols;
secondary carboxamide | allelochemical;
antimicrobial agent;
phytoalexin;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-amylcinnamoylanthranilic acid | | amidobenzoic acid;
cinnamamides;
secondary carboxamide | EC 3.1.1.4 (phospholipase A2) inhibitor;
TRP channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| batimastat | | hydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide | angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pederin | | cyclic ketal;
diol;
oxanes;
polyketide;
secondary alcohol;
secondary carboxamide | antimitotic;
antineoplastic agent;
bacterial metabolite;
vesicant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pepstatin | | pentapeptide;
secondary carboxamide | bacterial metabolite;
EC 3.4.23.* (aspartic endopeptidase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ximelagatran | | amidoxime;
azetidines;
carboxamide;
ethyl ester;
hydroxylamines;
secondary amino compound;
secondary carboxamide;
tertiary carboxamide | anticoagulant;
EC 3.4.21.5 (thrombin) inhibitor;
prodrug;
serine protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (6R,7R)-7-[[(2R)-2-carboxy-2-(4-hydroxyphenyl)-1-oxoethyl]amino]-7-methoxy-3-[[(1-methyl-5-tetrazolyl)thio]methyl]-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid | | dicarboxylic acid;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salubrinal | | aminal;
organochlorine compound;
quinolines;
secondary carboxamide;
thioureas | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oroidin | | pyrroles;
secondary carboxamide | metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 42-5892 | | cyclopropanes;
diol;
L-histidine derivative;
secondary carboxamide;
sulfone | antihypertensive agent;
EC 3.4.23.15 (renin) inhibitor;
peptidomimetic;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kalimantacin a | | alpha,beta-unsaturated monocarboxylic acid;
carbamate ester;
fatty acid derivative;
secondary carboxamide | antibacterial agent;
antimicrobial agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 744832 | | benzenes;
ether;
isopropyl ester;
secondary carboxamide;
sulfone;
thiol | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mocetinostat | | aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 779976 | | benzimidazoles;
indoles;
piperidinecarboxamide;
primary amino compound;
secondary carboxamide | neuroprotective agent;
somatostatin receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dysidenin | | 1,3-thiazoles;
organochlorine compound;
secondary carboxamide;
tertiary carboxamide | animal metabolite;
marine metabolite;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| avenanthramide b | | amidobenzoic acid;
cinnamamides;
monohydroxybenzoic acid;
monomethoxybenzene;
phenols;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
phytoalexin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd2858 | | aromatic amine;
N-methylpiperazine;
pyrazines;
pyridines;
secondary carboxamide;
sulfonamide | antineoplastic agent;
bone density conservation agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| betrixaban | | benzamides;
guanidines;
monochloropyridine;
monomethoxybenzene;
secondary carboxamide | anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fr 900848 | | cyclopropanes;
nucleoside analogue;
olefinic compound;
polyketide;
secondary carboxamide | antifungal agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-benzylhexadecanamide | | macamide;
secondary carboxamide | EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7519 | | dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyantraniliprole | | nitrile;
organobromine compound;
organochlorine compound;
pyrazole insecticide;
pyridines;
secondary carboxamide | ryanodine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| VPC 23019 | | aromatic amide;
D-serine derivative;
organic phosphate;
phosphoric ester;
secondary carboxamide | sphingosine-1-phosphate receptor 1 antagonist;
sphingosine-1-phosphate receptor 3 antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| narlaprevir | | azabicyclohexane;
cyclopropanes;
pyrrolidinecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide;
ureas | anticoronaviral agent;
antiviral drug;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
hepatitis C protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tosedostat | | carboxylic ester;
hydroxamic acid;
secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-chloro-N-[1-[[5-(ethylthio)-1,3,4-thiadiazol-2-yl]amino]-3-methyl-1-oxobutan-2-yl]benzamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S)-2-[[[5-[[5-[[(2-methylpropan-2-yl)oxy-oxomethyl]amino]pentylamino]-oxomethyl]-1H-imidazol-4-yl]-oxomethyl]amino]propanoic acid tert-butyl ester | | secondary carboxamide;
tert-butyl ester | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S)-2-[[[5-[[methyl-(phenylmethyl)amino]-oxomethyl]-1H-imidazol-4-yl]-oxomethyl]amino]-6-[[(2-methylpropan-2-yl)oxy-oxomethyl]amino]hexanoic acid tert-butyl ester | | secondary carboxamide;
tert-butyl ester;
tertiary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (2S,3S,4R)-4-cyclopropyl-2-ethoxy-3-(3-hydroxypropyl)-N-prop-2-ynyl-3,4-dihydro-2H-pyran-6-carboxamide | | secondary carboxamide | | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sid 26681509 | | carbohydrazide;
L-tryptophan derivative;
secondary carboxamide;
tert-butyl ester;
thioester | antiplasmodial drug;
cathepsin L (EC 3.4.22.15) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sm 164 | | benzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| GRL-0617 | | benzamides;
naphthalenes;
secondary carboxamide;
substituted aniline | anticoronaviral agent;
protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| entrectinib | | benzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cx 5461 | | diazepine;
naphthyridine derivative;
organic heterotetracyclic compound;
pyrazines;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.7.6 (RNA polymerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| KOM70144 | | acetamides;
benzamides;
naphthalenes;
secondary carboxamide | anticoronaviral agent;
protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| EG00229 | | benzothiadiazole;
dicarboxylic acid monoamide;
L-arginine derivative;
secondary carboxamide;
sulfonamide;
thiophenes | angiogenesis inhibitor;
antineoplastic agent;
neuropilin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lgk974 | | bipyridines;
pyrazines;
pyridines;
secondary carboxamide | Wnt signalling inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk-5498a | | (trifluoromethyl)benzenes;
difluorobenzene;
pyrazoles;
secondary carboxamide | calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| raltegravir | | 1,2,4-oxadiazole;
dicarboxylic acid amide;
hydroxypyrimidine;
monofluorobenzenes;
pyrimidone;
secondary carboxamide | antiviral drug;
HIV-1 integrase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk1265744 | | difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide | HIV-1 integrase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dolutegravir | | difluorobenzene;
monocarboxylic acid amide;
organic heterotricyclic compound;
secondary carboxamide | HIV-1 integrase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acp-196 | | aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk343 | | aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| atogepant | | azaspiro compound;
organic heterotetracyclic compound;
piperidones;
secondary carboxamide;
trifluorobenzene | calcitonin gene-related peptide receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bictegravir | | monocarboxylic acid amide;
organic heterotetracyclic compound;
secondary carboxamide;
trifluorobenzene | HIV-1 integrase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AZ3451 | | benzimidazoles;
benzodioxoles;
nitrile;
organobromine compound;
secondary carboxamide | anti-inflammatory agent;
autophagy inducer;
PAR2 negative allosteric modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| althiomycin | | 1,3-thiazoles;
aldoxime;
ether;
gamma-lactam;
pentapeptide;
peptide antibiotic;
primary alcohol;
pyrroline;
secondary carboxamide;
tertiary carboxamide | antibacterial agent;
bacterial metabolite;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| colibactin | | 1,3-thiazoles;
azaspiro compound;
polyketide;
pyrroline;
secondary carboxamide | alkylating agent;
carcinogenic agent;
Escherichia coli metabolite;
genotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N-[(2S)-3-cyclohexyl-1-oxo-1-({(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}amino)propan-2-yl]-1H-indole-2-carboxamide | | aldehyde;
indolecarboxamide;
oligopeptide;
pyrrolidin-2-ones;
secondary carboxamide | anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-fluoro-Nalpha-(1H-indol-2-ylcarbonyl)-N-{(2S)-1-oxo-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl}-L-phenylalaninamide | | aldehyde;
indolecarboxamide;
monofluorobenzenes;
oligopeptide;
pyrrolidin-2-ones;
secondary carboxamide | anticoronaviral agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| cgp 52411 | | phthalimides | geroprotector;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| emodin | | trihydroxyanthraquinone | antineoplastic agent;
laxative;
plant metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxy-2-naphthalenyl-methyl phosphonic acid trisacetoxymethylester | | acetate ester;
naphthalenes;
organic phosphonate | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| leflunomide | | (trifluoromethyl)benzenes;
isoxazoles;
monocarboxylic acid amide | antineoplastic agent;
antiparasitic agent;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
hepatotoxic agent;
immunosuppressive agent;
non-steroidal anti-inflammatory drug;
prodrug;
pyrimidine synthesis inhibitor;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-NA-PP1 | | pyrazolopyrimidine | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| imatinib | | aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines | antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| picropodophyllin | | furonaphthodioxole;
lignan;
organic heterotetracyclic compound | antineoplastic agent;
insulin-like growth factor receptor 1 antagonist;
plant metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| imatinib mesylate | | methanesulfonate salt | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor | 2015 | 2021 | 5.5 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| canertinib | | monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2023 | 7.9 | low | 2 | 0 | 0 | 1 | 28 | 4 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2014 | 2022 | 6.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| pd 173955 | | aryl sulfide;
dichlorobenzene;
methyl sulfide;
pyridopyrimidine | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3',4,5'-tetrahydroxystilbene | | catechols;
polyphenol;
resorcinols;
stilbenol | antineoplastic agent;
apoptosis inducer;
geroprotector;
hypoglycemic agent;
plant metabolite;
protein kinase inhibitor;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dasatinib | | 1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2016 | 2022 | 5.4 | low | 1 | 0 | 0 | 0 | 6 | 2 |
| zd 6474 | | aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-tert-butyl-3-naphthalen-1-ylmethyl-1h-pyrazolo(3,4-d)pyrimidin-4-ylemine | | pyrazolopyrimidine | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| biochanin a | | 4'-methoxyisoflavones;
7-hydroxyisoflavones | antineoplastic agent;
EC 3.5.1.99 (fatty acid amide hydrolase) inhibitor;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| genistein | | 7-hydroxyisoflavones | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
geroprotector;
human urinary metabolite;
phytoestrogen;
plant metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| butein | | chalcones;
polyphenol | antineoplastic agent;
antioxidant;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
geroprotector;
hypoglycemic agent;
plant metabolite;
radiosensitizing agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| herbimycin | | 1,4-benzoquinones;
lactam;
macrocycle | antimicrobial agent;
apoptosis inducer;
herbicide;
Hsp90 inhibitor;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bosutinib | | aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monorden | | cyclic ketone;
enone;
epoxide;
macrolide antibiotic;
monochlorobenzenes;
phenols | antifungal agent;
metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| axitinib | | aryl sulfide;
benzamides;
indazoles;
pyridines | antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hki 272 | | nitrile;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| masitinib | | 1,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines | antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pazopanib | | aminopyrimidine;
indazoles;
sulfonamide | angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ponatinib | | (trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PP121 | | aromatic amine;
cyclopentanes;
pyrazolopyrimidine;
pyrrolopyridine | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dcc-2036 | | organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cabozantinib | | aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thiopental sodium | | organochlorine compound;
piperazines;
pyrimidines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teriflunomide | | (trifluoromethyl)benzenes;
aromatic amide;
enamide;
enol;
nitrile;
secondary carboxamide | drug metabolite;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| protocatechuic acid | | catechols;
dihydroxybenzoic acid | antineoplastic agent;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.14.11.2 (procollagen-proline dioxygenase) inhibitor;
human xenobiotic metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminolevulinic acid | | 4-oxo monocarboxylic acid;
amino acid zwitterion;
delta-amino acid | antineoplastic agent;
dermatologic drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite;
prodrug;
Saccharomyces cerevisiae metabolite | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gallic acid | | trihydroxybenzoic acid | antineoplastic agent;
antioxidant;
apoptosis inducer;
astringent;
cyclooxygenase 2 inhibitor;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
geroprotector;
human xenobiotic metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perillic acid | | alpha,beta-unsaturated monocarboxylic acid;
cyclohexenecarboxylic acid | antineoplastic agent;
human metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pk 11195 | | aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 173074 | | aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminopropionitrile | | aminopropionitrile | antineoplastic agent;
antirheumatic drug;
collagen cross-linking inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(n,n-hexamethylene)amiloride | | aromatic amine;
azepanes;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines | antineoplastic agent;
apoptosis inducer;
odorant receptor antagonist;
sodium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7,8-dihydroxyflavone | | dihydroxyflavone | antidepressant;
antineoplastic agent;
antioxidant;
plant metabolite;
tropomyosin-related kinase B receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 48-8071 | | aromatic ether;
aromatic ketone;
bromobenzenes;
monofluorobenzenes;
olefinic compound;
tertiary amino compound | antineoplastic agent;
EC 5.4.99.7 (lanosterol synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rtki cpd | | aromatic ether;
monochlorobenzenes;
quinazolines | antineoplastic agent;
antiviral agent;
epidermal growth factor receptor antagonist;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alfuzosin | | monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| am 251 | | amidopiperidine;
carbohydrazide;
dichlorobenzene;
organoiodine compound;
pyrazoles | antidepressant;
antineoplastic agent;
apoptosis inducer;
CB1 receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| am 580 | | amidobenzoic acid;
tetralins | antineoplastic agent;
retinoic acid receptor alpha/beta agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminoglutethimide | | dicarboximide;
piperidones;
substituted aniline | adrenergic agent;
anticonvulsant;
antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amsacrine | | acridines;
aromatic ether;
sulfonamide | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| anastrozole | | nitrile;
triazoles | antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azathioprine | | aryl sulfide;
C-nitro compound;
imidazoles;
thiopurine | antimetabolite;
antineoplastic agent;
carcinogenic agent;
DNA synthesis inhibitor;
hepatotoxic agent;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azelaic acid | | alpha,omega-dicarboxylic acid;
dicarboxylic fatty acid | antibacterial agent;
antineoplastic agent;
dermatologic drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| berberine | | alkaloid antibiotic;
berberine alkaloid;
botanical anti-fungal agent;
organic heteropentacyclic compound | antilipemic drug;
antineoplastic agent;
antioxidant;
EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor;
EC 1.21.3.3 (reticuline oxidase) inhibitor;
EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
EC 3.1.1.4 (phospholipase A2) inhibitor;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
geroprotector;
hypoglycemic agent;
metabolite;
potassium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| buformin | | biguanides | antineoplastic agent;
antiviral agent;
geroprotector;
hypoglycemic agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| busulfan | | methanesulfonate ester | alkylating agent;
antineoplastic agent;
carcinogenic agent;
insect sterilant;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| camostat | | benzoate ester;
carboxylic ester;
diester;
guanidines;
tertiary carboxamide | anti-inflammatory agent;
anticoronaviral agent;
antifibrinolytic drug;
antihypertensive agent;
antineoplastic agent;
antiviral agent;
serine protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carmustine | | N-nitrosoureas;
organochlorine compound | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cgs 15943 | | aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline | adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chelerythrine | | benzophenanthridine alkaloid;
organic cation | antibacterial agent;
antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorambucil | | aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound | alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ci 994 | | acetamides;
benzamides;
substituted aniline | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ciglitazone | | aromatic ether;
thiazolidinone | antineoplastic agent;
insulin-sensitizing drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cl 387785 | | bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clioquinol | | monohydroxyquinoline;
organochlorine compound;
organoiodine compound | antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antiprotozoal drug;
chelator;
copper chelator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofibric acid | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dacarbazine | | imidazoles;
monocarboxylic acid amide;
triazene derivative | alkylating agent;
antineoplastic agent;
carcinogenic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dequalinium | | quinolinium ion | antifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3'-diindolylmethane | | indoles | antineoplastic agent;
P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| disulfiram | | organic disulfide;
organosulfur acaricide | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxazosin | | aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines | alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ebselen | | benzoselenazole | anti-inflammatory drug;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 1.8.1.12 (trypanothione-disulfide reductase) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 3.1.3.25 (inositol-phosphate phosphatase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 3.5.4.1 (cytosine deaminase) inhibitor;
EC 5.1.3.2 (UDP-glucose 4-epimerase) inhibitor;
enzyme mimic;
ferroptosis inhibitor;
genotoxin;
hepatoprotective agent;
neuroprotective agent;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ellipticine | | indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound;
polycyclic heteroarene | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| embelin | | dihydroxy-1,4-benzoquinones | antimicrobial agent;
antineoplastic agent;
hepatitis C protease inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etanidazole | | C-nitro compound;
imidazoles;
monocarboxylic acid amide | alkylating agent;
antineoplastic agent;
prodrug;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etidronate | | 1,1-bis(phosphonic acid) | antineoplastic agent;
bone density conservation agent;
chelator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluorouracil | | nucleobase analogue;
organofluorine compound | antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic | 2010 | 2023 | 7.6 | low | 1 | 0 | 0 | 1 | 4 | 2 |
| flutamide | | (trifluoromethyl)benzenes;
monocarboxylic acid amide | androgen antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| miltefosine | | phosphocholines;
phospholipid | anti-inflammatory agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
apoptosis inducer;
immunomodulator;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-thujaplicin | | cyclic ketone;
enol;
monoterpenoid | antibacterial agent;
antifungal agent;
antineoplastic agent;
antiplasmodial drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxyurea | | one-carbon compound;
ureas | antimetabolite;
antimitotic;
antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
genotoxin;
immunomodulator;
radical scavenger;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ifosfamide | | ifosfamides | alkylating agent;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| indole-3-carbinol | | indolyl alcohol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-lapachone | | benzochromenone;
orthoquinones | anti-inflammatory agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| letrozole | | nitrile;
triazoles | antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lomustine | | N-nitrosoureas;
organochlorine compound | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-anilino-5,8-quinolinedione | | aminoquinoline;
aromatic amine;
p-quinones;
quinolone | antineoplastic agent;
EC 4.6.1.2 (guanylate cyclase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | | benzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| meclofenamic acid | | aminobenzoic acid;
organochlorine compound;
secondary amino compound | analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vitamin k 3 | | 1,4-naphthoquinones;
vitamin K | angiogenesis inhibitor;
antineoplastic agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
human urinary metabolite;
nutraceutical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxsalen | | aromatic ether;
psoralens | antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nocodazole | | aromatic ketone;
benzimidazoles;
carbamate ester;
thiophenes | antimitotic;
antineoplastic agent;
microtubule-destabilising agent;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| midazolam | | imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound | anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mitoxantrone | | dihydroxyanthraquinone | analgesic;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| entinostat | | benzamides;
carbamate ester;
primary amino compound;
pyridines;
substituted aniline | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n(1), n(12)-diethylspermine | | polyazaalkane;
secondary amino compound;
substituted spermine;
tetramine | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nilutamide | | (trifluoromethyl)benzenes;
C-nitro compound;
imidazolidinone | androgen antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nortriptyline | | organic tricyclic compound;
secondary amine | adrenergic uptake inhibitor;
analgesic;
antidepressant;
antineoplastic agent;
apoptosis inducer;
drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | | aromatic ether;
C-nitro compound;
sulfonamide | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxyphenbutazone | | phenols;
pyrazolidines | antimicrobial agent;
antineoplastic agent;
antipyretic;
drug metabolite;
gout suppressant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 158780 | | aromatic amine;
bromobenzenes;
diamine;
pyridopyrimidine;
secondary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-phenylbutyric acid | | monocarboxylic acid | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oxophenylarsine | | arsine oxides | antineoplastic agent;
apoptosis inducer;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phloretin | | dihydrochalcones | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pipobroman | | N-acylpiperazine;
organobromine compound;
tertiary carboxamide | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pj-34 | | phenanthridines;
secondary carboxamide;
tertiary amino compound | angiogenesis inhibitor;
anti-inflammatory agent;
antiatherosclerotic agent;
antineoplastic agent;
apoptosis inducer;
cardioprotective agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| procarbazine | | benzamides;
hydrazines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salicylsalicylic acid | | benzoate ester;
benzoic acids;
phenols;
salicylates | antineoplastic agent;
antirheumatic drug;
EC 3.5.2.6 (beta-lactamase) inhibitor;
hypoglycemic agent;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| semustine | | N-nitrosoureas;
organochlorine compound | alkylating agent;
antineoplastic agent;
carcinogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| streptonigrin | | pyridines;
quinolone | antimicrobial agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| SU6656 | | oxindoles;
sulfonamide | antineoplastic agent;
Aurora kinase inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vorinostat | | dicarboxylic acid diamide;
hydroxamic acid | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sulforaphane | | isothiocyanate;
sulfoxide | antineoplastic agent;
antioxidant;
EC 3.5.1.98 (histone deacetylase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| suramin | | naphthalenesulfonic acid;
phenylureas;
secondary carboxamide | angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| temozolomide | | imidazotetrazine;
monocarboxylic acid amide;
triazene derivative | alkylating agent;
antineoplastic agent;
prodrug | 2015 | 2021 | 5.6 | low | 2 | 0 | 0 | 0 | 5 | 2 |
| terazosin | | furans;
piperazines;
primary amino compound;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,2'-thiodiethanol | | aliphatic sulfide;
diol | antineoplastic agent;
antioxidant;
metabolite;
solvent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tilorone | | aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound | anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| troglitazone | | chromanes;
thiazolidinone | anticoagulant;
anticonvulsant;
antineoplastic agent;
antioxidant;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
hypoglycemic agent;
platelet aggregation inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole | | aromatic primary alcohol;
furans;
indazoles | antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mitomycin | | mitomycin | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prednisolone | | 11beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone | adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| floxuridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prednisone | | 11-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone | adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| estrone | | 17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols | antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azauridine | | N-glycosyl-1,2,4-triazine | antimetabolite;
antineoplastic agent;
drug metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mechlorethamine hydrochloride | | hydrochloride | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| allyl isothiocyanate | | alkenyl isothiocyanate;
isothiocyanate | antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lachrymator;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincristine | | acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyltestosterone | | 17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
enone | anabolic agent;
androgen;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dromostanolone | | 17beta-hydroxy steroid;
3-oxo-5alpha-steroid;
anabolic androgenic steroid | anabolic agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromodeoxyuridine | | pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tributyrin | | butyrate ester;
triglyceride | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor;
prodrug;
protective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethyl methanesulfonate | | methanesulfonate ester | alkylating agent;
antineoplastic agent;
carcinogenic agent;
genotoxin;
mutagen;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triaziquone | | 1,4-benzoquinones;
aziridines | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tubercidin | | antibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
ribonucleoside | antimetabolite;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cytarabine | | beta-D-arabinoside;
monosaccharide derivative;
pyrimidine nucleoside | antimetabolite;
antineoplastic agent;
antiviral agent;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifluridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
EC 2.1.1.45 (thymidylate synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| medroxyprogesterone acetate | | 20-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
corticosteroid;
steroid ester | adjuvant;
androgen;
antineoplastic agent;
antioxidant;
female contraceptive drug;
inhibitor;
progestin;
synthetic oral contraceptive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluoxymesterone | | 11beta-hydroxy steroid;
17beta-hydroxy steroid;
3-oxo-Delta(4) steroid;
anabolic androgenic steroid;
fluorinated steroid | anabolic agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rotenone | | organic heteropentacyclic compound;
rotenones | antineoplastic agent;
metabolite;
mitochondrial NADH:ubiquinone reductase inhibitor;
phytogenic insecticide;
piscicide;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acetopyrrothine | | acetamides;
dithiolopyrrolone antibiotic | angiogenesis inhibitor;
antibacterial agent;
antifungal agent;
antineoplastic agent;
bacterial metabolite;
chelator;
EC 2.7.7.6 (RNA polymerase) inhibitor;
marine metabolite;
protein synthesis inhibitor;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenformin | | biguanides | antineoplastic agent;
geroprotector;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dibenzoylmethane | | aromatic ketone;
beta-diketone | antimutagen;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| suramin sodium | | organic sodium salt | angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrazolanthrone | | anthrapyrazole;
aromatic ketone;
cyclic ketone | antineoplastic agent;
c-Jun N-terminal kinase inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diazooxonorleucine | | amino acid zwitterion;
diazo compound;
ketone;
non-proteinogenic L-alpha-amino acid | analgesic;
antibacterial agent;
antimetabolite;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
bacterial metabolite;
EC 2.4.2.14 (amidophosphoribosyltransferase) inhibitor;
EC 3.5.1.2 (glutaminase) inhibitor;
EC 6.3.4.2 [CTP synthase (glutamine hydrolyzing)] inhibitor;
EC 6.3.5.1 [NAD(+) synthase (glutamine-hydrolysing)] inhibitor;
EC 6.3.5.2 [GMP synthase (glutamine-hydrolysing)] inhibitor;
EC 6.3.5.3 (phosphoribosylformylglycinamidine synthase) inhibitor;
EC 6.3.5.4 [asparagine synthase (glutamine-hydrolysing)] inhibitor;
EC 6.3.5.5 [carbamoyl-phosphate synthase (glutamine-hydrolysing)] inhibitor;
glutamine antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azacitidine | | N-glycosyl-1,3,5-triazine;
nucleoside analogue | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diazomethane | | diazo compound | alkylating agent;
antineoplastic agent;
carcinogenic agent;
poison | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| procarbazine hydrochloride | | hydrochloride | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naphthazarin | | hydroxy-1,4-naphthoquinone | acaricide;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
geroprotector;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| liriodenine | | alkaloid antibiotic;
cyclic ketone;
organic heteropentacyclic compound;
oxacycle;
oxoaporphine alkaloid | antifungal agent;
antimicrobial agent;
antineoplastic agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lucanthone | | thioxanthenes | adjuvant;
antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
mutagen;
photosensitizing agent;
prodrug;
schistosomicide drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plumbagin | | hydroxy-1,4-naphthoquinone;
phenols | anticoagulant;
antineoplastic agent;
immunological adjuvant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aloe emodin | | aromatic primary alcohol;
dihydroxyanthraquinone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| emetine | | isoquinoline alkaloid;
pyridoisoquinoline | antiamoebic agent;
anticoronaviral agent;
antiinfective agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
expectorant;
plant metabolite;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thymoquinone | | 1,4-benzoquinones | adjuvant;
anti-inflammatory agent;
antidepressant;
antineoplastic agent;
antioxidant;
cardioprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| podophyllotoxin | | furonaphthodioxole;
lignan;
organic heterotetracyclic compound | antimitotic;
antineoplastic agent;
keratolytic drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| physcione | | dihydroxyanthraquinone | anti-inflammatory agent;
antibacterial agent;
antifungal agent;
antineoplastic agent;
apoptosis inducer;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dequalinium chloride | | organic chloride salt | antifungal agent;
antineoplastic agent;
antiseptic drug;
mitochondrial NADH:ubiquinone reductase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methyl-1-(1-methylethyl)-3-cyclohexen-1-ol | | terpineol;
tertiary alcohol | anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
antiparasitic agent;
apoptosis inducer;
plant metabolite;
volatile oil component | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| formestane | | 17-oxo steroid;
3-oxo-Delta(4) steroid;
enol;
hydroxy steroid | antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorotrianisene | | chloroalkene | antineoplastic agent;
estrogen receptor modulator;
xenoestrogen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| megestrol acetate | | 20-oxo steroid;
3-oxo-Delta(4) steroid;
acetate ester;
steroid ester | antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toyocamycin | | antibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
nitrile;
ribonucleoside | antimetabolite;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxyacetanilide | | acetamides;
phenols | anti-inflammatory agent;
antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
platelet aggregation inhibitor;
xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxyacetic acid | | ether;
monocarboxylic acid | antineoplastic agent;
apoptosis inducer;
human xenobiotic metabolite;
mutagen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hadacidin | | aldehyde;
monocarboxylic acid;
N-hydroxy-alpha-amino-acid | antimicrobial agent;
antineoplastic agent;
Penicillium metabolite;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-fluoroadenine | | organofluorine compound;
purines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetramethylpyrazine | | alkaloid;
pyrazines | antineoplastic agent;
apoptosis inhibitor;
bacterial metabolite;
neuroprotective agent;
platelet aggregation inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| guanazole | | aromatic amine;
triazoles | antineoplastic agent;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diallyl trisulfide | | organic trisulfide | anti-inflammatory agent;
antilipemic drug;
antineoplastic agent;
antioxidant;
antiprotozoal drug;
apoptosis inducer;
estrogen receptor antagonist;
insecticide;
platelet aggregation inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diallyl disulfide | | organic disulfide | antifungal agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phenethyl isothiocyanate | | isothiocyanate | antineoplastic agent;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glaucine | | aporphine alkaloid;
organic heterotetracyclic compound;
polyether;
tertiary amino compound | antibacterial agent;
antineoplastic agent;
antitussive;
muscle relaxant;
NF-kappaB inhibitor;
plant metabolite;
platelet aggregation inhibitor;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acadesine | | 1-ribosylimidazolecarboxamide;
aminoimidazole;
nucleoside analogue | antineoplastic agent;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxifluridine | | organofluorine compound;
pyrimidine 5'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| megestrol | | 17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(4) steroid;
tertiary alpha-hydroxy ketone | antineoplastic agent;
appetite enhancer;
contraceptive drug;
progestin;
synthetic oral contraceptive | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mitomycin a | | ether;
mitomycin | alkylating agent;
antimicrobial agent;
antineoplastic agent;
toxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cladribine | | organochlorine compound;
purine 2'-deoxyribonucleoside | antineoplastic agent;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tabersonine | | alkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vidarabine | | beta-D-arabinoside;
purine nucleoside | antineoplastic agent;
bacterial metabolite;
nucleoside antibiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyclophosphamide | | hydrate | alkylating agent;
antineoplastic agent;
carcinogenic agent;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| helenalin | | cyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
secondary alcohol;
sesquiterpene lactone | anti-inflammatory agent;
antineoplastic agent;
metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| etidronate disodium | | organic sodium salt | antineoplastic agent;
bone density conservation agent;
chelator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| camptothecin | | delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| isopentenyladenosine | | N-ribosyl-N(6)-isopentenyladenine;
nucleoside analogue | antineoplastic agent;
plant growth regulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc-145,668 | | hydrochloride | antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ancitabine | | diol;
organic heterotricyclic compound | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clodronic acid | | 1,1-bis(phosphonic acid);
one-carbon compound;
organochlorine compound | antineoplastic agent;
bone density conservation agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetradecanoylphorbol acetate | | acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester | antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| streptozocin | | N-acylglucosamine;
N-nitrosoureas | antimicrobial agent;
antineoplastic agent;
DNA synthesis inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| daunorubicin | | aminoglycoside antibiotic;
anthracycline;
p-quinones;
tetracenequinones | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fludarabine phosphate | | nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate | antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,6-diaminopurine | | 2,6-diaminopurines;
primary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| silybin | | aromatic ether;
benzodioxine;
flavonolignan;
polyphenol;
secondary alpha-hydroxy ketone | antineoplastic agent;
antioxidant;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glucaric acid | | glucaric acid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| paclitaxel | | taxane diterpenoid;
tetracyclic diterpenoid | antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent | 2009 | 2022 | 7.4 | low | 6 | 0 | 0 | 1 | 10 | 3 |
| etoposide | | beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound | antineoplastic agent;
DNA synthesis inhibitor | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| promegestone | | 20-oxo steroid;
3-oxo-Delta(4) steroid | antineoplastic agent;
progesterone receptor agonist;
progestin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| perfosfamide | | nitrogen mustard;
organochlorine compound;
peroxol;
phosphorodiamide | alkylating agent;
antineoplastic agent;
drug allergen;
immunosuppressive agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nimustine | | aminopyrimidine;
N-nitrosoureas;
organochlorine compound | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lonidamine | | dichlorobenzene;
indazoles;
monocarboxylic acid | antineoplastic agent;
antispermatogenic agent;
EC 2.7.1.1 (hexokinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vindesine | | methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
primary carboxamide;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epirubicin | | aminoglycoside;
anthracycline antibiotic;
anthracycline;
deoxy hexoside;
monosaccharide derivative;
p-quinones;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone | antimicrobial agent;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diaziquone | | 1,4-benzoquinones;
aziridines;
carbamate ester;
enamine | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| midazolam hydrochloride | | hydrochloride;
imidazobenzodiazepine | anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oltipraz | | 1,2-dithiole;
pyrazines | angiogenesis modulating agent;
antimutagen;
antineoplastic agent;
antioxidant;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
neurotoxin;
protective agent;
schistosomicide drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fazarabine | | N-glycosyl-1,3,5-triazine;
nucleoside analogue | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mitoxantrone hydrochloride | | hydrochloride | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bisantrene | | anthracenes;
hydrazone;
imidazolidines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| swainsonine | | indolizidine alkaloid | antineoplastic agent;
EC 3.2.1.114 (mannosyl-oligosaccharide 1,3-1,6-alpha-mannosidase) inhibitor;
immunological adjuvant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lovastatin | | delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
polyketide;
statin (naturally occurring) | anticholesteremic drug;
antineoplastic agent;
Aspergillus metabolite;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cabergoline | | N-acylurea | antineoplastic agent;
antiparkinson drug;
dopamine agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nitrogenase stabilizing-protective protein, bacteria | | N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide | androgen antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bmy 25067 | | C-nitro compound;
organic disulfide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brequinar | | biphenyls;
monocarboxylic acid;
monofluorobenzenes;
quinolinemonocarboxylic acid | anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral agent;
EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor;
immunosuppressive agent;
pyrimidine synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| imiquimod | | imidazoquinoline | antineoplastic agent;
interferon inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aromasil | | 17-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid | antineoplastic agent;
EC 1.14.14.14 (aromatase) inhibitor;
environmental contaminant;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cidofovir anhydrous | | phosphonic acids;
pyrimidone | anti-HIV agent;
antineoplastic agent;
antiviral drug;
photosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| topotecan | | pyranoindolizinoquinoline | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| gemcitabine hydrochloride | | hydrochloride;
organofluorine compound | anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemcitabine | | organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic | 2013 | 2023 | 6.6 | low | 6 | 0 | 0 | 0 | 13 | 3 |
| irinotecan | | carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| capecitabine | | carbamate ester;
cytidines;
organofluorine compound | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nelfinavir mesylate | | methanesulfonate salt | antineoplastic agent;
HIV protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nelfinavir | | aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound | antineoplastic agent;
HIV protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| betulinic acid | | hydroxy monocarboxylic acid;
pentacyclic triterpenoid | anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| baicalin | | dihydroxyflavone;
glucosiduronic acid;
glycosyloxyflavone;
monosaccharide derivative | antiatherosclerotic agent;
antibacterial agent;
anticoronaviral agent;
antineoplastic agent;
antioxidant;
cardioprotective agent;
EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
ferroptosis inhibitor;
neuroprotective agent;
non-steroidal anti-inflammatory drug;
plant metabolite;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 5-3335 | | 1,4-benzodiazepinone;
organochlorine compound;
pyrroles | anti-HIV-1 agent;
antineoplastic agent;
HIV-1 Tat inhibitor;
RUNX1 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plerixafor | | azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound | anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epigallocatechin gallate | | flavans;
gallate ester;
polyphenol | antineoplastic agent;
antioxidant;
apoptosis inducer;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvin | | abietane diterpenoid;
carbotricyclic compound;
catechols;
monocarboxylic acid | angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
food preservative;
HIV protease inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose | | gallate ester;
galloyl beta-D-glucose | anti-inflammatory agent;
antineoplastic agent;
geroprotector;
hepatoprotective agent;
plant metabolite;
radiation protective agent;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrrolidine dithiocarbamate | | dithiocarbamic acids;
pyrrolidines | anticonvulsant;
antineoplastic agent;
geroprotector;
neuroprotective agent;
NF-kappaB inhibitor;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| triptonide | | butenolide;
cyclic ketone;
diterpene triepoxide;
organic heteroheptacyclic compound | anti-inflammatory agent;
antineoplastic agent;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3'-deoxyadenosine 5'-triphosphate | | purine ribonucleoside 5'-triphosphate | antifungal agent;
antimetabolite;
antineoplastic agent;
antiviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-methoxyestradiol | | 17beta-hydroxy steroid;
3-hydroxy steroid | angiogenesis modulating agent;
antimitotic;
antineoplastic agent;
human metabolite;
metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toxoflavin | | carbonyl compound;
pyrimidotriazine | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
toxin;
virulence factor;
Wnt signalling inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lupulon | | beta-bitter acid | angiogenesis inhibitor;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pinocembrin | | (2S)-flavan-4-one;
dihydroxyflavanone | antineoplastic agent;
antioxidant;
metabolite;
neuroprotective agent;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tangeretin | | pentamethoxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethinylestradiol-3-sulfate | | 17beta-hydroxy steroid;
steroid sulfate | antineoplastic agent;
estrogen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lonazolac | | monocarboxylic acid;
monochlorobenzenes;
pyrazoles | antineoplastic agent;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromopyruvate | | 2-oxo monocarboxylic acid;
organobromine compound;
oxo carboxylic acid | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enrofloxacin | | cyclopropanes;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone | antibacterial agent;
antimicrobial agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dexrazoxane | | razoxane | antineoplastic agent;
cardiovascular drug;
chelator;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| masoprocol | | nordihydroguaiaretic acid | antineoplastic agent;
hypoglycemic agent;
lipoxygenase inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dw a 2114r | | platinum coordination entity;
pyrrolidines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prednisolone phosphate | | 11beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
3-oxo-Delta(1),Delta(4)-steroid;
glucocorticoid;
steroid phosphate;
tertiary alpha-hydroxy ketone | anti-inflammatory agent;
antineoplastic agent;
glucocorticoid receptor agonist;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hesperetin | | 3'-hydroxyflavanones;
4'-methoxyflavanones;
monomethoxyflavanone;
trihydroxyflavanone | antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sesamin | | benzodioxoles;
furofuran;
lignan | antineoplastic agent;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| betulin | | diol;
pentacyclic triterpenoid | analgesic;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nobiletin | | methoxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alantolactone | | naphthofuran;
olefinic compound;
sesquiterpene lactone | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kaurenoic acid | | ent-kaurane diterpenoid | anti-HIV-1 agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dehydrocostus lactone | | gamma-lactone;
guaiane sesquiterpenoid;
organic heterotricyclic compound;
sesquiterpene lactone | antimycobacterial drug;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 2 inhibitor;
metabolite;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xanthomicrol | | dihydroxyflavone;
trimethoxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| voacamine | | alkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brazilin | | catechols;
organic heterotetracyclic compound;
tertiary alcohol | anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
biological pigment;
hepatoprotective agent;
histological dye;
NF-kappaB inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uvaretin | | aromatic ether;
dihydrochalcones;
polyketide;
resorcinol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fangchinoline | | aromatic ether;
bisbenzylisoquinoline alkaloid;
macrocycle | anti-HIV-1 agent;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| maslinic acid | | dihydroxy monocarboxylic acid;
pentacyclic triterpenoid | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tetrazolium violet | | organic chloride salt | antineoplastic agent;
apoptosis inducer;
dye | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| irinotecan hydrochloride | | hydrochloride | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(3-methyl-1-triazeno)imidazole-4-carboxamide | | imidazoles;
monocarboxylic acid amide;
triazene derivative | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydroxyguanidine | | guanidines;
one-carbon compound | antineoplastic agent;
antiviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cryptolepine | | indole alkaloid;
organic heterotetracyclic compound;
organonitrogen heterocyclic compound | anti-inflammatory agent;
antimalarial;
antineoplastic agent;
cysteine protease inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bexarotene | | benzoic acids;
naphthalenes;
retinoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,4-dihydroxyphenylethanol | | catechols;
primary alcohol | antineoplastic agent;
antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| terreic acid | | arene epoxide;
diketone;
monohydroxy-1,4-benzoquinones;
tertiary alpha-hydroxy ketone | antibacterial agent;
antineoplastic agent;
Aspergillus metabolite;
EC 2.3.1.* (acyltransferase transferring other than amino-acyl group) inhibitor;
EC 2.5.1.7 (UDP-N-acetylglucosamine 1-carboxyvinyltransferase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
mycotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methylumbelliferyl glucuronide | | beta-D-glucosiduronic acid;
coumarins;
monosaccharide derivative | antineoplastic agent;
chromogenic compound;
hyaluronan synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-hydroxyellipticine | | organic heterotetracyclic compound;
organonitrogen heterocyclic compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nimustine | | hydrochloride | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-peltatin | | furonaphthodioxole;
gamma-lactone;
lignan;
organic heterotetracyclic compound;
phenols | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alpha-peltatin | | furonaphthodioxole;
gamma-lactone;
lignan;
organic heterotetracyclic compound;
phenols | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cryptopleurine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | antineoplastic agent;
antiviral agent;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sugiol | | abietane diterpenoid;
carbotricyclic compound;
cyclic terpene ketone;
meroterpenoid;
phenols | antineoplastic agent;
antioxidant;
antiviral agent;
plant metabolite;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eupatorin | | dihydroxyflavone;
polyphenol;
trimethoxyflavone | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
Brassica napus metabolite;
calcium channel blocker;
P450 inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1-methyltryptophan | | non-proteinogenic alpha-amino acid;
tryptophan derivative | antineoplastic agent;
EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| atromentin | | dihydroxy-1,4-benzoquinones;
polyphenol | antibacterial agent;
anticoagulant;
antineoplastic agent;
apoptosis inducer;
biological pigment;
EC 1.3.1.9 [enoyl-[acyl-carrier-protein] reductase (NADH)] inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diosgenin | | 3beta-sterol;
hexacyclic triterpenoid;
sapogenin;
spiroketal | antineoplastic agent;
antiviral agent;
apoptosis inducer;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alpha-glutamyltryptophan | | dipeptide | angiogenesis modulating agent;
antineoplastic agent;
immunomodulator;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fulvestrant | | 17beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide | antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ici 164384 | | 17beta-hydroxy steroid;
3-hydroxy steroid;
tertiary carboxamide | anti-estrogen;
antineoplastic agent;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sn 38 | | delta-lactone;
phenols;
pyranoindolizinoquinoline;
tertiary alcohol | antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hc toxin | | homodetic cyclic peptide;
tetrapeptide | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
metabolite;
phytotoxin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deguelin | | aromatic ether;
diether;
organic heteropentacyclic compound;
rotenones | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
mitochondrial NADH:ubiquinone reductase inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fingolimod | | aminodiol;
primary amino compound | antineoplastic agent;
CB1 receptor antagonist;
immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cafestol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamibarotene | | dicarboxylic acid monoamide;
retinoid;
tetralins | antineoplastic agent;
retinoic acid receptor alpha/beta agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ecteinascidin 743 | | acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound | alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| homoorientin | | flavone C-glycoside;
tetrahydroxyflavone | antineoplastic agent;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kahweol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| selenomethylselenocysteine | | non-proteinogenic alpha-amino acid;
selenocysteines | antineoplastic agent;
human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tephrosin | | aromatic ether;
cyclic ketone;
organic heteropentacyclic compound;
rotenones | antineoplastic agent;
metabolite;
pesticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(tetradecyloxy)-2-furancarboxylic acid | | aromatic ether;
furoic acid | antineoplastic agent;
apoptosis inducer;
EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 58125 | | organofluorine compound;
pyrazoles;
sulfone | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marimastat | | hydroxamic acid;
secondary carboxamide | antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 1'-acetoxychavicol acetate | | acetate ester;
phenylpropanoid | antineoplastic agent;
NF-kappaB inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofarabine | | adenosines;
organofluorine compound | antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dioscin | | hexacyclic triterpenoid;
spiroketal;
spirostanyl glycoside;
trisaccharide derivative | anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 1.14.18.1 (tyrosinase) inhibitor;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside rh2 | | 12beta-hydroxy steroid;
20-hydroxy steroid;
beta-D-glucoside;
ginsenoside;
tetracyclic triterpenoid | antineoplastic agent;
apoptosis inducer;
bone density conservation agent;
cardioprotective agent;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trapoxin a | | epoxide;
homodetic cyclic peptide;
ketone | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| celastrol | | monocarboxylic acid;
pentacyclic triterpenoid | anti-inflammatory drug;
antineoplastic agent;
antioxidant;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Hsp90 inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4'-demethylepipodophyllotoxin | | furonaphthodioxole;
organic heterotetracyclic compound;
phenols | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aminolevulinic acid hydrochloride | | hydrochloride | antineoplastic agent;
dermatologic drug;
photosensitizing agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2008 | 2023 | 6.4 | low | 18 | 0 | 0 | 3 | 149 | 41 |
| cgp 42112a | | benzyl ester;
oligopeptide;
pyridinecarboxamide | angiotensin receptor agonist;
anti-inflammatory agent;
antineoplastic agent;
neuroprotective agent;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vadimezan | | monocarboxylic acid;
xanthones | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubimaillin | | benzochromene;
methyl ester;
phenols | acyl-CoA:cholesterol acyltransferase 2 inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
NF-kappaB inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-carbamoylimidazolium 5-olate | | hydroxyimidazole;
monocarboxylic acid amide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc 224070 | | 1,4-benzoquinones;
aziridines;
enamine;
primary alcohol;
secondary amino compound | alkylating agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| psorospermin | | epoxide;
organic heterotetracyclic compound;
xanthones | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ay 25545 | | acetate ester;
aromatic ether;
C-glycosyl compound;
naphthoisochromene;
olefinic compound;
phenols;
tertiary amine | antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methotrexate | | dicarboxylic acid;
monocarboxylic acid amide;
pteridines | abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent | 2014 | 2020 | 7.2 | low | 6 | 0 | 0 | 0 | 9 | 0 |
| 3,7-dihydroxytropolone | | alpha-hydroxy ketone;
cyclic ketone;
enol;
triol | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| delphinidin | | 5-hydroxyanthocyanidin | antineoplastic agent;
biological pigment;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamsulosin | | 5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide | alpha-adrenergic antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| saintopin | | tetracenequinones | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
fungal metabolite;
intercalator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-bromo-3-(bromomethyl)-7-methyl-2,3,7-trichloro-1-octene | | monoterpenoid;
organobromine compound;
organochlorine compound | algal metabolite;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ilomastat | | hydroxamic acid;
L-tryptophan derivative;
N-acyl-amino acid | anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
EC 3.4.24.24 (gelatinase A) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abiraterone | | 3beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
pyridines | antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| yakuchinone-a | | ketone;
monomethoxybenzene;
phenols | antineoplastic agent;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
EC 1.14.13.39 (nitric oxide synthase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pomalidomide | | aromatic amine;
dicarboximide;
isoindoles;
piperidones | angiogenesis inhibitor;
antineoplastic agent;
immunomodulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tempol | | aminoxyls;
hydroxypiperidine | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
catalyst;
hepatoprotective agent;
nephroprotective agent;
neuroprotective agent;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| selenomethylselenocysteine | | amino acid zwitterion;
L-selenocysteine derivative;
non-proteinogenic L-alpha-amino acid;
Se-methylselenocysteine | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 10-propargyl-10-deazaaminopterin | | N-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound | antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| docetaxel | | hydrate;
secondary alpha-hydroxy ketone | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| docetaxel anhydrous | | secondary alpha-hydroxy ketone;
tetracyclic diterpenoid | antimalarial;
antineoplastic agent;
photosensitizing agent | 2013 | 2022 | 7.2 | low | 3 | 0 | 0 | 0 | 12 | 2 |
| lonafarnib | | 4-{2-[4-(3,10-dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidin-1-yl]-2-oxoethyl}piperidine-1-carboxamide | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aclacinomycin | | aminoglycoside;
anthracycline;
deoxy hexoside;
methyl ester;
monosaccharide derivative;
phenols;
polyketide;
tertiary alcohol;
tetracenequinones;
zwitterion | antimicrobial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-azauridine-5'-monophosphate | | N-glycosyl-1,2,4-triazine;
nucleoside monophosphate analogue | antineoplastic agent;
EC 4.1.1.23 (orotidine-5'-phosphate decarboxylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ptk 787 | | succinate salt | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vatalanib | | monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyc 682 | | nitrile;
nucleoside analogue;
secondary carboxamide | antimetabolite;
antineoplastic agent;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyl 5-aminolevulinate hydrochloride | | hydrochloride | antineoplastic agent;
dermatologic drug;
photosensitizing agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methyl 5-aminolevulinate | | delta-amino acid ester | antineoplastic agent;
dermatologic drug;
photosensitizing agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tipifarnib | | imidazoles;
monochlorobenzenes;
primary amino compound;
quinolone | antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aklavinone | | anthracycline;
methyl ester;
tertiary alcohol;
tetracenequinones | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| actinodaphine | | aporphine alkaloid;
aromatic ether;
organic heteropentacyclic compound;
phenols;
secondary amino compound | antibacterial agent;
antifungal agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite;
platelet aggregation inhibitor;
topoisomerase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| i-677 | | L-serine derivative;
non-proteinogenic L-alpha-amino acid | antimetabolite;
antimicrobial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| anonaine | | aporphine alkaloid;
organic heteropentacyclic compound;
oxacycle | antineoplastic agent;
antiplasmodial drug;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4'-demethyldesoxypodophyllotoxin | | furonaphthodioxole;
gamma-lactone;
lignan;
methoxybenzenes;
phenols | antineoplastic agent;
antioxidant;
immunosuppressive agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvigenin | | monohydroxyflavone;
trimethoxyflavone | antilipemic drug;
antineoplastic agent;
apoptosis inhibitor;
autophagy inducer;
hypoglycemic agent;
immunomodulator;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deferrioxamine e | | cyclic desferrioxamine;
cyclic hydroxamic acid;
macrocycle | antineoplastic agent;
bacterial metabolite;
marine metabolite;
siderophore | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ampelopsin | | dihydromyricetin;
secondary alpha-hydroxy ketone | antineoplastic agent;
antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methylselenic acid | | one-carbon compound;
organoselenium compound | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
human xenobiotic metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acetyl aleuritolic acid | | acetate ester;
monocarboxylic acid;
pentacyclic triterpenoid | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| withanolide d | | 20-hydroxy steroid;
4-hydroxy steroid;
delta-lactone;
enone;
epoxy steroid;
ergostanoid;
secondary alcohol;
tertiary alcohol;
withanolide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| myricanone | | aromatic ether;
cyclic ketone;
diarylheptanoid;
methoxybenzenes;
phenols | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cirsilineol | | dihydroxyflavone;
trimethoxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pannarin | | aldehyde;
aromatic ether;
depsidones;
organic heterotricyclic compound;
organochlorine compound;
phenols | antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lichen metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methylthiohexyl isothiocyanate | | isothiocyanate;
methyl sulfide | antineoplastic agent;
Arabidopsis thaliana metabolite;
EC 4.1.1.17 (ornithine decarboxylase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pectolinarin | | dimethoxyflavone;
disaccharide derivative;
glycosyloxyflavone;
monohydroxyflavanone;
rutinoside | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| albicanol | | carbobicyclic compound;
homoallylic alcohol;
primary alcohol;
sesquiterpenoid | antifeedant;
antifungal agent;
antineoplastic agent;
fungal metabolite;
mammalian metabolite;
marine metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-o-methylembelin | | enol ether;
monohydroxy-1,4-benzoquinones | antileishmanial agent;
antineoplastic agent;
hepatitis C protease inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asperphenamate | | benzamides;
carboxylic ester;
L-phenylalanine derivative | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erlotinib | | aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound | antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erlotinib hydrochloride | | hydrochloride;
terminal acetylenic compound | antineoplastic agent;
protein kinase inhibitor | 2008 | 2023 | 6.6 | low | 16 | 0 | 0 | 3 | 153 | 35 |
| corynoline | | benzophenanthridine alkaloid;
cyclic acetal;
isoquinolines;
organic heterohexacyclic compound;
secondary alcohol | antineoplastic agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| helioxanthin | | benzodioxoles;
furonaphthodioxole;
lignan | anti-HBV agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| top 53 | | furonaphthodioxole;
gamma-lactone;
organic heterotetracyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-heptadecylresorcinol | | 5-alkylresorcinol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| minquartynoic acid | | acetylenic fatty acid;
hydroxy polyunsaturated fatty acid;
long-chain fatty acid;
straight-chain fatty acid;
tetrayne | antimalarial;
antineoplastic agent;
antiviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| scutellarin | | glucosiduronic acid;
glycosyloxyflavone;
monosaccharide derivative;
trihydroxyflavone | antineoplastic agent;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ergolide | | acetate ester;
cyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone | anti-inflammatory agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,5-dihydroxybenzyl alcohol | | aromatic primary alcohol;
phenols | antineoplastic agent;
antioxidant;
apoptosis inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chrysosplenol c | | trihydroxyflavone;
trimethoxyflavone | antineoplastic agent;
antiviral agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lanperisone | | 2-methyl-3-(pyrrolidin-1-yl)-1-[4-(trifluoromethyl)phenyl]propan-1-one | antineoplastic agent;
calcium channel blocker;
ferroptosis inducer;
muscle relaxant;
voltage-gated sodium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (-)-gallocatechin gallate | | catechin;
gallate ester;
polyphenol | antineoplastic agent;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
human xenobiotic metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| orantinib | | monocarboxylic acid;
oxindoles;
pyrroles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| firocoxib | | butenolide;
cyclopropanes;
enol ether;
sulfone | antineoplastic agent;
cyclooxygenase 2 inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-morpholinoanilino)-6-cyclohexylaminopurine | | morpholines;
purines;
secondary amino compound;
tertiary amino compound | adenosine A3 receptor antagonist;
antineoplastic agent;
Aurora kinase inhibitor;
cell dedifferentiation agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lenalidomide | | aromatic amine;
dicarboximide;
isoindoles;
piperidones | angiogenesis inhibitor;
antineoplastic agent;
immunomodulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lasofoxifene | | aromatic ether;
N-alkylpyrrolidine;
naphthols;
tetralins | antineoplastic agent;
bone density conservation agent;
cardioprotective agent;
estrogen receptor agonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 778,123 | | hydrochloride | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 778,123 | | imidazoles;
monochlorobenzenes;
nitrile;
piperazinone;
tertiary amino compound | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(3-chloro-7-indolyl)-1,4-benzenedisulphonamide | | chloroindole;
organochlorine compound;
sulfonamide | antineoplastic agent;
EC 4.2.1.1 (carbonic anhydrase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflomotecan | | epsilon-lactone;
organic heteropentacyclic compound;
organofluorine compound;
organonitrogen heterocyclic compound;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| demecolcine | | alkaloid;
secondary amino compound | antineoplastic agent;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dromostanolone propionate | | 3-oxo-5alpha-steroid;
steroid ester | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincaleukoblastine | | acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincristine sulfate | | organic sulfate salt | antineoplastic agent;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| anisomycin | | monohydroxypyrrolidine;
organonitrogen heterocyclic antibiotic | anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
antiparasitic agent;
bacterial metabolite;
DNA synthesis inhibitor;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| estramustine | | 17beta-hydroxy steroid;
carbamate ester;
organochlorine compound | alkylating agent;
antineoplastic agent;
radiation protective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| withaferin a | | 27-hydroxy steroid;
4-hydroxy steroid;
delta-lactone;
enone;
epoxy steroid;
ergostanoid;
primary alcohol;
secondary alcohol;
withanolide | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| noscapine | | aromatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound | antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| homoharringtonine | | alkaloid ester;
enol ether;
organic heteropentacyclic compound;
tertiary alcohol | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acivicin | | isoxazoles;
non-proteinogenic L-alpha-amino acid;
organochlorine compound | antileishmanial agent;
antimetabolite;
antimicrobial agent;
antineoplastic agent;
EC 2.3.2.2 (gamma-glutamyltransferase) inhibitor;
glutamine antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| elesclomol | | carbohydrazide;
thiocarbonyl compound | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wortmannin | | acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound | anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rocaglamide | | monocarboxylic acid amide;
monomethoxybenzene;
organic heterotricyclic compound | antileishmanial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| anthricin | | furonaphthodioxole;
gamma-lactone;
lignan;
methoxybenzenes | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acronine | | acridone derivatives;
alkaloid | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| taiwanin c | | benzodioxoles;
furonaphthodioxole;
lignan | antineoplastic agent;
plant metabolite;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| o-(chloroacetylcarbamoyl)fumagillol | | carbamate ester;
organochlorine compound;
semisynthetic derivative;
sesquiterpenoid;
spiro-epoxide | angiogenesis inhibitor;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
methionine aminopeptidase 2 inhibitor;
retinoic acid receptor alpha antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bortezomib | | amino acid amide;
L-phenylalanine derivative;
pyrazines | antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gant 61 | | aminal;
dialkylarylamine;
pyridines;
substituted aniline;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
glioma-associated oncogene inhibitor;
Hedgehog signaling pathway inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carnosine | | amino acid zwitterion;
dipeptide | anticonvulsant;
antineoplastic agent;
antioxidant;
Daphnia magna metabolite;
geroprotector;
human metabolite;
mouse metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| puromycin | | puromycins | antiinfective agent;
antimicrobial agent;
antineoplastic agent;
EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor;
EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor;
nucleoside antibiotic;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pentostatin | | coformycins | antimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| canaline | | amino acid zwitterion;
non-proteinogenic L-alpha-amino acid | antimetabolite;
antineoplastic agent;
phytogenic insecticide;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hippeastrine | | delta-lactone;
indole alkaloid;
organic heteropentacyclic compound;
secondary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| peonidin | | 5-hydroxyanthocyanidin | antineoplastic agent;
antioxidant;
apoptosis inducer;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glaucarubinone | | carboxylic ester;
organic heteropentacyclic compound;
quassinoid;
secondary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone;
tetrol | antimalarial;
antineoplastic agent;
geroprotector;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| helveticoside | | 14beta-hydroxy steroid;
5beta-hydroxy steroid;
cardenolide glycoside;
digitoxoside;
monosaccharide derivative;
steroid aldehyde;
steroid lactone | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside re | | 12beta-hydroxy steroid;
3beta-hydroxy-4,4-dimethylsteroid;
3beta-hydroxy steroid;
beta-D-glucoside;
disaccharide derivative;
ginsenoside;
tetracyclic triterpenoid | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
nephroprotective agent;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside rf | | 12beta-hydroxy steroid;
20-hydroxy steroid;
3beta-hydroxy-4,4-dimethylsteroid;
3beta-hydroxy steroid;
beta-D-glucoside;
disaccharide derivative;
ginsenoside;
tetracyclic triterpenoid | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ferruginol | | abietane diterpenoid;
carbotricyclic compound;
meroterpenoid;
phenols | antibacterial agent;
antineoplastic agent;
plant metabolite;
protective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stevioside | | beta-D-glucoside;
bridged compound;
diterpene glycoside;
ent-kaurane diterpenoid;
tetracyclic diterpenoid | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
hypoglycemic agent;
plant metabolite;
sweetening agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| decursinol | | cyclic ether;
delta-lactone;
organic heterotricyclic compound;
secondary alcohol | analgesic;
antineoplastic agent;
EC 3.1.1.7 (acetylcholinesterase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| naringin | | (2S)-flavan-4-one;
4'-hydroxyflavanones;
dihydroxyflavanone;
disaccharide derivative;
neohesperidoside | anti-inflammatory agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eugeniin | | beta-D-glucoside;
ellagitannin;
gallate ester;
lactone | anti-HSV-1 agent;
antifungal agent;
antineoplastic agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| knipholone | | aromatic ketone;
dihydroxyanthraquinone;
methoxybenzenes;
methyl ketone;
polyphenol;
resorcinols | antineoplastic agent;
antioxidant;
antiplasmodial drug;
leukotriene antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gingerol | | beta-hydroxy ketone;
guaiacols | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mucronulatol | | hydroxyisoflavans;
methoxyisoflavan | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| syringaresinol | | syringaresinol | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enkephalin, methionine | | pentapeptide;
peptide zwitterion | analgesic;
antineoplastic agent;
delta-opioid receptor agonist;
human metabolite;
mu-opioid receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| devazepide | | 1,4-benzodiazepinone;
indolecarboxamide | antineoplastic agent;
apoptosis inducer;
cholecystokinin antagonist;
gastrointestinal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sodium arsenite | | arsenic molecular entity;
inorganic sodium salt | antibacterial agent;
antifungal agent;
antineoplastic agent;
carcinogenic agent;
herbicide;
insecticide;
rodenticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| surfactin c | | cyclodepsipeptide;
lipopeptide antibiotic;
macrocyclic lactone | antibacterial agent;
antifungal agent;
antineoplastic agent;
antiviral agent;
metabolite;
platelet aggregation inhibitor;
surfactant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kerriamycin b | | angucycline antibiotic | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carubicin | | aminoglycoside antibiotic;
anthracycline antibiotic;
p-quinones;
tertiary alpha-hydroxy ketone;
tetracenequinones | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tretinoin | | retinoic acid;
vitamin A | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
AP-1 antagonist;
human metabolite;
keratolytic drug;
retinoic acid receptor agonist;
retinoid X receptor agonist;
signalling molecule | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| docosahexaenoate | | docosahexaenoic acid;
omega-3 fatty acid | algal metabolite;
antineoplastic agent;
Daphnia tenebrosa metabolite;
human metabolite;
mouse metabolite;
nutraceutical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eicosapentaenoic acid | | icosapentaenoic acid;
omega-3 fatty acid | anticholesteremic drug;
antidepressant;
antineoplastic agent;
Daphnia galeata metabolite;
fungal metabolite;
micronutrient;
mouse metabolite;
nutraceutical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mycophenolic acid | | 2-benzofurans;
gamma-lactone;
monocarboxylic acid;
phenols | anticoronaviral agent;
antimicrobial agent;
antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
environmental contaminant;
immunosuppressive agent;
mycotoxin;
Penicillium metabolite;
xenobiotic | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| formycin | | formycin | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neocarzinostatin chromophore | | cyclopentacyclononaoxirene;
D-galactosaminide;
dioxolane;
monosaccharide derivative;
naphthoate ester | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epothilone b | | epothilone;
epoxide | antineoplastic agent;
apoptosis inducer;
microtubule-stabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| adenosine-5'-(n-ethylcarboxamide) | | adenosines;
monocarboxylic acid amide | adenosine A1 receptor agonist;
adenosine A2A receptor agonist;
antineoplastic agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n(1)-guanyl-1,7-diaminoheptane | | guanidines;
primary amino compound | antineoplastic agent;
EC 2.5.1.46 (deoxyhypusine synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diethylstilbestrol | | olefinic compound;
polyphenol | antifungal agent;
antineoplastic agent;
autophagy inducer;
calcium channel blocker;
carcinogenic agent;
EC 1.1.1.146 (11beta-hydroxysteroid dehydrogenase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
endocrine disruptor;
xenoestrogen | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 214662 | | benzenes;
benzodiazepine;
imidazoles;
nitrile;
sulfonamide;
thiophenes | antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| epothilone a | | epothilone;
epoxide | antineoplastic agent;
metabolite;
microtubule-stabilising agent;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | | 6-aminopurines;
acetylenic compound;
methoxybenzenes;
monochlorobenzenes;
organofluorine compound | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alitretinoin | | retinoic acid | antineoplastic agent;
keratolytic drug;
metabolite;
retinoid X receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| afimoxifene | | phenols;
tertiary amino compound | antineoplastic agent;
estrogen receptor antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aclarubicin | | aminoglycoside;
anthracycline;
methyl ester;
phenols;
polyketide;
tetracenequinones;
trisaccharide derivative;
zwitterion | antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teniposide | | aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| steviol | | bridged compound;
ent-kaurane diterpenoid;
monocarboxylic acid;
tertiary allylic alcohol;
tetracyclic diterpenoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tiazofurin | | 1,3-thiazoles;
C-glycosyl compound;
monocarboxylic acid amide | antineoplastic agent;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aphidicolin | | tetracyclic diterpenoid | antimicrobial agent;
antimitotic;
antineoplastic agent;
antiviral drug;
apoptosis inducer;
Aspergillus metabolite;
DNA synthesis inhibitor;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azaserine | | carboxylic ester;
diazo compound;
L-serine derivative;
non-proteinogenic L-alpha-amino acid | antifungal agent;
antimetabolite;
antimicrobial agent;
antineoplastic agent;
glutamine antagonist;
immunosuppressive agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| melphalan | | L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound | alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prinomastat | | aromatic ether;
hydroxamic acid;
pyridines;
sulfonamide;
thiomorpholines | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubitecan | | C-nitro compound;
delta-lactone;
pyranoindolizinoquinoline;
semisynthetic derivative;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arsenic trioxide | | arsenic oxide | antineoplastic agent;
insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhapontin | | rhaponticin | angiogenesis inhibitor;
anti-allergic agent;
anti-inflammatory agent;
antilipemic drug;
antineoplastic agent;
apoptosis inducer;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
hypoglycemic agent;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoliquiritigenin | | chalcones | antineoplastic agent;
biological pigment;
EC 1.14.18.1 (tyrosinase) inhibitor;
GABA modulator;
geroprotector;
metabolite;
NMDA receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antofine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | angiogenesis inhibitor;
anti-inflammatory agent;
antimicrobial agent;
antineoplastic agent;
antiviral agent;
phytotoxin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xanthohumol | | aromatic ether;
chalcones;
polyphenol | anti-HIV-1 agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.3.1.20 (diacylglycerol O-acyltransferase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vedelianin | | cyclic ether;
organic heterotricyclic compound;
resorcinols;
stilbenoid | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amygdalin | | amygdalin | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trilostane | | 17beta-hydroxy steroid;
3-hydroxy steroid;
androstanoid;
epoxy steroid;
nitrile | abortifacient;
antineoplastic agent;
EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| leuprolide acetate | | acetate salt | antineoplastic agent;
gonadotropin releasing hormone agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| leuprolide | | oligopeptide | anti-estrogen;
antineoplastic agent;
gonadotropin releasing hormone agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mercaptopurine | | aryl thiol;
purines;
thiocarbonyl compound | anticoronaviral agent;
antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| iFSP1 | | aromatic amine;
nitrile;
primary amino compound;
pyridobenzimidazole;
toluenes | antineoplastic agent;
ferroptosis inducer;
ferroptosis suppressor protein 1 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-iodo-6-phenylpyrimidine | | biaryl;
organoiodine compound;
pyrimidines | antineoplastic agent;
apoptosis inducer;
macrophage migration inhibitory factor inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oncrasin-1 | | arenecarbaldehyde;
indoles;
monochlorobenzenes | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| curcumin | | aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| cct018159 | | benzodioxine;
pyrazoles;
resorcinols | antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac | | monocarboxylic acid;
organofluorine compound;
sulfoxide | analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aurapten | | coumarins;
monoterpenoid | antihypertensive agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
dopaminergic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
gamma-secretase modulator;
gastrointestinal drug;
hepatoprotective agent;
matrix metalloproteinase inhibitor;
neuroprotective agent;
plant metabolite;
PPARalpha agonist;
vulnerary | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xl147 | | aromatic amine;
benzothiadiazole;
quinoxaline derivative;
sulfonamide | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mcb-613 | | cyclic ketone;
enone;
pyridines | antineoplastic agent;
steroid receptor coactivator stimulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thioguanine anhydrous | | 2-aminopurines | anticoronaviral agent;
antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamoxifen | | stilbenoid;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| stattic | | 1-benzothiophenes;
C-nitro compound;
sulfone | antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| krn 7000 | | glycophytoceramide;
N-acyl-beta-D-galactosylphytosphingosine | allergen;
antigen;
antineoplastic agent;
epitope;
immunological adjuvant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 10058-F4 | | olefinic compound;
thiazolidinone | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monastrol | | enoate ester;
ethyl ester;
phenols;
racemate;
thioureas | antileishmanial agent;
antimitotic;
antineoplastic agent;
EC 3.5.1.5 (urease) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toremifene | | aromatic ether;
organochlorine compound;
tertiary amine | antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| u 0126 | | aryl sulfide;
dinitrile;
enamine;
substituted aniline | antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
osteogenesis regulator;
vasoconstrictor agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beauvericin | | cyclodepsipeptide | antibiotic insecticide;
antifungal agent;
antineoplastic agent;
apoptosis inhibitor;
fungal metabolite;
ionophore;
mycotoxin;
P450 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nelarabine | | beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside | antineoplastic agent;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 387032 | | 1,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manool | | labdane diterpenoid;
tertiary alcohol | antibacterial agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amrubicin | | anthracycline antibiotic;
methyl ketone;
primary amino compound;
quinone;
tetracenes | antineoplastic agent;
prodrug;
topoisomerase II inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ospemifene | | aromatic ether;
organochlorine compound;
primary alcohol | anti-inflammatory agent;
antineoplastic agent;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tandutinib | | aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| emetine dihydrochloride | | hydrochloride | anticoronaviral agent;
antimalarial;
antineoplastic agent;
antiprotozoal drug;
antiviral agent;
autophagy inhibitor;
emetic;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bigelovin | | acetate ester;
cyclic ketone;
gamma-lactone;
organic heterotricyclic compound;
sesquiterpene lactone | antineoplastic agent;
apoptosis inducer;
immunomodulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 663536 | | aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes | antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | | benzenes;
thiadiazolidine | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 560 | | aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alsterpaullone | | C-nitro compound;
caprolactams;
organic heterotetracyclic compound | anti-HIV-1 agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginkgetin | | biflavonoid;
hydroxyflavone;
methoxyflavone;
ring assembly | anti-HSV-1 agent;
antineoplastic agent;
cyclooxygenase 2 inhibitor;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eupatilin | | dihydroxyflavone;
trimethoxyflavone | anti-inflammatory agent;
anti-ulcer drug;
antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quercetin | | 7-hydroxyflavonol;
pentahydroxyflavone | antibacterial agent;
antineoplastic agent;
antioxidant;
Aurora kinase inhibitor;
chelator;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
geroprotector;
phytoestrogen;
plant metabolite;
protein kinase inhibitor;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vitexin | | C-glycosyl compound;
trihydroxyflavone | antineoplastic agent;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
plant metabolite;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| apigenin | | trihydroxyflavone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| luteolin | | 3'-hydroxyflavonoid;
tetrahydroxyflavone | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
c-Jun N-terminal kinase inhibitor;
EC 2.3.1.85 (fatty acid synthase) inhibitor;
immunomodulator;
nephroprotective agent;
plant metabolite;
radical scavenger;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| calcitriol | | D3 vitamins;
hydroxycalciol;
triol | antineoplastic agent;
antipsoriatic;
bone density conservation agent;
calcium channel agonist;
calcium channel modulator;
hormone;
human metabolite;
immunomodulator;
metabolite;
mouse metabolite;
nutraceutical | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| herbacetin | | 7-hydroxyflavonol;
pentahydroxyflavone | angiogenesis inhibitor;
anti-inflammatory agent;
antilipemic drug;
antineoplastic agent;
apoptosis inducer;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 4.1.1.17 (ornithine decarboxylase) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hymecromone | | hydroxycoumarin | antineoplastic agent;
hyaluronic acid synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chrysoeriol | | monomethoxyflavone;
trihydroxyflavone | antineoplastic agent;
antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dexmedetomidine | | trihydroxyflavone;
trimethoxyflavone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bryostatin 1 | | acetate ester;
bryostatins;
cyclic hemiketal;
enoate ester;
methyl ester;
organic heterotetracyclic compound;
secondary alcohol | alpha-secretase activator;
anti-HIV-1 agent;
antineoplastic agent;
marine metabolite;
protein kinase C agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quercetin 3-o-glucopyranoside | | beta-D-glucoside;
monosaccharide derivative;
quercetin O-glucoside;
tetrahydroxyflavone | antineoplastic agent;
antioxidant;
antipruritic drug;
bone density conservation agent;
geroprotector;
histamine antagonist;
osteogenesis regulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-deoxy-9,10-didehydro-12,13-didehydro-13,14-dihydroprostaglandin d2 | | prostaglandins J;
secondary alcohol | antineoplastic agent;
antiviral agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrvinium | | quinolinium ion | anthelminthic drug;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyclobenzaprine | | 9,11,13-octadecatrienoic acid | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cucurbitacin i | | cucurbitacin;
tertiary alpha-hydroxy ketone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| daphnoretin | | aromatic ether;
hydroxycoumarin | antineoplastic agent;
antiviral agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| costunolide | | germacranolide;
heterobicyclic compound | anthelminthic drug;
antiinfective agent;
antineoplastic agent;
antiparasitic agent;
antiviral drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eupatolide | | gamma-lactone;
germacranolide;
homoallylic alcohol;
secondary alcohol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oleuropein | | beta-D-glucoside;
catechols;
diester;
methyl ester;
pyrans;
secoiridoid glycoside | anti-inflammatory agent;
antihypertensive agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
NF-kappaB inhibitor;
nutraceutical;
plant metabolite;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| agathisflavone | | biaryl;
biflavonoid;
hydroxyflavone | antineoplastic agent;
antiviral agent;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| baicalein | | trihydroxyflavone | angiogenesis inhibitor;
anti-inflammatory agent;
antibacterial agent;
anticoronaviral agent;
antifungal agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor;
EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor;
EC 3.4.21.26 (prolyl oligopeptidase) inhibitor;
EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor;
EC 4.1.1.17 (ornithine decarboxylase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hormone antagonist;
plant metabolite;
prostaglandin antagonist;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chrysin | | 7-hydroxyflavonol;
dihydroxyflavone | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
EC 2.7.11.18 (myosin-light-chain kinase) inhibitor;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diosmetin | | 3'-hydroxyflavonoid;
monomethoxyflavone;
trihydroxyflavone | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
bone density conservation agent;
cardioprotective agent;
plant metabolite;
tropomyosin-related kinase B receptor agonist;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hinokiflavone | | aromatic ether;
biflavonoid;
hydroxyflavone | antineoplastic agent;
metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hispidulin | | monomethoxyflavone;
trihydroxyflavone | anti-inflammatory agent;
anticonvulsant;
antineoplastic agent;
antioxidant;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gartanin | | polyphenol;
xanthones | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mangostin | | aromatic ether;
phenols;
xanthones | antimicrobial agent;
antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| norathyriol | | polyphenol;
xanthones | antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| morin | | 7-hydroxyflavonol;
pentahydroxyflavone | angiogenesis modulating agent;
anti-inflammatory agent;
antibacterial agent;
antihypertensive agent;
antineoplastic agent;
antioxidant;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
hepatoprotective agent;
metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| morusin | | extended flavonoid;
trihydroxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| myricetin | | 7-hydroxyflavonol;
hexahydroxyflavone | antineoplastic agent;
antioxidant;
cyclooxygenase 1 inhibitor;
food component;
geroprotector;
hypoglycemic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| robustaflavone | | biflavonoid;
hydroxyflavone;
ring assembly | anti-HBV agent;
antineoplastic agent;
antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tricetin | | pentahydroxyflavone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wogonin | | dihydroxyflavone;
monomethoxyflavone | angiogenesis inhibitor;
antineoplastic agent;
cyclooxygenase 2 inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| daidzein | | 7-hydroxyisoflavones | antineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
EC 3.2.1.20 (alpha-glucosidase) inhibitor;
phytoestrogen;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| astringin | | beta-D-glucoside;
monosaccharide derivative;
polyphenol;
stilbenoid | antineoplastic agent;
antioxidant;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pterostilbene | | diether;
methoxybenzenes;
stilbenol | anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
neuroprotective agent;
neurotransmitter;
plant metabolite;
radical scavenger | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| irilone | | hydroxyisoflavone;
organic heterotricyclic compound;
oxacycle | antineoplastic agent;
immunomodulator;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| caffeic acid phenethyl ester | | alkyl caffeate ester | anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
antioxidant;
antiviral agent;
immunomodulator;
metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wedelolactone | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| maytansine | | alpha-amino acid ester;
carbamate ester;
epoxide;
maytansinoid;
organic heterotetracyclic compound;
organochlorine compound | antimicrobial agent;
antimitotic;
antineoplastic agent;
plant metabolite;
tubulin modulator | 2013 | 2017 | 9.0 | low | 0 | 0 | 0 | 0 | 6 | 0 |
| rottlerin | | aromatic ketone;
benzenetriol;
chromenol;
enone;
methyl ketone | anti-allergic agent;
antihypertensive agent;
antineoplastic agent;
apoptosis inducer;
K-ATP channel agonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tectochrysin | | monohydroxyflavone;
monomethoxyflavone | antidiarrhoeal drug;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plaunotol | | diterpenoid;
primary alcohol | anti-ulcer drug;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
nephroprotective agent;
plant metabolite;
vulnerary | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tranilast | | amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide | anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tocotrienol, beta | | tocotrienol;
vitamin E | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gamma-tocotrienol | | tocotrienol;
vitamin E | antineoplastic agent;
antioxidant;
apoptosis inducer;
hepatoprotective agent;
plant metabolite;
radiation protective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tocotrienol, delta | | tocotrienol;
vitamin E | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bone density conservation agent;
NF-kappaB inhibitor;
plant metabolite;
radiation protective agent;
Saccharomyces cerevisiae metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4'-hydroxychalcone | | chalcones;
phenols | anti-inflammatory agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isotretinoin | | retinoic acid | antineoplastic agent;
keratolytic drug;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9,11-linoleic acid | | octadeca-9,11-dienoic acid | anti-inflammatory agent;
antiatherogenic agent;
antineoplastic agent;
apoptosis inducer;
bacterial xenobiotic metabolite;
human metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| camostat mesylate | | methanesulfonate salt | anti-inflammatory agent;
anticoronaviral agent;
antifibrinolytic drug;
antihypertensive agent;
antineoplastic agent;
antiviral agent;
serine protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sirolimus | | antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol | antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2009 | 2017 | 10.6 | low | 1 | 0 | 0 | 1 | 6 | 0 |
| 3',4',7-trihydroxyisoflavone | | 7-hydroxyisoflavones | antineoplastic agent;
EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alvocidib | | dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound | antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fenretinide | | monocarboxylic acid amide;
retinoid | antineoplastic agent;
antioxidant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| geldanamycin | | 1,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound | antimicrobial agent;
antineoplastic agent;
antiviral agent;
cysteine protease inhibitor;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-oxoretinol | | cyclic ketone;
enone;
primary allylic alcohol;
retinoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-(2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl)benzoic acid | | benzoic acids;
naphthalenes;
retinoid | antineoplastic agent;
retinoic acid receptor agonist;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vinorelbine | | acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
ring assembly;
vinca alkaloid | antineoplastic agent;
photosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| centaureidin | | trihydroxyflavone;
trimethoxyflavone | antineoplastic agent;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,3'-di-o-methylquercetin | | 3'-methoxyflavones;
dimethoxyflavone;
trihydroxyflavone | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ethyl caffeate | | alkyl caffeate ester;
ethyl ester;
hydroxycinnamic acid | anti-inflammatory agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| andrographolide | | carbobicyclic compound;
gamma-lactone;
labdane diterpenoid;
primary alcohol;
secondary alcohol | anti-HIV agent;
anti-inflammatory drug;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoginkgetin | | aromatic ether;
biflavonoid | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cudraflavone c | | tetrahydroxyflavone | antibacterial agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neobavaisoflavone | | 7-hydroxyisoflavones | antineoplastic agent;
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitor;
plant metabolite;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neoglycyrol | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one | | dihydroxyflavone;
monomethoxyflavone | antineoplastic agent;
EC 1.14.13.39 (nitric oxide synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiraeoside | | beta-D-glucoside;
flavonols;
monosaccharide derivative;
quercetin O-glucoside;
tetrahydroxyflavone | antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhamnazin | | aromatic ether;
dimethoxyflavone;
phenols;
trihydroxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oridonin | | cyclic hemiketal;
enone;
ent-kaurane diterpenoid;
organic heteropentacyclic compound;
secondary alcohol | angiogenesis inhibitor;
anti-asthmatic agent;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 166866 | | biaryl;
dimethoxybenzene;
primary arylamine;
pyridopyrimidine;
ureas | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| semaxinib | | olefinic compound;
oxindoles;
pyrroles | angiogenesis modulating agent;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| su 11248 | | monocarboxylic acid amide;
pyrroles | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| palbociclib | | aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mitoguazone | | guanidines;
hydrazone | antineoplastic agent;
apoptosis inducer;
EC 4.1.1.50 (adenosylmethionine decarboxylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| reumycin | | carbonyl compound;
pyrimidotriazine | antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ergosterol-5,8-peroxide | | 3beta-sterol;
ergostanoid;
organic peroxide;
phytosterols | antimycobacterial drug;
antineoplastic agent;
metabolite;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ermanin | | dihydroxyflavone;
dimethoxyflavone | anti-inflammatory agent;
antimycobacterial drug;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| romidepsin | | cyclodepsipeptide;
heterocyclic antibiotic;
organic disulfide | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac sulfide | | aryl sulfide;
monocarboxylic acid;
organofluorine compound | antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bay 11-7085 | | benzenes;
nitrile;
sulfone | anti-inflammatory agent;
antibacterial agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.11.10 (IkappaB kinase) inhibitor;
ferroptosis inducer;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| macluraxanthone b | | phenols;
xanthones | anti-HIV agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| flavokawain b | | chalcones;
dimethoxybenzene;
phenols | anti-inflammatory agent;
antileishmanial agent;
antineoplastic agent;
apoptosis inducer;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamsulosin hydrochloride | | hydrochloride | alpha-adrenergic antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| batimastat | | hydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide | angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glyceryl behenate | | 1-monoglyceride;
fatty acid ester | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jaceosidin | | dimethoxyflavone;
trihydroxyflavone | anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7,3'-trihydroxy-3,4'-dimethoxyflavone | | dimethoxyflavone;
trihydroxyflavone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pederin | | cyclic ketal;
diol;
oxanes;
polyketide;
secondary alcohol;
secondary carboxamide | antimitotic;
antineoplastic agent;
bacterial metabolite;
vesicant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| artocarpin lectin | | monomethoxyflavone;
trihydroxyflavone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cisplatin | | diamminedichloroplatinum | antineoplastic agent;
apoptosis inducer;
cross-linking reagent;
ferroptosis inducer;
genotoxin;
mutagen;
nephrotoxin;
photosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bleomycin | | bleomycin | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-aminopropionitrile fumarate (2:1) | | fumarate salt | antineoplastic agent;
antirheumatic drug;
collagen cross-linking inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gamma-mangostin | | phenols;
xanthones | antineoplastic agent;
plant metabolite;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| demethoxycurcumin | | beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cystothiazole a | | 1,3-thiazoles;
biaryl;
enoate ester;
enol ether;
methyl ester;
organonitrogen heterocyclic antibiotic | antifungal agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lespenefril | | alpha-L-rhamnoside;
dihydroxyflavone;
glycosyloxyflavone;
monosaccharide derivative;
polyphenol | anti-inflammatory agent;
antidepressant;
antineoplastic agent;
apoptosis inducer;
bone density conservation agent;
hypoglycemic agent;
immunomodulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| baohuoside i | | glycosyloxyflavone | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| arglabin | | epoxide;
gamma-lactone;
organic heterotetracyclic compound;
sesquiterpene lactone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one | | enone;
pyridines | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.1.105 (6-phosphofructo-2-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ma-1 | | carboxamidine;
organochlorine compound;
pyrimidone;
pyrrolidines | antineoplastic agent;
EC 2.4.2.4 (thymidine phosphorylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| apratoxin a | | 1,3-thiazoles;
apratoxin | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| coronardine | | alkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound | antileishmanial agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascofuranone | | dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid;
tetrahydrofuranone | angiogenesis inhibitor;
antilipemic drug;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| columbianadin | | alpha,beta-unsaturated carboxylic ester;
furanocoumarin | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
hepatoprotective agent;
plant metabolite;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| germacrone | | germacrane sesquiterpenoid;
olefinic compound | androgen antagonist;
anti-inflammatory agent;
antifeedant;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
antioxidant;
antitussive;
antiviral agent;
apoptosis inducer;
autophagy inducer;
hepatoprotective agent;
insecticide;
neuroprotective agent;
plant metabolite;
volatile oil component | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhizoxin | | 1,3-oxazoles;
epoxide;
macrolide antibiotic | antimitotic;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sibiromycin | | aminoglycoside antibiotic;
hemiaminal;
phenols;
pyrrolobenzodiazepine | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bryostatin 2 | | bryostatins;
cyclic hemiketal;
enoate ester;
methyl ester;
organic heterotetracyclic compound;
secondary alcohol | antineoplastic agent;
marine metabolite;
protein kinase C agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manumycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| thermozymocidin | | alpha-amino fatty acid;
hydroxy monocarboxylic acid;
non-proteinogenic alpha-amino acid;
sphingoid | antifungal agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.3.1.50 (serine C-palmitoyltransferase) inhibitor;
fungal metabolite;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asukamycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| everolimus | | cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol | anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2013 | 2022 | 6.6 | low | 0 | 0 | 0 | 0 | 3 | 2 |
| 13(S)-HODE | | HODE | antineoplastic agent;
human xenobiotic metabolite;
mouse metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ixabepilone | | 1,3-thiazoles;
beta-hydroxy ketone;
epoxide;
lactam;
macrocycle | antineoplastic agent;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvianolic acid B | | 1-benzofurans;
catechols;
dicarboxylic acid;
enoate ester;
polyphenol | anti-inflammatory agent;
antidepressant;
antineoplastic agent;
antioxidant;
apoptosis inducer;
autophagy inhibitor;
cardioprotective agent;
hepatoprotective agent;
hypoglycemic agent;
neuroprotective agent;
osteogenesis regulator;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 744832 | | benzenes;
ether;
isopropyl ester;
secondary carboxamide;
sulfone;
thiol | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sophoraflavanone a | | (2S)-flavan-4-one;
4'-hydroxyflavanones;
trihydroxyflavanone | antibacterial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tanespimycin | | 1,4-benzoquinones;
ansamycin;
carbamate ester;
organic heterobicyclic compound;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manzamine a | | alkaloid;
beta-carbolines;
isoquinolines | animal metabolite;
anti-HSV-1 agent;
antimalarial;
antineoplastic agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aureothin | | 4-pyranones;
C-nitro compound;
ketene acetal;
olefinic compound;
oxolanes | antibacterial agent;
antifungal agent;
antineoplastic agent;
antiparasitic agent;
bacterial metabolite;
EC 1.6.5.3 [NADH:ubiquinone reductase (H(+)-translocating)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fostriecin | | 2-pyranones;
olefinic compound;
phosphate monoester;
polyketide;
primary allylic alcohol;
secondary allylic alcohol;
triol | antineoplastic agent;
apoptosis inhibitor;
bacterial metabolite;
EC 3.1.3.16 (phosphoprotein phosphatase) inhibitor;
topoisomerase II inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| artesunate | | artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid | antimalarial;
antineoplastic agent;
ferroptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ru 58668 | | 17beta-hydroxy steroid;
3-hydroxy steroid;
aromatic ether;
organofluorine compound;
sulfone | anti-estrogen;
antineoplastic agent;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| soblidotin | | tetrapeptide | antineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| beta-elemene | | beta-elemene | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| laulimalide | | carboxylic ester;
epoxide;
macrolide;
secondary alcohol;
secondary allylic alcohol | animal metabolite;
antimitotic;
antineoplastic agent;
marine metabolite;
microtubule-stabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jwh-133 | | benzochromene;
dibenzopyran;
organic heterotricyclic compound | analgesic;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inhibitor;
CB2 receptor agonist;
opioid analgesic;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| belinostat | | hydroxamic acid;
olefinic compound;
sulfonamide | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| on 01910 | | N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.21 (polo kinase) inhibitor;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| panobinostat | | cinnamamides;
hydroxamic acid;
methylindole;
secondary amino compound | angiogenesis modulating agent;
antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bml 210 | | dicarboxylic acid diamide | antineoplastic agent;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bufalin | | 14beta-hydroxy steroid;
3beta-hydroxy steroid | animal metabolite;
anti-inflammatory agent;
antineoplastic agent;
cardiotonic drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alpha-solanine | | glycoalkaloid;
organic heterohexacyclic compound;
steroid saponin;
trisaccharide derivative | antineoplastic agent;
apoptosis inducer;
phytotoxin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhosin | | D-tryptophan derivative;
hydrazone;
quinoxaline derivative | antineoplastic agent;
RhoA inhibitor;
RhoC inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| s-allylcysteine | | L-alpha-amino acid zwitterion;
S-hydrocarbyl-L-cysteine | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxy-9-cis-octadecenoic acid | | 2-hydroxy fatty acid;
hydroxy monounsaturated fatty acid;
long-chain fatty acid | antihypertensive agent;
antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dolastatin 10 | | 1,3-thiazoles;
tetrapeptide | animal metabolite;
antineoplastic agent;
apoptosis inducer;
marine metabolite;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plitidepsin | | didemnin | anticoronaviral agent;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abiraterone acetate | | pyridines;
sterol ester | antineoplastic agent;
EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lenvatinib | | aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc 716970 | | aromatic amine;
aromatic ether;
indolecarboxamide;
organochlorine compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 0325901 | | difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound | antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| midostaurin | | benzamides;
gamma-lactam;
indolocarbazole;
organic heterooctacyclic compound | antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jasplakinolide | | cyclodepsipeptide;
phenols | actin polymerisation inducer;
animal metabolite;
antifungal agent;
antineoplastic agent;
apoptosis inducer;
marine metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| muromonab-cd3 | | alkaloid;
macrocycle;
organic heteropentacyclic compound;
organonitrogen heterocyclic compound;
oxacycle;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
IP3 receptor antagonist;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside m1 | | 12beta-hydroxy steroid;
3beta-hydroxy-4,4-dimethylsteroid;
3beta-hydroxy steroid;
beta-D-glucoside;
ginsenoside;
tetracyclic triterpenoid | anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cabazitaxel | | tetracyclic diterpenoid | antineoplastic agent;
microtubule-stabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| elisidepsin | | cyclodepsipeptide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fr 148083 | | aromatic ether;
macrolide;
phenols;
secondary alcohol;
secondary alpha-hydroxy ketone | antibacterial agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mocetinostat | | aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tln 4601 | | dibenzodiazepine;
farnesane sesquiterpenoid;
olefinic compound;
secondary amine;
triol | antineoplastic agent;
antioxidant;
cathepsin L (EC 3.4.22.15) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| scio-469 | | aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tmc-95a | | indoles;
lactam;
macrocycle;
phenols;
secondary alcohol;
tertiary alcohol | antimicrobial agent;
antineoplastic agent;
bacterial metabolite;
fungal metabolite;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cp 724714 | | 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-methoxycanthin-6-one | | aromatic ether;
indole alkaloid;
organic heterotetracyclic compound | antineoplastic agent;
antiplasmodial drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| topopyrone c | | naphthochromene;
p-quinones;
phenols | antimicrobial agent;
antineoplastic agent;
antiviral agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pi103 | | aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-chloro-6-(1-(2-iminopyrrolidinyl) methyl)uracil hydrochloride | | hydrochloride;
iminium salt | antineoplastic agent;
EC 2.4.2.4 (thymidine phosphorylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fty 720p | | monoalkyl phosphate;
primary alcohol;
primary amino compound | antineoplastic agent;
immunosuppressive agent;
sphingosine-1-phosphate receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hmr 1275 | | hydrochloride | antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zm 447439 | | aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside f2 | | 12beta-hydroxy steroid;
beta-D-glucoside;
ginsenoside;
tetracyclic triterpenoid | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ginsenoside rg3 | | ginsenoside;
glycoside;
tetracyclic triterpenoid | angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| es-285 | | amino alcohol;
sphingoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nidulalin a | | methyl ester;
phenols;
xanthones | antimicrobial agent;
antineoplastic agent;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hypothemycin | | aromatic ether;
diol;
enone;
epoxide;
macrolide;
phenols;
polyketide;
secondary alpha-hydroxy ketone | antifungal agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rucaparib | | azepinoindole;
caprolactams;
organofluorine compound;
secondary amino compound | antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jte 607 | | hydrochloride | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
cardioprotective agent;
CPSF3 inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pasireotide | | homodetic cyclic peptide;
peptide hormone | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| npi 2358 | | 2,5-diketopiperazines;
benzenes;
imidazoles;
olefinic compound | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubraxanthone | | aromatic ether;
polyphenol;
xanthones | antibacterial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| NNC 55-0396 (free base) | | benzimidazoles;
cyclopropanecarboxylate ester;
organofluorine compound;
tertiary amino compound;
tetralins | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sr 11302 | | alpha,beta-unsaturated monocarboxylic acid;
retinoid;
toluenes | antineoplastic agent;
AP-1 antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch 51344 | | aromatic amine;
aromatic ether;
primary alcohol;
pyrazoloquinoline;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4alpha-methylergosta-8,24(28)-dien-3,7,11-trione-26-oic acid | | 11-oxo steroid;
3-oxo steroid;
7-oxo steroid;
ergostanoid;
monocarboxylic acid;
steroid acid | anti-inflammatory agent;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osu 03012 | | antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly2090314 | | diazepinoindole;
imidazopyridine;
maleimides;
monofluorobenzenes;
piperidinecarboxamide;
ureas | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cerberin | | acetate ester;
cardenolide glycoside;
monosaccharide derivative | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pateamine a | | 1,3-thiazoles;
macrodiolide;
olefinic compound;
primary amino compound;
tertiary amino compound | antineoplastic agent;
antiviral agent;
eukaryotic initiation factor 4F inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-hydroxytaxol | | taxane diterpenoid;
tetracyclic diterpenoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| avenanthramide b | | amidobenzoic acid;
cinnamamides;
monohydroxybenzoic acid;
monomethoxybenzene;
phenols;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
phytoalexin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ageladine a | | alkaloid;
aromatic amine;
imidazopyridine;
organobromine compound;
pyrroles | angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly-2157299 | | aromatic amide;
methylpyridines;
monocarboxylic acid amide;
pyrrolopyrazole;
quinolines | antineoplastic agent;
TGFbeta receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 6244 | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd2858 | | aromatic amine;
N-methylpiperazine;
pyrazines;
pyridines;
secondary carboxamide;
sulfonamide | antineoplastic agent;
bone density conservation agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bl1521 | | enamide;
hydroxamic acid;
monocarboxylic acid amide | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jte 013 | | chloropyridine;
pyrazolopyridine | anti-asthmatic agent;
anti-inflammatory agent;
antineoplastic agent;
osteogenesis regulator;
pro-angiogenic agent;
sphingosine-1-phosphate receptor 2 antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| holomycin | | acetamides;
dithiolopyrrolone antibiotic | antibacterial agent;
antineoplastic agent;
bacterial metabolite;
chelator;
EC 2.7.7.6 (RNA polymerase) inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| binimetinib | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monofluorobenzenes;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aee 788 | | 6-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| saracatinib | | aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| crenolanib | | aminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trilobacin | | butenolide;
polyketide;
triol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manassantin b | | benzodioxoles;
dimethoxybenzene;
lignan;
oxolanes;
secondary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pha 665752 | | dichlorobenzene;
enamide;
indolones;
N-acylpyrrolidine;
pyrrolecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PB28 | | aromatic ether;
piperazines;
tetralins | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tmc-95b | | indoles;
lactam;
macrocycle;
phenols;
secondary alcohol;
tertiary alcohol | antimicrobial agent;
antineoplastic agent;
fungal metabolite;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fr 901464 | | acetate ester;
cyclic hemiketal;
monocarboxylic acid amide;
pyrans;
spiro-epoxide | antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vinflunine | | acetate ester;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
semisynthetic derivative;
vinca alkaloid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| homocamptothecin | | epsilon-lactone;
organic heteropentacyclic compound;
organonitrogen heterocyclic compound;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-dimethoxy-4-hydroxybenzyl alcohol-4-O-beta-D-glucopyranoside | | aromatic ether;
benzyl alcohols;
beta-D-glucoside;
monosaccharide derivative;
primary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jaspamide b | | cyclodepsipeptide;
organobromine compound | animal metabolite;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ossamycin | | cyclic hemiketal;
macrolide antibiotic;
organic heterotetracyclic compound;
secondary alcohol;
spiroketal;
tertiary alcohol | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nigranoic acid | | dicarboxylic acid;
tetracyclic triterpenoid | antineoplastic agent;
HIV-1 reverse transcriptase inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| esculeoside a | | azaspiro compound;
oxaspiro compound;
saponin;
steroid alkaloid;
steroid saponin | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azadirone | | acetate ester;
cyclic terpene ketone;
furans;
limonoid;
tetracyclic triterpenoid | antineoplastic agent;
antiplasmodial drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| iejimalide b | | ether;
formamides;
macrolide | antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| migrastatin | | ether;
macrolide antibiotic;
piperidones;
secondary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cembra-2,7,11-triene-4,6-diol | | cembrane diterpenoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3,6,8-tetrahydroxy-1-(3-methylbut-2-enyl)-5-(2-methylbut-3-en-2-yl)-9h-xanthen-9-one | | polyphenol;
xanthones | anti-inflammatory agent;
antineoplastic agent;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7867 | | monochlorobenzenes;
piperidines;
pyrazoles | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ym 155 | | organic bromide salt | antineoplastic agent;
apoptosis inducer;
survivin suppressant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bielschowskysin | | acetate ester;
cyclic acetal;
diterpenoid;
gamma-lactone;
organic heterohexacyclic compound | antimalarial;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erastin | | aromatic ether;
diether;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
quinazolines;
tertiary carboxamide | antineoplastic agent;
ferroptosis inducer;
voltage-dependent anion channel inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-737 | | aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound | anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brivanib | | aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rx-3117 | | organofluorine compound;
primary allylic alcohol;
triol | antimetabolite;
antineoplastic agent;
apoptosis inducer;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascochlorin | | cyclohexanones;
dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid | angiogenesis inhibitor;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiculoic acid a | | carbobicyclic compound;
cyclic ketone;
oxo monocarboxylic acid;
styrenes | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| N(2)-([biphenyl]-4-ylsulfonyl)-N-hydroxy-N(2)-isopropoxy-D-valinamide | | D-valine derivative;
hydroxamic acid | antineoplastic agent;
autophagy inducer;
EC 3.4.24.24 (gelatinase A) inhibitor;
melanin synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7519 | | dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ym 216391 | | 1,3-oxazoles;
1,3-thiazoles;
azamacrocycle;
benzenes;
heterodetic cyclic peptide | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marizomib | | beta-lactone;
gamma-lactam;
organic heterobicyclic compound;
organochlorine compound;
salinosporamide | antineoplastic agent;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| er-086526 | | cyclic ketal;
cyclic ketone;
macrocycle;
polycyclic ether;
polyether;
primary amino compound | antineoplastic agent;
microtubule-destabilising agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| obolactone | | 2-pyranones;
4-pyranones | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| episilvestrol | | dioxanes;
ether;
methyl ester;
organic heterotricyclic compound | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt 869 | | aromatic amine;
indazoles;
phenylureas | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152 | | anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 00299804 | | enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ki11502 | | aromatic ether;
benzamides;
quinolines;
thioureas | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| carfilzomib | | epoxide;
morpholines;
tetrapeptide | antineoplastic agent;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | | aminopyridine;
aromatic ether;
dichlorobenzene;
organofluorine compound;
pyrazolylpiperidine;
racemate | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| idelalisib | | aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| crizotinib | | 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2013 | 2022 | 6.9 | low | 0 | 0 | 0 | 0 | 26 | 4 |
| zstk474 | | benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trametinib | | acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lyoniresinol | | dimethoxybenzene;
lignan;
polyphenol;
primary alcohol;
tetralins | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| GDC-0879 | | indanes;
ketoxime;
primary alcohol;
pyrazoles;
pyridines | antineoplastic agent;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| physalin b | | enone;
lactone;
organic heteroheptacyclic compound;
physalin | antimalarial;
antimicrobial agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amrubicinol | | diastereoisomeric mixture;
quinone;
secondary alcohol;
tetracenes | antineoplastic agent;
apoptosis inducer;
topoisomerase II inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| silvestrol | | dioxanes;
ether;
methyl ester;
organic heterotricyclic compound | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 13387 | | benzamides;
isoindoles;
N-alkylpiperazine;
resorcinols;
tertiary carboxamide | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cytotrienin a | | cyclopropanecarboxylate ester;
ether;
hydroquinones;
lactam;
macrocycle;
secondary alcohol | antibacterial agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dactolisib | | imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bgt226 | | aromatic ether;
imidazoquinoline;
N-arylpiperazine;
organofluorine compound;
pyridines | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2'-methoxykurarinone | | 4'-hydroxyflavanones;
dihydroxyflavanone;
dimethoxyflavanone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gedunin | | acetate ester;
enone;
epoxide;
furans;
lactone;
limonoid;
organic heteropentacyclic compound;
pentacyclic triterpenoid | antimalarial;
antineoplastic agent;
Hsp90 inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monascin | | alpha,beta-unsaturated ketone;
gamma-lactone;
organic heterotricyclic compound;
polyketide | antilipemic drug;
antineoplastic agent;
fungal metabolite;
PPARgamma agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monascorubrin | | azaphilone;
enone;
gamma-lactone;
polyketide;
triketone | anti-inflammatory agent;
antineoplastic agent;
biological pigment;
food colouring;
fungal metabolite;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-one | | alkaloid;
chromones;
hydroxypiperidine;
resorcinols;
tertiary amino compound | anti-inflammatory agent;
anti-ulcer drug;
anticholesteremic drug;
antileishmanial agent;
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
fungal metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| SYC-435 | | benzenes;
cyclic hydroxamic acid;
pyridone | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ligstroside | | beta-D-glucoside;
diester;
methyl ester;
phenols;
pyrans;
secoiridoid glycoside | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mogrol | | hydroxy seco-steroid;
tetracyclic triterpenoid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| simalikalactone D | | cyclic ether;
delta-lactone;
enone;
organic heteropentacyclic compound;
quassinoid;
secondary alcohol;
secondary alpha-hydroxy ketone;
triol | antimalarial;
antineoplastic agent;
antiviral agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 4-methyl-5-pentylbenzene-1,3-diol | | resorcinols | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mdv 3100 | | (trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound | androgen antagonist;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152-hqpa | | anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| adonixanthin | | carotenone;
cyclic ketone;
secondary alcohol | algal metabolite;
animal metabolite;
antineoplastic agent;
bacterial metabolite;
marine metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| schweinfurthin g | | cyclic ether;
organic heterotricyclic compound;
resorcinols;
stilbenoid | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abarelix | | polypeptide | antineoplastic agent;
hormone antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| forapin | | peptidyl amide;
polypeptide | animal metabolite;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.13 (protein kinase C) inhibitor;
hepatoprotective agent;
neuroprotective agent;
venom | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gastrin 17 | | gastrin | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gdc-0973 | | aromatic amine;
difluorobenzene;
N-acylazetidine;
organoiodine compound;
piperidines;
secondary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| buparlisib | | aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tubocapsanolide a | | 4-hydroxy steroid;
delta-lactone;
enone;
epoxy steroid;
ergostanoid;
secondary alcohol;
withanolide | antineoplastic agent;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro5126766 | | aryloxypyrimidine;
coumarins;
organofluorine compound;
pyridines;
sulfamides | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pevonedistat | | cyclopentanols;
indanes;
pyrrolopyrimidine;
secondary amino compound;
sulfamidate | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tg101209 | | N-alkylpiperazine;
N-arylpiperazine;
pyrimidines;
secondary amino compound;
sulfonamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk690693 | | 1,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cnf 2024 | | 2-aminopurines;
aromatic ether;
organochlorine compound;
pyridines | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ku 0063794 | | benzyl alcohols;
monomethoxybenzene;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| respirantin | | benzamides;
cyclodepsipeptide;
formamides;
phenols | antimicrobial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sm 164 | | benzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| berkeleydione | | beta-diketone;
cyclic terpene ketone;
meroterpenoid;
methyl ester;
organic heterotetracyclic compound;
terpene lactone;
tertiary alcohol;
tertiary alpha-hydroxy ketone | antineoplastic agent;
cysteine protease inhibitor;
Penicillium metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lucidenic acid n | | cyclic terpene ketone;
dioxo monocarboxylic acid;
secondary alcohol;
tetracyclic triterpenoid | antineoplastic agent;
EC 3.1.1.8 (cholinesterase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bromophycolide a | | diterpenoid;
macrolide;
organobromine compound;
phenols;
tertiary alcohol | anti-HIV agent;
antibacterial agent;
antifungal agent;
antimalarial;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nnc 55-0396 | | hydrochloride | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| meclofenamate sodium anhydrous | | hydrate | analgesic;
anticonvulsant;
antineoplastic agent;
antipyretic;
antirheumatic drug;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brequinar sodium | | organic sodium salt | anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral agent;
EC 1.3.5.2 [dihydroorotate dehydrogenase (quinone)] inhibitor;
immunosuppressive agent;
pyrimidine synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| borrelidin | | aliphatic nitrile;
diol;
macrolide;
monocarboxylic acid;
secondary alcohol | antifungal agent;
antimalarial;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| olaparib | | cyclopropanes;
monofluorobenzenes;
N-acylpiperazine;
phthalazines | antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plx 4720 | | aromatic ketone;
difluorobenzene;
organochlorine compound;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lcl161 | | 1,3-thiazoles;
aromatic ketone;
L-alanine derivative;
monofluorobenzenes;
N-acylpyrrolidine | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aspergillide b | | bridged compound;
cyclic ether;
macrolide;
secondary alcohol | antineoplastic agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tenovin-6 | | monocarboxylic acid amide;
tertiary amino compound;
thioureas | antineoplastic agent;
p53 activator;
Sir2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lde225 | | aminopyridine;
aromatic ether;
benzamides;
biphenyls;
morpholines;
organofluorine compound;
tertiary amino compound | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gdc 0449 | | benzamides;
monochlorobenzenes;
pyridines;
sulfone | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 754807 | | pyrazoles;
pyridines;
pyrrolidines;
pyrrolotriazine | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marinopyrrole a | | aromatic ketone;
organochlorine compound;
phenols;
pyrroles | antibacterial agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| delanzomib | | C-terminal boronic acid peptide;
phenylpyridine;
secondary alcohol;
threonine derivative | antineoplastic agent;
apoptosis inducer;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| grassypeptolide | | cyclodepsipeptide;
macrocycle | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pci 32765 | | acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| spiruchostatin b | | macrocyclic lactone;
organic disulfide;
organic heterobicyclic compound;
spiruchostatin | antineoplastic agent;
bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AMG-208 | | aromatic ether;
quinolines;
triazolopyridazine | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch772984 | | biaryl;
indazoles;
N-acylpiperazine;
N-alkylpyrrolidine;
N-arylpiperazine;
pyridines;
pyrimidines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary amino compound;
tertiary carboxamide | analgesic;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| papuamide b | | cyclodepsipeptide;
olefinic compound;
secondary alcohol;
tertiary alcohol | anti-HIV-1 agent;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antroquinonol d | | enol ether;
enone;
secondary alcohol | antineoplastic agent;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| quizartinib | | benzoimidazothiazole;
isoxazoles;
morpholines;
phenylureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
necroptosis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxyspirotryprostatin b | | aromatic ether;
azaspiro compound;
indole alkaloid;
indolones | antineoplastic agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| niraparib | | benzenes;
indazoles;
piperidines;
primary carboxamide | antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| niraparib | | 2-[4-(piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| navitoclax | | aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lucitanib | | aromatic ether;
cyclopropanes;
naphthalenecarboxamide;
primary amino compound;
quinolines | antineoplastic agent;
fibroblast growth factor receptor antagonist;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chondramide c | | chondramide;
indoles;
phenols | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | | aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound | anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cetrorelix | | oligopeptide | antineoplastic agent;
GnRH antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| histrelin | | oligopeptide | antineoplastic agent;
gonadotropin releasing hormone agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvileucalin b | | bridged compound;
diterpenoid;
furans;
gamma-lactone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| incb-018424 | | nitrile;
pyrazoles;
pyrrolopyrimidine | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| poziotinib | | acrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asp3026 | | aromatic amine;
diamino-1,3,5-triazine;
monomethoxybenzene;
N-methylpiperazine;
piperidines;
secondary amino compound;
sulfone | antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 6.1.1.6 (lysine--tRNA ligase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| entrectinib | | benzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pexidartinib | | aminopyridine;
organochlorine compound;
organofluorine compound;
pyrrolopyridine;
secondary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| TAK-580 | | 1,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glasdegib | | benzimidazoles;
nitrile;
phenylureas;
piperidines | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk 2126458 | | aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ixazomib | | benzamides;
boronic acids;
dichlorobenzene;
glycine derivative | antineoplastic agent;
apoptosis inducer;
drug metabolite;
orphan drug;
proteasome inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cx 5461 | | diazepine;
naphthyridine derivative;
organic heterotetracyclic compound;
pyrazines;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.7.6 (RNA polymerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | | benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plx4032 | | aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| GDC-0623 | | hydroxamic acid ester;
imidazopyridine;
monofluorobenzenes;
organoiodine compound;
primary alcohol;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| INDY | | benzothiazoles;
enone;
organic hydroxy compound | antineoplastic agent;
drug metabolite;
EC 2.7.12.1 (dual-specificity kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 7,8-dihydroxyflavanone | | dihydroxyflavanone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dabrafenib | | 1,3-thiazoles;
aminopyrimidine;
organofluorine compound;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cblc137 | | aromatic ketone;
carbazoles;
methyl ketone;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
NF-kappaB inhibitor;
p53 activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2,3-dihydro-3beta-O-sulfate withaferin A | | 27-hydroxy steroid;
4-hydroxy steroid;
delta-lactone;
epoxy steroid;
ergostanoid;
primary alcohol;
steroid sulfate;
withanolide | antineoplastic agent;
metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| leachianone a | | 4'-hydroxyflavanones;
monomethoxyflavanone;
trihydroxyflavanone | antimalarial;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| EG00229 | | benzothiadiazole;
dicarboxylic acid monoamide;
L-arginine derivative;
secondary carboxamide;
sulfonamide;
thiophenes | angiogenesis inhibitor;
antineoplastic agent;
neuropilin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jadomycin b | | glycoside;
jadomycin;
organic heteropentacyclic compound | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tak-632 | | (trifluoromethyl)benzenes;
aromatic ether;
benzothiazoles;
cyclopropylcarboxamide;
monofluorobenzenes;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
necroptosis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chondramide a | | chondramide;
indoles;
phenols | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| englerin a | | cinnamate ester;
glycolate ester;
guaiane sesquiterpenoid | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lrrk2-in1 | | aromatic amine;
aromatic ether;
N-acylpiperidine;
N-alkylpiperazine;
pyrimidobenzodiazepine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| jq1 compound | | carboxylic ester;
organochlorine compound;
tert-butyl ester;
thienotriazolodiazepine | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
bromodomain-containing protein 4 inhibitor;
cardioprotective agent;
ferroptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML-210 | | C-nitro compound;
diarylmethane;
isoxazoles;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
tertiary carboxamide | antineoplastic agent;
EC 1.11.1.9 (glutathione peroxidase) inhibitor;
ferroptosis inducer;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| eurycomanone | | cyclic ether;
delta-lactone;
enone;
organic heteropentacyclic compound;
pentol;
quassinoid;
secondary alcohol;
secondary alpha-hydroxy ketone;
tertiary alcohol | antimalarial;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gilteritinib | | aromatic amine;
monomethoxybenzene;
N-methylpiperazine;
oxanes;
piperidines;
primary carboxamide;
pyrazines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alectinib | | aromatic ketone;
morpholines;
nitrile;
organic heterotetracyclic compound;
piperidines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML240 | | aromatic amine;
aromatic ether;
benzimidazoles;
primary amino compound;
quinazolines;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 1 | | N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-199 | | aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pracinostat | | benzimidazole;
hydroxamic acid;
olefinic compound;
tertiary amino compound | antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| physalin f | | enone;
epoxy steroid;
lactone;
physalin | antileishmanial agent;
antimalarial;
antineoplastic agent;
apoptosis inducer;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xl765 | | aromatic amine;
aromatic ether;
benzamides;
quinoxaline derivative;
sulfonamide | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| DMH1 | | aromatic ether;
pyrazolopyrimidine;
quinolines | antineoplastic agent;
bone morphogenetic protein receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 2 | | aminopyridine;
organofluorine compound;
primary amino compound;
pyridoquinoline | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oligomycin a | | antibiotic antifungal agent;
diketone;
oligomycin;
pentol | antineoplastic agent;
EC 3.6.3.14 (H(+)-transporting two-sector ATPase) inhibitor;
nematicide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-(4-(4-ethylpiperazin-1-yl)-phenylamino)pyrimidin-4-yl)-1-methylurea | | aminopyrimidine;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
phenylureas | antineoplastic agent;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3alpha,12alpha-dihydroxy-4alpha-methylergosta-8,24(28)-dien-7,11-dione-26-oic acid | | 11-oxo steroid;
12alpha-hydroxy steroid;
3alpha-hydroxy steroid;
7-oxo steroid;
monocarboxylic acid;
secondary alpha-hydroxy ketone;
steroid acid | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3alpha-hydroxy-4alpha-methylergosta-8,24(28)-dien-7,11-dione-26-oic acid | | 11-oxo steroid;
3alpha-hydroxy steroid;
7-oxo steroid;
monocarboxylic acid;
steroid acid | antineoplastic agent;
cholinergic antagonist;
metabolite;
serotonergic antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chir 98014 | | aminopyrimidine;
C-nitro compound;
diaminopyridine;
dichlorobenzene;
imidazoles;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
hypoglycemic agent;
tau aggregation inhibitor;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2656157 | | biaryl;
indoles;
methylpyridines;
organofluorine compound;
pyrrolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
PERK inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2-(5-methoxy-2-oxo-2,3-dihydro-1h-indol-3-yl)ethyl)acetamide | | acetamides;
hydroxyindoles;
tryptamines | antineoplastic agent;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| coumermycin | | aromatic amide;
coumarins;
glycoside;
heteroarenecarboxylate ester;
pyrroles | antimicrobial agent;
antineoplastic agent;
bacterial metabolite;
DNA synthesis inhibitor;
Hsp90 inhibitor;
topoisomerase IV inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lfm a13 | | aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AZD3463 | | aminopiperidine;
aminopyrimidine;
indoles;
monomethoxybenzene;
organochlorine compound;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| calicheamicin gamma(1)i | | calicheamicin;
enediyne antibiotic;
organoiodine compound | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asperfuranone | | 2-benzofurans;
cyclic ketone;
diol;
polyketide;
secondary alcohol;
tertiary alcohol;
tertiary alpha-hydroxy ketone | antineoplastic agent;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ceritinib | | aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pelabresib | | monochlorobenzenes;
organic heterotricyclic compound;
primary carboxamide | antineoplastic agent;
bromodomain-containing protein 4 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MK-8353 | | aromatic ether;
dihydropyridine;
indazoles;
methyl sulfide;
N-alkylpyrrolidine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2879552 | | benzenes;
benzoic acids;
cyclopropanes;
monocarboxylic acid;
piperidines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ssr128129e | | organic sodium salt | antineoplastic agent;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| aspergillide a | | bridged compound;
cyclic ether;
macrolide;
secondary alcohol | antineoplastic agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| capilliposide b | | alpha-L-arabinopyranoside;
bridged compound;
cyclic ether;
diol;
hexacyclic triterpenoid;
hexanoate ester;
lactol;
secondary alcohol;
tetrasaccharide derivative;
triterpenoid saponin | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brasilicardin a | | benzoate ester;
carbotricyclic compound;
diterpenoid;
N-acetyl-D-glucosaminide;
non-proteinogenic alpha-amino acid;
phenols | antimicrobial agent;
antineoplastic agent;
bacterial metabolite;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| surfactin A | | cyclodepsipeptide;
lipopeptide antibiotic;
macrocyclic lactone | antibacterial agent;
antifungal agent;
antineoplastic agent;
antiviral agent;
metabolite;
surfactant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acp-196 | | aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk343 | | aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| myriaporone 3 | | beta-hydroxy ketone;
epoxide;
lactol;
oxanes;
primary alcohol;
secondary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| GSK1059615 | | pyridines;
quinolines;
thiazolidinone | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osimertinib | | acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ivosidenib | | cyanopyridine;
monochlorobenzenes;
organofluorine compound;
pyrrolidin-2-ones;
secondary carboxamide;
tertiary carboxamide | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| phleomycin d1 | | bi-1,3-thiazole;
chelate-forming peptide;
disaccharide derivative;
glycopeptide;
guanidines | antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ly3009120 | | aminotoluene;
aromatic amine;
biaryl;
monofluorobenzenes;
phenylureas;
pyridopyrimidine;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
B-Raf inhibitor;
necroptosis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf-06463922 | | aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| as 1842856 | | organofluorine compound;
primary amino compound;
quinolinemonocarboxylic acid;
quinolone;
secondary amino compound;
tertiary amino compound | anti-obesity agent;
antineoplastic agent;
apoptosis inducer;
autophagy inhibitor;
forkhead box protein O1 inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| physalin d | | 5alpha-hydroxy steroid;
6beta-hydroxy steroid;
cyclic ether;
enone;
lactone;
organic heteroheptacyclic compound;
physalin | antimalarial;
antimycobacterial drug;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acarbose | | chondramide;
indoles;
organochlorine compound;
phenols | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sr9243 | | bromobenzenes;
sulfonamide;
sulfone | antineoplastic agent;
apoptosis inducer;
liver X receptor inverse agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| CCT251545 | | azaspiro compound;
chloropyridine;
pyrazoles | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
Wnt signalling inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ldc4297 | | aromatic ether;
piperidines;
pyrazoles;
pyrazolotriazine;
secondary amino compound | antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hg-9-91-01 | | aminopyrimidine;
dimethoxybenzene;
N-alkylpiperazine;
N-arylpiperazine;
phenylureas;
secondary amino compound | antineoplastic agent;
salt-inducible kinase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cigb-300 | | heterodetic cyclic peptide;
polypeptide | angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chondramide d | | chondramide;
indoles;
phenols | antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bassianolide | | cyclodepsipeptide;
cyclooctadepsipeptide | antineoplastic agent;
fungal metabolite;
insecticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enasidenib | | 1,3,5-triazines;
aminopyridine;
aromatic amine;
organofluorine compound;
secondary amino compound;
tertiary alcohol | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| BDA-366 | | anthraquinone;
epoxide;
secondary alcohol;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ebc-46 | | diester;
diterpenoid;
organic heteropentacyclic compound;
phorbol ester | antineoplastic agent;
plant metabolite;
protein kinase C agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| THZ531 | | aminopyrimidine;
enamide;
indoles;
N-acylpiperidine;
organochlorine compound;
secondary amino compound;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| can 508 | | aromatic amine;
monoazo compound;
phenols;
pyrazoles | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| levoleucovorin | | 5-formyltetrahydrofolic acid | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rifampin | | cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion | angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor | 2014 | 2014 | 10.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| azaguanine | | nucleobase analogue;
triazolopyrimidines | antimetabolite;
antineoplastic agent;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pemetrexed | | N-acyl-L-glutamic acid;
pyrrolopyrimidine | antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor | 2010 | 2023 | 7.5 | low | 8 | 0 | 0 | 1 | 21 | 3 |
| tirapazamine | | aromatic amine;
benzotriazines;
N-oxide | antibacterial agent;
antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pyrazofurin | | C-glycosyl compound;
pyrazoles | antimetabolite;
antimicrobial agent;
antineoplastic agent;
EC 4.1.1.23 (orotidine-5'-phosphate decarboxylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MMP-9-IN-1 | | aromatic compound;
organic sulfide;
organofluorine compound;
pyrimidone;
secondary carboxamide | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydrazinocurcumin | | aromatic ether;
olefinic compound;
polyphenol;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-arabinofuranosylguanine | | beta-D-arabinoside;
purine nucleoside | antineoplastic agent;
DNA synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cerulomycin | | aldoxime;
aromatic ether;
bipyridines;
pyridine alkaloid | antineoplastic agent;
bacterial metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| undecylprodigiosin | | alkaloid;
aromatic ether;
tripyrrole | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
biological pigment;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ver 52296 | | aromatic amide;
isoxazoles;
monocarboxylic acid amide;
morpholines;
resorcinols | angiogenesis inhibitor;
antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | | hydroxyindoles;
morpholines;
nitrile;
pyridines;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
tau aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| XL413 | | benzofuropyrimidine;
organochlorine compound;
pyrrolidines | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pp242 | | aromatic amine;
biaryl;
hydroxyindoles;
phenols;
primary amino compound;
pyrazolopyrimidine | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marineosin a | | azaspiro compound;
ether;
macrocycle;
oxaspiro compound;
pyrroles | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marineosin b | | azaspiro compound;
ether;
macrocycle;
oxaspiro compound;
pyrroles | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ARS-1620 | | quinazolines | antineoplastic agent;
antiviral agent;
inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sotorasib | | acrylamides;
methylpyridines;
monofluorobenzenes;
N-acylpiperazine;
phenols;
pyridopyrimidine;
tertiary amino compound;
tertiary carboxamide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| canertinib | | monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2023 | 7.9 | low | 2 | 0 | 0 | 1 | 28 | 4 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2014 | 2022 | 6.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dasatinib | | 1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2016 | 2022 | 5.4 | low | 1 | 0 | 0 | 0 | 6 | 2 |
| zd 6474 | | aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bosutinib | | aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| monorden | | cyclic ketone;
enone;
epoxide;
macrolide antibiotic;
monochlorobenzenes;
phenols | antifungal agent;
metabolite;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| dcc-2036 | | organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines | tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cabozantinib | | aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teriflunomide | | (trifluoromethyl)benzenes;
aromatic amide;
enamide;
enol;
nitrile;
secondary carboxamide | drug metabolite;
EC 1.3.98.1 [dihydroorotate oxidase (fumarate)] inhibitor;
hepatotoxic agent;
non-steroidal anti-inflammatory drug;
tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pk 11195 | | aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pd 173074 | | aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro 48-8071 | | aromatic ether;
aromatic ketone;
bromobenzenes;
monofluorobenzenes;
olefinic compound;
tertiary amino compound | antineoplastic agent;
EC 5.4.99.7 (lanosterol synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rtki cpd | | aromatic ether;
monochlorobenzenes;
quinazolines | antineoplastic agent;
antiviral agent;
epidermal growth factor receptor antagonist;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alfuzosin | | monocarboxylic acid amide;
quinazolines;
tetrahydrofuranol | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| amsacrine | | acridines;
aromatic ether;
sulfonamide | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cgs 15943 | | aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline | adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| chlorambucil | | aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound | alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ciglitazone | | aromatic ether;
thiazolidinone | antineoplastic agent;
insulin-sensitizing drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cl 387785 | | bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofibric acid | | aromatic ether;
monocarboxylic acid;
monochlorobenzenes | anticholesteremic drug;
antilipemic drug;
antineoplastic agent;
herbicide;
marine xenobiotic metabolite;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxazosin | | aromatic amine;
benzodioxine;
monocarboxylic acid amide;
N-acylpiperazine;
N-arylpiperazine;
quinazolines | alpha-adrenergic antagonist;
antihyperplasia drug;
antihypertensive agent;
antineoplastic agent;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fluorouracil | | nucleobase analogue;
organofluorine compound | antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic | 2010 | 2023 | 7.6 | low | 1 | 0 | 0 | 1 | 4 | 2 |
| 4-(dimethylamino)-n-(7-(hydroxyamino)-7-oxoheptyl)benzamide | | benzamides;
hydroxamic acid;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| methoxsalen | | aromatic ether;
psoralens | antineoplastic agent;
cross-linking reagent;
dermatologic drug;
photosensitizing agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide | | aromatic ether;
C-nitro compound;
sulfonamide | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pj-34 | | phenanthridines;
secondary carboxamide;
tertiary amino compound | angiogenesis inhibitor;
anti-inflammatory agent;
antiatherosclerotic agent;
antineoplastic agent;
apoptosis inducer;
cardioprotective agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| suramin | | naphthalenesulfonic acid;
phenylureas;
secondary carboxamide | angiogenesis inhibitor;
antinematodal drug;
antineoplastic agent;
apoptosis inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
GABA antagonist;
GABA-gated chloride channel antagonist;
purinergic receptor P2 antagonist;
ryanodine receptor agonist;
trypanocidal drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| terazosin | | furans;
piperazines;
primary amino compound;
quinazolines | alpha-adrenergic antagonist;
antihypertensive agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tilorone | | aromatic ether;
diether;
fluoren-9-ones;
tertiary amino compound | anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
interferon inducer;
nicotinic acetylcholine receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole | | aromatic primary alcohol;
furans;
indazoles | antineoplastic agent;
apoptosis inducer;
platelet aggregation inhibitor;
soluble guanylate cyclase activator;
vasodilator agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| floxuridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincristine | | acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trifluridine | | nucleoside analogue;
organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
EC 2.1.1.45 (thymidylate synthase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-fluoroadenine | | organofluorine compound;
purines | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| glaucine | | aporphine alkaloid;
organic heterotetracyclic compound;
polyether;
tertiary amino compound | antibacterial agent;
antineoplastic agent;
antitussive;
muscle relaxant;
NF-kappaB inhibitor;
plant metabolite;
platelet aggregation inhibitor;
rat metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| doxifluridine | | organofluorine compound;
pyrimidine 5'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fludarabine phosphate | | nucleoside analogue;
organofluorine compound;
purine arabinonucleoside monophosphate | antimetabolite;
antineoplastic agent;
antiviral agent;
DNA synthesis inhibitor;
immunosuppressive agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| silybin | | aromatic ether;
benzodioxine;
flavonolignan;
polyphenol;
secondary alpha-hydroxy ketone | antineoplastic agent;
antioxidant;
hepatoprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vindesine | | methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
primary carboxamide;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemcitabine hydrochloride | | hydrochloride;
organofluorine compound | anticoronaviral agent;
antimetabolite;
antineoplastic agent;
antiviral drug;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gemcitabine | | organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic | 2013 | 2023 | 6.6 | low | 6 | 0 | 0 | 0 | 13 | 3 |
| irinotecan | | carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| capecitabine | | carbamate ester;
cytidines;
organofluorine compound | antimetabolite;
antineoplastic agent;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nelfinavir | | aryl sulfide;
benzamides;
organic heterobicyclic compound;
phenols;
secondary alcohol;
tertiary amino compound | antineoplastic agent;
HIV protease inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plerixafor | | azacycloalkane;
azamacrocycle;
benzenes;
crown amine;
secondary amino compound;
tertiary amino compound | anti-HIV agent;
antineoplastic agent;
C-X-C chemokine receptor type 4 antagonist;
immunological adjuvant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lonazolac | | monocarboxylic acid;
monochlorobenzenes;
pyrazoles | antineoplastic agent;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enrofloxacin | | cyclopropanes;
N-alkylpiperazine;
N-arylpiperazine;
organofluorine compound;
quinolinemonocarboxylic acid;
quinolone | antibacterial agent;
antimicrobial agent;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| voacamine | | alkaloid ester;
methyl ester;
monoterpenoid indole alkaloid;
organic heteropentacyclic compound;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| uvaretin | | aromatic ether;
dihydrochalcones;
polyketide;
resorcinol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fangchinoline | | aromatic ether;
bisbenzylisoquinoline alkaloid;
macrocycle | anti-HIV-1 agent;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
neuroprotective agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cryptopleurine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | antineoplastic agent;
antiviral agent;
protein synthesis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fulvestrant | | 17beta-hydroxy steroid;
3-hydroxy steroid;
organofluorine compound;
sulfoxide | antineoplastic agent;
estrogen antagonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| deguelin | | aromatic ether;
diether;
organic heteropentacyclic compound;
rotenones | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
mitochondrial NADH:ubiquinone reductase inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cafestol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
hypoglycemic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ecteinascidin 743 | | acetate ester;
azaspiro compound;
bridged compound;
hemiaminal;
isoquinoline alkaloid;
lactone;
organic heteropolycyclic compound;
organic sulfide;
oxaspiro compound;
polyphenol;
tertiary amino compound | alkylating agent;
angiogenesis modulating agent;
anti-inflammatory agent;
antineoplastic agent;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| kahweol | | diterpenoid;
furans;
organic heteropentacyclic compound;
primary alcohol;
tertiary alcohol | angiogenesis inhibitor;
anti-inflammatory agent;
antineoplastic agent;
antioxidant;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tephrosin | | aromatic ether;
cyclic ketone;
organic heteropentacyclic compound;
rotenones | antineoplastic agent;
metabolite;
pesticide | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5-(tetradecyloxy)-2-furancarboxylic acid | | aromatic ether;
furoic acid | antineoplastic agent;
apoptosis inducer;
EC 6.4.1.2 (acetyl-CoA carboxylase) inhibitor;
PPARalpha agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 58125 | | organofluorine compound;
pyrazoles;
sulfone | antineoplastic agent;
cyclooxygenase 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| marimastat | | hydroxamic acid;
secondary carboxamide | antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| clofarabine | | adenosines;
organofluorine compound | antimetabolite;
antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2008 | 2023 | 6.4 | low | 18 | 0 | 0 | 3 | 149 | 41 |
| ay 25545 | | acetate ester;
aromatic ether;
C-glycosyl compound;
naphthoisochromene;
olefinic compound;
phenols;
tertiary amine | antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vatalanib | | monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cyc 682 | | nitrile;
nucleoside analogue;
secondary carboxamide | antimetabolite;
antineoplastic agent;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tipifarnib | | imidazoles;
monochlorobenzenes;
primary amino compound;
quinolone | antineoplastic agent;
apoptosis inducer;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| actinodaphine | | aporphine alkaloid;
aromatic ether;
organic heteropentacyclic compound;
phenols;
secondary amino compound | antibacterial agent;
antifungal agent;
antineoplastic agent;
apoptosis inducer;
plant metabolite;
platelet aggregation inhibitor;
topoisomerase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| myricanone | | aromatic ether;
cyclic ketone;
diarylheptanoid;
methoxybenzenes;
phenols | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pannarin | | aldehyde;
aromatic ether;
depsidones;
organic heterotricyclic compound;
organochlorine compound;
phenols | antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
lichen metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erlotinib | | aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound | antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| top 53 | | furonaphthodioxole;
gamma-lactone;
organic heterotetracyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-(4-morpholinoanilino)-6-cyclohexylaminopurine | | morpholines;
purines;
secondary amino compound;
tertiary amino compound | adenosine A3 receptor antagonist;
antineoplastic agent;
Aurora kinase inhibitor;
cell dedifferentiation agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lasofoxifene | | aromatic ether;
N-alkylpyrrolidine;
naphthols;
tetralins | antineoplastic agent;
bone density conservation agent;
cardioprotective agent;
estrogen receptor agonist;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 778,123 | | imidazoles;
monochlorobenzenes;
nitrile;
piperazinone;
tertiary amino compound | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
EC 2.5.1.59 (protein geranylgeranyltransferase type I) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| diflomotecan | | epsilon-lactone;
organic heteropentacyclic compound;
organofluorine compound;
organonitrogen heterocyclic compound;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| vincaleukoblastine | | acetate ester;
indole alkaloid fundamental parent;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid | antineoplastic agent;
immunosuppressive agent;
microtubule-destabilising agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| noscapine | | aromatic ether;
benzylisoquinoline alkaloid;
cyclic acetal;
isobenzofuranone;
organic heterobicyclic compound;
organic heterotricyclic compound;
tertiary amino compound | antineoplastic agent;
antitussive;
apoptosis inducer;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gant 61 | | aminal;
dialkylarylamine;
pyridines;
substituted aniline;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
glioma-associated oncogene inhibitor;
Hedgehog signaling pathway inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 8-(2-chloro-3,4,5-trimethoxybenzyl)-2-fluoro-9-pent-4-yn-1-yl-9H-purin-6-amine | | 6-aminopurines;
acetylenic compound;
methoxybenzenes;
monochlorobenzenes;
organofluorine compound | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| afimoxifene | | phenols;
tertiary amino compound | antineoplastic agent;
estrogen receptor antagonist;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| teniposide | | aromatic ether;
beta-D-glucoside;
cyclic acetal;
furonaphthodioxole;
gamma-lactone;
monosaccharide derivative;
phenols;
thiophenes | antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| prinomastat | | aromatic ether;
hydroxamic acid;
pyridines;
sulfonamide;
thiomorpholines | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| antofine | | alkaloid antibiotic;
alkaloid;
aromatic ether;
organic heteropentacyclic compound | angiogenesis inhibitor;
anti-inflammatory agent;
antimicrobial agent;
antineoplastic agent;
antiviral agent;
phytotoxin;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xanthohumol | | aromatic ether;
chalcones;
polyphenol | anti-HIV-1 agent;
antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.3.1.20 (diacylglycerol O-acyltransferase) inhibitor;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| oncrasin-1 | | arenecarbaldehyde;
indoles;
monochlorobenzenes | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| curcumin | | aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| sulindac | | monocarboxylic acid;
organofluorine compound;
sulfoxide | analgesic;
antineoplastic agent;
antipyretic;
apoptosis inducer;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
prodrug;
tocolytic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tamoxifen | | stilbenoid;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
bone density conservation agent;
EC 1.2.3.1 (aldehyde oxidase) inhibitor;
EC 2.7.11.13 (protein kinase C) inhibitor;
estrogen antagonist;
estrogen receptor antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| toremifene | | aromatic ether;
organochlorine compound;
tertiary amine | antineoplastic agent;
bone density conservation agent;
estrogen antagonist;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bms 387032 | | 1,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ospemifene | | aromatic ether;
organochlorine compound;
primary alcohol | anti-inflammatory agent;
antineoplastic agent;
estrogen receptor modulator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tandutinib | | aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 663536 | | aryl sulfide;
indoles;
monocarboxylic acid;
monochlorobenzenes | antineoplastic agent;
EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor;
leukotriene antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sc 560 | | aromatic ether;
monochlorobenzenes;
organofluorine compound;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
apoptosis inducer;
cyclooxygenase 1 inhibitor;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| daphnoretin | | aromatic ether;
hydroxycoumarin | antineoplastic agent;
antiviral agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hinokiflavone | | aromatic ether;
biflavonoid;
hydroxyflavone | antineoplastic agent;
metabolite;
neuroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mangostin | | aromatic ether;
phenols;
xanthones | antimicrobial agent;
antineoplastic agent;
antioxidant;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| wedelolactone | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
hepatoprotective agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tranilast | | amidobenzoic acid;
cinnamamides;
dimethoxybenzene;
secondary carboxamide | anti-allergic agent;
anti-asthmatic drug;
antineoplastic agent;
aryl hydrocarbon receptor agonist;
calcium channel blocker;
hepatoprotective agent;
nephroprotective agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| alvocidib | | dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound | antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| isoginkgetin | | aromatic ether;
biflavonoid | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| neoglycyrol | | aromatic ether;
coumestans;
delta-lactone;
polyphenol | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rhamnazin | | aromatic ether;
dimethoxyflavone;
phenols;
trihydroxyflavone | antineoplastic agent;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| palbociclib | | aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sulindac sulfide | | aryl sulfide;
monocarboxylic acid;
organofluorine compound | antineoplastic agent;
apoptosis inducer;
non-steroidal anti-inflammatory drug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| batimastat | | hydroxamic acid;
L-phenylalanine derivative;
organic sulfide;
secondary carboxamide;
thiophenes;
triamide | angiogenesis inhibitor;
antineoplastic agent;
matrix metalloproteinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pederin | | cyclic ketal;
diol;
oxanes;
polyketide;
secondary alcohol;
secondary carboxamide | antimitotic;
antineoplastic agent;
bacterial metabolite;
vesicant | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascofuranone | | dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid;
tetrahydrofuranone | angiogenesis inhibitor;
antilipemic drug;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| manumycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antiatherosclerotic agent;
antimicrobial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| asukamycin | | enamide;
epoxide;
organic heterobicyclic compound;
polyketide;
secondary carboxamide;
tertiary alcohol | antibacterial agent;
antifungal agent;
antimicrobial agent;
antineoplastic agent;
bacterial metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| l 744832 | | benzenes;
ether;
isopropyl ester;
secondary carboxamide;
sulfone;
thiol | antineoplastic agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ru 58668 | | 17beta-hydroxy steroid;
3-hydroxy steroid;
aromatic ether;
organofluorine compound;
sulfone | anti-estrogen;
antineoplastic agent;
estrogen receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lenvatinib | | aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| nsc 716970 | | aromatic amine;
aromatic ether;
indolecarboxamide;
organochlorine compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| muromonab-cd3 | | alkaloid;
macrocycle;
organic heteropentacyclic compound;
organonitrogen heterocyclic compound;
oxacycle;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
IP3 receptor antagonist;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| fr 148083 | | aromatic ether;
macrolide;
phenols;
secondary alcohol;
secondary alpha-hydroxy ketone | antibacterial agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| mocetinostat | | aminopyrimidine;
benzamides;
pyridines;
secondary amino compound;
secondary carboxamide;
substituted aniline | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
cardioprotective agent;
EC 3.5.1.98 (histone deacetylase) inhibitor;
hepatotoxic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 9-methoxycanthin-6-one | | aromatic ether;
indole alkaloid;
organic heterotetracyclic compound | antineoplastic agent;
antiplasmodial drug;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pi103 | | aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zm 447439 | | aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hypothemycin | | aromatic ether;
diol;
enone;
epoxide;
macrolide;
phenols;
polyketide;
secondary alpha-hydroxy ketone | antifungal agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rucaparib | | azepinoindole;
caprolactams;
organofluorine compound;
secondary amino compound | antineoplastic agent;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rubraxanthone | | aromatic ether;
polyphenol;
xanthones | antibacterial agent;
antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| NNC 55-0396 (free base) | | benzimidazoles;
cyclopropanecarboxylate ester;
organofluorine compound;
tertiary amino compound;
tetralins | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
neuroprotective agent;
potassium channel blocker;
T-type calcium channel blocker | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch 51344 | | aromatic amine;
aromatic ether;
primary alcohol;
pyrazoloquinoline;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osu 03012 | | antibiotic antifungal drug;
aromatic amide;
glycine derivative;
organofluorine compound;
phenanthrenes;
pyrazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pateamine a | | 1,3-thiazoles;
macrodiolide;
olefinic compound;
primary amino compound;
tertiary amino compound | antineoplastic agent;
antiviral agent;
eukaryotic initiation factor 4F inhibitor;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| avenanthramide b | | amidobenzoic acid;
cinnamamides;
monohydroxybenzoic acid;
monomethoxybenzene;
phenols;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
phytoalexin | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 6244 | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd2858 | | aromatic amine;
N-methylpiperazine;
pyrazines;
pyridines;
secondary carboxamide;
sulfonamide | antineoplastic agent;
bone density conservation agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
Wnt signalling activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bl1521 | | enamide;
hydroxamic acid;
monocarboxylic acid amide | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| saracatinib | | aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| crenolanib | | aminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pha 665752 | | dichlorobenzene;
enamide;
indolones;
N-acylpyrrolidine;
pyrrolecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| PB28 | | aromatic ether;
piperazines;
tetralins | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
sigma-2 receptor agonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3,5-dimethoxy-4-hydroxybenzyl alcohol-4-O-beta-D-glucopyranoside | | aromatic ether;
benzyl alcohols;
beta-D-glucoside;
monosaccharide derivative;
primary alcohol | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azadirone | | acetate ester;
cyclic terpene ketone;
furans;
limonoid;
tetracyclic triterpenoid | antineoplastic agent;
antiplasmodial drug;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7867 | | monochlorobenzenes;
piperidines;
pyrazoles | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| erastin | | aromatic ether;
diether;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
quinazolines;
tertiary carboxamide | antineoplastic agent;
ferroptosis inducer;
voltage-dependent anion channel inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-737 | | aromatic amine;
aryl sulfide;
biphenyls;
C-nitro compound;
monochlorobenzenes;
N-arylpiperazine;
N-sulfonylcarboxamide;
secondary amino compound;
tertiary amino compound | anti-allergic agent;
anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| brivanib | | aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| rx-3117 | | organofluorine compound;
primary allylic alcohol;
triol | antimetabolite;
antineoplastic agent;
apoptosis inducer;
DNA synthesis inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ascochlorin | | cyclohexanones;
dihydroxybenzaldehyde;
meroterpenoid;
monochlorobenzenes;
olefinic compound;
resorcinols;
sesquiterpenoid | angiogenesis inhibitor;
antifungal agent;
antineoplastic agent;
antiprotozoal drug;
fungal metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| at 7519 | | dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152 | | anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf 00299804 | | enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ki11502 | | aromatic ether;
benzamides;
quinolines;
thioureas | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | | aminopyridine;
aromatic ether;
dichlorobenzene;
organofluorine compound;
pyrazolylpiperidine;
racemate | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| idelalisib | | aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| zstk474 | | benzimidazoles;
morpholines;
organofluorine compound;
triamino-1,3,5-triazine | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| trametinib | | acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| bgt226 | | aromatic ether;
imidazoquinoline;
N-arylpiperazine;
organofluorine compound;
pyridines | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gedunin | | acetate ester;
enone;
epoxide;
furans;
lactone;
limonoid;
organic heteropentacyclic compound;
pentacyclic triterpenoid | antimalarial;
antineoplastic agent;
Hsp90 inhibitor;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-one | | alkaloid;
chromones;
hydroxypiperidine;
resorcinols;
tertiary amino compound | anti-inflammatory agent;
anti-ulcer drug;
anticholesteremic drug;
antileishmanial agent;
antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor;
fungal metabolite;
plant metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| azd 1152-hqpa | | anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| buparlisib | | aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ro5126766 | | aryloxypyrimidine;
coumarins;
organofluorine compound;
pyridines;
sulfamides | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk690693 | | 1,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cnf 2024 | | 2-aminopurines;
aromatic ether;
organochlorine compound;
pyridines | antineoplastic agent;
Hsp90 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ku 0063794 | | benzyl alcohols;
monomethoxybenzene;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sm 164 | | benzenes;
organic heterobicyclic compound;
secondary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tenovin-6 | | monocarboxylic acid amide;
tertiary amino compound;
thioureas | antineoplastic agent;
p53 activator;
Sir2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lde225 | | aminopyridine;
aromatic ether;
benzamides;
biphenyls;
morpholines;
organofluorine compound;
tertiary amino compound | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gdc 0449 | | benzamides;
monochlorobenzenes;
pyridines;
sulfone | antineoplastic agent;
Hedgehog signaling pathway inhibitor;
SMO receptor antagonist;
teratogenic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pci 32765 | | acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AMG-208 | | aromatic ether;
quinolines;
triazolopyridazine | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sch772984 | | biaryl;
indazoles;
N-acylpiperazine;
N-alkylpyrrolidine;
N-arylpiperazine;
pyridines;
pyrimidines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary amino compound;
tertiary carboxamide | analgesic;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 6-methoxyspirotryprostatin b | | aromatic ether;
azaspiro compound;
indole alkaloid;
indolones | antineoplastic agent;
Aspergillus metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| navitoclax | | aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lucitanib | | aromatic ether;
cyclopropanes;
naphthalenecarboxamide;
primary amino compound;
quinolines | antineoplastic agent;
fibroblast growth factor receptor antagonist;
vascular endothelial growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | | aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound | anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| salvileucalin b | | bridged compound;
diterpenoid;
furans;
gamma-lactone | antineoplastic agent;
metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| poziotinib | | acrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| entrectinib | | benzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pexidartinib | | aminopyridine;
organochlorine compound;
organofluorine compound;
pyrrolopyridine;
secondary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| TAK-580 | | 1,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk 2126458 | | aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cx 5461 | | diazepine;
naphthyridine derivative;
organic heterotetracyclic compound;
pyrazines;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.7.6 (RNA polymerase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | | benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| plx4032 | | aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dabrafenib | | 1,3-thiazoles;
aminopyrimidine;
organofluorine compound;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
B-Raf inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cblc137 | | aromatic ketone;
carbazoles;
methyl ketone;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
NF-kappaB inhibitor;
p53 activator | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| EG00229 | | benzothiadiazole;
dicarboxylic acid monoamide;
L-arginine derivative;
secondary carboxamide;
sulfonamide;
thiophenes | angiogenesis inhibitor;
antineoplastic agent;
neuropilin receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| tak-632 | | (trifluoromethyl)benzenes;
aromatic ether;
benzothiazoles;
cyclopropylcarboxamide;
monofluorobenzenes;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
necroptosis inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lrrk2-in1 | | aromatic amine;
aromatic ether;
N-acylpiperidine;
N-alkylpiperazine;
pyrimidobenzodiazepine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML-210 | | C-nitro compound;
diarylmethane;
isoxazoles;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
tertiary carboxamide | antineoplastic agent;
EC 1.11.1.9 (glutathione peroxidase) inhibitor;
ferroptosis inducer;
prodrug | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ML240 | | aromatic amine;
aromatic ether;
benzimidazoles;
primary amino compound;
quinazolines;
secondary amino compound | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 1 | | N-acylpiperazine;
N-arylpiperazine;
organofluorine compound;
pyridoquinoline;
quinolines | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| abt-199 | | aromatic ether;
C-nitro compound;
monochlorobenzenes;
N-alkylpiperazine;
N-arylpiperazine;
N-sulfonylcarboxamide;
oxanes;
pyrrolopyridine | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pracinostat | | benzimidazole;
hydroxamic acid;
olefinic compound;
tertiary amino compound | antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| xl765 | | aromatic amine;
aromatic ether;
benzamides;
quinoxaline derivative;
sulfonamide | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| DMH1 | | aromatic ether;
pyrazolopyrimidine;
quinolines | antineoplastic agent;
bone morphogenetic protein receptor antagonist;
protein kinase inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| torin 2 | | aminopyridine;
organofluorine compound;
primary amino compound;
pyridoquinoline | antineoplastic agent;
mTOR inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2656157 | | biaryl;
indoles;
methylpyridines;
organofluorine compound;
pyrrolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
PERK inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| lfm a13 | | aromatic amide;
dibromobenzene;
enamide;
enol;
nitrile;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 2.7.11.21 (polo kinase) inhibitor;
geroprotector;
platelet aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| AZD3463 | | aminopiperidine;
aminopyrimidine;
indoles;
monomethoxybenzene;
organochlorine compound;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ceritinib | | aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pelabresib | | monochlorobenzenes;
organic heterotricyclic compound;
primary carboxamide | antineoplastic agent;
bromodomain-containing protein 4 inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MK-8353 | | aromatic ether;
dihydropyridine;
indazoles;
methyl sulfide;
N-alkylpyrrolidine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
triazoles | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk2879552 | | benzenes;
benzoic acids;
cyclopropanes;
monocarboxylic acid;
piperidines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 1.14.99.66 (lysine-specific histone demethylase 1A) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| acp-196 | | aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| gsk343 | | aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| osimertinib | | acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ivosidenib | | cyanopyridine;
monochlorobenzenes;
organofluorine compound;
pyrrolidin-2-ones;
secondary carboxamide;
tertiary carboxamide | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| pf-06463922 | | aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| as 1842856 | | organofluorine compound;
primary amino compound;
quinolinemonocarboxylic acid;
quinolone;
secondary amino compound;
tertiary amino compound | anti-obesity agent;
antineoplastic agent;
apoptosis inducer;
autophagy inhibitor;
forkhead box protein O1 inhibitor;
hypoglycemic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ldc4297 | | aromatic ether;
piperidines;
pyrazoles;
pyrazolotriazine;
secondary amino compound | antineoplastic agent;
antiviral agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| enasidenib | | 1,3,5-triazines;
aminopyridine;
aromatic amine;
organofluorine compound;
secondary amino compound;
tertiary alcohol | antineoplastic agent;
EC 1.1.1.42 (isocitrate dehydrogenase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| BDA-366 | | anthraquinone;
epoxide;
secondary alcohol;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| THZ531 | | aminopyrimidine;
enamide;
indoles;
N-acylpiperidine;
organochlorine compound;
secondary amino compound;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| MMP-9-IN-1 | | aromatic compound;
organic sulfide;
organofluorine compound;
pyrimidone;
secondary carboxamide | antineoplastic agent;
EC 3.4.24.35 (gelatinase B) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| hydrazinocurcumin | | aromatic ether;
olefinic compound;
polyphenol;
pyrazoles | angiogenesis modulating agent;
antineoplastic agent;
EC 2.3.1.48 (histone acetyltransferase) inhibitor;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| cerulomycin | | aldoxime;
aromatic ether;
bipyridines;
pyridine alkaloid | antineoplastic agent;
bacterial metabolite;
marine metabolite | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| undecylprodigiosin | | alkaloid;
aromatic ether;
tripyrrole | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
bacterial metabolite;
biological pigment;
immunosuppressive agent;
radiosensitizing agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | | hydroxyindoles;
morpholines;
nitrile;
pyridines;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
tau aggregation inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| ARS-1620 | | quinazolines | antineoplastic agent;
antiviral agent;
inhibitor | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| sotorasib | | acrylamides;
methylpyridines;
monofluorobenzenes;
N-acylpiperazine;
phenols;
pyridopyrimidine;
tertiary amino compound;
tertiary carboxamide | antineoplastic agent | 0 | 0 | | low | 0 | 0 | 0 | 0 | 0 | 0 |
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| pd 173074 | | aromatic amine;
biaryl;
dimethoxybenzene;
pyridopyrimidine;
tertiary amino compound;
ureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 2012 | 2013 | 11.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| verapamil | | aromatic ether;
nitrile;
polyether;
tertiary amino compound | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| carbonyl cyanide m-chlorophenyl hydrazone | | hydrazone;
monochlorobenzenes;
nitrile | antibacterial agent;
geroprotector;
ionophore | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| chloroquine | | aminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cisapride | | benzamides | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cl 387785 | | bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 2012 | 2013 | 11.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| fasudil | | isoquinolines;
N-sulfonyldiazepane | antihypertensive agent;
calcium channel blocker;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
geroprotector;
neuroprotective agent;
nootropic agent;
vasodilator agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | | chromones;
morpholines;
organochlorine compound | autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| nifedipine | | C-nitro compound;
dihydropyridine;
methyl ester | calcium channel blocker;
human metabolite;
tocolytic agent;
vasodilator agent | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pd 153035 | | aromatic amine;
aromatic ether;
bromobenzenes;
quinazolines;
secondary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| pd168393 | | acrylamides;
bromobenzenes;
quinazolines;
secondary carboxamide;
substituted aniline | epidermal growth factor receptor antagonist | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| propranolol | | naphthalenes;
propanolamine;
secondary amine | anti-arrhythmia drug;
antihypertensive agent;
anxiolytic drug;
beta-adrenergic antagonist;
environmental contaminant;
human blood serum metabolite;
vasodilator agent;
xenobiotic | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| imatinib | | aromatic amine;
benzamides;
N-methylpiperazine;
pyridines;
pyrimidines | antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor | 2011 | 2020 | 7.8 | low | 0 | 0 | 0 | 0 | 5 | 0 |
| vorinostat | | dicarboxylic acid diamide;
hydroxamic acid | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| colchicine | | alkaloid;
colchicine | anti-inflammatory agent;
gout suppressant;
mutagen | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bisbenzimidazole trihydrochloride | | | | 2020 | 2020 | 4.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| paclitaxel | | taxane diterpenoid;
tetracyclic diterpenoid | antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| triciribine phosphate | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| staurosporine | | indolocarbazole alkaloid;
organic heterooctacyclic compound | apoptosis inducer;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
geroprotector | 2011 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 5 | 0 |
| bendamustine | | benzimidazoles | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| picropodophyllin | | furonaphthodioxole;
lignan;
organic heterotetracyclic compound | antineoplastic agent;
insulin-like growth factor receptor 1 antagonist;
plant metabolite;
tyrosine kinase inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| clofarabine | | adenosines;
organofluorine compound | antimetabolite;
antineoplastic agent | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2009 | 2021 | 7.0 | low | 0 | 0 | 0 | 2 | 23 | 3 |
| lestaurtinib | | indolocarbazole | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| 10-propargyl-10-deazaaminopterin | | N-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound | antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| perifosine | | ammonium betaine;
phospholipid | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| vatalanib | | monochlorobenzenes;
phthalazines;
pyridines;
secondary amino compound | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
vascular endothelial growth factor receptor antagonist | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ruboxistaurin | | | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| canertinib | | monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2019 | 8.2 | medium | 0 | 0 | 0 | 1 | 11 | 0 |
| birb 796 | | aromatic ether;
morpholines;
naphthalenes;
pyrazoles;
ureas | EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
immunomodulator | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cyc 202 | | 2,6-diaminopurines | antiviral drug;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| frenolicin b | | benzoisochromanequinone;
p-quinones | metabolite | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sb 203580 | | imidazoles;
monofluorobenzenes;
pyridines;
sulfoxide | EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector;
Hsp90 inhibitor;
neuroprotective agent | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sb 216763 | | indoles;
maleimides | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| enzastaurin | | indoles;
maleimides | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| erlotinib | | aromatic ether;
quinazolines;
secondary amino compound;
terminal acetylenic compound | antineoplastic agent;
epidermal growth factor receptor antagonist;
protein kinase inhibitor | 2009 | 2021 | 7.1 | medium | 0 | 0 | 0 | 1 | 17 | 3 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2011 | 2021 | 5.7 | low | 0 | 0 | 0 | 0 | 8 | 1 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2011 | 2019 | 8.2 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| n-phenylacrylamide | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| wortmannin | | acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound | anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lithium chloride | | inorganic chloride;
lithium salt | antimanic drug;
geroprotector | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| quinidine | | cinchona alkaloid | alpha-adrenergic antagonist;
anti-arrhythmia drug;
antimalarial;
drug allergen;
EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor;
EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor;
muscarinic antagonist;
P450 inhibitor;
potassium channel blocker;
sodium channel blocker | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| trichostatin a | | antibiotic antifungal agent;
hydroxamic acid;
trichostatin | bacterial metabolite;
EC 3.5.1.98 (histone deacetylase) inhibitor;
geroprotector | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pd 173955 | | aryl sulfide;
dichlorobenzene;
methyl sulfide;
pyridopyrimidine | tyrosine kinase inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ketoconazole | | cis-1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| artenimol | | | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| shikonin | | hydroxy-1,4-naphthoquinone | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| xl147 | | aromatic amine;
benzothiadiazole;
quinoxaline derivative;
sulfonamide | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| thioguanine anhydrous | | 2-aminopurines | anticoronaviral agent;
antimetabolite;
antineoplastic agent | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| stattic | | 1-benzothiophenes;
C-nitro compound;
sulfone | antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| lch-7749944 | | | | 2019 | 2019 | 5.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| nelarabine | | beta-D-arabinoside;
monosaccharide derivative;
purine nucleoside | antineoplastic agent;
DNA synthesis inhibitor;
prodrug | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| bms 387032 | | 1,3-oxazoles;
1,3-thiazoles;
organic sulfide;
piperidinecarboxamide;
secondary carboxamide | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| sf 2370 | | bridged compound;
gamma-lactam;
methyl ester;
organic heterooctacyclic compound | antimicrobial agent;
bacterial metabolite;
EC 2.7.11.13 (protein kinase C) inhibitor;
tropomyosin-related kinase B receptor antagonist | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tandutinib | | aromatic ether;
N-arylpiperazine;
N-carbamoylpiperazine;
phenylureas;
piperidines;
quinazolines;
tertiary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| vx-745 | | aryl sulfide;
dichlorobenzene;
difluorobenzene;
pyrimidopyridazine | anti-inflammatory drug;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dasatinib | | 1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2011 | 2021 | 7.6 | low | 0 | 0 | 0 | 0 | 11 | 2 |
| ha 1100 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 7-epi-hydroxystaurosporine | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| zd 6474 | | aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine | antineoplastic agent;
tyrosine kinase inhibitor | 2011 | 2021 | 6.6 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | | benzenes;
thiadiazolidine | anti-inflammatory agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent | 2012 | 2021 | 8.6 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| imd 0354 | | benzamides | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 7-hydroxycoumarin | | hydroxycoumarin | fluorescent probe;
food component;
plant metabolite | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sirolimus | | antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol | antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| alvocidib | | dihydroxyflavone;
hydroxypiperidine;
monochlorobenzenes;
tertiary amino compound | antineoplastic agent;
antirheumatic drug;
apoptosis inducer;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| bosutinib | | aminoquinoline;
aromatic ether;
dichlorobenzene;
N-methylpiperazine;
nitrile;
tertiary amino compound | antineoplastic agent;
tyrosine kinase inhibitor | 2011 | 2019 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| orantinib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| su 11248 | | monocarboxylic acid amide;
pyrroles | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist | 2011 | 2021 | 7.9 | low | 0 | 0 | 0 | 0 | 10 | 2 |
| m475271 | | | | 2019 | 2019 | 5.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| palbociclib | | aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| vx680 | | N-arylpiperazine | | 2010 | 2017 | 11.3 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| cyc 116 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| everolimus | | cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol | anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ekb 569 | | aminoquinoline;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile | protein kinase inhibitor | 2013 | 2020 | 6.4 | low | 0 | 0 | 0 | 0 | 5 | 0 |
| axitinib | | aryl sulfide;
benzamides;
indazoles;
pyridines | antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| manzamine a | | alkaloid;
beta-carbolines;
isoquinolines | animal metabolite;
anti-HSV-1 agent;
antimalarial;
antineoplastic agent;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
marine metabolite | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| artesunate | | artemisinin derivative;
cyclic acetal;
dicarboxylic acid monoester;
hemisuccinate;
semisynthetic derivative;
sesquiterpenoid | antimalarial;
antineoplastic agent;
ferroptosis inducer | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| temsirolimus | | macrolide lactam | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pd 184352 | | aminobenzoic acid | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| on 01910 | | N-[2-methoxy-5-({[2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonyl}methyl)phenyl]glycine | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.21 (polo kinase) inhibitor;
microtubule-destabilising agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| av 412 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| telatinib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| y-39983 | | pyrrolopyridine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cp 547632 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bms345541 | | quinoxaline derivative | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| spc-839 | | | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lenvatinib | | aromatic amide;
aromatic ether;
cyclopropanes;
monocarboxylic acid amide;
monochlorobenzenes;
phenylureas;
quinolines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist;
orphan drug;
vascular endothelial growth factor receptor antagonist | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| pd 0325901 | | difluorobenzene;
hydroxamic acid ester;
monofluorobenzenes;
organoiodine compound;
propane-1,2-diols;
secondary amino compound | antineoplastic agent;
EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| midostaurin | | benzamides;
gamma-lactam;
indolocarbazole;
organic heterooctacyclic compound | antineoplastic agent;
EC 2.7.11.13 (protein kinase C) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| px-866 | | acetate ester;
delta-lactone;
organic heterotetracyclic compound;
tertiary amino compound | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ripasudil | | isoquinolines | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| fr 148083 | | aromatic ether;
macrolide;
phenols;
secondary alcohol;
secondary alpha-hydroxy ketone | antibacterial agent;
antineoplastic agent;
metabolite;
NF-kappaB inhibitor | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| osi 930 | | aromatic amide | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ki 20227 | | | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| scio-469 | | aromatic amide;
aromatic ketone;
chloroindole;
dicarboxylic acid diamide;
indolecarboxamide;
monofluorobenzenes;
N-acylpiperazine;
N-alkylpiperazine | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cp 724714 | | 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| pi103 | | aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hmn-214 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| tivozanib | | aromatic ether | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| zm 447439 | | aromatic ether;
benzamides;
morpholines;
polyether;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
Aurora kinase inhibitor | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hki 272 | | nitrile;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2022 | 7.3 | low | 0 | 0 | 0 | 1 | 7 | 1 |
| tofacitinib | | N-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound | antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2011 | 2017 | 9.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| n-(6-chloro-7-methoxy-9h-beta-carbolin-8-yl)-2-methylnicotinamide | | | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cediranib | | aromatic ether | | 2011 | 2019 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| palmarumycin cp2 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| masitinib | | 1,3-thiazoles;
benzamides;
N-alkylpiperazine;
pyridines | antineoplastic agent;
antirheumatic drug;
tyrosine kinase inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ly-2157299 | | aromatic amide;
methylpyridines;
monocarboxylic acid amide;
pyrrolopyrazole;
quinolines | antineoplastic agent;
TGFbeta receptor antagonist | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pazopanib | | aminopyrimidine;
indazoles;
sulfonamide | angiogenesis modulating agent;
antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| azd 6244 | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2011 | 2020 | 8.0 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| su 14813 | | | | 2011 | 2017 | 10.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| binimetinib | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monofluorobenzenes;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sotrastaurin | | indoles;
maleimides;
N-alkylpiperazine;
N-arylpiperazine;
quinazolines | anticoronaviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunosuppressive agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| aee 788 | | 6-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist;
trypanocidal drug | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| saracatinib | | aromatic ether;
benzodioxoles;
diether;
N-methylpiperazine;
organochlorine compound;
oxanes;
quinazolines;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
autophagy inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
radiosensitizing agent | 2017 | 2019 | 5.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| vx 702 | | phenylpyridine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| crenolanib | | aminopiperidine;
aromatic ether;
benzimidazoles;
oxetanes;
quinolines;
tertiary amino compound | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tg100-115 | | pteridines | | 2011 | 2017 | 10.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| cc 401 | | pyrazoles;
ring assembly | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bms 599626 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| (S)-Isosclerone | | tetralins | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| exel-7647 | | | | 2017 | 2019 | 6.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| volasertib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pha 665752 | | dichlorobenzene;
enamide;
indolones;
N-acylpyrrolidine;
pyrrolecarboxamide;
secondary carboxamide;
sulfone;
tertiary carboxamide | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd 7762 | | aromatic amide;
thiophenes | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 2016 | 2017 | 7.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| 6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)-4-pyrimidinyl]amino]-2,2-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one | | methoxybenzenes;
substituted aniline | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| brivanib | | aromatic ether;
diether;
fluoroindole;
pyrrolotriazine;
secondary alcohol | angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
drug metabolite;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
fibroblast growth factor receptor antagonist | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| mp470 | | N-arylpiperazine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rgb 286638 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| np 031112 | | benzenes;
naphthalenes;
thiadiazolidine | anti-inflammatory agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
neuroprotective agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| at 7519 | | dichlorobenzene;
piperidines;
pyrazoles;
secondary carboxamide | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| bms-690514 | | | | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| bi 2536 | | | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| inno-406 | | biaryl | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| nvp-ast487 | | | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| kw 2449 | | | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| danusertib | | piperazines | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| nvp-aew541 | | | | 2015 | 2021 | 6.2 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| abt 869 | | aromatic amine;
indazoles;
phenylureas | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| azd 8931 | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
tertiary amino compound | EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 2017 | 2019 | 5.7 | high | 0 | 0 | 0 | 0 | 3 | 0 |
| arq 197 | | indoles | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd 1152 | | anilide;
monoalkyl phosphate;
monofluorobenzenes;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor;
prodrug | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pf 00299804 | | enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2012 | 2022 | 5.8 | low | 0 | 0 | 0 | 0 | 8 | 4 |
| ridaforolimus | | macrolide lactam | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ch 4987655 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| 6-(5-((cyclopropylamino)carbonyl)-3-fluoro-2-methylphenyl)-n-(2,2-dimethylprpyl)-3-pyridinecarboxamide | | phenylpyridine | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| lapatinib ditosylate | | quinazolines | | 2009 | 2009 | 15.0 | medium | 0 | 0 | 0 | 1 | 0 | 0 |
| cc-930 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| gw 2580 | | | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tak 285 | | | | 2017 | 2020 | 5.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| idelalisib | | aromatic amine;
organofluorine compound;
purines;
quinazolines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2021 | 4.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| crizotinib | | 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2011 | 2020 | 8.2 | low | 0 | 0 | 0 | 0 | 5 | 0 |
| osi 906 | | cyclobutanes;
quinolines | | 2014 | 2017 | 8.5 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| chir-265 | | aromatic ether | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| motesanib | | pyridinecarboxamide | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| fostamatinib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| jnj 28312141 | | | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| trametinib | | acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| mln8054 | | benzazepine | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| pf-562,271 | | indoles | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| GDC-0879 | | indanes;
ketoxime;
primary alcohol;
pyrazoles;
pyridines | antineoplastic agent;
B-Raf inhibitor | 2011 | 2011 | 13.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| jnj-26483327 | | | | 2017 | 2019 | 6.0 | high | 0 | 0 | 0 | 0 | 2 | 0 |
| ly2603618 | | ureas | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tg100801 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| dactolisib | | imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bgt226 | | aromatic ether;
imidazoquinoline;
N-arylpiperazine;
organofluorine compound;
pyridines | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gsk 461364 | | (trifluoromethyl)benzenes | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| azd 1152-hqpa | | anilide;
monofluorobenzenes;
primary alcohol;
pyrazoles;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
Aurora kinase inhibitor | 2011 | 2019 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| nvp-tae684 | | piperidines | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| enmd 2076 | | | | 2017 | 2018 | 6.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine | | quinazolines | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| e 7050 | | aromatic ether | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-5-yl)-7-pyrido[2,3-d]pyrimidinone | | pyrazolopyridine | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| tak-901 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gdc-0973 | | aromatic amine;
difluorobenzene;
N-acylazetidine;
organoiodine compound;
piperidines;
secondary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| buparlisib | | aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd 1480 | | | | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| azd8330 | | pyridinecarboxamide | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pha 848125 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ro5126766 | | aryloxypyrimidine;
coumarins;
organofluorine compound;
pyridines;
sulfamides | antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fedratinib | | sulfonamide | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| gsk690693 | | 1,2,5-oxadiazole;
acetylenic compound;
aromatic amine;
aromatic ether;
imidazopyridine;
piperidines;
primary amino compound;
tertiary alcohol | antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| cnf 2024 | | 2-aminopurines;
aromatic ether;
organochlorine compound;
pyridines | antineoplastic agent;
Hsp90 inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo(19.3.1.1(2,6).1(8,12))heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd5438 | | sulfonamide | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pf 04217903 | | quinolines | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gdc 0941 | | indazoles;
morpholines;
piperazines;
sulfonamide;
thienopyrimidine | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| icotinib | | | | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ph 797804 | | aromatic ether;
benzamides;
organobromine compound;
organofluorine compound;
pyridone | anti-inflammatory agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| kx-01 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| olaparib | | cyclopropanes;
monofluorobenzenes;
N-acylpiperazine;
phthalazines | antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| plx 4720 | | aromatic ketone;
difluorobenzene;
organochlorine compound;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mk 5108 | | aromatic ether | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cx 4945 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cudc 101 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| arry-614 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| tak 593 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| mln 8237 | | benzazepine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sgx 523 | | aryl sulfide;
biaryl;
pyrazoles;
quinolines;
triazolopyridazine | c-Met tyrosine kinase inhibitor;
nephrotoxic agent | 2011 | 2017 | 10.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| bms 754807 | | pyrazoles;
pyridines;
pyrrolidines;
pyrrolotriazine | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bms 777607 | | aromatic amide | | 2014 | 2017 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| sgi 1776 | | imidazoles | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pci 32765 | | acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2012 | 2022 | 6.1 | low | 0 | 0 | 0 | 0 | 7 | 2 |
| ponatinib | | (trifluoromethyl)benzenes;
acetylenic compound;
benzamides;
imidazopyridazine;
N-methylpiperazine | antineoplastic agent;
tyrosine kinase inhibitor | 2014 | 2021 | 6.4 | low | 0 | 0 | 0 | 0 | 6 | 1 |
| amg 900 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mk-1775 | | piperazines | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| AMG-208 | | aromatic ether;
quinolines;
triazolopyridazine | antineoplastic agent;
c-Met tyrosine kinase inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| quizartinib | | benzoimidazothiazole;
isoxazoles;
morpholines;
phenylureas | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
necroptosis inhibitor | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| at13148 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tak 733 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mk 2206 | | organic heterotricyclic compound | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sns 314 | | ureas | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lucitanib | | aromatic ether;
cyclopropanes;
naphthalenecarboxamide;
primary amino compound;
quinolines | antineoplastic agent;
fibroblast growth factor receptor antagonist;
vascular endothelial growth factor receptor antagonist | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pf-04691502 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| n-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide | | aminopyrimidine;
benzamides;
morpholines;
nitrile;
secondary amino compound;
tertiary amino compound | anti-anaemic agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dcc-2036 | | organofluorine compound;
phenylureas;
pyrazoles;
pyridinecarboxamide;
quinolines | tyrosine kinase inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cabozantinib | | aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 2015 | 2021 | 6.4 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| defactinib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ly2584702 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| incb-018424 | | nitrile;
pyrazoles;
pyrrolopyrimidine | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2011 | 2021 | 7.2 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| poziotinib | | acrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist | 2017 | 2022 | 4.2 | medium | 0 | 0 | 0 | 0 | 4 | 2 |
| asp3026 | | aromatic amine;
diamino-1,3,5-triazine;
monomethoxybenzene;
N-methylpiperazine;
piperidines;
secondary amino compound;
sulfone | antimalarial;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
EC 6.1.1.6 (lysine--tRNA ligase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| entrectinib | | benzamides;
difluorobenzene;
indazoles;
N-methylpiperazine;
oxanes;
secondary amino compound;
secondary carboxamide | antibacterial agent;
antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pexidartinib | | aminopyridine;
organochlorine compound;
organofluorine compound;
pyrrolopyridine;
secondary amino compound | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| TAK-580 | | 1,3-thiazolecarboxamide;
aminopyrimidine;
chloropyridine;
organofluorine compound;
pyrimidinecarboxamide;
secondary carboxamide | antineoplastic agent;
apoptosis inducer;
B-Raf inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gsk 2126458 | | aromatic ether;
difluorobenzene;
pyridazines;
pyridines;
quinolines;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
autophagy inducer;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor;
radiosensitizing agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| emd1214063 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gsk 1838705a | | organonitrogen compound;
organooxygen compound | | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pf 3758309 | | organic heterobicyclic compound;
organonitrogen heterocyclic compound;
organosulfur heterocyclic compound | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gdc 0980 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| azd2014 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | | benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
mTOR inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| plx4032 | | aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| gsk 1363089 | | aromatic ether | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| arry-334543 | | | | 2017 | 2019 | 6.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| kin-193 | | pyridopyrimidine | | 2017 | 2020 | 5.5 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| mk 2461 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bay 869766 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| as 703026 | | pyridinecarboxamide | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| baricitinib | | azetidines;
nitrile;
pyrazoles;
pyrrolopyrimidine;
sulfonamide | anti-inflammatory agent;
antirheumatic drug;
antiviral agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
immunosuppressive agent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dabrafenib | | 1,3-thiazoles;
aminopyrimidine;
organofluorine compound;
sulfonamide | anticoronaviral agent;
antineoplastic agent;
B-Raf inhibitor | 2017 | 2020 | 5.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| pki 587 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| n-(3-fluoro-4-((1-methyl-6-(1h-pyrazol-4-yl)-1h-indazol-5 yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| N-[3-[[5-chloro-2-[4-(4-methyl-1-piperazinyl)anilino]-4-pyrimidinyl]oxy]phenyl]-2-propenamide | | piperazines | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| thiopental sodium | | organochlorine compound;
piperazines;
pyrimidines | antineoplastic agent;
tyrosine kinase inhibitor | 2012 | 2021 | 7.2 | high | 0 | 0 | 0 | 0 | 10 | 1 |
| ribociclib | | | | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| mk-8033 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pha 793887 | | piperidinecarboxamide | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sb 1518 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| abemaciclib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mk-8776 | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| afuresertib | | amphetamines | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gsk 1070916 | | pyrazoles;
ring assembly | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| jnj38877605 | | quinolines | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dinaciclib | | pyrazolopyrimidine | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gilteritinib | | aromatic amine;
monomethoxybenzene;
N-methylpiperazine;
oxanes;
piperidines;
primary carboxamide;
pyrazines;
secondary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| alectinib | | aromatic ketone;
morpholines;
nitrile;
organic heterotetracyclic compound;
piperidines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| glpg0634 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ipi-145 | | isoquinolines | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| encorafenib | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bms-911543 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd4547 | | benzamides;
N-arylpiperazine;
pyrazoles | fibroblast growth factor receptor antagonist | 2015 | 2017 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| gsk2141795 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd8186 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-(4-(4-ethylpiperazin-1-yl)-phenylamino)pyrimidin-4-yl)-1-methylurea | | aminopyrimidine;
dichlorobenzene;
N-alkylpiperazine;
N-arylpiperazine;
phenylureas | antineoplastic agent;
fibroblast growth factor receptor antagonist | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| palinurin | | | | 2012 | 2013 | 11.5 | high | 0 | 0 | 0 | 0 | 2 | 0 |
| byl719 | | proline derivative | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cep-32496 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rociletinib | | | | 2016 | 2021 | 5.8 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| ceritinib | | aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2020 | 5.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| azd1208 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| vx-509 | | | | 2015 | 2017 | 8.0 | medium | 0 | 0 | 0 | 0 | 2 | 0 |
| debio 1347 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| volitinib | | | | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| acp-196 | | aromatic amine;
benzamides;
imidazopyrazine;
pyridines;
pyrrolidinecarboxamide;
secondary carboxamide;
tertiary carboxamide;
ynone | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| osimertinib | | acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2014 | 2022 | 5.2 | low | 0 | 0 | 0 | 0 | 17 | 6 |
| pf-06463922 | | aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| azd3759 | | | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| at 9283 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| otssp167 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| chir 258 | | | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| osi 027 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ganciclovir | | 2-aminopurines;
oxopurine | antiinfective agent;
antiviral drug | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pemetrexed | | N-acyl-L-glutamic acid;
pyrrolopyrimidine | antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| nintedanib | | | | 2011 | 2017 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| 2-hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1h-indole-5-carbonitrile | | hydroxyindoles;
morpholines;
nitrile;
pyridines;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 2.7.11.26 (tau-protein kinase) inhibitor;
tau aggregation inhibitor | 2017 | 2017 | 7.0 | medium | 0 | 0 | 0 | 0 | 1 | 0 |
| bay 80-6946 | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pp242 | | aromatic amine;
biaryl;
hydroxyindoles;
phenols;
primary amino compound;
pyrazolopyrimidine | antineoplastic agent;
mTOR inhibitor | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis, and docking studies of quinazoline analogues bearing aryl semicarbazone scaffolds as potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 06-15, Volume: 25, Issue:12, 2017
Design, synthesis, and docking studies of afatinib analogs bearing cinnamamide moiety as potent EGFR inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 24, Issue:7, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis, and evaluation of A-ring-modified lamellarin N analogues as noncovalent inhibitors of the EGFR T790M/L858R mutant.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.Journal of medicinal chemistry, , Dec-13, Volume: 55, Issue:23, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Design, synthesis and biological evaluation of novel 6-alkenylamides substituted of 4-anilinothieno[2,3-d]pyrimidines as irreversible epidermal growth factor receptor inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 22, Issue:7, 2014
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 22, Issue:23, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.ACS medicinal chemistry letters, , Apr-10, Volume: 5, Issue:4, 2014
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Identification of spirobisnaphthalene derivatives with anti-tumor activities from the endophytic fungus Rhytidhysteron rufulum AS21B.Bioorganic & medicinal chemistry, , 06-01, Volume: 25, Issue:11, 2017
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β).Bioorganic & medicinal chemistry, , 11-01, Volume: 26, Issue:20, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 59, Issue:8, 2016
Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 24, Issue:24, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The Exploration of Chirality for Improved Druggability within the Human Kinome.Journal of medicinal chemistry, , 01-23, Volume: 63, Issue:2, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Irreversible protein kinase inhibitors: balancing the benefits and risks.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
Design, synthesis and SAR study of 2-aminopyrimidines with diverse Michael addition acceptors for chemically tuning the potency against EGFRBioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Proteome-wide Identification of Off-Targets of a Potent EGFRACS medicinal chemistry letters, , Feb-10, Volume: 13, Issue:2, 2022
Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach.Journal of medicinal chemistry, , 10-22, Volume: 63, Issue:20, 2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12, 2019
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 27, Issue:21, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Discovery and Structural Optimization of N5-Substituted 6,7-Dioxo-6,7-dihydropteridines as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Development of Selective Covalent Janus Kinase 3 Inhibitors.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
| Substance | Studies | Classes | Roles | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| aminolevulinic acid | | 4-oxo monocarboxylic acid;
amino acid zwitterion;
delta-amino acid | antineoplastic agent;
dermatologic drug;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
photosensitizing agent;
plant metabolite;
prodrug;
Saccharomyces cerevisiae metabolite | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ethylene glycol | | ethanediol;
glycol | metabolite;
mouse metabolite;
solvent;
toxin | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| adenine | | 6-aminopurines;
purine nucleobase | Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite | 2015 | 2021 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| carbamates | | amino-acid anion | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| salicylic acid | | monohydroxybenzoic acid | algal metabolite;
antifungal agent;
antiinfective agent;
EC 1.11.1.11 (L-ascorbate peroxidase) inhibitor;
keratolytic drug;
plant hormone;
plant metabolite | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dimethylamine | | methylamines;
secondary aliphatic amine | metabolite | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| dimethyl sulfoxide | | sulfoxide;
volatile organic compound | alkylating agent;
antidote;
Escherichia coli metabolite;
geroprotector;
MRI contrast agent;
non-narcotic analgesic;
polar aprotic solvent;
radical scavenger | 2018 | 2019 | 5.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| formamide | | carboximidic acid;
formamides;
monocarboxylic acid amide;
one-carbon compound | solvent | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| niacinamide | | pyridine alkaloid;
pyridinecarboxamide;
vitamin B3 | anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor | 2010 | 2016 | 10.7 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| nitrites | | monovalent inorganic anion;
nitrogen oxoanion;
reactive nitrogen species | human metabolite | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| phenol | | phenols | antiseptic drug;
disinfectant;
human xenobiotic metabolite;
mouse metabolite | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| pteridines | | azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
pteridines | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| betaxolol | | propanolamine | antihypertensive agent;
beta-adrenergic antagonist;
sympatholytic agent | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| verapamil | | aromatic ether;
nitrile;
polyether;
tertiary amino compound | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| carvedilol | | carbazoles;
secondary alcohol;
secondary amino compound | alpha-adrenergic antagonist;
antihypertensive agent;
beta-adrenergic antagonist;
cardiovascular drug;
vasodilator agent | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| celecoxib | | organofluorine compound;
pyrazoles;
sulfonamide;
toluenes | cyclooxygenase 2 inhibitor;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| cl 387785 | | bromobenzenes;
quinazolines;
secondary carboxamide;
ynamide | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
epidermal growth factor receptor antagonist | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| clotrimazole | | conazole antifungal drug;
imidazole antifungal drug;
imidazoles;
monochlorobenzenes | antiinfective agent;
environmental contaminant;
xenobiotic | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dapsone | | substituted aniline;
sulfone | anti-inflammatory drug;
antiinfective agent;
antimalarial;
leprostatic drug | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| ethacrynic acid | | aromatic ether;
aromatic ketone;
dichlorobenzene;
monocarboxylic acid | EC 2.5.1.18 (glutathione transferase) inhibitor;
ion transport inhibitor;
loop diuretic | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fluorouracil | | nucleobase analogue;
organofluorine compound | antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic | 2010 | 2023 | 7.6 | low | 1 | 0 | 0 | 1 | 4 | 2 |
| furosemide | | chlorobenzoic acid;
furans;
sulfonamide | environmental contaminant;
loop diuretic;
xenobiotic | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| metformin | | guanidines | environmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic | 2020 | 2021 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| oxonic acid | | 1,3,5-triazines;
monocarboxylic acid | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| pd168393 | | acrylamides;
bromobenzenes;
quinazolines;
secondary carboxamide;
substituted aniline | epidermal growth factor receptor antagonist | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| resorcinol | | benzenediol;
phenolic donor;
resorcinols | erythropoietin inhibitor;
sensitiser | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| vorinostat | | dicarboxylic acid diamide;
hydroxamic acid | antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tegafur | | organohalogen compound;
pyrimidines | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| temozolomide | | imidazotetrazine;
monocarboxylic acid amide;
triazene derivative | alkylating agent;
antineoplastic agent;
prodrug | 2015 | 2021 | 5.6 | low | 2 | 0 | 0 | 0 | 5 | 2 |
| thalidomide | | phthalimides;
piperidones | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| prednisolone | | 11beta-hydroxy steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone | adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
drug metabolite;
environmental contaminant;
immunosuppressive agent;
xenobiotic | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| lysine | | aspartate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
lysine;
organic molecular entity;
proteinogenic amino acid | algal metabolite;
anticonvulsant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| tyrosine | | amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine | EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dimethylnitrosamine | | nitrosamine | geroprotector;
mutagen | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| methionine | | aspartate family amino acid;
L-alpha-amino acid;
methionine zwitterion;
methionine;
proteinogenic amino acid | antidote to paracetamol poisoning;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| cycloheximide | | antibiotic fungicide;
cyclic ketone;
dicarboximide;
piperidine antibiotic;
piperidones;
secondary alcohol | anticoronaviral agent;
bacterial metabolite;
ferroptosis inhibitor;
neuroprotective agent;
protein synthesis inhibitor | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| valine | | L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid;
valine | algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| methylprednisolone | | 6-methylprednisolone;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone | adrenergic agent;
anti-inflammatory drug;
antiemetic;
environmental contaminant;
neuroprotective agent;
xenobiotic | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| n-vinyl-2-pyrrolidinone | | pyrrolidin-2-ones | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| decalin | | ortho-fused bicyclic hydrocarbon | solvent | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pyrroles | | pyrrole;
secondary amine | | 2013 | 2022 | 6.2 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| thiophenes | | mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound | non-polar solvent | 2017 | 2021 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| quinazolines | | azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines | | 2007 | 2023 | 8.7 | medium | 85 | 0 | 0 | 15 | 463 | 12 |
| indazoles | | indazole | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| isoxazoles | | isoxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| thiazoles | | 1,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene | | 2015 | 2019 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| pyrimidine | | diazine;
pyrimidines | Daphnia magna metabolite | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| pyrazines | | diazine;
pyrazines | Daphnia magna metabolite | 2013 | 2016 | 9.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| 6-aminonicotinamide | | aminopyridine;
monocarboxylic acid amide;
primary amino compound | antimetabolite;
EC 1.1.1.44 (NADP(+)-dependent decarboxylating phosphogluconate dehydrogenase) inhibitor;
teratogenic agent | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| alpha-aminopyridine | | | | 2013 | 2021 | 6.4 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| deoxycytidine | | pyrimidine 2'-deoxyribonucleoside | Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite | 2013 | 2023 | 6.6 | low | 6 | 0 | 0 | 0 | 13 | 3 |
| fluorescein-5-isothiocyanate | | fluorescein isothiocyanate | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| platinum | | elemental platinum;
nickel group element atom;
platinum group metal atom | | 2014 | 2022 | 6.5 | low | 3 | 0 | 0 | 0 | 4 | 2 |
| gold | | copper group element atom;
elemental gold | | 2015 | 2016 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| camptothecin | | delta-lactone;
pyranoindolizinoquinoline;
quinoline alkaloid;
tertiary alcohol | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
genotoxin;
plant metabolite | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| phosphotyrosine | | L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid;
O(4)-phosphotyrosine | Escherichia coli metabolite;
immunogen | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| alovudine | | pyrimidine 2',3'-dideoxyribonucleoside | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| paclitaxel | | taxane diterpenoid;
tetracyclic diterpenoid | antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent | 2009 | 2022 | 7.4 | low | 6 | 0 | 0 | 1 | 10 | 3 |
| etoposide | | beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound | antineoplastic agent;
DNA synthesis inhibitor | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| ribavirin | | 1-ribosyltriazole;
aromatic amide;
monocarboxylic acid amide;
primary carboxamide | anticoronaviral agent;
antiinfective agent;
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| pirfenidone | | pyridone | antipyretic;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fenoxaprop ethyl | | aromatic ether | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| simvastatin | | delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic) | EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug | 2017 | 2017 | 7.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| topotecan | | pyranoindolizinoquinoline | antineoplastic agent;
EC 5.99.1.2 (DNA topoisomerase) inhibitor | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| gemcitabine | | organofluorine compound;
pyrimidine 2'-deoxyribonucleoside | antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic | 2013 | 2023 | 6.6 | low | 6 | 0 | 0 | 0 | 13 | 3 |
| irinotecan | | carbamate ester;
delta-lactone;
N-acylpiperidine;
pyranoindolizinoquinoline;
ring assembly;
tertiary alcohol;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
prodrug | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| adenosine | | adenosines;
purines D-ribonucleoside | analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent | 2020 | 2022 | 3.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| thiazolyl blue | | organic bromide salt | colorimetric reagent;
dye | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fluorodeoxyglucose f18 | | 2-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose | | 2013 | 2018 | 8.0 | low | 1 | 0 | 0 | 0 | 3 | 0 |
| fascaplysine | | | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| 4-aminoquinazoline | | | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| nicotine | | 3-(1-methylpyrrolidin-2-yl)pyridine | anxiolytic drug;
biomarker;
immunomodulator;
mitogen;
neurotoxin;
nicotinic acetylcholine receptor agonist;
peripheral nervous system drug;
phytogenic insecticide;
plant metabolite;
psychotropic drug;
teratogenic agent;
xenobiotic | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| n-methyladenosine | | methyladenosine | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| u 73122 | | aromatic ether;
aza-steroid;
maleimides | EC 3.1.4.11 (phosphoinositide phospholipase C) inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| fingolimod hydrochloride | | hydrochloride | immunosuppressive agent;
prodrug;
sphingosine-1-phosphate receptor agonist | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| deoxyglucose | | | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| celastrol | | monocarboxylic acid;
pentacyclic triterpenoid | anti-inflammatory drug;
antineoplastic agent;
antioxidant;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
Hsp90 inhibitor;
metabolite | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| bruceine d | | | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| imatinib mesylate | | methanesulfonate salt | anticoronaviral agent;
antineoplastic agent;
apoptosis inducer;
tyrosine kinase inhibitor | 2015 | 2021 | 5.5 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| gefitinib | | aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
morpholines;
quinazolines;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2008 | 2023 | 6.4 | low | 18 | 0 | 0 | 3 | 149 | 41 |
| methotrexate | | dicarboxylic acid;
monocarboxylic acid amide;
pteridines | abortifacient;
antimetabolite;
antineoplastic agent;
antirheumatic drug;
dermatologic drug;
DNA synthesis inhibitor;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
immunosuppressive agent | 2014 | 2020 | 7.2 | low | 6 | 0 | 0 | 0 | 9 | 0 |
| docetaxel anhydrous | | secondary alpha-hydroxy ketone;
tetracyclic diterpenoid | antimalarial;
antineoplastic agent;
photosensitizing agent | 2013 | 2022 | 7.2 | low | 3 | 0 | 0 | 0 | 12 | 2 |
| canertinib | | monochlorobenzenes;
morpholines;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2018 | 10.4 | low | 0 | 0 | 0 | 2 | 3 | 0 |
| methyl 5-aminolevulinate | | delta-amino acid ester | antineoplastic agent;
dermatologic drug;
photosensitizing agent;
prodrug | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| boswellic acid | | triterpenoid | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| erlotinib hydrochloride | | hydrochloride;
terminal acetylenic compound | antineoplastic agent;
protein kinase inhibitor | 2008 | 2023 | 6.6 | low | 16 | 0 | 0 | 3 | 153 | 35 |
| lapatinib | | furans;
organochlorine compound;
organofluorine compound;
quinazolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2023 | 7.9 | low | 2 | 0 | 0 | 1 | 28 | 4 |
| tolvaptan | | benzazepine;
benzenedicarboxamide | aquaretic;
vasopressin receptor antagonist | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
phenylureas;
pyridinecarboxamide | angiogenesis inhibitor;
anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
ferroptosis inducer;
tyrosine kinase inhibitor | 2014 | 2022 | 6.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| senicapoc | | | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| erianin | | | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| bortezomib | | amino acid amide;
L-phenylalanine derivative;
pyrazines | antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| ritonavir | | 1,3-thiazoles;
carbamate ester;
carboxamide;
L-valine derivative;
ureas | antiviral drug;
environmental contaminant;
HIV protease inhibitor;
xenobiotic | 2014 | 2014 | 10.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| carboplatin | | | | 2016 | 2022 | 5.1 | low | 4 | 0 | 0 | 0 | 6 | 2 |
| shikonin | | hydroxy-1,4-naphthoquinone | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| isomethyleugenol | | isomethyleugenol | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| s 1033 | | (trifluoromethyl)benzenes;
imidazoles;
pyridines;
pyrimidines;
secondary amino compound;
secondary carboxamide | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| curcumin | | aromatic ether;
beta-diketone;
diarylheptanoid;
enone;
polyphenol | anti-inflammatory agent;
antifungal agent;
antineoplastic agent;
biological pigment;
contraceptive drug;
dye;
EC 1.1.1.205 (IMP dehydrogenase) inhibitor;
EC 1.1.1.21 (aldehyde reductase) inhibitor;
EC 1.1.1.25 (shikimate dehydrogenase) inhibitor;
EC 1.6.5.2 [NAD(P)H dehydrogenase (quinone)] inhibitor;
EC 1.8.1.9 (thioredoxin reductase) inhibitor;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
flavouring agent;
food colouring;
geroprotector;
hepatoprotective agent;
immunomodulator;
iron chelator;
ligand;
lipoxygenase inhibitor;
metabolite;
neuroprotective agent;
nutraceutical;
radical scavenger | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| thiourea | | one-carbon compound;
thioureas;
ureas | antioxidant;
chromophore | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| stattic | | 1-benzothiophenes;
C-nitro compound;
sulfone | antineoplastic agent;
radiosensitizing agent;
STAT3 inhibitor | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rtki cpd | | | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dasatinib | | 1,3-thiazoles;
aminopyrimidine;
monocarboxylic acid amide;
N-(2-hydroxyethyl)piperazine;
N-arylpiperazine;
organochlorine compound;
secondary amino compound;
tertiary amino compound | anticoronaviral agent;
antineoplastic agent;
tyrosine kinase inhibitor | 2016 | 2022 | 5.4 | low | 1 | 0 | 0 | 0 | 6 | 2 |
| zd 6474 | | aromatic ether;
organobromine compound;
organofluorine compound;
piperidines;
quinazolines;
secondary amine | antineoplastic agent;
tyrosine kinase inhibitor | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| alpha-chymotrypsin | | | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| naphthoquinones | | | | 2017 | 2020 | 5.8 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| cinnamamide | | cinnamamide | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| dinoprostone | | prostaglandins E | human metabolite;
mouse metabolite;
oxytocic | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| leukotriene b4 | | dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid | human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| maytansine | | alpha-amino acid ester;
carbamate ester;
epoxide;
maytansinoid;
organic heterotetracyclic compound;
organochlorine compound | antimicrobial agent;
antimitotic;
antineoplastic agent;
plant metabolite;
tubulin modulator | 2013 | 2017 | 9.0 | low | 0 | 0 | 0 | 0 | 6 | 0 |
| sirolimus | | antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol | antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2009 | 2017 | 10.6 | low | 1 | 0 | 0 | 1 | 6 | 0 |
| su 11248 | | monocarboxylic acid amide;
pyrroles | angiogenesis inhibitor;
antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
immunomodulator;
neuroprotective agent;
vascular endothelial growth factor receptor antagonist | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| palbociclib | | aminopyridine;
aromatic ketone;
cyclopentanes;
piperidines;
pyridopyrimidine;
secondary amino compound;
tertiary amino compound | antineoplastic agent;
EC 2.7.11.22 (cyclin-dependent kinase) inhibitor | 2019 | 2020 | 4.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ramipril | | azabicycloalkane;
cyclopentapyrrole;
dicarboxylic acid monoester;
dipeptide;
ethyl ester | bradykinin receptor B2 agonist;
cardioprotective agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
matrix metalloproteinase inhibitor;
prodrug | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sulfur | | chalcogen;
nonmetal atom | macronutrient | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| enalapril | | dicarboxylic acid monoester;
dipeptide | antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cysteine | | cysteinium | fundamental metabolite | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| phytochlorin | | | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| everolimus | | cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol | anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor | 2013 | 2022 | 6.6 | low | 0 | 0 | 0 | 0 | 3 | 2 |
| ekb 569 | | aminoquinoline;
monocarboxylic acid amide;
monochlorobenzenes;
nitrile | protein kinase inhibitor | 2009 | 2017 | 11.0 | low | 0 | 0 | 0 | 1 | 2 | 0 |
| axitinib | | aryl sulfide;
benzamides;
indazoles;
pyridines | antineoplastic agent;
tyrosine kinase inhibitor;
vascular endothelial growth factor receptor antagonist | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bufalin | | 14beta-hydroxy steroid;
3beta-hydroxy steroid | animal metabolite;
anti-inflammatory agent;
antineoplastic agent;
cardiotonic drug | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| s 1743 | | magnesium salt | anti-ulcer drug;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor | 2022 | 2022 | 2.0 | low | 1 | 0 | 0 | 0 | 0 | 1 |
| cp 724714 | | 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide | antineoplastic agent;
apoptosis inducer;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor;
hepatotoxic agent | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pi103 | | aromatic amine;
morpholines;
organic heterotricyclic compound;
phenols;
tertiary amino compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| 2-((aminocarbonyl)amino)-5-(4-fluorophenyl)-3-thiophenecarboxamide | | aromatic amide;
thiophenes | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| hki 272 | | nitrile;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 2009 | 2019 | 9.6 | low | 0 | 0 | 0 | 2 | 23 | 0 |
| sepantronium | | organic cation | | 2017 | 2020 | 5.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| azd 6244 | | benzimidazoles;
bromobenzenes;
hydroxamic acid ester;
monochlorobenzenes;
organofluorine compound;
secondary amino compound | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor | 2021 | 2021 | 3.0 | low | 1 | 0 | 0 | 0 | 0 | 1 |
| volasertib | | | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| regorafenib | | (trifluoromethyl)benzenes;
aromatic ether;
monochlorobenzenes;
monofluorobenzenes;
phenylureas;
pyridinecarboxamide | antineoplastic agent;
hepatotoxic agent;
tyrosine kinase inhibitor | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| erastin | | aromatic ether;
diether;
monochlorobenzenes;
N-acylpiperazine;
N-alkylpiperazine;
quinazolines;
tertiary carboxamide | antineoplastic agent;
ferroptosis inducer;
voltage-dependent anion channel inhibitor | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| mp470 | | N-arylpiperazine | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| nvp-aew541 | | | | 2013 | 2017 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| arq 197 | | indoles | | 2014 | 2021 | 6.5 | low | 0 | 0 | 0 | 0 | 2 | 2 |
| pf 00299804 | | enamide;
monochlorobenzenes;
monofluorobenzenes;
piperidines;
quinazolines;
secondary amino compound;
secondary carboxamide;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2009 | 2022 | 6.9 | medium | 0 | 0 | 0 | 2 | 12 | 6 |
| ridaforolimus | | macrolide lactam | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| carfilzomib | | epoxide;
morpholines;
tetrapeptide | antineoplastic agent;
proteasome inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| sitagliptin phosphate | | | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| crizotinib | | 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | antineoplastic agent;
biomarker;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2013 | 2022 | 6.9 | low | 0 | 0 | 0 | 0 | 26 | 4 |
| trametinib | | acetamides;
aromatic amine;
cyclopropanes;
organofluorine compound;
organoiodine compound;
pyridopyrimidine;
ring assembly | anticoronaviral agent;
antineoplastic agent;
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor;
geroprotector | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| dactolisib | | imidazoquinoline;
nitrile;
quinolines;
ring assembly;
ureas | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
mTOR inhibitor | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mdv 3100 | | (trifluoromethyl)benzenes;
benzamides;
imidazolidinone;
monofluorobenzenes;
nitrile;
thiocarbonyl compound | androgen antagonist;
antineoplastic agent | 2021 | 2022 | 2.5 | low | 0 | 0 | 0 | 0 | 0 | 2 |
| oligonucleotides | | | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| buparlisib | | aminopyridine;
aminopyrimidine;
morpholines;
organofluorine compound | antineoplastic agent;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor | 2020 | 2021 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| icotinib | | | | 2014 | 2023 | 5.4 | low | 0 | 0 | 0 | 0 | 5 | 3 |
| chiniofon | | | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| olaparib | | cyclopropanes;
monofluorobenzenes;
N-acylpiperazine;
phthalazines | antineoplastic agent;
apoptosis inducer;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| mln 8237 | | benzazepine | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| bms 777607 | | aromatic amide | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pci 32765 | | acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2015 | 2021 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| navitoclax | | aryl sulfide;
monochlorobenzenes;
morpholines;
N-sulfonylcarboxamide;
organofluorine compound;
piperazines;
secondary amino compound;
sulfone;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
B-cell lymphoma 2 inhibitor | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| cabozantinib | | aromatic ether;
dicarboxylic acid diamide;
organofluorine compound;
quinolines | antineoplastic agent;
tyrosine kinase inhibitor | 2019 | 2021 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| incb-018424 | | nitrile;
pyrazoles;
pyrrolopyrimidine | antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| poziotinib | | acrylamides;
aromatic ether;
dichlorobenzene;
diether;
monofluorobenzenes;
N-acylpiperidine;
quinazolines;
secondary amino compound;
substituted aniline | antineoplastic agent;
apoptosis inducer;
epidermal growth factor receptor antagonist | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| (5-(2,4-bis((3s)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol | | benzyl alcohols;
morpholines;
pyridopyrimidine;
tertiary amino compound | antineoplastic agent;
apoptosis inducer;
mTOR inhibitor | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| plx4032 | | aromatic ketone;
difluorobenzene;
monochlorobenzenes;
pyrrolopyridine;
sulfonamide | antineoplastic agent;
B-Raf inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| gsk 1363089 | | aromatic ether | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| piperidines | | | | 2015 | 2021 | 5.1 | low | 0 | 0 | 0 | 0 | 5 | 2 |
| interleukin-8 | | | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| thiopental sodium | | organochlorine compound;
piperazines;
pyrimidines | antineoplastic agent;
tyrosine kinase inhibitor | 2013 | 2015 | 9.8 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| apatinib | | | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| alectinib | | aromatic ketone;
morpholines;
nitrile;
organic heterotetracyclic compound;
piperidines | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2018 | 2021 | 4.5 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| encorafenib | | | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| tetracycline | | | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| minocycline | | | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| s 1 (combination) | | | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| byl719 | | proline derivative | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| epidermal growth factor | | | | 2009 | 2022 | 6.4 | low | 0 | 0 | 0 | 1 | 2 | 2 |
| transforming growth factor beta | | | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| rociletinib | | | | 2015 | 2016 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| ceritinib | | aminopyrimidine;
aromatic ether;
organochlorine compound;
piperidines;
secondary amino compound;
sulfone | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2017 | 2021 | 5.7 | low | 0 | 0 | 0 | 0 | 2 | 1 |
| osimertinib | | acrylamides;
aminopyrimidine;
biaryl;
indoles;
monomethoxybenzene;
secondary amino compound;
secondary carboxamide;
substituted aniline;
tertiary amino compound | antineoplastic agent;
epidermal growth factor receptor antagonist | 2015 | 2023 | 4.0 | low | 7 | 0 | 0 | 0 | 48 | 41 |
| pf-06463922 | | aminopyridine;
aromatic ether;
azamacrocycle;
benzamides;
cyclic ether;
monofluorobenzenes;
nitrile;
organic heterotetracyclic compound;
pyrazoles | antineoplastic agent;
EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| imetelstat | | | | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| cyclin d1 | | | | 2019 | 2022 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| transforming growth factor alpha | | | | 2013 | 2021 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| cyclosporine | | | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| acyclovir | | 2-aminopurines;
oxopurine | antimetabolite;
antiviral drug | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| guanine | | 2-aminopurines;
oxopurine;
purine nucleobase | algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite | 2010 | 2015 | 11.1 | low | 4 | 0 | 0 | 1 | 7 | 0 |
| rifampin | | cyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion | angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor | 2014 | 2014 | 10.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| dacarbazine | | dacarbazine | | 2015 | 2021 | 7.0 | low | 2 | 0 | 0 | 0 | 2 | 1 |
| valacyclovir | | L-valyl ester | antiviral drug | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| pemetrexed | | N-acyl-L-glutamic acid;
pyrrolopyrimidine | antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor | 2010 | 2023 | 7.5 | low | 8 | 0 | 0 | 1 | 21 | 3 |
| nintedanib | | | | 2011 | 2018 | 10.0 | low | 4 | 0 | 0 | 0 | 6 | 0 |
| pyrimidinones | | | | 2019 | 2020 | 4.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|
| Ache | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Acneiform Eruptions | 0 | | 2016 | 2021 | 5.2 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| Actinic Keratosis | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Disease | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Kidney Failure | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Kidney Injury | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Liver Injury, Drug-Induced | 0 | | 2015 | 2021 | 7.0 | low | 0 | 0 | 0 | 0 | 5 | 1 |
| Acute Lung Injury | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Myelogenous Leukemia | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Acute Promyelocytic Leukemia | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Adenocarcinoma | 0 | | 2008 | 2023 | 8.1 | low | 15 | 0 | 0 | 1 | 98 | 6 |
| Adenocarcinoma Of Kidney | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Adenocarcinoma of Lung | 0 | | 2012 | 2023 | 6.2 | low | 9 | 0 | 0 | 0 | 86 | 23 |
| Adenocarcinoma, Basal Cell | 0 | | 2008 | 2023 | 8.1 | low | 15 | 0 | 0 | 1 | 98 | 6 |
| Adenocarcinoma, Papillary | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Adverse Drug Event | 0 | | 2016 | 2020 | 5.5 | low | 4 | 0 | 0 | 0 | 13 | 0 |
| Agranulocytosis | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Allergic Acute Coronary Syndrome | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Alopecia | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Alopecia Cicatrisata | 0 | | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Androgen-Independent Prostatic Cancer | 0 | | 2014 | 2022 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 1 |
| Anemia | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Anemia, Fanconi | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Angiogenesis, Pathologic | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 2 |
| Angiogranuloma | 0 | | 2017 | 2019 | 6.0 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Arteriosclerosis, Coronary | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Ascites | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Asthenia | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Astrocytoma, Grade IV | 0 | | 2015 | 2021 | 5.6 | low | 2 | 0 | 0 | 0 | 5 | 2 |
| B-Cell Lymphoma | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Benign Meningeal Neoplasms | 0 | | 2014 | 2020 | 7.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Benign Neoplasms | 0 | | 2008 | 2023 | 8.4 | low | 19 | 0 | 0 | 3 | 41 | 3 |
| Benign Neoplasms, Brain | 0 | | 2015 | 2023 | 5.3 | low | 6 | 0 | 0 | 0 | 30 | 12 |
| Bile Duct Cancer | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Bile Duct Neoplasms | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Biliary Tract Cancer | 0 | | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Biliary Tract Neoplasms | 0 | | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Bladder Cancer | 0 | | 2013 | 2015 | 10.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Blast Crisis | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Blast Phase | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Blood Pressure, Low | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Bone Cancer | 0 | | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Bone Loss, Osteoclastic | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Bone Neoplasms | 0 | | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Brain Neoplasms | 1 | | 2015 | 2023 | 5.3 | low | 6 | 0 | 0 | 0 | 30 | 12 |
| Breast Cancer | 0 | | 2009 | 2022 | 8.1 | low | 10 | 0 | 0 | 1 | 29 | 5 |
| Breast Neoplasms | 1 | | 2009 | 2022 | 8.1 | low | 10 | 0 | 0 | 1 | 29 | 5 |
| Breathlessness | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Bright Disease | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Bronchiolitis Obliterans | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Bronchiolitis, Exudative | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Bullous Dermatoses | 0 | | 2018 | 2020 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cancer of Cecum | 0 | | 2014 | 2014 | 10.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Cervix | 0 | | 2012 | 2017 | 9.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Cancer of Colon | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Endometrium | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Esophagus | 0 | | 2016 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 2 |
| Cancer of Gallbladder | 0 | | 2019 | 2023 | 3.7 | low | 1 | 0 | 0 | 0 | 2 | 1 |
| Cancer of Gastrointestinal Tract | 0 | | 2015 | 2019 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cancer of Head | 0 | | 2013 | 2023 | 6.1 | low | 15 | 0 | 0 | 0 | 28 | 9 |
| Cancer of Kidney | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Cancer of Liver | 0 | | 2012 | 2022 | 6.0 | low | 0 | 0 | 0 | 0 | 5 | 1 |
| Cancer of Lung | 0 | | 2008 | 2023 | 6.0 | medium | 82 | 0 | 0 | 11 | 484 | 174 |
| Cancer of Mouth | 0 | | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Nasopharynx | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Oropharnyx | 0 | | 2015 | 2018 | 7.5 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Cancer of Ovary | 0 | | 2012 | 2023 | 6.3 | low | 0 | 0 | 0 | 0 | 5 | 2 |
| Cancer of Pancreas | 0 | | 2011 | 2023 | 5.9 | low | 3 | 0 | 0 | 0 | 9 | 6 |
| Cancer of Pelvis | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Salivary Gland | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Cancer of Skin | 0 | | 2019 | 2020 | 4.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Cancer of Stomach | 0 | | 2013 | 2023 | 4.3 | low | 1 | 0 | 0 | 0 | 9 | 6 |
| Cancer of the Retina | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Cancer of the Thyroid | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of the Urethra | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cancer of the Urinary Tract | 0 | | 2016 | 2016 | 8.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Cancer of the Uterus | 0 | | 2014 | 2017 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cancer, Second Primary | 0 | | 2014 | 2018 | 8.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Canine Diseases | 0 | | 2021 | 2023 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 2 |
| Carcinogenesis | 0 | | 2014 | 2023 | 5.8 | low | 0 | 0 | 0 | 0 | 7 | 2 |
| Carcinoma | 0 | | 2015 | 2022 | 5.2 | low | 0 | 0 | 0 | 0 | 2 | 2 |
| Carcinoma in Situ | 0 | | 2023 | 2023 | 1.0 | low | 1 | 0 | 0 | 0 | 0 | 1 |
| Carcinoma, Adenosquamous | 0 | | 2009 | 2015 | 12.0 | low | 0 | 0 | 0 | 1 | 1 | 0 |
| Carcinoma, Anaplastic | 0 | | 2015 | 2022 | 5.2 | low | 0 | 0 | 0 | 0 | 2 | 2 |
| Carcinoma, Ductal, Breast | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Carcinoma, Ductal, Pancreatic | 0 | | 2015 | 2023 | 4.6 | low | 1 | 0 | 0 | 0 | 3 | 2 |
| Carcinoma, Epidermoid | 0 | | 2007 | 2023 | 6.3 | low | 19 | 0 | 0 | 1 | 45 | 12 |
| Carcinoma, Hepatocellular | 0 | | 2019 | 2022 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Carcinoma, Intraepithelial | 0 | | 2023 | 2023 | 1.0 | low | 1 | 0 | 0 | 0 | 0 | 1 |
| Carcinoma, Large Cell | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Carcinoma, Lewis Lung | 0 | | 2020 | 2021 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Carcinoma, Non-Small Cell Lung | 0 | | 2008 | 2023 | 5.7 | medium | 66 | 0 | 0 | 8 | 363 | 143 |
| Carcinoma, Non-Small-Cell Lung | 1 | | 2008 | 2023 | 5.7 | medium | 66 | 0 | 0 | 8 | 363 | 143 |
| Carcinoma, Pancreatic Ductal | 0 | | 2015 | 2023 | 4.6 | low | 1 | 0 | 0 | 0 | 3 | 2 |
| Carcinoma, Renal Cell | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Carcinoma, Small Cell Lung | 0 | | 2013 | 2022 | 6.2 | low | 0 | 0 | 0 | 0 | 7 | 1 |
| Carcinoma, Squamous Cell | 1 | | 2007 | 2023 | 6.3 | low | 19 | 0 | 0 | 1 | 45 | 12 |
| Carcinoma, Squamous Cell of Head and Neck | 0 | | 2013 | 2023 | 5.8 | low | 13 | 0 | 0 | 0 | 20 | 10 |
| Carcinomatous Meningitis | 0 | | 2014 | 2022 | 5.9 | low | 1 | 0 | 0 | 0 | 9 | 2 |
| Cardiac Toxicity | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cardiomyopathies | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cardiomyopathies, Primary | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cardiotoxicity | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Cardiovascular Diseases | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cell Transformation, Neoplastic | 0 | | 2013 | 2023 | 7.0 | low | 0 | 0 | 0 | 0 | 8 | 1 |
| Cells, Neoplasm Circulating | 0 | | 2016 | 2020 | 6.0 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Chemical and Drug Induced Liver Injury | 0 | | 2015 | 2021 | 7.0 | low | 0 | 0 | 0 | 0 | 5 | 1 |
| Cholangiocarcinoma | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Cholangiocellular Carcinoma | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Cholera Infantum | 0 | | 2013 | 2021 | 7.7 | low | 2 | 0 | 0 | 0 | 2 | 1 |
| Chordoma | 1 | | 2018 | 2021 | 4.2 | low | 0 | 0 | 0 | 0 | 3 | 2 |
| Choroid Neoplasms | 0 | | 2016 | 2020 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Chromosomal Translocation | 0 | | 2015 | 2017 | 7.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Chronic Kidney Diseases | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Chronic Kidney Failure | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Chronic Lung Injury | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Cirrhosis | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Colonic Neoplasms | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Colorectal Cancer | 0 | | 2011 | 2021 | 7.9 | low | 3 | 0 | 0 | 0 | 12 | 2 |
| Colorectal Neoplasms | 1 | | 2011 | 2021 | 7.9 | low | 3 | 0 | 0 | 0 | 12 | 2 |
| Cornea Injuries | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Corneal Injuries | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Corneal Ulcer | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Coronary Artery Disease | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cough | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Cystadenocarcinoma, Serous | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Cystitis | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Degenerative Diseases, Central Nervous System | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Dermatitis Medicamentosa | 0 | | 2016 | 2021 | 5.8 | low | 0 | 0 | 0 | 0 | 3 | 2 |
| Dermatoses | 0 | | 2013 | 2022 | 5.7 | low | 2 | 0 | 0 | 0 | 4 | 2 |
| Diarrhea | 0 | | 2013 | 2023 | 6.5 | low | 6 | 0 | 0 | 0 | 20 | 3 |
| Diffuse Parenchymal Lung Disease | 0 | | 2015 | 2021 | 6.1 | low | 0 | 0 | 0 | 0 | 9 | 2 |
| Disease Exacerbation | 0 | | 2012 | 2022 | 6.7 | low | 12 | 0 | 0 | 0 | 37 | 4 |
| Disease Models, Animal | 0 | | 2008 | 2022 | 7.4 | low | 0 | 0 | 0 | 2 | 11 | 3 |
| Drug Withdrawal Symptoms | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Drug-Induced Stevens Johnson Syndrome | 0 | | 2016 | 2018 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Drug-Related Side Effects and Adverse Reactions | 0 | | 2016 | 2020 | 5.5 | low | 4 | 0 | 0 | 0 | 13 | 0 |
| Dysplastic Nevus Syndrome, Hereditary | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Dyspnea | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Electrocardiogram QT Prolonged | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Emesis | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Endometrial Neoplasms | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Eosinophilia | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Eosinophilia, Tropical | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| ER-Negative PR-Negative HER2-Negative Breast Cancer | 0 | | 2020 | 2022 | 3.0 | low | 0 | 0 | 0 | 0 | 2 | 2 |
| Esophageal Neoplasms | 1 | | 2016 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 2 |
| Esophageal Squamous Cell Carcinoma | 0 | | 2018 | 2023 | 3.5 | low | 1 | 0 | 0 | 0 | 2 | 2 |
| Esophagitis | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Exanthem | 0 | | 2013 | 2022 | 7.0 | low | 1 | 0 | 0 | 0 | 11 | 2 |
| Exanthema | 0 | | 2013 | 2022 | 7.0 | low | 1 | 0 | 0 | 0 | 11 | 2 |
| Experimental Lung Inflammation | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Experimental Neoplasms | 0 | | 2014 | 2021 | 7.8 | low | 0 | 0 | 0 | 0 | 9 | 1 |
| Eye Cancer, Retinoblastoma | 0 | | 2016 | 2022 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Fanconi Anemia | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Fatigue | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Febrile Neutropenia | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Female Genital Neoplasms | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Fibrosis | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Fibrosis, Inflammatory Perianeurysmal | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Gallbladder Neoplasms | 1 | | 2019 | 2023 | 3.7 | low | 1 | 0 | 0 | 0 | 2 | 1 |
| Gastrointestinal Hemorrhage | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Gastrointestinal Stromal Neoplasm | 0 | | 2012 | 2015 | 10.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Gastrointestinal Stromal Tumors | 0 | | 2012 | 2015 | 10.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Genetic Predisposition | 0 | | 2014 | 2016 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Genital Neoplasms, Female | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Glial Cell Tumors | 0 | | 2014 | 2023 | 4.7 | low | 0 | 0 | 0 | 0 | 1 | 2 |
| Glioblastoma | 1 | | 2015 | 2021 | 5.6 | low | 2 | 0 | 0 | 0 | 5 | 2 |
| Glioma | 1 | | 2014 | 2023 | 4.7 | low | 0 | 0 | 0 | 0 | 1 | 2 |
| Glomerulonephritis | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Granulocytic Leukemia, Chronic | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Hand Dermatoses | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hand Dermatosis | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hand-Schu00FCller-Christian Disease | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Head and Neck Neoplasms | 1 | | 2013 | 2023 | 6.1 | low | 15 | 0 | 0 | 0 | 28 | 9 |
| Hematochezia | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Hematuria | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hepatocellular Carcinoma | 0 | | 2019 | 2022 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Herpes Simplex | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Herpes Simplex Virus Infection | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Histiocytosis, Langerhans-Cell | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hoarseness | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hormone-Dependent Neoplasms | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| HPV Infection | 0 | | 2018 | 2023 | 3.2 | low | 1 | 0 | 0 | 0 | 2 | 2 |
| Hypertrichosis | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hypokalemia | 0 | | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Hyponatremia | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Hypopharyngeal Cancer | 0 | | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Hypopharyngeal Neoplasms | 0 | | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 |
| Hypotension | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Ichthyosis | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Infection, Toxoplasma gondii | 0 | | 2016 | 2020 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Inflammation | 0 | | 2019 | 2022 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Inflammatory Breast Cancer | 0 | | 2015 | 2016 | 8.5 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Inflammatory Breast Neoplasms | 0 | | 2015 | 2016 | 8.5 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Innate Inflammatory Response | 0 | | 2019 | 2022 | 3.5 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Intestinal Perforation | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Invasiveness, Neoplasm | 0 | | 2015 | 2020 | 6.0 | low | 2 | 0 | 0 | 0 | 5 | 0 |
| Itching | 0 | | 2013 | 2016 | 9.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Kahler Disease | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Keratitis, Ulcerative | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Keratosis, Actinic | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Kidney Failure, Chronic | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Kidney Neoplasms | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Lassa Fever | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Lassa Virus Infection | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Lassitude | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Leishmania Infection | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Leishmaniasis | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Leucocythaemia | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Leukemia | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Leukemia, Myelogenous, Chronic, BCR-ABL Positive | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Leukemia, Myeloid, Acute | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Leukemia, Myelomonocytic, Chronic | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Leukemia, Promyelocytic, Acute | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Leukocytopenia | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Leukopenia | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Li-Fraumeni Syndrome | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Liver Diseases | 1 | | 2014 | 2016 | 9.0 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Liver Dysfunction | 0 | | 2014 | 2016 | 9.0 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Liver Neoplasms | 0 | | 2012 | 2022 | 6.0 | low | 0 | 0 | 0 | 0 | 5 | 1 |
| Local Neoplasm Recurrence | 0 | | 2014 | 2023 | 5.9 | low | 10 | 0 | 0 | 0 | 19 | 5 |
| Long QT Syndrome | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Lung Adenocarcinoma | 0 | | 2012 | 2023 | 6.2 | low | 9 | 0 | 0 | 0 | 86 | 23 |
| Lung Diseases, Interstitial | 0 | | 2015 | 2021 | 6.1 | low | 0 | 0 | 0 | 0 | 9 | 2 |
| Lung Injury, Acute | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Lung Neoplasms | 1 | | 2008 | 2023 | 6.0 | medium | 82 | 0 | 0 | 11 | 484 | 174 |
| Lymph Node Metastasis | 0 | | 2012 | 2017 | 9.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Lymphoma, B-Cell | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Malignant Melanoma | 0 | | 2012 | 2022 | 5.8 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| Malignant Mesothelioma | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Melanoma | 0 | | 2012 | 2022 | 5.8 | low | 0 | 0 | 0 | 0 | 3 | 1 |
| Meningeal Carcinomatosis | 0 | | 2014 | 2022 | 5.9 | low | 1 | 0 | 0 | 0 | 9 | 2 |
| Meningeal Neoplasms | 0 | | 2014 | 2020 | 7.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Mesothelioma | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Metastase | 0 | | 2012 | 2022 | 7.4 | low | 19 | 0 | 0 | 0 | 36 | 3 |
| Minimal Disease, Residual | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Mouth Neoplasms | 0 | | 2019 | 2019 | 5.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| MS (Multiple Sclerosis) | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Mucositis | 0 | | 2014 | 2019 | 7.5 | low | 2 | 0 | 0 | 0 | 4 | 0 |
| Mucositis, Oral | 0 | | 2014 | 2018 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Multiple Myeloma | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Multiple Primary Neoplasms | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Multiple Sclerosis | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Myelomonocytic Leukemia, Chronic | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Nasopharyngeal Carcinoma | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Nasopharyngeal Neoplasms | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Nausea | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Neoplasm Metastasis | 1 | | 2012 | 2022 | 7.4 | low | 19 | 0 | 0 | 0 | 36 | 3 |
| Neoplasm Metastasis, Unknown Primary | 0 | | 2020 | 2020 | 4.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Neoplasms | 1 | | 2008 | 2023 | 8.4 | low | 19 | 0 | 0 | 3 | 41 | 3 |
| Neoplasms, Cystic, Mucinous, and Serous | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Neoplasms, Squamous Cell | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Nerve Pain | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Neuralgia | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Neuroblastoma | 0 | | 2017 | 2023 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Neurodegenerative Diseases | 0 | | 2019 | 2019 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Neutropenia | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Nicotine Addiction | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Oropharyngeal Neoplasms | 0 | | 2015 | 2018 | 7.5 | low | 1 | 0 | 0 | 0 | 2 | 0 |
| Osteogenic Sarcoma | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Osteosarcoma | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Ovarian Neoplasms | 0 | | 2012 | 2023 | 6.3 | low | 0 | 0 | 0 | 0 | 5 | 2 |
| Pain | 0 | | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Pancreatic Neoplasms | 1 | | 2011 | 2023 | 5.9 | low | 3 | 0 | 0 | 0 | 9 | 6 |
| Papillomavirus Infections | 0 | | 2018 | 2023 | 3.2 | low | 1 | 0 | 0 | 0 | 2 | 2 |
| Paraneoplastic Syndromes | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Paronychia | 0 | | 2013 | 2019 | 7.3 | low | 0 | 0 | 0 | 0 | 7 | 0 |
| Peritoneal Carcinomatosis | 0 | | 2014 | 2019 | 7.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Peritoneal Neoplasms | 0 | | 2014 | 2019 | 7.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Peritonitis | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Petechiae | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Pneumonia | 0 | | 2017 | 2017 | 7.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Primary Peritonitis | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Prostatic Neoplasms, Castration-Resistant | 0 | | 2014 | 2022 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 1 |
| Pruritus | 0 | | 2013 | 2016 | 9.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Purpura | 0 | | 2021 | 2021 | 3.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Recrudescence | 0 | | 2015 | 2023 | 5.0 | low | 0 | 0 | 0 | 0 | 4 | 1 |
| Renal Insufficiency, Chronic | 0 | | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Response Evaluation Criteria in Solid Tumors | 0 | | 2014 | 2020 | 6.7 | low | 1 | 0 | 0 | 0 | 3 | 0 |
| Retinoblastoma | 0 | | 2016 | 2022 | 5.0 | low | 0 | 0 | 0 | 0 | 1 | 1 |
| Retroperitoneal Fibrosis | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Retroperitoneal Neoplasms | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Rodent Diseases | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Salivary Gland Neoplasms | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Sarcoma | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Sarcoma, Epithelioid | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Sarcopenia | 0 | | 2023 | 2023 | 1.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Scalp Dermatoses | 0 | | 2018 | 2020 | 5.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Sensitivity and Specificity | 0 | | 2014 | 2018 | 7.5 | low | 0 | 0 | 0 | 0 | 4 | 0 |
| Skin Diseases | 0 | | 2013 | 2022 | 5.7 | low | 2 | 0 | 0 | 0 | 4 | 2 |
| Skin Neoplasms | 0 | | 2019 | 2020 | 4.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Small Cell Lung Carcinoma | 1 | | 2013 | 2022 | 6.2 | low | 0 | 0 | 0 | 0 | 7 | 1 |
| Spinal Neoplasms | 0 | | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Squamous Cell Carcinoma of Head and Neck | 0 | | 2013 | 2023 | 5.8 | low | 13 | 0 | 0 | 0 | 20 | 10 |
| Stevens-Johnson Syndrome | 0 | | 2016 | 2018 | 7.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Stomach Neoplasms | 0 | | 2013 | 2023 | 4.3 | low | 1 | 0 | 0 | 0 | 9 | 6 |
| Stomatitis | 0 | | 2014 | 2018 | 8.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Substance Withdrawal Syndrome | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Thrombocytopenia | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Thrombopenia | 0 | | 2015 | 2015 | 9.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Thyroid Cancer, Anaplastic | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Thyroid Carcinoma, Anaplastic | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Thyroid Neoplasms | 0 | | 2018 | 2018 | 6.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Tobacco Use Disorder | 0 | | 2014 | 2014 | 10.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Toxoplasmosis | 0 | | 2016 | 2020 | 6.0 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Triple Negative Breast Neoplasms | 0 | | 2020 | 2022 | 3.0 | low | 0 | 0 | 0 | 0 | 2 | 2 |
| Urethral Neoplasms | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Urinary Bladder Neoplasms | 0 | | 2013 | 2015 | 10.3 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Uterine Cervical Neoplasms | 0 | | 2012 | 2017 | 9.7 | low | 0 | 0 | 0 | 0 | 3 | 0 |
| Uterine Neoplasms | 1 | | 2014 | 2017 | 8.5 | low | 0 | 0 | 0 | 0 | 2 | 0 |
| Uveal Neoplasms | 0 | | 2022 | 2022 | 2.0 | low | 0 | 0 | 0 | 0 | 0 | 1 |
| Viremia | 0 | | 2012 | 2012 | 12.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
| Vomiting | 0 | | 2018 | 2018 | 6.0 | low | 1 | 0 | 0 | 0 | 1 | 0 |
| Xeroderma | 0 | | 2016 | 2016 | 8.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
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Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
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The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
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Successful treatment of Afatinib plus Apatinib using for a lung adenocarcinoma patient with HER-2 V659D mutation: a rare case report.Anti-cancer drugs, , 04-01, Volume: 32, Issue:4, 2021
Long-term response to afatinib in an elderly patient with uncommon epidermal growth factor receptor mutation-positive lung adenocarcinoma.Thoracic cancer, , Volume: 12, Issue:6, 2021
Drug-induced Hypersensitivity Syndrome by EGFR-TKI in a Patient with Lung Cancer.Internal medicine (Tokyo, Japan), , Volume: 60, Issue:3, 2021
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
Drastic antitumor response following administration of afatinib immediately after atezolizumab in a patient with epidermal growth factor receptor tyrosine kinase inhibitor-resistant lung cancer.Thoracic cancer, , Volume: 12, Issue:13, 2021
Afatinib and osimertinib in lung adenocarcinoma harbored EGFR T751_I759delinsS mutation: A case report.Thoracic cancer, , Volume: 12, Issue:24, 2021
Comparing survival and treatment response of patients with acquired T790M mutation second-line osimertinib versus sequential treatment of chemotherapy followed by osimertinib: A real-world study.Thoracic cancer, , Volume: 12, Issue:23, 2021
Successful treatment of an osimertinib-resistant lung adenocarcinoma with an exon 18 EGFR mutation (G719S) with afatinib plus bevacizumab.Investigational new drugs, , Volume: 39, Issue:1, 2021
Lower starting dose of afatinib for the treatment of metastatic lung adenocarcinoma harboring exon 21 and exon 19 mutations.BMC cancer, , May-03, Volume: 21, Issue:1, 2021
Major Clinical Response to Afatinib Monotherapy in Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion Mutation.Clinical lung cancer, , Volume: 22, Issue:1, 2021
Afatinib treatment response in advanced lung adenocarcinomas harboring uncommon mutations.Thoracic cancer, , Volume: 12, Issue:21, 2021
Lung carcinoma with diffuse cystic lesions misdiagnosed as pulmonary langerhans cell histocytosis: a case report.BMC pulmonary medicine, , Feb-04, Volume: 20, Issue:1, 2020
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Afatinib response in a lung adenocarcinoma with novel compound S720F+L861R mutation in EGFR.Lung cancer (Amsterdam, Netherlands), , Volume: 148, 2020
Mutation Variants and Co-Mutations as Genomic Modifiers of Response to Afatinib in HER2-Mutant Lung Adenocarcinoma.The oncologist, , Volume: 25, Issue:3, 2020
[Two cases of EGFR-mutated lung adenocarcinoma treated with bronchial recanalization and first-line therapy with afatinib.]Recenti progressi in medicina, , Volume: 111, Issue:12, 2020
Resolving Resistance to Osimertinib Therapy With Afatinib in an NSCLC Patient With EGFR L718Q Mutation.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Osimertinib induced cardiomyopathy: A case report.Medicine, , Sep-25, Volume: 99, Issue:39, 2020
Retroperitoneal Metastasis, with Marked Fibrosis, of Lung Adenocarcinoma after Afatinib Treatment: An Autopsy Case Report.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 59, Issue:22, 2020
Multiple intraventricular metastases from lung adenocarcinoma with EGFR G719X mutation: a case report.BMC pulmonary medicine, , May-11, Volume: 20, Issue:1, 2020
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib.Journal of visualized experiments : JoVE, , 06-26, Issue:148, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Small Cell Lung Cancer Derived from Adenocarcinoma with Mutant Epidermal Growth Factor Receptor Provides a Signature of Transcriptional Alteration in Tumor Cells.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 58, Issue:22, 2019
Successful treatment of a lung adenocarcinoma patient with a novel EGFR exon 20-ins mutation with afatinib: A case report.Medicine, , Volume: 98, Issue:1, 2019
Afatinib is effective in the treatment of lung adenocarcinoma with uncommon EGFR p.L747P and p.L747S mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Efficacy of afatinib treatment for lung adenocarcinoma harboring exon 18 delE709_T710insD mutation.Japanese journal of clinical oncology, , Aug-01, Volume: 49, Issue:8, 2019
The EGFR Exon 19 Mutant L747-A750>P Exhibits Distinct Sensitivity to Tyrosine Kinase Inhibitors in Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , 11-01, Volume: 25, Issue:21, 2019
Afatinib in patients with metastatic or recurrent HER2-mutant lung cancers: a retrospective international multicentre study.European journal of cancer (Oxford, England : 1990), , Volume: 109, 2019
Identification of a Novel MET Exon 14 Skipping Variant Coexistent with EGFR Mutation in Lung Adenocarcinoma Sensitive to Combined Treatment with Afatinib and Crizotinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:4, 2019
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
Durable Response of Low-Dose Afatinib plus Cetuximab in an Adenocarcinoma Patient with a Novel EGFR Exon 20 Insertion Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:10, 2019
EGFR exon 18 DelE709_T710insD as an Acquired Resistance Mechanism to Afatinib in an Advanced EGFR exon 18 E709H Lung Adenocarcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Efficacy of thoracic radiotherapy in patients with stage IIIB-IV epidermal growth factor receptor-mutant lung adenocarcinomas who received and responded to tyrosine kinase inhibitor treatment.Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, , Volume: 129, Issue:1, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Mechanisms of acquired resistance to afatinib clarified with liquid biopsy.PloS one, , Volume: 13, Issue:12, 2018
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
Efficacy generated by afatinib in a lung adenocarcinoma patient harboring HER2 S310Y mutation.Cancer biology & therapy, , 06-03, Volume: 19, Issue:6, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Treatment effectiveness and tolerability of afatinib at different doses in patients with EGFR-mutated lung adenocarcinoma: How low can we go?European journal of cancer (Oxford, England : 1990), , Volume: 103, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Primary Resistance to Afatinib in a Patient with Lung Adenocarcinoma Harboring Uncommon EGFR Mutations: S768I and V769L.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
Afatinib as first-line treatment for advanced lung adenocarcinoma patients harboring HER2 mutation: A case report and review of the literature.Thoracic cancer, , Volume: 9, Issue:12, 2018
Afatinib restrains K-RAS-driven lung tumorigenesis.Science translational medicine, , 06-20, Volume: 10, Issue:446, 2018
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
Blocking autophagy improves the anti-tumor activity of afatinib in lung adenocarcinoma with activating EGFR mutations in vitro and in vivo.Scientific reports, , 07-04, Volume: 7, Issue:1, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.BMC pharmacology & toxicology, , 12-13, Volume: 18, Issue:1, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
Survival of Lung Adenocarcinoma Patients Predicted from Expression of PD-L1, Galectin-9, and XAGE1 (GAGED2a) on Tumor Cells and Tumor-Infiltrating T Cells.Cancer immunology research, , Volume: 4, Issue:12, 2016
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients.Oncotarget, , Mar-15, Volume: 7, Issue:11, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Long progression-free survival with afatinib in a patient with EGFR-unknown lung adenocarcinoma after erlotinib failure: a case report.Tumori, , Apr-28, Volume: 101, Issue:2, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Reply to F. De Marinis et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Reply to E.R. Haspinger et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.Cancer research, , Nov-15, Volume: 72, Issue:22, 2012
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.American journal of therapeutics, , Volume: 27, Issue:5
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
[Afatinib maintenance therapy does not confer any benefit in the adjuvant treatment of head and neck tumors].Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al], , Volume: 199, Issue:4, 2023
Afatinib maintenance therapy following post-operative radiochemotherapy in head and neck squamous cell carcinoma: Results from the phase III randomised double-blind placebo-controlled study BIB2992ORL (GORTEC 2010-02).European journal of cancer (Oxford, England : 1990), , Volume: 178, 2023
Simultaneously targeting ErbB family kinases and PI3K in HPV-positive head and neck squamous cell carcinoma.Oral oncology, , Volume: 131, 2022
Short-course pembrolizumab and continuous afatinib therapy for recurrent or metastatic head and neck squamous cell carcinoma: a real-world data analysis.BMC cancer, , Nov-28, Volume: 22, Issue:1, 2022
Afatinib and Pembrolizumab for Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (ALPHA Study): A Phase II Study with Biomarker Analysis.Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-14, Volume: 28, Issue:8, 2022
Afatinib induces pro-survival autophagy and increases sensitivity to apoptosis in stem-like HNSCC cells.Cell death & disease, , 07-22, Volume: 12, Issue:8, 2021
Combinatorial approaches targeting the EGFR family and c-Met in SCCHN.Oral oncology, , Volume: 112, 2021
Gefitinib and Afatinib Show Potential Efficacy for Fanconi Anemia-Related Head and Neck Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, , 06-15, Volume: 26, Issue:12, 2020
Rationale for Using Irreversible Epidermal Growth Factor Receptor Inhibitors in Combination with Phosphatidylinositol 3-Kinase Inhibitors for Advanced Head and Neck Squamous Cell Carcinoma.Molecular pharmacology, , Volume: 95, Issue:5, 2019
Afatinib versus methotrexate as second-line treatment in Asian patients with recurrent or metastatic squamous cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 3): an open-label, randomised phase III trialAnnals of oncology : official journal of the European Society for Medical Oncology, , 11-01, Volume: 30, Issue:11, 2019
Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.Oral oncology, , Volume: 97, 2019
Activity and safety of afatinib in a window preoperative EORTC study in patients with squamous cell carcinoma of the head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Predictive biomarkers and EGFR inhibitors in squamous cell carcinoma of head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Melanoma-associated antigen A11 reduces erlotinib and afatinib efficacy in head and neck cancer.Journal of cranio-maxillo-facial surgery : official publication of the European Association for Cranio-Maxillo-Facial Surgery, , Volume: 46, Issue:3, 2018
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Afatinib in squamous cell carcinoma of the head and neck.Expert opinion on pharmacotherapy, , Volume: 17, Issue:9, 2016
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:8, 2016
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Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
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A randomized, phase II study of afatinib versus cetuximab in metastatic or recurrent squamous cell carcinoma of the head and neck.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 25, Issue:9, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
Afatinib in the treatment of head and neck squamous cell carcinoma.Expert opinion on investigational drugs, , Volume: 23, Issue:1, 2014
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.BMC cancer, , Jun-28, Volume: 14, 2014
Afatinib versus placebo as adjuvant therapy after chemoradiation in a double-blind, phase III study (LUX-Head & Neck 2) in patients with primary unresected, clinically intermediate-to-high-risk head and neck cancer: study protocol for a randomized controlTrials, , Nov-29, Volume: 15, 2014
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinib.Molecular cancer therapeutics, , Volume: 12, Issue:8, 2013
A case of crescentic glomerulonephritis induced by afatinib for lung adenocarcinoma.CEN case reports, , Volume: 12, Issue:2, 2023
Long-term response in a patient with adenocarcinoma harboring both common and uncommon EGFR mutations.Investigational new drugs, , Volume: 40, Issue:6, 2022
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
AGAPP: efficacy of first-line cisplatin, 5-fluorouracil with afatinib in inoperable gastric and gastroesophageal junction carcinomas. A Hellenic Cooperative Oncology Group study.Acta oncologica (Stockholm, Sweden), , Volume: 60, Issue:6, 2021
Successful Treatment of Afatinib Reversing Epidermal Growth Factor Receptor Exon19Deletion/G724S Mutation Resistance Guided by Protein-Drug Docking.The oncologist, , Volume: 26, Issue:11, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
Successful Treatment of a Patient with Lung Adenocarcinoma Harboring Compound EGFR Gene Mutations, G719X and S768I, with Afatinib.The Tokai journal of experimental and clinical medicine, , Sep-20, Volume: 45, Issue:3, 2020
Variety Is the Spice of Life, but Maybe Not in Gastroesophageal Adenocarcinomas.Cancer discovery, , Volume: 9, Issue:2, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
Responsiveness to Full-Dose Afatinib in a Patient With Lung Adenocarcinoma Harboring EGFR S768I and V769L Mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:2, 2019
Afatinib treatment for her-2 amplified metastatic colorectal cancer based on patient-derived xenograft models and next generation sequencing.Cancer biology & therapy, , Volume: 20, Issue:4, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Miliary Adenocarcinoma of the Lung Responds to Gefitinib and Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Stevens-Johnson syndrome/toxic epidermal necrolysis overlap in a NSCLC patient treated with afatinib.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG, , Volume: 16, Issue:2, 2018
Therapeutic Potential of Afatinib for Cancers with The oncologist, , Volume: 23, Issue:2, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.Respiratory investigation, , Volume: 55, Issue:1, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
Triplet therapy with afatinib, cetuximab, and bevacizumab induces deep remission in lung cancer cells harboring EGFR T790M in vivo.Molecular oncology, , Volume: 11, Issue:6, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
EGFR L858M/L861Q cis Mutations Confer Selective Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
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Afatinib, an Irreversible EGFR Family Inhibitor, Shows Activity Toward Pancreatic Cancer Cells, Alone and in Combination with Radiotherapy, Independent of KRAS Status.Targeted oncology, , Volume: 11, Issue:3, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
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A Triple Rare E709K and L833V/H835L EGFR Mutation Responsive to an Irreversible Pan-HER Inhibitor: A Case Report of Lung Adenocarcinoma Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:5, 2016
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Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:6, 2016
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
Stevens-Johnson syndrome-like erosive dermatitis possibly related to afatinib.European journal of dermatology : EJD, , Aug-01, Volume: 26, Issue:4, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
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Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
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Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
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Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Is progression-free survival associated with a better health-related quality of life in patients with lung cancer? Evidence from two randomised trials with afatinib.BMJ open, , Oct-31, Volume: 4, Issue:10, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
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[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
A randomised, open-label phase II trial of afatinib versus cetuximab in patients with metastatic colorectal cancer.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:18, 2014
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Afatinib, erlotinib and gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: a review.Onkologie, , Volume: 36, Issue:9, 2013
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Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
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EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.Molecular cancer therapeutics, , Volume: 11, Issue:3, 2012
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Stimulation of Eryptosis by Afatinib.Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, , Volume: 47, Issue:3, 2018
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
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Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
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The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Efficacy of tyrosine kinase inhibitors for the treatment of patients with HER2-positive breast cancer with brain metastases: a systematic review and meta-analysis.ESMO open, , Volume: 7, Issue:3, 2022
Androgen Receptor Activation in Glioblastoma Can Be Achieved by Ligand-Independent Signaling through EGFR-A Potential Therapeutic Target.International journal of molecular sciences, , Oct-11, Volume: 22, Issue:20, 2021
Afatinib and radiotherapy, with or without temozolomide, in patients with newly diagnosed glioblastoma: results of a phase I trial.Journal of neuro-oncology, , Volume: 155, Issue:3, 2021
The NRG3/ERBB4 signaling cascade as a novel therapeutic target for canine glioma.Experimental cell research, , 03-15, Volume: 400, Issue:2, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
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Efficacy of EGFR plus TNF inhibition in a preclinical model of temozolomide-resistant glioblastoma.Neuro-oncology, , 12-17, Volume: 21, Issue:12, 2019
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Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
Afatinib and Temozolomide combination inhibits tumorigenesis by targeting EGFRvIII-cMet signaling in glioblastoma cells.Journal of experimental & clinical cancer research : CR, , Jun-18, Volume: 38, Issue:1, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
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Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
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Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
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First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
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Better treatments needed for breast cancer brain metastases.The Lancet. Oncology, , Volume: 16, Issue:16, 2015
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Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
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Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Phase II Study of Afatinib in Patients With Tumors With Human Epidermal Growth Factor Receptor 2-Activating Mutations: Results From the National Cancer Institute-Molecular Analysis for Therapy Choice ECOG-ACRIN Trial (EAY131) Subprotocol EAY131-B.JCO precision oncology, , Volume: 6, 2022
Neoadjuvant afatinib with paclitaxel for triple-negative breast cancer and the molecular characteristics in responders and non-responders.Journal of the Formosan Medical Association = Taiwan yi zhi, , Volume: 121, Issue:12, 2022
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
HER-targeted tyrosine kinase inhibitors enhance response to trastuzumab and pertuzumab in HER2-positive breast cancer.Investigational new drugs, , Volume: 37, Issue:3, 2019
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Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer.Cancer treatment reviews, , Volume: 67, 2018
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Afatinib in combination with GEMOX chemotherapy as the adjuvant treatment in patients with ErbB pathway mutated, resectable gallbladder cancer: study protocol for a ctDNA-based, multicentre, open-label, randomised, controlled, phase II trial.BMJ open, , 02-28, Volume: 13, Issue:2, 2023
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The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Non-small cell lung cancer with EGFR (L858R and E709X) and CNNB1 mutations responded to afatinib.Thoracic cancer, , Volume: 14, Issue:4, 2023
The second-generation tyrosine kinase inhibitor afatinib inhibits IL-1β secretion via blocking assembly of NLRP3 inflammasome independent of epidermal growth factor receptor signaling in macrophage.Molecular immunology, , Volume: 153, 2023
Older patients with EGFR mutation-positive non-small cell lung cancer treated with afatinib in clinical practice: A subset analysis of the non-interventional GIDEON study.Journal of geriatric oncology, , Volume: 14, Issue:1, 2023
Afatinib triggers a NiFundamental & clinical pharmacology, , Volume: 37, Issue:2, 2023
All EGFR mutations are (not) created equal: focus on uncommon EGFR mutations.Journal of cancer research and clinical oncology, , Volume: 149, Issue:4, 2023
Real-life comparison of afatinib and erlotinib in non-small cell lung cancer with rare EGFR exon 18 and exon 20 mutations: a Turkish Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 149, Issue:2, 2023
Epidermal growth factor receptor tyrosine kinase inhibitors for non-small cell lung cancer harboring uncommon EGFR mutations: Real-world data from Taiwan.Thoracic cancer, , Volume: 14, Issue:1, 2023
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
Treatment outcomes of non-small cell lung cancers treated with EGFR tyrosine kinase inhibitors: a real-world cohort study.Acta oncologica (Stockholm, Sweden), , Volume: 62, Issue:12, 2023
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs.Thoracic cancer, , Volume: 14, Issue:32, 2023
Survival outcomes of east Asian patients with advanced non-small cell lung cancer treated with first-line EGFR tyrosine kinase inhibitors: A network meta-analysis of real-world evidence.Thoracic cancer, , Volume: 14, Issue:32, 2023
A randomized phase II study of afatinib alone or combined with bevacizumab for treating chemo-naïve patients with non-small cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 184, 2023
Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.Neoplasia (New York, N.Y.), , Volume: 43, 2023
Effects of targeted lung cancer drugs on cardiomyocytes studied by atomic force microscopy.Analytical methods : advancing methods and applications, , 08-24, Volume: 15, Issue:33, 2023
Neoadjuvant Afatinib for stage III EGFR-mutant non-small cell lung cancer: a phase II study.Nature communications, , 08-03, Volume: 14, Issue:1, 2023
Comprehensive assessment of pretreatment sarcopenia impacts on patients with EGFR-mutated NSCLC treated with afatinib.Thoracic cancer, , Volume: 14, Issue:25, 2023
Afatinib for the Treatment of NSCLC with Uncommon EGFR Mutations: A Narrative Review.Current oncology (Toronto, Ont.), , 05-28, Volume: 30, Issue:6, 2023
Alternating Therapy With Osimertinib and Afatinib Blockades EGFR Secondary Mutation in EGFR-Mutant Lung Cancer: A Single-Arm Phase II Trial.Clinical lung cancer, , Volume: 24, Issue:6, 2023
Natural Cyclophilin A Inhibitors Suppress the Growth of Cancer Stem Cells in Non-Small Cell Lung Cancer by Disrupting Crosstalk between CypA/CD147 and EGFR.International journal of molecular sciences, , May-29, Volume: 24, Issue:11, 2023
Flashback Foreword: Afatinib for the Treatment of Epidermal Growth Factor Receptor Mutation-Positive Non-Small-Cell Lung Cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , 06-01, Volume: 41, Issue:16, 2023
Final Report on Real-World Effectiveness of Sequential Afatinib and Osimertinib in EGFR-Positive Advanced Non-Small Cell Lung Cancer: Updated Analysis of the RESET Study.Cancer research and treatment, , Volume: 55, Issue:4, 2023
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 181, 2023
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
A real-world study of Afatinib plus ramucirumab in treatment-naïve, EGFR-mutated, non-small cell lung cancer.BMC cancer, , May-08, Volume: 23, Issue:1, 2023
Clinical Outcomes of Afatinib Versus Osimertinib in Patients With Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: A Pooled Analysis.The oncologist, , 06-02, Volume: 28, Issue:6, 2023
The Use of Cytotoxic Drugs as First Line Chemotherapy for EGFR (+) Nonsquamous NSCLC: A Network Meta-Analysis.Disease markers, , Volume: 2023, 2023
Determining plasma and cerebrospinal fluid concentrations of EGFR-TKI in lung cancer patients.Analytical biochemistry, , 05-15, Volume: 669, 2023
Monitoring of T790M in plasma ctDNA of advanced EGFR-mutant NSCLC patients on first- or second-generation tyrosine kinase inhibitors.BMC cancer, , Mar-13, Volume: 23, Issue:1, 2023
NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity.European journal of pharmacology, , May-05, Volume: 946, 2023
Absence of copy number gain of EGFR: A possible predictive marker of long-term response to afatinib.Cancer science, , Volume: 114, Issue:3, 2023
Drug Repurposing against KRAS Mutant G12C: A Machine Learning, Molecular Docking, and Molecular Dynamics Study.International journal of molecular sciences, , Dec-30, Volume: 24, Issue:1, 2022
The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
Advanced Lung Cancer Patients' Use of EGFR Tyrosine Kinase Inhibitors and Overall Survival: Real-World Evidence from Quebec, Canada.Current oncology (Toronto, Ont.), , 10-26, Volume: 29, Issue:11, 2022
Real-world data with afatinib in Spanish patients with treatment-naïve non-small-cell lung cancer harboring exon 19 deletions in epidermal growth factor receptor (Del19 EGFR): Clinical experience of the Galician Lung Cancer Group.Cancer treatment and research communications, , Volume: 33, 2022
Prevalence, Treatment Patterns, and Outcomes of Individuals with Current oncology (Toronto, Ont.), , 09-30, Volume: 29, Issue:10, 2022
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
Application of several machine learning algorithms for the prediction of afatinib treatment outcome in advanced-stage EGFR-mutated non-small-cell lung cancer.Thoracic cancer, , Volume: 13, Issue:23, 2022
Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.Journal of cancer research and therapeutics, , Volume: 18, Issue:5, 2022
Durable response to afatinib rechallenge in a long-term survivor of non-small cell lung cancer harboring EGFR L858R and L747V mutations.Thoracic cancer, , Volume: 13, Issue:22, 2022
Liquid biopsy for detecting epidermal growth factor receptor mutation among patients with non-small cell lung cancer treated with afatinib: a multicenter prospective study.BMC cancer, , Oct-04, Volume: 22, Issue:1, 2022
Afatinib Targeted Therapy Affects the Immune Function and Serum Levels of EGFR and Gastrin-Releasing Peptide Precursor (pro-GRP) in Patients with Non-Small-Cell Lung Cancer (NSCLC).Disease markers, , Volume: 2022, 2022
Early-Onset Pulmonary Events with Combined Brigatinib and Afatinib Treatment of L858/cisT790M/cisC797S NSCLC: A Case Report.The American journal of case reports, , Sep-23, Volume: 23, 2022
Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 155, 2022
A case of multiple primary lung adenocarcinoma with a CD74-NRG1 fusion protein and HER2 mutation benefit from combined target therapy.Thoracic cancer, , Volume: 13, Issue:21, 2022
Efficacy and potential resistance mechanisms of afatinib in advanced non-small cell lung cancer patients with EGFR G719X/L861Q/S768I.Cancer, , 11-01, Volume: 128, Issue:21, 2022
Rare EGFR E709-T710delinsX: Molecular characteristics and superior response to afatinib treatment in NSCLC patients.Lung cancer (Amsterdam, Netherlands), , Volume: 172, 2022
Non-small cell lung cancer harboring EGFR G724S mutation and exon 19 deletion responded to afatinib monotherapy after multiple lines of target therapies.Anti-cancer drugs, , 10-01, Volume: 33, Issue:9, 2022
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Efficacy of Combined Use of Everolimus and Second-Generation Pan-EGRF Inhibitors in International journal of molecular sciences, , Jul-14, Volume: 23, Issue:14, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
The EGFR-STYK1-FGF1 axis sustains functional drug tolerance to EGFR inhibitors in EGFR-mutant non-small cell lung cancer.Cell death & disease, , 07-15, Volume: 13, Issue:7, 2022
Audit of Molecular Mechanisms of Primary and Secondary Resistance to Various Generations of Tyrosine Kinase Inhibitors in Known Epidermal Growth Factor Receptor-Mutant Non-small Cell Lung Cancer Patients in a Tertiary Centre.Clinical oncology (Royal College of Radiologists (Great Britain)), , Volume: 34, Issue:11, 2022
Survival benefits from afatinib compared with gefitinib and erlotinib among patients with common EGFR mutation in first-line setting.Thoracic cancer, , Volume: 13, Issue:14, 2022
Application of afatinib combined with np regimen in the treatment of stage iv non-small cell lung cancer and its effect on patient survival.Pakistan journal of pharmaceutical sciences, , Volume: 35, Issue:2(Special), 2022
Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
The effect of afatinib and radiotherapy on a patient with lung adenocarcinoma with a rare EGFR extracellular domain M277E mutation and high PD-L1 expression.Journal of cancer research and therapeutics, , Volume: 18, Issue:2, 2022
A Phase 2 Trial of Afatinib in Patients with Solid Tumors that Harbor Genomic Aberrations in the HER family: The MOBILITY3 Basket Study.Targeted oncology, , Volume: 17, Issue:3, 2022
Epidermal growth factor receptor tyrosine kinase inhibitors for de novo T790M mutation: A retrospective study of 44 patients.Thoracic cancer, , Volume: 13, Issue:13, 2022
Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L).Lung cancer (Amsterdam, Netherlands), , Volume: 168, 2022
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
Development and validation of a new liquid chromatography-tandem mass spectrometry assay for the simultaneous quantification of afatinib, dacomitinib, osimertinib, and the active metabolites of osimertinib in human serum.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , May-30, Volume: 1199, 2022
Utilization and costs of epidermal growth factor receptor mutation testing and targeted therapy in Medicare patients with metastatic lung adenocarcinoma.BMC health services research, , Apr-09, Volume: 22, Issue:1, 2022
Durable clinical benefit from afatinib in a lung adenocarcinoma patient with acquired EGFR L718V mutation-mediated resistance towards osimertinib: a case report and literature review.Annals of palliative medicine, , Volume: 11, Issue:3, 2022
Real-world Afatinib Outcomes in Advanced Non-small Cell Lung Cancer Harboring Anticancer research, , Volume: 42, Issue:4, 2022
Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Preclinical assessment of combination therapy of EGFR tyrosine kinase inhibitors in a highly heterogeneous tumor model.Oncogene, , Volume: 41, Issue:17, 2022
Metabolic complete tumor response in a patient with The Journal of international medical research, , Volume: 50, Issue:3, 2022
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
First-line Afatinib in Patients With Non-small-cell Lung Cancer With Uncommon EGFR Mutations in South Korea.Anticancer research, , Volume: 42, Issue:3, 2022
Classification and regression tree for estimating predictive markers to detect T790M mutations after acquired resistance to first line EGFR-TKI: HOPE-002.Investigational new drugs, , Volume: 40, Issue:2, 2022
Determination of Afatinib in Human Plasma by 2-Dimensional Liquid Chromatography.Pharmacology, , Volume: 107, Issue:5-6, 2022
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry.Clinica chimica acta; international journal of clinical chemistry, , Feb-15, Volume: 527, 2022
The EPICAL trial, a phase Ib study combining first line afatinib with anti-EGF vaccination in EGFR-mutant metastatic NSCLC.Lung cancer (Amsterdam, Netherlands), , Volume: 164, 2022
Successful erlotinib rechallenge in an EGFR-mutant metastatic non-small cell lung cancer patient with afatinib-induced drug rash with eosinophilia and systemic symptoms: A case report.Thoracic cancer, , Volume: 13, Issue:3, 2022
Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.European journal of cancer (Oxford, England : 1990), , Volume: 160, 2022
Cost-effectiveness analysis of the first-line EGFR-TKIs in patients with advanced EGFR-mutated non-small-cell lung cancer.Expert review of pharmacoeconomics & outcomes research, , Volume: 22, Issue:4, 2022
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.Investigational new drugs, , Volume: 40, Issue:2, 2022
Hypotension from afatinib in epidermal growth factor receptor-mutated non-small cell lung cancer: a case report and literature review.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Elucidation of the inhibitory potential of flavonoids against PKP1 protein in non-small cell lung cancer.Cellular and molecular biology (Noisy-le-Grand, France), , Nov-30, Volume: 68, Issue:11, 2022
Severe EGFR inhibitor-induced acneiform eruption responding to dapsone.Dermatology online journal, , Jul-15, Volume: 27, Issue:7, 2021
Feasibility and effectiveness of afatinib for poor performance status patients with EGFR-mutation-positive non-small-cell lung cancer: a retrospective cohort study.BMC cancer, , Jul-27, Volume: 21, Issue:1, 2021
Sequential treatment of afatinib and osimertinib or other regimens in patients with advanced non-small-cell lung cancer harboring EGFR mutations: Results from a real-world study in South Korea.Cancer medicine, , Volume: 10, Issue:17, 2021
An open-label expanded access program of afatinib in EGFR tyrosine kinase inhibitor-naïve patients with locally advanced or metastatic non-small cell lung cancer harboring EGFR mutations.BMC cancer, , Jul-12, Volume: 21, Issue:1, 2021
Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds.BMC pulmonary medicine, , Jul-01, Volume: 21, Issue:1, 2021
Randomized Phase II Study of 3 Months or 2 Years of Adjuvant Afatinib in Patients With Surgically Resected Stage I-III JCO precision oncology, , Volume: 5, 2021
Survival of chemo-naïve patients with EGFR mutation-positive advanced non-small cell lung cancer after treatment with afatinib and bevacizumab: updates from the Okayama Lung Cancer Study Group Trial 1404.Japanese journal of clinical oncology, , Aug-01, Volume: 51, Issue:8, 2021
Effectiveness and Tolerability of First-Line Afatinib for Advanced EGFR-Mutant Non-Small Cell Lung Cancer in Vietnam.Asian Pacific journal of cancer prevention : APJCP, , May-01, Volume: 22, Issue:5, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Successful treatment of triple EGFR mutation T785A/L861Q/H297_E298 with afatinib.Thoracic cancer, , Volume: 12, Issue:13, 2021
Relationship between Epidermal Growth Factor Receptor Mutations and Adverse Events in Non-Small Cell Lung Cancer Patients treated with Afatinib.The journal of medical investigation : JMI, , Volume: 68, Issue:1.2, 2021
A multicenter cohort study of osimertinib compared with afatinib as first-line treatment for EGFR-mutated non-small-cell lung cancer from practical dataset: CJLSG1903.ESMO open, , Volume: 6, Issue:3, 2021
Response to: Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 12, Issue:11, 2021
Limited effect of afatinib in a non-small cell lung cancer patient harboring an epidermal growth factor receptor K860I missense mutation: A case report.Thoracic cancer, , Volume: 12, Issue:11, 2021
Real-life Effectiveness of Afatinib Anticancer research, , Volume: 41, Issue:4, 2021
Efficacy and dose of afatinib in patients with non-small cell lung cancer after failure of prior gefitinib or erlotinib treatment.Thoracic cancer, , Volume: 12, Issue:10, 2021
Cost-Effectiveness Analysis of Afatinib, Erlotinib, and Gefitinib as First-Line Treatments for EGFR Mutation-Positive Non-Small-Cell Lung Cancer in Ontario, Canada.PharmacoEconomics, , Volume: 39, Issue:5, 2021
Afatinib Exerts Immunomodulatory Effects by Targeting the Pyrimidine Biosynthesis Enzyme CAD.Cancer research, , 06-15, Volume: 81, Issue:12, 2021
Afatinib as First-Line Treatment in Asian Patients with EGFR Mutation-Positive NSCLC: A Narrative Review of Real-World Evidence.Advances in therapy, , Volume: 38, Issue:5, 2021
Afatinib therapy in case of EGFR G724S emergence as resistance mechanism to osimertinib.Anti-cancer drugs, , 08-01, Volume: 32, Issue:7, 2021
Combination therapy with afatinib and bevacizumab in an EGFR-mutated non-small cell lung cancer patient with acquired ERBB2 amplification: A case report.Medicine, , Feb-26, Volume: 100, Issue:8, 2021
A phase II study of first-line afatinib for patients aged ≥75 years with EGFR mutation-positive advanced non-small cell lung cancer: North East Japan Study Group trial NEJ027.BMC cancer, , Mar-01, Volume: 21, Issue:1, 2021
EGFR mutation-guided use of afatinib, erlotinib and gefitinib for advanced non-small-cell lung cancer in Hong Kong - A cost-effectiveness analysis.PloS one, , Volume: 16, Issue:3, 2021
Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).Thoracic cancer, , Volume: 12, Issue:8, 2021
Overall survival in stage IV EGFR mutation‑positive NSCLC: Comparing first‑, second‑ and third‑generation EGFR‑TKIs (Review).International journal of oncology, , Volume: 58, Issue:2, 2021
Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury.International journal of molecular sciences, , Jan-14, Volume: 22, Issue:2, 2021
Clinical utility of liquid biopsy for EGFR driver, T790M mutation and EGFR amplification in plasma in patients with acquired resistance to afatinib.BMC cancer, , Jan-12, Volume: 21, Issue:1, 2021
Real-life comparison of the afatinib and first-generation tyrosine kinase inhibitors in nonsmall cell lung cancer harboring EGFR exon 19 deletion: a Turk Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 147, Issue:7, 2021
Afatinib in EGFR TKI-naïve patients with locally advanced or metastatic EGFR mutation-positive non-small cell lung cancer: Interim analysis of a Phase 3b study.Lung cancer (Amsterdam, Netherlands), , Volume: 152, 2021
Synergy between vinorelbine and afatinib in the inhibition of non-small cell lung cancer progression by EGFR and p53 signaling pathways.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 134, 2021
HER2 amplification as a potential mechanism of acquired resistance to afatinib in an advanced non-small-cell lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 151, 2021
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.The oncologist, , Volume: 26, Issue:4, 2021
Celastrol acts synergistically with afatinib to suppress non-small cell lung cancer cell proliferation by inducing paraptosis.Journal of cellular physiology, , Volume: 236, Issue:6, 2021
Does metformin improve the efficacy of standard epidermal growth factor receptor-tyrosine kinase inhibitor treatment for patients with advanced non-small-cell lung cancer?Interactive cardiovascular and thoracic surgery, , 01-01, Volume: 32, Issue:1, 2021
Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells.International journal of radiation biology, , Volume: 97, Issue:2, 2021
EGFR tyrosine kinase inhibitors in non-small cell lung cancer: treatment paradigm, current evidence, and challenges.Tumori, , Volume: 107, Issue:5, 2021
Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Therapeutic Potential of Afatinib in NRG1 Fusion-Driven Solid Tumors: A Case Series.The oncologist, , Volume: 26, Issue:1, 2021
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , 03-18, Volume: 3, 2021
Afatinib-loaded inhalable PLGA nanoparticles for localized therapy of non-small cell lung cancer (NSCLC)-development and in-vitro efficacy.Drug delivery and translational research, , Volume: 11, Issue:3, 2021
Incremental cost-effectiveness analysis of tyrosine kinase inhibitors in advanced non-small cell lung cancer with mutations of the epidermal growth factor receptor in Colombia.Expert review of pharmacoeconomics & outcomes research, , Volume: 21, Issue:4, 2021
Afatinib for the treatment of advanced non-small-cell lung cancer harboring an epidermal growth factor receptor exon 18 E709_T710delinsD mutation: a case report.Journal of medical case reports, , Nov-22, Volume: 15, Issue:1, 2021
REPORT- Clinical outcomes of using second - versus first-Generation EGFR-tkis for the First-Line treatment of advanced NSCLC patients with EGFR mutations: A meta-analysis.Pakistan journal of pharmaceutical sciences, , Volume: 34, Issue:4, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
An elderly advanced non-small cell lung cancer patient harboring rare epidermal growth factor receptor mutations L861R benefited from afatinib: A case report.Medicine, , Nov-12, Volume: 100, Issue:45, 2021
Sequential afatinib and osimertinib in patients with EGFR mutation-positive NSCLC and acquired T790M: A global non-interventional study (UpSwinG).Lung cancer (Amsterdam, Netherlands), , Volume: 162, 2021
Comparison Between Second- and Third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors as First-line Treatment in Patients With Non-small-cell Lung Cancer: A Retrospective Analysis.Anticancer research, , Volume: 41, Issue:10, 2021
A prospective, phase II trial of monotherapy with low-dose afatinib for patients with EGFR, mutation-positive, non-small cell lung cancer: Thoracic oncology research group 1632.Lung cancer (Amsterdam, Netherlands), , Volume: 161, 2021
Structure-based classification predicts drug response in EGFR-mutant NSCLC.Nature, , Volume: 597, Issue:7878, 2021
New strategy for suppressing the growth of lung cancer cells harboring mutations in the ATP-binding region of EGFR by targeting the molecular motor MYO1D.Clinical and translational medicine, , Volume: 11, Issue:8, 2021
Healthcare resource utilization and costs associated with patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive NSCLC in the United States.Journal of medical economics, , Volume: 23, Issue:1, 2020
Knockdown of lncRNA BLACAT1 reverses the resistance of afatinib to non-small cell lung cancer via modulating STAT3 signalling.Journal of drug targeting, , Volume: 28, Issue:3, 2020
A randomized, multi-center, open-label study to compare the safety and efficacy between afatinib monotherapy and combination therapy of afatinib and HAD-B1 for the locally advanced or metastatic NSCLC patients with EGFR mutations.Medicine, , 12-04, Volume: 99, Issue:49, 2020
New lung-cancer drugs extend survival times.Nature, , Volume: 587, Issue:7834, 2020
Quantitative Structure-Mutation-Activity Relationship Tests (QSMART) model for protein kinase inhibitor response prediction.BMC bioinformatics, , Nov-12, Volume: 21, Issue:1, 2020
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.Medicine, , Oct-23, Volume: 99, Issue:43, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Site-Specific and Targeted Therapy Based on Molecular Profiling by Next-Generation Sequencing for Cancer of Unknown Primary Site: A Nonrandomized Phase 2 Clinical Trial.JAMA oncology, , Dec-01, Volume: 6, Issue:12, 2020
Treatment of Patients With Non-small-cell Lung Cancer With Uncommon Anticancer research, , Volume: 40, Issue:10, 2020
PLCγ1‑dependent invasion and migration of cells expressing NSCLC‑associated EGFR mutants.International journal of oncology, , Volume: 57, Issue:4, 2020
Afatinib for the first-line treatment of Future oncology (London, England), , Volume: 16, Issue:31, 2020
The efficacy of first-line tyrosine kinase inhibitors combined with co-medications in Asian patients with EGFR mutation non-small cell lung cancer.Scientific reports, , 09-11, Volume: 10, Issue:1, 2020
NRG1 fusion-driven tumors: biology, detection, and the therapeutic role of afatinib and other ErbB-targeting agents.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 31, Issue:12, 2020
Molecular profiling of afatinib-resistant non-small cell lung cancer cells in vivo derived from mice.Pharmacological research, , Volume: 161, 2020
Cost-effectiveness analysis of first and second-generation EGFR tyrosine kinase inhibitors as first line of treatment for patients with NSCLC harboring EGFR mutations.BMC cancer, , Sep-01, Volume: 20, Issue:1, 2020
Sequential afatinib and osimertinib in patients with Future oncology (London, England), , Volume: 16, Issue:34, 2020
Photo-induced specific intracellular release EGFR inhibitor from enzyme/ROS-dual sensitive nano-platforms for molecular targeted-photodynamic combinational therapy of non-small cell lung cancer.Journal of materials chemistry. B, , 09-21, Volume: 8, Issue:35, 2020
Role of YES1 amplification in EGFR mutation-positive non-small cell lung cancer: Primary resistance to afatinib in a patient.Thoracic cancer, , Volume: 11, Issue:9, 2020
Afatinib in patients with advanced non-small cell lung cancer harboring HER2 mutations, previously treated with chemotherapy: A phase II trial.Lung cancer (Amsterdam, Netherlands), , Volume: 147, 2020
Simultaneous Single Cell Gene Expression and EGFR Mutation Analysis of Circulating Tumor Cells Reveals Distinct Phenotypes in NSCLC.Advanced biosystems, , Volume: 4, Issue:8, 2020
Durable complete response after afatinib and crizotinib in an advanced non-small cell lung cancer patient with EGFR L861Q mutation and acquired MET amplification: a case report.Annals of palliative medicine, , Volume: 9, Issue:5, 2020
Propensity score analysis of overall survival between first- and second-generation EGFR-TKIs using real-world data.Cancer science, , Volume: 111, Issue:10, 2020
Nationwide Real-world Cohort Study of First-line Tyrosine Kinase Inhibitor Treatment in Epidermal Growth Factor Receptor-mutated Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:6, 2020
Phase II Study of Low-Dose Afatinib Maintenance Treatment Among Patients with EGFR-Mutated Non-Small Cell Lung Cancer: North Japan Lung Cancer Study Group Trial 1601 (NJLCG1601).The oncologist, , Volume: 25, Issue:10, 2020
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 11, Issue:8, 2020
QT interval prolongation related to afatinib treatment in a patient with metastatic non-small-cell lung cancer.Current problems in cancer, , Volume: 44, Issue:6, 2020
Effects of tyrosine kinase inhibitor therapy on skin toxicity and skin-related quality of life in patients with lung cancer: An observational study.Medicine, , Jun-05, Volume: 99, Issue:23, 2020
Afatinib + bevacizumab combination therapy in EGFR-mutant NSCLC patients with osimertinib resistance: Protocol of an open-label, phase II, multicenter, single-arm trial.Thoracic cancer, , Volume: 11, Issue:8, 2020
Clinical Activity of Afatinib in Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Spanish Retrospective Multicenter Study.Clinical lung cancer, , Volume: 21, Issue:5, 2020
Real-world assessment of afatinib for patients with EGFR-positive non-small cell lung cancer.Investigational new drugs, , Volume: 38, Issue:6, 2020
Inflammatory changes in actinic keratoses associated with afatinib therapy.Cutis, , Volume: 105, Issue:3, 2020
Budget impact of sequential treatment with first-line afatinib versus first-line osimertinib in non-small-cell lung cancer patients with common EGFR mutations.The European journal of health economics : HEPAC : health economics in prevention and care, , Volume: 21, Issue:6, 2020
Comparative effectiveness and cost-effectiveness of three first-line EGFR-tyrosine kinase inhibitors: Analysis of real-world data in a tertiary hospital in Taiwan.PloS one, , Volume: 15, Issue:4, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Complete Response to Immunotherapy Plus Chemotherapy After an Unusual Clinical Response to Afatinib and Stereotactic Radiosurgery in a Patient With Metastatic EGFR-Mutant Non-Small-Cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Differential significance of molecular subtypes which were classified into EGFR exon 19 deletion on the first line afatinib monotherapy.BMC cancer, , Feb-06, Volume: 20, Issue:1, 2020
Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol cliniMedicine, , Volume: 99, Issue:4, 2020
Determination of Somatic Mutations and Tumor Mutation Burden in Plasma by CAPP-Seq during Afatinib Treatment in NSCLC Patients Resistance to Osimertinib.Scientific reports, , 01-20, Volume: 10, Issue:1, 2020
Observational Study of Sequential Afatinib and Osimertinib in EGFR Mutation-Positive NSCLC: Patients Treated with a 40-mg Starting Dose of Afatinib.Advances in therapy, , Volume: 37, Issue:2, 2020
Comparing the effectiveness of different EGFR-TKIs in patients with EGFR mutant non-small-cell lung cancer: A retrospective cohort study in Taiwan.International journal of cancer, , 08-15, Volume: 147, Issue:4, 2020
ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib.Cancer, , 03-15, Volume: 126, Issue:6, 2020
Successful treatment of an elderly patient with an uncommon L861Q epidermal growth factor receptor mutation with low-dose afatinib: A case report.Thoracic cancer, , Volume: 11, Issue:2, 2020
Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.Clinical lung cancer, , Volume: 21, Issue:3, 2020
Durable Responses to Afatinib as First-line Therapy for HER2-mutated Metastatic Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Dissecting the mThe pharmacogenomics journal, , Volume: 20, Issue:2, 2020
Clinical Features and Progression Pattern of Acquired T790M-positive Compared With T790M-negative EGFR Mutant Non-small-cell Lung Cancer: Catching Tumor and Clinical Heterogeneity Over Time Through Liquid Biopsy.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
Clinical significance of monitoring EGFR mutation in plasma using multiplexed digital PCR in EGFR mutated patients treated with afatinib (West Japan Oncology Group 8114LTR study).Lung cancer (Amsterdam, Netherlands), , Volume: 131, 2019
Real-world study of afatinib in first-line or re-challenge settings for patients with EGFR mutant non-small cell lung cancer.Medical oncology (Northwood, London, England), , May-14, Volume: 36, Issue:6, 2019
Efficacy and safety of afatinib in a Chinese population with advanced lung adenocarcinoma with sensitive EGFR mutations.Thoracic cancer, , Volume: 10, Issue:6, 2019
Sequencing of therapy following first-line afatinib in patients with EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 132, 2019
Cx32 mediates norepinephrine-promoted EGFR-TKI resistance in a gap junction-independent manner in non-small-cell lung cancer.Journal of cellular physiology, , Volume: 234, Issue:12, 2019
Outcome Differences Between First- and Second-generation EGFR Inhibitors in Advanced EGFR Mutated NSCLC in a Large Population-based Cohort.Clinical lung cancer, , Volume: 20, Issue:5, 2019
First-line afatinib for advanced EGFRm+ NSCLC: Analysis of long-term responders in the LUX-Lung 3, 6, and 7 trials.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Cardiac Toxicity From Afatinib in EGFR-Mutated NSCLC: A Rare But Possible Side Effect.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:7, 2019
Monomer Preference of EGFR Tyrosine Kinase Inhibitors Influences the Synergistic Efficacy of Combination Therapy with Cetuximab.Molecular cancer therapeutics, , Volume: 18, Issue:9, 2019
The dual PI3K/mTOR inhibitor BEZ235 restricts the growth of lung cancer tumors regardless of EGFR status, as a potent accompanist in combined therapeutic regimens.Journal of experimental & clinical cancer research : CR, , Jul-01, Volume: 38, Issue:1, 2019
Which Is Better EGFR-TKI Followed by Osimertinib: Afatinib or Gefitinib/Erlotinib?Anticancer research, , Volume: 39, Issue:7, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
A phase Ib study of the combination of afatinib and ruxolitinib in EGFR mutant NSCLC with progression on EGFR-TKIs.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.Scientific reports, , 12-03, Volume: 9, Issue:1, 2019
Afatinib Overcomes Pemetrexed-Acquired Resistance in Non-Small Cell Lung Cancer Cells Harboring an EML4-ALK Rearrangement.Cells, , 11-28, Volume: 8, Issue:12, 2019
Acquired EGFR L718V Mutation and Loss of T790M-Mediated Resistance to Osimertinib in a Patient With NSCLC Who Responded to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:12, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
Survival outcome of tyrosine kinase inhibitors beyond progression in association to radiotherapy in oligoprogressive EGFR-mutant non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:33, 2019
PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.Advanced healthcare materials, , Volume: 8, Issue:23, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
Development of two different formats of heterogeneous fluorescence immunoassay for bioanalysis of afatinib by employing fluorescence plate reader and KinExA 3200 immunosensor.Scientific reports, , 10-14, Volume: 9, Issue:1, 2019
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib.Seminars in oncology, , Volume: 46, Issue:3, 2019
[Comparison of Effectiveness of Gefitinib, Erlotinib, and Afatinib in Advanced Non-small Cell Lung Cancer Patients with EGFR Mutation Positive in Indonesian Population].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , 09-20, Volume: 22, Issue:9, 2019
Real-world experience of first-line afatinib in patients with EGFR-mutant advanced NSCLC: a multicenter observational study.BMC cancer, , Sep-09, Volume: 19, Issue:1, 2019
A phase II study of low starting dose of afatinib as first-line treatment in patients with EGFR mutation-positive non-small-cell lung cancer (KTORG1402).Lung cancer (Amsterdam, Netherlands), , Volume: 135, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Acquired Resistance of MET-Amplified Non-small Cell Lung Cancer Cells to the MET Inhibitor Capmatinib.Cancer research and treatment, , Volume: 51, Issue:3, 2019
Cost-utility of afatinib and gefitinib as first-line treatment for EGFR-mutated advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:2, 2019
Successful Treatment of a Patient With NSCLC Harboring an EGFR Mutation and a Concomitant Met Exon 14 Skipping Mutation Combining Afatinib and Crizotinib.Clinical lung cancer, , Volume: 20, Issue:1, 2019
Fingolimod augments Pemetrexed killing of non-small cell lung cancer and overcomes resistance to ERBB inhibition.Cancer biology & therapy, , Volume: 20, Issue:5, 2019
Bilateral Ulcerative Keratitis Associated With Afatinib Treatment for Non-Small-cell Lung Carcinoma.Cornea, , Volume: 38, Issue:3, 2019
Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib.Cancer research and treatment, , Volume: 51, Issue:2, 2019
Impact of Exon 19 Deletion Subtypes in EGFR-Mutant Metastatic Non-Small-Cell Lung Cancer Treated With First-Line Tyrosine Kinase Inhibitors.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Potential for afatinib as an optimal treatment for advanced non-small cell lung carcinoma in patients with uncommon EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Dual blockade of EGFR tyrosine kinase using osimertinib and afatinib eradicates EGFR‑mutant Ba/F3 cells.Oncology reports, , Volume: 41, Issue:2, 2019
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Phase 2 Study of Afatinib Alone or Combined With Bevacizumab in Chemonaive Patients With Advanced Non-Small-Cell Lung Cancer Harboring EGFR Mutations: AfaBev-CS Study Protocol.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Prospective exosome-focused translational research for afatinib study of non-small cell lung cancer patients expressing EGFR (EXTRA study).Thoracic cancer, , Volume: 10, Issue:2, 2019
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Palbociclib overcomes afatinib resistance in non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 109, 2019
HER2 exon 20 insertions in non-small-cell lung cancer are sensitive to the irreversible pan-HER receptor tyrosine kinase inhibitor pyrotinib.Annals of oncology : official journal of the European Society for Medical Oncology, , 03-01, Volume: 30, Issue:3, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Impact of afatinib dose modification on safety and effectiveness in patients with EGFR mutation-positive advanced NSCLC: Results from a global real-world study (RealGiDo).Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Efficacy of afatinib or osimertinib plus cetuximab combination therapy for non-small-cell lung cancer with EGFR exon 20 insertion mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Cost-effectiveness of afatinib, gefitinib, erlotinib and pemetrexed-based chemotherapy as first-line treatments for advanced non-small cell lung cancer in China.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Afatinib-loaded immunoliposomes functionalized with cetuximab: A novel strategy targeting the epidermal growth factor receptor for treatment of non-small-cell lung cancer.International journal of pharmaceutics, , Apr-05, Volume: 560, 2019
Re-challenge of afatinib after 1st generation EGFR-TKI failure in patients with previously treated non-small cell lung cancer harboring EGFR mutation.Cancer chemotherapy and pharmacology, , Volume: 83, Issue:5, 2019
First-line afatinib vs gefitinib for patients with EGFR mutation-positive NSCLC (LUX-Lung 7): impact of afatinib dose adjustment and analysis of mode of initial progression for patients who continued treatment beyond progression.Journal of cancer research and clinical oncology, , Volume: 145, Issue:6, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Afatinib in NSCLC With HER2 Mutations: Results of the Prospective, Open-Label Phase II NICHE Trial of European Thoracic Oncology Platform (ETOP).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Secreted Phosphoprotein 1 (SPP1) Contributes to Second-Generation EGFR Tyrosine Kinase Inhibitor Resistance in Non-Small Cell Lung Cancer.Oncology research, , Aug-08, Volume: 27, Issue:8, 2019
From Diagnostic-Therapeutic Pathways to Real-World Data: A Multicenter Prospective Study on Upfront Treatment for The oncologist, , Volume: 24, Issue:6, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
Strategies to overcome acquired resistance to EGFR TKI in the treatment of non-small cell lung cancer.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 21, Issue:10, 2019
Repeat biopsy procedures and T790M rates after afatinib, gefitinib, or erlotinib therapy in patients with lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 130, 2019
Duration of treatment among patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive non-small-cell lung cancer in the USA.Future oncology (London, England), , Volume: 15, Issue:13, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Tyrosine Kinase Inhibitor Gold Nanoconjugates for the Treatment of Non-Small Cell Lung Cancer.ACS applied materials & interfaces, , May-08, Volume: 11, Issue:18, 2019
Clinical analysis of EGFR-positive non-small cell lung cancer patients treated with first-line afatinib: A Nagano Lung Cancer Research Group.Thoracic cancer, , Volume: 10, Issue:5, 2019
An Evolving Algorithm to Select and Sequence Therapies in EGFR Mutation-positive NSCLC: A Strategic Approach.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Afatinib Therapy: Practical Management of Adverse Events With an Oral Agent for Non-Small Cell Lung Cancer Treatment.Clinical journal of oncology nursing, , 10-01, Volume: 22, Issue:5, 2018
Exploration of resistance mechanisms for epidermal growth factor receptor-tyrosine kinase inhibitors based on plasma analysis by digital polymerase chain reaction and next-generation sequencing.Cancer science, , Volume: 109, Issue:12, 2018
[Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Sep-20, Volume: 21, Issue:9, 2018
An observational study of the epidermal growth factor receptor-tyrosine kinase inhibitor resistance mechanism in epidermal growth factor receptor gene mutation-positive non-small cell lung cancer.Medicine, , Volume: 97, Issue:40, 2018
Real Clinical Practice of Using Afatinib Therapy in NSCLC Patients with an Acquired Anticancer research, , Volume: 38, Issue:9, 2018
Ankyrin Repeat Domain 1 Overexpression is Associated with Common Resistance to Afatinib and Osimertinib in EGFR-mutant Lung Cancer.Scientific reports, , 10-05, Volume: 8, Issue:1, 2018
Afatinib plus bevacizumab combination after acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant non-small cell lung cancer: Multicenter, single-arm, phase 2 trial (ABC Study).Cancer, , 10-01, Volume: 124, Issue:19, 2018
Activity of Afatinib in Heavily Pretreated Patients With ERBB2 Mutation-Positive Advanced NSCLC: Findings From a Global Named Patient Use Program.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Sequential treatment with afatinib and osimertinib in patients with EGFR mutation-positive non-small-cell lung cancer: an observational study.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Phase I Study Evaluating the Combination of Afatinib with Carboplatin and Pemetrexed After First-line EGFR-TKIs.Anticancer research, , Volume: 38, Issue:8, 2018
A phase II trial of EGFR-TKI readministration with afatinib in advanced non-small-cell lung cancer harboring a sensitive non-T790M EGFR mutation: Okayama Lung Cancer Study Group trial 1403.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
Overview of the LUX-Lung clinical trial program of afatinib for non-small cell lung cancer.Cancer treatment reviews, , Volume: 69, 2018
Sensitivity of epidermal growth factor receptor with single or double uncommon mutations to afatinib confirmed by a visual assay.Cancer science, , Volume: 109, Issue:11, 2018
Irreversible tyrosine kinase inhibition of epidermal growth factor receptor with afatinib in Current oncology (Toronto, Ont.), , Volume: 25, Issue:Suppl 1, 2018
Relationship between Paronychia and Drug Concentrations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.Oncology, , Volume: 95, Issue:4, 2018
Anti-tumor activity of Shikonin against afatinib resistant non-small cell lung cancer via negative regulation of PI3K/Akt signaling pathway.Bioscience reports, , 12-21, Volume: 38, Issue:6, 2018
Economic analysis of osimertinib in previously untreated EGFR-mutant advanced non-small cell lung cancer in Canada.Lung cancer (Amsterdam, Netherlands), , Volume: 125, 2018
Afatinib with subsequent surgery in stage III NSCLC with EGFR mutation: Lessons learned from two clinical experiences.Tumori, , Volume: 104, Issue:6, 2018
Afatinib in advanced pretreated non-small-cell lung cancer- a Canadian experience.Current oncology (Toronto, Ont.), , Volume: 25, Issue:5, 2018
Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the EGFR inhibitors afatinib, erlotinib and osimertinib, the ALK inhibitor crizotinib and the VEGFR inhibitor nintedanib in human plasma from non-small cell lung cancJournal of pharmaceutical and biomedical analysis, , Sep-05, Volume: 158, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Cost-effectiveness of Osimertinib in the First-Line Treatment of Patients With EGFR-Mutated Advanced Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Budget Impact Analysis of Afatinib for First-Line Treatment of Patients with Metastatic Non-Small Cell Lung Cancer with Epidermal Growth Factor Receptor Exon 19 Deletions or Exon 21 Substitution Mutations in a U.S. Health Plan.Journal of managed care & specialty pharmacy, , Volume: 24, Issue:6, 2018
Influence of afatinib dose on outcomes of advanced EGFR-mutant NSCLC patients with brain metastases.BMC cancer, , Dec-03, Volume: 18, Issue:1, 2018
Effects of secondary EGFR mutations on resistance against upfront osimertinib in cells with EGFR-activating mutations in vitro.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Afatinib in Osimertinib-Resistant EGFR ex19del/T790M/P794L Mutated NSCLC.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:9, 2018
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer.Nature medicine, , Volume: 24, Issue:5, 2018
Afatinib in heavily pretreated advanced NSCLC patients who progressed following prior gefitinib or erlotinib: Compassionate use program in Korea.Lung cancer (Amsterdam, Netherlands), , Volume: 119, 2018
Afatinib as First-line Treatment of Older Patients With EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Subgroup Analyses of the LUX-Lung 3, LUX-Lung 6, and LUX-Lung 7 Trials.Clinical lung cancer, , Volume: 19, Issue:4, 2018
Cost effectiveness analysis of afatinib versus pemetrexed-cisplatin for first-line treatment of locally advanced or metastatic EGFR mutation positive non-small-cell lung cancer from the Singapore healthcare payer's perspective.BMC cancer, , 03-27, Volume: 18, Issue:1, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 118, 2018
Therapeutic Strategies in EGFR Mutant Non-Small Cell Lung Cancer.Current treatment options in oncology, , 09-29, Volume: 19, Issue:11, 2018
Cardiovascular safety of novel non-small cell lung cancer oncotherapy in a patient treated with novel generations of tyrosine kinase inhibitors.Kardiologia polska, , Volume: 76, Issue:3, 2018
Therapeutic strategies for afatinib-resistant lung cancer harboring HER2 alterations.Cancer science, , Volume: 109, Issue:5, 2018
Case sharing of a patient re-challenged with afatinib for EGFR-mutated advanced non-small cell lung cancer.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Best Response According to RECIST During First-line EGFR-TKI Treatment Predicts Survival in EGFR Mutation-positive Non-Small-cell Lung Cancer Patients.Clinical lung cancer, , Volume: 19, Issue:3, 2018
A phase I study of afatinib for patients aged 75 or older with advanced non-small cell lung cancer harboring EGFR mutations.Medical oncology (Northwood, London, England), , Feb-08, Volume: 35, Issue:3, 2018
EGFR-mediated interleukin enhancer-binding factor 3 contributes to formation and survival of cancer stem-like tumorspheres as a therapeutic target against EGFR-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 116, 2018
Improvement of erosive pustular dermatosis of the scalp following discontinuation of chemotherapy with afatinib.European journal of dermatology : EJD, , 04-01, Volume: 28, Issue:2, 2018
Global named patient use program of afatinib in advanced non-small-cell lung carcinoma patients who progressed following prior therapies.Future oncology (London, England), , Volume: 14, Issue:15, 2018
Optimizing outcomes in EGFR mutation-positive NSCLC: which tyrosine kinase inhibitor and when?Future oncology (London, England), , Volume: 14, Issue:11, 2018
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
A phase I trial of afatinib and bevacizumab in chemo-naïve patients with advanced non-small-cell lung cancer harboring EGFR mutations: Okayama Lung Cancer Study Group Trial 1404.Lung cancer (Amsterdam, Netherlands), , Volume: 115, 2018
Utilization of Molecular Testing and Survival Outcomes of Treatment with First- or Second-line Tyrosine Kinase Inhibitors in Advanced Non-small Cell Lung Cancer in a Dutch Population.Anticancer research, , Volume: 38, Issue:1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
Efficacy of Afatinib in a Previously-Treated Patient with Non-Small Cell Lung Cancer Harboring HER2 Mutation: Case Report.Journal of Korean medical science, , Jan-01, Volume: 33, Issue:1, 2018
Does EGFR Mutation Type Influence Patient-Reported Outcomes in Patients with Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer? Analysis of Two Large, Phase III Studies Comparing Afatinib with Chemotherapy (LUX-Lung 3 and LUX-Lung 6).The patient, , Volume: 11, Issue:1, 2018
Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Appendix 7: Metastatic non-small-cell lung cancer (1): MCBS eUpdate published online 28 June 2017 (www.esmo.org/Guidelines/Lung-and-Chest-Tumours).Annals of oncology : official journal of the European Society for Medical Oncology, , Jul-01, Volume: 28, Issue:suppl_4, 2017
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.Anticancer research, , Volume: 37, Issue:9, 2017
Overall survival in EGFR mutated non-small-cell lung cancer patients treated with afatinib after EGFR TKI and resistant mechanisms upon disease progression.PloS one, , Volume: 12, Issue:8, 2017
Cost-Effectiveness Analysis of Afatinib versus Gefitinib for First-Line Treatment of Advanced EGFR-Mutated Advanced Non-Small Cell Lung Cancers.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:10, 2017
Cerebrospinal Fluid Penetration Rate and Efficacy of Afatinib in Patients with EGFR Mutation-positive Non-small Cell Lung Cancer with Leptomeningeal Carcinomatosis: A Multicenter Prospective Study.Anticancer research, , Volume: 37, Issue:8, 2017
Significance of neutrophil-to-lymphocyte ratio in Western advanced EGFR-mutated non-small cell lung cancer receiving a targeted therapy.Tumori, , Sep-18, Volume: 103, Issue:5, 2017
Case series on the association between blood levels and side effects of afatinib maleate.Cancer chemotherapy and pharmacology, , Volume: 80, Issue:3, 2017
Treatment in EGFR-mutated non-small cell lung cancer: how to block the receptor and overcome resistance mechanisms.Tumori, , Jul-31, Volume: 103, Issue:4, 2017
The Effect of Afatinib Treatment in Non-small Cell Lung Cancer Cells.Anticancer research, , Volume: 37, Issue:7, 2017
Update on afatinib-based combination regimens for the treatment of EGFR mutation-positive non-small-cell lung cancer.Future oncology (London, England), , Volume: 13, Issue:21, 2017
Matrine increases the inhibitory effects of afatinib on H1975 cells via the IL‑6/JAK1/STAT3 signaling pathway.Molecular medicine reports, , Volume: 16, Issue:3, 2017
HER2 regulates cancer stem-like cell phenotype in ALK translocated NSCLC.International journal of oncology, , Volume: 51, Issue:2, 2017
A phase Ib trial of continuous once-daily oral afatinib plus sirolimus in patients with epidermal growth factor receptor mutation-positive non-small cell lung cancer and/or disease progression following prior erlotinib or gefitinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Association Between EGFR T790M Status and Progression Patterns During Initial EGFR-TKI Treatment in Patients Harboring EGFR Mutation.Clinical lung cancer, , Volume: 18, Issue:6, 2017
Purpuric Drug Eruptions Caused by Epidermal Growth Factor Receptor Inhibitors for Non-Small Cell Lung Cancer: A Clinicopathologic Study of 32 Cases.JAMA dermatology, , 09-01, Volume: 153, Issue:9, 2017
Activation of signal transducer and activator of transcription 3 (STAT3) signaling in EGFR mutant non-small-cell lung cancer (NSCLC).Oncotarget, , Jul-18, Volume: 8, Issue:29, 2017
Therapeutic Efficacy Comparison of 5 Major EGFR-TKIs in Advanced EGFR-positive Non-Small-cell Lung Cancer: A Network Meta-analysis Based on Head-to-Head Trials.Clinical lung cancer, , Volume: 18, Issue:5, 2017
Recent Management of Patients with Advanced Epidermal Growth Factor Receptor Mutation Non-small Cell Lung Cancer: Role of Afatinib and Lesson Learned for Developing Countries.Acta medica Indonesiana, , Volume: 49, Issue:1, 2017
Afatinib versus gefitinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: overall survival data from the phase IIb LUX-Lung 7 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , 02-01, Volume: 28, Issue:2, 2017
Efficacy of continuous EGFR-inhibition and role of Hedgehog in EGFR acquired resistance in human lung cancer cells with activating mutation of EGFR.Oncotarget, , Apr-04, Volume: 8, Issue:14, 2017
Treatment Paradigms for Advanced Non-Small Cell Lung Cancer at Academic Medical Centers: Involvement in Clinical Trial Endpoint Design.The oncologist, , Volume: 22, Issue:6, 2017
Prognostic value of early response assessment using (18F)FDG-PET in patients with advanced non-small cell lung cancer treated with tyrosine-kinase inhibitors.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 65, Issue:5, 2017
Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 23, Issue:3, 2017
Phase II Study of the EGFR-TKI Rechallenge With Afatinib in Patients With Advanced NSCLC Harboring Sensitive EGFR Mutation Without T790M: Okayama Lung Cancer Study Group Trial OLCSG 1403.Clinical lung cancer, , Volume: 18, Issue:2, 2017
Variations in EGFR ctDNA Correlates to the Clinical Efficacy of Afatinib in Non Small Cell Lung Cancer with Acquired Resistance.Pathology oncology research : POR, , Volume: 23, Issue:2, 2017
The European Society for Medical Oncology Magnitude of Clinical Benefit Scale (ESMO-MCBS) applied to pivotal phase III randomized-controlled trials of tyrosine kinase inhibitors in first-line for advanced non-small cell lung cancer with activating epidermExpert review of pharmacoeconomics & outcomes research, , Volume: 17, Issue:1, 2017
Advanced non-small cell lung cancer (NSCLC) with activating EGFR mutations: first-line treatment with afatinib and other EGFR TKIs.Expert review of anticancer therapy, , Volume: 17, Issue:2, 2017
Successful afatinib treatment of advanced non-small-cell lung cancer patients undergoing hemodialysis.Cancer chemotherapy and pharmacology, , Volume: 79, Issue:1, 2017
HER2 Transmembrane Domain (TMD) Mutations (V659/G660) That Stabilize Homo- and Heterodimerization Are Rare Oncogenic Drivers in Lung Adenocarcinoma That Respond to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:3, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
Rapid Acquisition of T790M Mutation after Treatment with Afatinib in an NSCLC Patient Harboring EGFR Exon 20 S768I Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:1, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
Risk of Treatment-Related Toxicities from EGFR Tyrosine Kinase Inhibitors: A Meta-analysis of Clinical Trials of Gefitinib, Erlotinib, and Afatinib in Advanced EGFR-Mutated Non-Small Cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Clinical Efficacy of Afatinib Treatment for a Patient with Leptomeningeal Carcinomatosis.Chemotherapy, , Volume: 62, Issue:3, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
Randomized Phase II Study of Afatinib Plus Simvastatin Versus Afatinib Alone in Previously Treated Patients with Advanced Nonadenocarcinomatous Non-small Cell Lung Cancer.Cancer research and treatment, , Volume: 49, Issue:4, 2017
Novel EGFR Exon 18 (G721R) Mutation in a Patient with Non-Small Cell Lung Carcinoma with Lack of Response to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
Novel EGFR Inhibitors in Non-small Cell Lung Cancer: Current Status of Afatinib.Current oncology reports, , Volume: 19, Issue:1, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
[Precision first-line therapy for advanced non-small-cell lung cancer patients harboring EGFR mutation].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Feb-23, Volume: 39, Issue:2, 2017
Chronic myelomonocytic leukemia blast crisis in a patient with advanced non-small cell lung cancer treated with EGFR tyrosine kinase inhibitors.Respiratory investigation, , Volume: 55, Issue:2, 2017
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.Clinical drug investigation, , Volume: 37, Issue:6, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.Science translational medicine, , Nov-08, Volume: 9, Issue:415, 2017
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
A Phase Ib/II Study of Afatinib in Combination with Nimotuzumab in Non-Small Cell Lung Cancer Patients with Acquired Resistance to Gefitinib or Erlotinib.Clinical cancer research : an official journal of the American Association for Cancer Research, , 05-01, Volume: 22, Issue:9, 2016
Afatinib and chemotherapy in non-small-cell lung cancer.The Lancet. Oncology, , Volume: 17, Issue:2, 2016
Epidermal growth factor receptor tyrosine kinase inhibitors in previously treated advanced non-small-cell lung cancer with wild-type EGFR.Expert opinion on pharmacotherapy, , Volume: 17, Issue:2, 2016
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1, 2016
First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
Resistance mechanisms after tyrosine kinase inhibitors afatinib and crizotinib in non-small cell lung cancer, a review of the literature.Critical reviews in oncology/hematology, , Volume: 100, 2016
therascreen® EGFR RGQ PCR Kit: A Companion Diagnostic for Afatinib and Gefitinib in Non-Small Cell Lung Cancer.Molecular diagnosis & therapy, , Volume: 20, Issue:2, 2016
Efficacy and safety of afatinib in Chinese patients with EGFR-mutated metastatic non-small-cell lung cancer (NSCLC) previously responsive to first-generation tyrosine-kinase inhibitors (TKI) and chemotherapy: comparison with historical cohort using erlotiBMC cancer, , Feb-24, Volume: 16, 2016
Afatinib in the first-line treatment of epidermal-growth-factor-receptor mutation-positive non-small cell lung cancer: a review of the clinical evidence.Therapeutic advances in respiratory disease, , Volume: 10, Issue:3, 2016
Selectivity profile of afatinib for EGFR-mutated non-small-cell lung cancer.Molecular bioSystems, , 04-26, Volume: 12, Issue:5, 2016
Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience.Cancer chemotherapy and pharmacology, , Volume: 77, Issue:5, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial.The Lancet. Oncology, , Volume: 17, Issue:5, 2016
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , May-25, Issue:5, 2016
[Not Available].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Current status of EGFR/ErbB inhibitors in non-small cell lung carcinoma].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Mechanism of action and preclinical development of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib as first-line therapy in mutation-positive EGFR. Results by type of mutation].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Evidence on afatinib in patients progressing on a first-line treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20, 2016
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
Non-small Cell Lung Cancer in South Wales: Are Exon 19 Deletions and L858R Different?Anticancer research, , Volume: 36, Issue:8, 2016
Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:11, 2016
The safety of afatinib for the treatment of non-small cell lung cancer.Expert opinion on drug safety, , Volume: 15, Issue:11, 2016
Case report: Durable response to afatinib in a patient with lung cancer harboring two uncommon mutations of EGFR and a KRAS mutation.Lung cancer (Amsterdam, Netherlands), , Volume: 101, 2016
Tyrosine kinase inhibitors for epidermal growth factor receptor gene mutation-positive non-small cell lung cancers: an update for recent advances in therapeutics.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 22, Issue:3, 2016
Afatinib: A Review in Advanced Non-Small Cell Lung Cancer.Targeted oncology, , Volume: 11, Issue:6, 2016
Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells.Molecular carcinogenesis, , Volume: 55, Issue:5, 2016
Clinical analysis of patients treated with afatinib for advanced non-small cell lung cancer: A Nagano Lung Cancer Research Group observational study.Respiratory investigation, , Volume: 54, Issue:6, 2016
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors.Critical reviews in oncology/hematology, , Volume: 97, 2016
[The efficacy of TKIs in treatment of human primary small cell lung cancer xenograft model in vivo].Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology, , Jun-08, Volume: 32, Issue:6, 2016
Functionalized gold nanoparticles improve afatinib delivery into cancer cells.Expert opinion on drug delivery, , Volume: 13, Issue:1, 2016
Detection of T790M, the Acquired Resistance EGFR Mutation, by Tumor Biopsy versus Noninvasive Blood-Based Analyses.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-01, Volume: 22, Issue:5, 2016
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer.Biomedical chromatography : BMC, , Volume: 30, Issue:7, 2016
Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations.Cancer science, , Volume: 107, Issue:1, 2016
Risk of elevated transaminases in non-small cell lung cancer (NSCLC) patients treated with erlotinib, gefitinib and afatinib: a meta-analysis.Expert review of respiratory medicine, , Volume: 10, Issue:2, 2016
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with erlotinib: a case report.Anti-cancer drugs, , Volume: 27, Issue:3, 2016
Different EGFR Gene Mutations in Exon 18, 19 and 21 as Prognostic and Predictive Markers in NSCLC: A Single Institution Analysis.Molecular diagnosis & therapy, , Volume: 20, Issue:1, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Afatinib beyond progression in patients with non-small-cell lung cancer following chemotherapy, erlotinib/gefitinib and afatinib: phase III randomized LUX-Lung 5 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:3, 2016
Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer.JAMA dermatology, , Volume: 152, Issue:3, 2016
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
E-Cadherin and EpCAM expression by NSCLC tumour cells associate with normal fibroblast activation through a pathway initiated by integrin αvβ6 and maintained through TGFβ signalling.Oncogene, , Feb-05, Volume: 34, Issue:6, 2015
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Afatinib resistance in non-small cell lung cancer involves the PI3K/AKT and MAPK/ERK signalling pathways and epithelial-to-mesenchymal transition.Targeted oncology, , Volume: 10, Issue:3, 2015
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.Expert opinion on drug safety, , Volume: 14, Issue:1, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in EGFR FISH-positive non-small-cell lung cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:4, 2015
Afatinib induces apoptosis in NSCLC without EGFR mutation through Elk-1-mediated suppression of CIP2A.Oncotarget, , Feb-10, Volume: 6, Issue:4, 2015
Common EGFR-mutated subgroups (Del19/L858R) in advanced non-small-cell lung cancer: chasing better outcomes with tyrosine kinase inhibitors.Future oncology (London, England), , Volume: 11, Issue:8, 2015
CD133-Positive Cells from Non-Small Cell Lung Cancer Show Distinct Sensitivity to Cisplatin and Afatinib.Archivum immunologiae et therapiae experimentalis, , Volume: 63, Issue:3, 2015
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Afatinib increases sensitivity to radiation in non-small cell lung cancer cells with acquired EGFR T790M mutation.Oncotarget, , Mar-20, Volume: 6, Issue:8, 2015
[Pharmacological and clinical profile of afatinib (Giotrif®)].Nihon yakurigaku zasshi. Folia pharmacologica Japonica, , Volume: 145, Issue:2, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.The oncologist, , Volume: 20, Issue:4, 2015
Risk of fatal pulmonary events in patients with advanced non-small-cell lung cancer treated with EGF receptor tyrosine kinase inhibitors: a comparative meta-analysis.Future oncology (London, England), , Volume: 11, Issue:7, 2015
Overcoming Resistance Without the Risk of Reaction: Use of Afatinib and Panitumumab in Two Cases of Epidermal Growth Factor Receptor--Mutated Non--Small-Cell Lung Cancer With T790M Mutations.Clinical lung cancer, , Volume: 16, Issue:5, 2015
Afatinib is especially effective against non-small cell lung cancer carrying an EGFR exon 19 deletion.Anticancer research, , Volume: 35, Issue:4, 2015
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
Symptom and Quality of Life Improvement in LUX-Lung 6: An Open-Label Phase III Study of Afatinib Versus Cisplatin/Gemcitabine in Asian Patients With EGFR Mutation-Positive Advanced Non-small-cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:6, 2015
[Hange-Shashin-to for preventing diarrhea during afatinib therapy].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:5, 2015
Afatinib (Gilotrif) for advanced non-small cell lung cancer.The Medical letter on drugs and therapeutics, , May-25, Volume: 57, Issue:1469, 2015
Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6.The Lancet. Oncology, , Volume: 16, Issue:7, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
[Is chemotherapy still an option in oncogene-addicted non-small cell lung cancer? No].Bulletin du cancer, , Volume: 102, Issue:6 Suppl 1, 2015
Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy, , Volume: 29, Issue:3, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.The oncologist, , Volume: 20, Issue:8, 2015
Acquisition of cancer stem cell-like properties in non-small cell lung cancer with acquired resistance to afatinib.Cancer science, , Volume: 106, Issue:10, 2015
Cumulative meta-analysis of epidermal growth factor receptor-tyrosine kinase inhibitors as first-line therapy in metastatic non-small-cell lung cancer.Anti-cancer drugs, , Volume: 26, Issue:9, 2015
Afatinib: a second-generation EGF receptor and ErbB tyrosine kinase inhibitor for the treatment of advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 11, Issue:18, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
Managing acquired resistance in EGFR-mutated non-small cell lung cancer.Clinical advances in hematology & oncology : H&O, , Volume: 13, Issue:8, 2015
Afatinib in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations Pretreated With Reversible EGFR Inhibitors.The oncologist, , Volume: 20, Issue:10, 2015
Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.The Lancet. Oncology, , Volume: 16, Issue:9, 2015
Cost-Effectiveness and Value of Information of Erlotinib, Afatinib, and Cisplatin-Pemetrexed for First-Line Treatment of Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer in the United States.Value in health : the journal of the International Society for Pharmacoeconomics and Outcomes Research, , Volume: 18, Issue:6, 2015
The pan-HER family tyrosine kinase inhibitor afatinib overcomes HER3 ligand heregulin-mediated resistance to EGFR inhibitors in non-small cell lung cancer.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Current and Emerging Options in the Management of EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Considerations in the Elderly.Drugs & aging, , Volume: 32, Issue:11, 2015
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.British journal of cancer, , Nov-17, Volume: 113, Issue:10, 2015
[Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis].Voprosy onkologii, , Volume: 61, Issue:4, 2015
Dual ALK and EGFR inhibition targets a mechanism of acquired resistance to the tyrosine kinase inhibitor crizotinib in ALK rearranged lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 83, Issue:1, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
The current state of molecularly targeted drugs targeting HGF/Met.Japanese journal of clinical oncology, , Volume: 44, Issue:1, 2014
Afatinib: a review of its use in the treatment of advanced non-small cell lung cancer.Drugs, , Volume: 74, Issue:2, 2014
Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib for lung cancer: let there be light?The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Subsequent treatment choices for patients with acquired resistance to EGFR-TKIs in non-small cell lung cancer: restore after a drug holiday or switch to another EGFR-TKI?Asian Pacific journal of cancer prevention : APJCP, , Volume: 15, Issue:1, 2014
Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations.PloS one, , Volume: 9, Issue:2, 2014
Systemic treatment in EGFR-ALK NSCLC patients: second line therapy and beyond.Expert review of anticancer therapy, , Volume: 14, Issue:7, 2014
Afatinib for the treatment of advanced non-small-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 15, Issue:6, 2014
Afatinib use in non-small cell lung cancer previously sensitive to epidermal growth factor receptor inhibitors: the United Kingdom Named Patient Programme.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:10, 2014
LUX-Lung 3: redundancy, toxicity or a major step forward? Afatinib as front-line therapy for patients with metastatic EGFR-mutated lung cancer.Future oncology (London, England), , Volume: 10, Issue:4, 2014
Meta-analysis of first-line therapies in advanced non-small-cell lung cancer harboring EGFR-activating mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 9, Issue:6, 2014
Next generation tyrosine kinase inhibitor (TKI): afatinib.Recent patents on anti-cancer drug discovery, , Volume: 9, Issue:3, 2014
Afatinib with concurrent radiotherapy in a patient with metastatic non-small cell lung cancer.Oncology research and treatment, , Volume: 37, Issue:5, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Phase II study of Afatinib as third-line treatment for patients in Korea with stage IIIB/IV non-small cell lung cancer harboring wild-type EGFR.The oncologist, , Volume: 19, Issue:7, 2014
[Afatinib (BIBW 2992)].Revue de pneumologie clinique, , Volume: 70, Issue:5, 2014
Gefitinib and afatinib treatment in an advanced non-small cell lung cancer (NSCLC) patient undergoing hemodialysis.Anticancer research, , Volume: 34, Issue:6, 2014
Afatinib in the treatment of EGFR mutation-positive NSCLC--a network meta-analysis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:2, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
[A new perspective in the treatment of non-small-cell lung cancer (NSCLC). Role of afatinib: An oral and irreversible ErbB family blocker].Bulletin du cancer, , Volume: 101, Issue:6, 2014
FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor.Oncotarget, , Aug-15, Volume: 5, Issue:15, 2014
β-catenin contributes to lung tumor development induced by EGFR mutations.Cancer research, , Oct-15, Volume: 74, Issue:20, 2014
Patients with exon 19 deletion were associated with longer progression-free survival compared to those with L858R mutation after first-line EGFR-TKIs for advanced non-small cell lung cancer: a meta-analysis.PloS one, , Volume: 9, Issue:9, 2014
Experience with afatinib in patients with non-small cell lung cancer progressing after clinical benefit from gefitinib and erlotinib.The oncologist, , Volume: 19, Issue:10, 2014
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors.Clinical lung cancer, , Volume: 15, Issue:6, 2014
Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, , Volume: 47, Issue:11, 2014
Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22, 2014
New therapy targets resistant non-small-cell lung cancers.Journal of the National Cancer Institute, , Volume: 106, Issue:11, 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Afatinib and lung cancer.Expert review of anticancer therapy, , Volume: 14, Issue:12, 2014
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Synergistic effect of afatinib with su11274 in non-small cell lung cancer cells resistant to gefitinib or erlotinib.PloS one, , Volume: 8, Issue:3, 2013
Impact of EGFR inhibitor in non-small cell lung cancer on progression-free and overall survival: a meta-analysis.Journal of the National Cancer Institute, , May-01, Volume: 105, Issue:9, 2013
Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
Clinical perspective of afatinib in non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 81, Issue:2, 2013
Glycolysis inhibition sensitizes non-small cell lung cancer with T790M mutation to irreversible EGFR inhibitors via translational suppression of Mcl-1 by AMPK activation.Molecular cancer therapeutics, , Volume: 12, Issue:10, 2013
New kinase inhibitor approved for metastatic lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Aug-15, Volume: 70, Issue:16, 2013
Targeted therapies: Afatinib--new therapy option for EGFR-mutant lung cancer.Nature reviews. Clinical oncology, , Volume: 10, Issue:10, 2013
Afatinib: first global approval.Drugs, , Volume: 73, Issue:13, 2013
Afatinib for the treatment of patients with EGFR-positive non-small cell lung cancer.Drugs of today (Barcelona, Spain : 1998), , Volume: 49, Issue:9, 2013
[Development and biochemical characterization of EGFR/c-Met dual inhibitors].Acta pharmaceutica Hungarica, , Volume: 83, Issue:4, 2013
An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 15, Issue:5, 2013
Symptom and quality of life benefit of afatinib in advanced non-small-cell lung cancer patients previously treated with erlotinib or gefitinib: results of a randomized phase IIb/III trial (LUX-Lung 1).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 8, Issue:2, 2013
Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.Biochemical and biophysical research communications, , Feb-15, Volume: 431, Issue:3, 2013
Disseminated herpes simplex virus infection following epidermal growth factor tyrosine kinase inhibitor therapy for non-small-cell lung carcinoma.Internal medicine journal, , Volume: 42, Issue:11, 2012
Epidermal growth factor receptor (EGFR) inhibitors and derived treatments.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 23 Suppl 10, 2012
Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation.Molecular cancer therapeutics, , Volume: 11, Issue:10, 2012
Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4).Cancer chemotherapy and pharmacology, , Volume: 69, Issue:4, 2012
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.Molecular cancer therapeutics, , Volume: 11, Issue:3, 2012
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence.Critical reviews in oncology/hematology, , Volume: 83, Issue:3, 2012
Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab.BMC medicine, , Mar-21, Volume: 10, 2012
BIBW 2992 in non-small cell lung cancer.Expert opinion on investigational drugs, , Volume: 20, Issue:3, 2011
The search for improved systemic therapy of non-small cell lung cancer--what are today's options?Lung cancer (Amsterdam, Netherlands), , Volume: 72, Issue:3, 2011
The LUX-Lung clinical trial program of afatinib for non-small-cell lung cancer.Expert review of anticancer therapy, , Volume: 11, Issue:5, 2011
Afatinib (BIBW 2992) development in non-small-cell lung cancer.Future oncology (London, England), , Volume: 7, Issue:7, 2011
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.Cancer research, , Feb-01, Volume: 70, Issue:3, 2010
The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.Cancer investigation, , Volume: 28, Issue:4, 2010
Enhanced anticancer effect of the combination of BIBW2992 and thymidylate synthase-targeted agents in non-small cell lung cancer with the T790M mutation of epidermal growth factor receptor.Molecular cancer therapeutics, , Volume: 9, Issue:6, 2010
EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992.Targeted oncology, , Volume: 5, Issue:4, 2010
New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.Expert opinion on investigational drugs, , Volume: 19, Issue:12, 2010
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.Clinical lung cancer, , Volume: 10, Issue:4, 2009
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.Oncogene, , Aug-07, Volume: 27, Issue:34, 2008
Synergistic Effect of HAD-B1 and Afatinib Against Gefitinib Resistance of Non-Small Cell Lung Cancer.Integrative cancer therapies, , Volume: 21
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.Integrative cancer therapies, , Volume: 20
Skeletal muscle loss during anti-epidermal growth factor receptor therapy is an independent prognostic factor on non-small cell lung cancer patients survival.Journal of B.U.ON. : official journal of the Balkan Union of Oncology, , Volume: 26, Issue:3
Significance of Polar Charged Amino Acids in Compound Mutations in EGFR-mutated Patients Treated With First-line Afatinib.In vivo (Athens, Greece), , Volume: 36, Issue:4
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Afatinib in the first-line treatment of patients with non-small cell lung cancer: clinical evidence and experience.Therapeutic advances in respiratory disease, , Volume: 12
Identifying activating mutations in the EGFR gene: prognostic and therapeutic implications in non-small cell lung cancer.Jornal brasileiro de pneumologia : publicacao oficial da Sociedade Brasileira de Pneumologia e Tisilogia, , Volume: 41, Issue:4
"From molecular to clinic": The pivotal role of CDC42 in pathophysiology of human papilloma virus related cancers and a correlated sensitivity of afatinib.Frontiers in immunology, , Volume: 14, 2023
NRG1 promotes tumorigenesis and metastasis and afatinib treatment efficiency is enhanced by NRG1 inhibition in esophageal squamous cell carcinoma.Biochemical pharmacology, , Volume: 218, 2023
Afatinib maintenance therapy following post-operative radiochemotherapy in head and neck squamous cell carcinoma: Results from the phase III randomised double-blind placebo-controlled study BIB2992ORL (GORTEC 2010-02).European journal of cancer (Oxford, England : 1990), , Volume: 178, 2023
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Phase II study of afatinib plus pembrolizumab in patients with squamous cell carcinoma of the lung following progression during or after first-line chemotherapy (LUX-Lung-IO).Lung cancer (Amsterdam, Netherlands), , Volume: 166, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
Afatinib and Pembrolizumab for Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (ALPHA Study): A Phase II Study with Biomarker Analysis.Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-14, Volume: 28, Issue:8, 2022
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).Thoracic cancer, , Volume: 12, Issue:8, 2021
Real-world effectiveness of second-line Afatinib versus chemotherapy for the treatment of advanced lung squamous cell carcinoma in immunotherapy-naïve patients.BMC cancer, , Nov-15, Volume: 21, Issue:1, 2021
EGFR L861Q and CDK4 amplification responding to afatinib combined with palbociclib treatment in a patient with advanced lung squamous cell carcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 145, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Establishment and characterization of patient-derived xenografts as paraclinical models for head and neck cancer.BMC cancer, , Apr-15, Volume: 20, Issue:1, 2020
A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1, 2019
Afatinib With Pembrolizumab for Treatment of Patients With Locally Advanced/Metastatic Squamous Cell Carcinoma of the Lung: The LUX-Lung IO/KEYNOTE 497 Study Protocol.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
Emergence, development, and future of cardio-oncology in China: cardiohypersensitivity, cardiotoxicity and the Kounis syndrome.Chinese medical journal, , 03-20, Volume: 132, Issue:6, 2019
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
Osimertinib for Secondary T790M-Mutation-Positive Squamous Cell Carcinoma Transformation After Afatinib Failure.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Association of ERBB Mutations With Clinical Outcomes of Afatinib- or Erlotinib-Treated Patients With Lung Squamous Cell Carcinoma: Secondary Analysis of the LUX-Lung 8 Randomized Clinical Trial.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
In Search of an Oncogene Driver for Squamous Lung Cancer.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Afatinib treatment of a squamous lung cancer after tumor progression of nivolumab.Thoracic cancer, , Volume: 9, Issue:1, 2018
Symptom and Quality of Life Improvement in LUX-Lung 8, an Open-Label Phase III Study of Second-Line Afatinib Versus Erlotinib in Patients With Advanced Squamous Cell Carcinoma of the Lung After First-Line Platinum-Based Chemotherapy.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Afatinib and Erlotinib in the treatment of squamous-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 19, Issue:18, 2018
Predictive biomarkers and EGFR inhibitors in squamous cell carcinoma of head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
The clinical features of squamous cell lung carcinoma with sensitive EGFR mutations.International journal of clinical oncology, , Volume: 23, Issue:3, 2018
Phase I study of induction chemotherapy with afatinib, ribavirin, and weekly carboplatin and paclitaxel for stage IVA/IVB human papillomavirus-associated oropharyngeal squamous cell cancer.Head & neck, , Volume: 40, Issue:2, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Acquired Resistance to Afatinib Due to T790M-Positive Squamous Progression in EGFR-Mutant Adenosquamous Lung Carcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:1, 2018
Perspectives on window of opportunity trials in head and neck cancer: lessons from the EORTC 90111-24111-NOCI-HNCG study.European journal of cancer (Oxford, England : 1990), , Volume: 104, 2018
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Evaluation of the VeriStratLung cancer (Amsterdam, Netherlands), , Volume: 109, 2017
Afatinib radiosensitizes head and neck squamous cell carcinoma cells by targeting cancer stem cells.Oncotarget, , Mar-28, Volume: 8, Issue:13, 2017
Second-line therapy of squamous non-small cell lung cancer: an evolving landscape.Expert review of respiratory medicine, , Volume: 11, Issue:6, 2017
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
A phase I study afatinib/carboplatin/paclitaxel induction chemotherapy followed by standard chemoradiation in HPV-negative or high-risk HPV-positive locally advanced stage III/IVa/IVb head and neck squamous cell carcinoma.Oral oncology, , Volume: 53, 2016
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:8, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
Overview of Current Treatment Options and Investigational Targeted Therapies for Locally Advanced Squamous Cell Carcinoma of the Head and Neck.American journal of clinical oncology, , Volume: 39, Issue:4, 2016
Afatinib in squamous cell carcinoma of the head and neck.Expert opinion on pharmacotherapy, , Volume: 17, Issue:9, 2016
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.Targeted oncology, , Volume: 10, Issue:4, 2015
Afatinib versus erlotinib as second-line treatment of patients with advanced squamous cell carcinoma of the lung (LUX-Lung 8): an open-label randomised controlled phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:8, 2015
Afatinib versus methotrexate as second-line treatment in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 1): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:5, 2015
miR-124 Regulates the Epithelial-Restricted with Serine Box/Epidermal Growth Factor Receptor Signaling Axis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics, , Volume: 14, Issue:10, 2015
Afatinib in the treatment of head and neck squamous cell carcinoma.Expert opinion on investigational drugs, , Volume: 23, Issue:1, 2014
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.BMC cancer, , Jun-28, Volume: 14, 2014
Novel approach of MALDI drug imaging, immunohistochemistry, and digital image analysis for drug distribution studies in tissues.Analytical chemistry, , Nov-04, Volume: 86, Issue:21, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
A randomized, phase II study of afatinib versus cetuximab in metastatic or recurrent squamous cell carcinoma of the head and neck.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 25, Issue:9, 2014
Afatinib versus placebo as adjuvant therapy after chemoradiation in a double-blind, phase III study (LUX-Head & Neck 2) in patients with primary unresected, clinically intermediate-to-high-risk head and neck cancer: study protocol for a randomized controlTrials, , Nov-29, Volume: 15, 2014
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinib.Molecular cancer therapeutics, , Volume: 12, Issue:8, 2013
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Combination of EGFR/HER2 tyrosine kinase inhibition by BIBW 2992 and BIBW 2669 with irradiation in FaDu human squamous cell carcinoma.Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al], , Volume: 183, Issue:5, 2007
Cx32 inhibits TNFα-induced extrinsic apoptosis with and without EGFR suppression.Oncology reports, , Volume: 38, Issue:5, 2017
HER2 aberrations in cancer: implications for therapy.Cancer treatment reviews, , Volume: 40, Issue:6, 2014
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Drug combination screening as a translational approach toward an improved drug therapy for chordoma.Cellular oncology (Dordrecht), , Volume: 44, Issue:6, 2021
AZD8055 enhances in vivo efficacy of afatinib in chordomas.The Journal of pathology, , Volume: 255, Issue:1, 2021
Chordoma: A Case Report and Review of Literature.The American journal of case reports, , Jan-23, Volume: 21, 2020
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury.Molecular cancer therapeutics, , Volume: 17, Issue:3, 2018
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.Neoplasia (New York, N.Y.), , Volume: 43, 2023
Phase II Study of Afatinib in Patients With Tumors With Human Epidermal Growth Factor Receptor 2-Activating Mutations: Results From the National Cancer Institute-Molecular Analysis for Therapy Choice ECOG-ACRIN Trial (EAY131) Subprotocol EAY131-B.JCO precision oncology, , Volume: 6, 2022
Calcium-activated chloride channel is involved in the onset of diarrhea triggered by EGFR tyrosine kinase inhibitor treatment in rats.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 141, 2021
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
Intestinal epithelial potassium channels and CFTR chloride channels activated in ErbB tyrosine kinase inhibitor diarrhea.JCI insight, , 02-21, Volume: 4, Issue:4, 2019
A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1, 2019
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Phase I trial of afatinib and 3-weekly trastuzumab with optimal anti-diarrheal management in patients with HER2-positive metastatic cancer.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
Phase I open-label study of afatinib plus vinorelbine in patients with solid tumours overexpressing EGFR and/or HER2.British journal of cancer, , 02-06, Volume: 118, Issue:3, 2018
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
Risk of Treatment-Related Toxicities from EGFR Tyrosine Kinase Inhibitors: A Meta-analysis of Clinical Trials of Gefitinib, Erlotinib, and Afatinib in Advanced EGFR-Mutated Non-Small Cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Clinical analysis of patients treated with afatinib for advanced non-small cell lung cancer: A Nagano Lung Cancer Research Group observational study.Respiratory investigation, , Volume: 54, Issue:6, 2016
Management of the adverse events of afatinib: a consensus of the recommendations of the Spanish expert panel.Future oncology (London, England), , Volume: 11, Issue:2, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
[Hange-Shashin-to for preventing diarrhea during afatinib therapy].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:5, 2015
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors.Clinical lung cancer, , Volume: 15, Issue:6, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
Diarrhea associated with afatinib: an oral ErbB family blocker.Expert review of anticancer therapy, , Volume: 13, Issue:6, 2013
Association of Genetic Polymorphisms With Afatinib-induced Diarrhoea.In vivo (Athens, Greece), , Volume: 34, Issue:3
NRG1 promotes tumorigenesis and metastasis and afatinib treatment efficiency is enhanced by NRG1 inhibition in esophageal squamous cell carcinoma.Biochemical pharmacology, , Volume: 218, 2023
Remarkable inhibition effects of afatinib alone or combining with paclitaxel in esophageal squamous cell carcinoma.Journal of gastroenterology and hepatology, , Volume: 36, Issue:9, 2021
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
GPCR-mediated EGFR transactivation ameliorates skin toxicities induced by afatinib.Acta pharmacologica Sinica, , Volume: 43, Issue:6, 2022
Successful erlotinib rechallenge in an EGFR-mutant metastatic non-small cell lung cancer patient with afatinib-induced drug rash with eosinophilia and systemic symptoms: A case report.Thoracic cancer, , Volume: 13, Issue:3, 2022
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience.Cancer chemotherapy and pharmacology, , Volume: 77, Issue:5, 2016
Management of the adverse events of afatinib: a consensus of the recommendations of the Spanish expert panel.Future oncology (London, England), , Volume: 11, Issue:2, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
Dermatologic adverse events associated with afatinib: an oral ErbB family blocker.Expert review of anticancer therapy, , Volume: 13, Issue:6, 2013
Afatinib in combination with GEMOX chemotherapy as the adjuvant treatment in patients with ErbB pathway mutated, resectable gallbladder cancer: study protocol for a ctDNA-based, multicentre, open-label, randomised, controlled, phase II trial.BMJ open, , 02-28, Volume: 13, Issue:2, 2023
Banxia Xiexin Decoction () Combined with Afatinib in Treatment of Advanced Gallbladder Cancer: Case Report and Literature Review.Chinese journal of integrative medicine, , Volume: 25, Issue:4, 2019
ERBB2 and KRAS alterations mediate response to EGFR inhibitors in early stage gallbladder cancer.International journal of cancer, , 04-15, Volume: 144, Issue:8, 2019
Afatinib and radiotherapy, with or without temozolomide, in patients with newly diagnosed glioblastoma: results of a phase I trial.Journal of neuro-oncology, , Volume: 155, Issue:3, 2021
Androgen Receptor Activation in Glioblastoma Can Be Achieved by Ligand-Independent Signaling through EGFR-A Potential Therapeutic Target.International journal of molecular sciences, , Oct-11, Volume: 22, Issue:20, 2021
Boswellic acid has anti-inflammatory effects and enhances the anticancer activities of Temozolomide and Afatinib, an irreversible ErbB family blocker, in human glioblastoma cells.Phytotherapy research : PTR, , Volume: 33, Issue:6, 2019
Afatinib and Temozolomide combination inhibits tumorigenesis by targeting EGFRvIII-cMet signaling in glioblastoma cells.Journal of experimental & clinical cancer research : CR, , Jun-18, Volume: 38, Issue:1, 2019
Efficacy of EGFR plus TNF inhibition in a preclinical model of temozolomide-resistant glioblastoma.Neuro-oncology, , 12-17, Volume: 21, Issue:12, 2019
Afatinib, an irreversible ErbB family blocker, with protracted temozolomide in recurrent glioblastoma: a case report.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Phase I/randomized phase II study of afatinib, an irreversible ErbB family blocker, with or without protracted temozolomide in adults with recurrent glioblastoma.Neuro-oncology, , Volume: 17, Issue:3, 2015
Potential therapeutic efficiency of pan-ERBB inhibitors for canine glioma.Veterinary research communications, , Volume: 47, Issue:4, 2023
The NRG3/ERBB4 signaling cascade as a novel therapeutic target for canine glioma.Experimental cell research, , 03-15, Volume: 400, Issue:2, 2021
A novel lead compound CM-118: antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers.Cancer biology & therapy, , Jun-01, Volume: 15, Issue:6, 2014
Afatinib maintenance therapy following post-operative radiochemotherapy in head and neck squamous cell carcinoma: Results from the phase III randomised double-blind placebo-controlled study BIB2992ORL (GORTEC 2010-02).European journal of cancer (Oxford, England : 1990), , Volume: 178, 2023
[Afatinib maintenance therapy does not confer any benefit in the adjuvant treatment of head and neck tumors].Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al], , Volume: 199, Issue:4, 2023
Short-course pembrolizumab and continuous afatinib therapy for recurrent or metastatic head and neck squamous cell carcinoma: a real-world data analysis.BMC cancer, , Nov-28, Volume: 22, Issue:1, 2022
Afatinib and Pembrolizumab for Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (ALPHA Study): A Phase II Study with Biomarker Analysis.Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-14, Volume: 28, Issue:8, 2022
Simultaneously targeting ErbB family kinases and PI3K in HPV-positive head and neck squamous cell carcinoma.Oral oncology, , Volume: 131, 2022
Afatinib induces pro-survival autophagy and increases sensitivity to apoptosis in stem-like HNSCC cells.Cell death & disease, , 07-22, Volume: 12, Issue:8, 2021
Chordoma: A Case Report and Review of Literature.The American journal of case reports, , Jan-23, Volume: 21, 2020
Establishment and characterization of patient-derived xenografts as paraclinical models for head and neck cancer.BMC cancer, , Apr-15, Volume: 20, Issue:1, 2020
Gefitinib and Afatinib Show Potential Efficacy for Fanconi Anemia-Related Head and Neck Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, , 06-15, Volume: 26, Issue:12, 2020
Afatinib versus methotrexate as second-line treatment in Asian patients with recurrent or metastatic squamous cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 3): an open-label, randomised phase III trialAnnals of oncology : official journal of the European Society for Medical Oncology, , 11-01, Volume: 30, Issue:11, 2019
Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.Oral oncology, , Volume: 97, 2019
A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1, 2019
Rationale for Using Irreversible Epidermal Growth Factor Receptor Inhibitors in Combination with Phosphatidylinositol 3-Kinase Inhibitors for Advanced Head and Neck Squamous Cell Carcinoma.Molecular pharmacology, , Volume: 95, Issue:5, 2019
Predictive biomarkers and EGFR inhibitors in squamous cell carcinoma of head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Activity and safety of afatinib in a window preoperative EORTC study in patients with squamous cell carcinoma of the head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Perspectives on window of opportunity trials in head and neck cancer: lessons from the EORTC 90111-24111-NOCI-HNCG study.European journal of cancer (Oxford, England : 1990), , Volume: 104, 2018
Afatinib radiosensitizes head and neck squamous cell carcinoma cells by targeting cancer stem cells.Oncotarget, , Mar-28, Volume: 8, Issue:13, 2017
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
Afatinib in squamous cell carcinoma of the head and neck.Expert opinion on pharmacotherapy, , Volume: 17, Issue:9, 2016
A phase I study afatinib/carboplatin/paclitaxel induction chemotherapy followed by standard chemoradiation in HPV-negative or high-risk HPV-positive locally advanced stage III/IVa/IVb head and neck squamous cell carcinoma.Oral oncology, , Volume: 53, 2016
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:8, 2016
Co-treatment of wild-type EGFR head and neck cancer cell lines with afatinib and cisplatin.Molecular medicine reports, , Volume: 13, Issue:3, 2016
Overview of Current Treatment Options and Investigational Targeted Therapies for Locally Advanced Squamous Cell Carcinoma of the Head and Neck.American journal of clinical oncology, , Volume: 39, Issue:4, 2016
miR-124 Regulates the Epithelial-Restricted with Serine Box/Epidermal Growth Factor Receptor Signaling Axis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics, , Volume: 14, Issue:10, 2015
Afatinib versus methotrexate as second-line treatment in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 1): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:5, 2015
Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.Targeted oncology, , Volume: 10, Issue:4, 2015
Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
A randomized, phase II study of afatinib versus cetuximab in metastatic or recurrent squamous cell carcinoma of the head and neck.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 25, Issue:9, 2014
Afatinib versus placebo as adjuvant therapy after chemoradiation in a double-blind, phase III study (LUX-Head & Neck 2) in patients with primary unresected, clinically intermediate-to-high-risk head and neck cancer: study protocol for a randomized controlTrials, , Nov-29, Volume: 15, 2014
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.BMC cancer, , Jun-28, Volume: 14, 2014
Afatinib in the treatment of head and neck squamous cell carcinoma.Expert opinion on investigational drugs, , Volume: 23, Issue:1, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinib.Molecular cancer therapeutics, , Volume: 12, Issue:8, 2013
Ethoxy-erianin phosphate and afatinib synergistically inhibit liver tumor growth and angiogenesis via regulating VEGF and EGFR signaling pathways.Toxicology and applied pharmacology, , 03-01, Volume: 438, 2022
Afatinib, an EGFR inhibitor, decreases EMT and tumorigenesis of Huh‑7 cells by regulating the ERK‑VEGF/MMP9 signaling pathway.Molecular medicine reports, , Volume: 20, Issue:4, 2019
Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation.JCI insight, , 04-08, Volume: 7, Issue:7, 2022
Anti-inflammatory effect of afatinib (an EGFR-TKI) on OGD-induced neuroinflammation.Scientific reports, , 02-21, Volume: 9, Issue:1, 2019
Ethoxy-erianin phosphate and afatinib synergistically inhibit liver tumor growth and angiogenesis via regulating VEGF and EGFR signaling pathways.Toxicology and applied pharmacology, , 03-01, Volume: 438, 2022
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Afatinib, an EGFR inhibitor, decreases EMT and tumorigenesis of Huh‑7 cells by regulating the ERK‑VEGF/MMP9 signaling pathway.Molecular medicine reports, , Volume: 20, Issue:4, 2019
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
Treatment outcomes of non-small cell lung cancers treated with EGFR tyrosine kinase inhibitors: a real-world cohort study.Acta oncologica (Stockholm, Sweden), , Volume: 62, Issue:12, 2023
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs.Thoracic cancer, , Volume: 14, Issue:32, 2023
Survival outcomes of east Asian patients with advanced non-small cell lung cancer treated with first-line EGFR tyrosine kinase inhibitors: A network meta-analysis of real-world evidence.Thoracic cancer, , Volume: 14, Issue:32, 2023
A randomized phase II study of afatinib alone or combined with bevacizumab for treating chemo-naïve patients with non-small cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 184, 2023
Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.Neoplasia (New York, N.Y.), , Volume: 43, 2023
Effects of targeted lung cancer drugs on cardiomyocytes studied by atomic force microscopy.Analytical methods : advancing methods and applications, , 08-24, Volume: 15, Issue:33, 2023
Neoadjuvant Afatinib for stage III EGFR-mutant non-small cell lung cancer: a phase II study.Nature communications, , 08-03, Volume: 14, Issue:1, 2023
Comprehensive assessment of pretreatment sarcopenia impacts on patients with EGFR-mutated NSCLC treated with afatinib.Thoracic cancer, , Volume: 14, Issue:25, 2023
Afatinib for the Treatment of NSCLC with Uncommon EGFR Mutations: A Narrative Review.Current oncology (Toronto, Ont.), , 05-28, Volume: 30, Issue:6, 2023
Alternating Therapy With Osimertinib and Afatinib Blockades EGFR Secondary Mutation in EGFR-Mutant Lung Cancer: A Single-Arm Phase II Trial.Clinical lung cancer, , Volume: 24, Issue:6, 2023
Natural Cyclophilin A Inhibitors Suppress the Growth of Cancer Stem Cells in Non-Small Cell Lung Cancer by Disrupting Crosstalk between CypA/CD147 and EGFR.International journal of molecular sciences, , May-29, Volume: 24, Issue:11, 2023
Flashback Foreword: Afatinib for the Treatment of Epidermal Growth Factor Receptor Mutation-Positive Non-Small-Cell Lung Cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , 06-01, Volume: 41, Issue:16, 2023
Final Report on Real-World Effectiveness of Sequential Afatinib and Osimertinib in EGFR-Positive Advanced Non-Small Cell Lung Cancer: Updated Analysis of the RESET Study.Cancer research and treatment, , Volume: 55, Issue:4, 2023
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 181, 2023
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
A real-world study of Afatinib plus ramucirumab in treatment-naïve, EGFR-mutated, non-small cell lung cancer.BMC cancer, , May-08, Volume: 23, Issue:1, 2023
Clinical Outcomes of Afatinib Versus Osimertinib in Patients With Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: A Pooled Analysis.The oncologist, , 06-02, Volume: 28, Issue:6, 2023
The Use of Cytotoxic Drugs as First Line Chemotherapy for EGFR (+) Nonsquamous NSCLC: A Network Meta-Analysis.Disease markers, , Volume: 2023, 2023
Determining plasma and cerebrospinal fluid concentrations of EGFR-TKI in lung cancer patients.Analytical biochemistry, , 05-15, Volume: 669, 2023
Monitoring of T790M in plasma ctDNA of advanced EGFR-mutant NSCLC patients on first- or second-generation tyrosine kinase inhibitors.BMC cancer, , Mar-13, Volume: 23, Issue:1, 2023
NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity.European journal of pharmacology, , May-05, Volume: 946, 2023
Bruceine D and afatinib combination inhibits ovarian cancer cells proliferation and migration through DNA damage repair and EGFR pathway.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 71, Issue:5, 2023
Afatinib in Untreated Stage IIIB/IV Lung Adenocarcinoma with Major Uncommon Epidermal Growth Factor Receptor (EGFR) Mutations (G719X/L861Q/S768I): A Multicenter Observational Study in Taiwan.Targeted oncology, , Volume: 18, Issue:2, 2023
Afatinib plus osimertinib in the treatment of osimertinib-resistant non-small cell lung carcinoma: a phase I clinical trial.BMC cancer, , Jan-03, Volume: 23, Issue:1, 2023
The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Non-small cell lung cancer with EGFR (L858R and E709X) and CNNB1 mutations responded to afatinib.Thoracic cancer, , Volume: 14, Issue:4, 2023
The second-generation tyrosine kinase inhibitor afatinib inhibits IL-1β secretion via blocking assembly of NLRP3 inflammasome independent of epidermal growth factor receptor signaling in macrophage.Molecular immunology, , Volume: 153, 2023
Epidermal growth factor receptor tyrosine kinase inhibitors for non-small cell lung cancer harboring uncommon EGFR mutations: Real-world data from Taiwan.Thoracic cancer, , Volume: 14, Issue:1, 2023
Absence of copy number gain of EGFR: A possible predictive marker of long-term response to afatinib.Cancer science, , Volume: 114, Issue:3, 2023
Older patients with EGFR mutation-positive non-small cell lung cancer treated with afatinib in clinical practice: A subset analysis of the non-interventional GIDEON study.Journal of geriatric oncology, , Volume: 14, Issue:1, 2023
Afatinib triggers a NiFundamental & clinical pharmacology, , Volume: 37, Issue:2, 2023
A case of crescentic glomerulonephritis induced by afatinib for lung adenocarcinoma.CEN case reports, , Volume: 12, Issue:2, 2023
All EGFR mutations are (not) created equal: focus on uncommon EGFR mutations.Journal of cancer research and clinical oncology, , Volume: 149, Issue:4, 2023
Real-life comparison of afatinib and erlotinib in non-small cell lung cancer with rare EGFR exon 18 and exon 20 mutations: a Turkish Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 149, Issue:2, 2023
Long-term survival in a patient with advanced lung adenocarcinoma harboring synchronous EGFR exon 18 G719A and BRAF V600E mutations and treated with afatinib: a case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Elucidation of the inhibitory potential of flavonoids against PKP1 protein in non-small cell lung cancer.Cellular and molecular biology (Noisy-le-Grand, France), , Nov-30, Volume: 68, Issue:11, 2022
Drug Repurposing against KRAS Mutant G12C: A Machine Learning, Molecular Docking, and Molecular Dynamics Study.International journal of molecular sciences, , Dec-30, Volume: 24, Issue:1, 2022
Advanced Lung Cancer Patients' Use of EGFR Tyrosine Kinase Inhibitors and Overall Survival: Real-World Evidence from Quebec, Canada.Current oncology (Toronto, Ont.), , 10-26, Volume: 29, Issue:11, 2022
Real-world data with afatinib in Spanish patients with treatment-naïve non-small-cell lung cancer harboring exon 19 deletions in epidermal growth factor receptor (Del19 EGFR): Clinical experience of the Galician Lung Cancer Group.Cancer treatment and research communications, , Volume: 33, 2022
Prevalence, Treatment Patterns, and Outcomes of Individuals with Current oncology (Toronto, Ont.), , 09-30, Volume: 29, Issue:10, 2022
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
Application of several machine learning algorithms for the prediction of afatinib treatment outcome in advanced-stage EGFR-mutated non-small-cell lung cancer.Thoracic cancer, , Volume: 13, Issue:23, 2022
Study on the prognosis, immune and drug resistance of m6A-related genes in lung cancer.BMC bioinformatics, , Oct-19, Volume: 23, Issue:1, 2022
Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.Journal of cancer research and therapeutics, , Volume: 18, Issue:5, 2022
Durable response to afatinib rechallenge in a long-term survivor of non-small cell lung cancer harboring EGFR L858R and L747V mutations.Thoracic cancer, , Volume: 13, Issue:22, 2022
Liquid biopsy for detecting epidermal growth factor receptor mutation among patients with non-small cell lung cancer treated with afatinib: a multicenter prospective study.BMC cancer, , Oct-04, Volume: 22, Issue:1, 2022
Afatinib Targeted Therapy Affects the Immune Function and Serum Levels of EGFR and Gastrin-Releasing Peptide Precursor (pro-GRP) in Patients with Non-Small-Cell Lung Cancer (NSCLC).Disease markers, , Volume: 2022, 2022
Long-term response in a patient with adenocarcinoma harboring both common and uncommon EGFR mutations.Investigational new drugs, , Volume: 40, Issue:6, 2022
Early-Onset Pulmonary Events with Combined Brigatinib and Afatinib Treatment of L858/cisT790M/cisC797S NSCLC: A Case Report.The American journal of case reports, , Sep-23, Volume: 23, 2022
Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 155, 2022
A case of multiple primary lung adenocarcinoma with a CD74-NRG1 fusion protein and HER2 mutation benefit from combined target therapy.Thoracic cancer, , Volume: 13, Issue:21, 2022
Efficacy and potential resistance mechanisms of afatinib in advanced non-small cell lung cancer patients with EGFR G719X/L861Q/S768I.Cancer, , 11-01, Volume: 128, Issue:21, 2022
Rare EGFR E709-T710delinsX: Molecular characteristics and superior response to afatinib treatment in NSCLC patients.Lung cancer (Amsterdam, Netherlands), , Volume: 172, 2022
Non-small cell lung cancer harboring EGFR G724S mutation and exon 19 deletion responded to afatinib monotherapy after multiple lines of target therapies.Anti-cancer drugs, , 10-01, Volume: 33, Issue:9, 2022
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Efficacy of Combined Use of Everolimus and Second-Generation Pan-EGRF Inhibitors in International journal of molecular sciences, , Jul-14, Volume: 23, Issue:14, 2022
Plain language summary of NRG1 fusions in cancer: current knowledge and treatment with afatinib and other drugs.Future oncology (London, England), , Volume: 18, Issue:26, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
The EGFR-STYK1-FGF1 axis sustains functional drug tolerance to EGFR inhibitors in EGFR-mutant non-small cell lung cancer.Cell death & disease, , 07-15, Volume: 13, Issue:7, 2022
Audit of Molecular Mechanisms of Primary and Secondary Resistance to Various Generations of Tyrosine Kinase Inhibitors in Known Epidermal Growth Factor Receptor-Mutant Non-small Cell Lung Cancer Patients in a Tertiary Centre.Clinical oncology (Royal College of Radiologists (Great Britain)), , Volume: 34, Issue:11, 2022
Structural dynamics and kinase inhibitory activity of three generations of tyrosine kinase inhibitors against wild-type, L858R/T790M, and L858R/T790M/C797S forms of EGFR.Computers in biology and medicine, , Volume: 147, 2022
Ad hoc afatinib in an eldery lung cancer patient with EGFR exon 19 deletion L747-A750>P.Advances in respiratory medicine, , Volume: 90, Issue:3, 2022
Survival benefits from afatinib compared with gefitinib and erlotinib among patients with common EGFR mutation in first-line setting.Thoracic cancer, , Volume: 13, Issue:14, 2022
Application of afatinib combined with np regimen in the treatment of stage iv non-small cell lung cancer and its effect on patient survival.Pakistan journal of pharmaceutical sciences, , Volume: 35, Issue:2(Special), 2022
Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
The effect of afatinib and radiotherapy on a patient with lung adenocarcinoma with a rare EGFR extracellular domain M277E mutation and high PD-L1 expression.Journal of cancer research and therapeutics, , Volume: 18, Issue:2, 2022
A Phase 2 Trial of Afatinib in Patients with Solid Tumors that Harbor Genomic Aberrations in the HER family: The MOBILITY3 Basket Study.Targeted oncology, , Volume: 17, Issue:3, 2022
Epidermal growth factor receptor tyrosine kinase inhibitors for de novo T790M mutation: A retrospective study of 44 patients.Thoracic cancer, , Volume: 13, Issue:13, 2022
Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L).Lung cancer (Amsterdam, Netherlands), , Volume: 168, 2022
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
Development and validation of a new liquid chromatography-tandem mass spectrometry assay for the simultaneous quantification of afatinib, dacomitinib, osimertinib, and the active metabolites of osimertinib in human serum.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , May-30, Volume: 1199, 2022
Plain language summary of publication: new information for the potential role of afatinib in treating people with Future oncology (London, England), , Volume: 18, Issue:18, 2022
Utilization and costs of epidermal growth factor receptor mutation testing and targeted therapy in Medicare patients with metastatic lung adenocarcinoma.BMC health services research, , Apr-09, Volume: 22, Issue:1, 2022
Durable clinical benefit from afatinib in a lung adenocarcinoma patient with acquired EGFR L718V mutation-mediated resistance towards osimertinib: a case report and literature review.Annals of palliative medicine, , Volume: 11, Issue:3, 2022
Real-world Afatinib Outcomes in Advanced Non-small Cell Lung Cancer Harboring Anticancer research, , Volume: 42, Issue:4, 2022
Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Preclinical assessment of combination therapy of EGFR tyrosine kinase inhibitors in a highly heterogeneous tumor model.Oncogene, , Volume: 41, Issue:17, 2022
Metabolic complete tumor response in a patient with The Journal of international medical research, , Volume: 50, Issue:3, 2022
Phase II study of afatinib plus pembrolizumab in patients with squamous cell carcinoma of the lung following progression during or after first-line chemotherapy (LUX-Lung-IO).Lung cancer (Amsterdam, Netherlands), , Volume: 166, 2022
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
First-line Afatinib in Patients With Non-small-cell Lung Cancer With Uncommon EGFR Mutations in South Korea.Anticancer research, , Volume: 42, Issue:3, 2022
Classification and regression tree for estimating predictive markers to detect T790M mutations after acquired resistance to first line EGFR-TKI: HOPE-002.Investigational new drugs, , Volume: 40, Issue:2, 2022
Determination of Afatinib in Human Plasma by 2-Dimensional Liquid Chromatography.Pharmacology, , Volume: 107, Issue:5-6, 2022
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry.Clinica chimica acta; international journal of clinical chemistry, , Feb-15, Volume: 527, 2022
The EPICAL trial, a phase Ib study combining first line afatinib with anti-EGF vaccination in EGFR-mutant metastatic NSCLC.Lung cancer (Amsterdam, Netherlands), , Volume: 164, 2022
Successful erlotinib rechallenge in an EGFR-mutant metastatic non-small cell lung cancer patient with afatinib-induced drug rash with eosinophilia and systemic symptoms: A case report.Thoracic cancer, , Volume: 13, Issue:3, 2022
Complete Remission to Afatinib in a Patient Harboring a Novel Epidermal Growth Factor Mutation in De Novo Small-Cell Lung Cancer: A Case Report: Clinical Lung Cancer.Clinical lung cancer, , Volume: 23, Issue:4, 2022
Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.European journal of cancer (Oxford, England : 1990), , Volume: 160, 2022
Combination treatment with bevacizumab plus erlotinib for meningeal carcinomatosis of afatinib-resistant EGFR mutated lung cancer without T790M mutation: a case report.Annals of palliative medicine, , Volume: 11, Issue:8, 2022
Cost-effectiveness analysis of the first-line EGFR-TKIs in patients with advanced EGFR-mutated non-small-cell lung cancer.Expert review of pharmacoeconomics & outcomes research, , Volume: 22, Issue:4, 2022
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.Investigational new drugs, , Volume: 40, Issue:2, 2022
Hypotension from afatinib in epidermal growth factor receptor-mutated non-small cell lung cancer: a case report and literature review.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Real-life comparison of the afatinib and first-generation tyrosine kinase inhibitors in nonsmall cell lung cancer harboring EGFR exon 19 deletion: a Turk Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 147, Issue:7, 2021
Incremental cost-effectiveness analysis of tyrosine kinase inhibitors in advanced non-small cell lung cancer with mutations of the epidermal growth factor receptor in Colombia.Expert review of pharmacoeconomics & outcomes research, , Volume: 21, Issue:4, 2021
Afatinib in EGFR TKI-naïve patients with locally advanced or metastatic EGFR mutation-positive non-small cell lung cancer: Interim analysis of a Phase 3b study.Lung cancer (Amsterdam, Netherlands), , Volume: 152, 2021
Synergy between vinorelbine and afatinib in the inhibition of non-small cell lung cancer progression by EGFR and p53 signaling pathways.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 134, 2021
HER2 amplification as a potential mechanism of acquired resistance to afatinib in an advanced non-small-cell lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 151, 2021
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.The oncologist, , Volume: 26, Issue:4, 2021
Phase II open-label multicenter study to assess the antitumor activity of afatinib in lung cancer patients with activating epidermal growth factor receptor mutation from circulating tumor DNA: Liquid-Lung-A.Thoracic cancer, , Volume: 12, Issue:4, 2021
Celastrol acts synergistically with afatinib to suppress non-small cell lung cancer cell proliferation by inducing paraptosis.Journal of cellular physiology, , Volume: 236, Issue:6, 2021
Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells.International journal of radiation biology, , Volume: 97, Issue:2, 2021
EGFR tyrosine kinase inhibitors in non-small cell lung cancer: treatment paradigm, current evidence, and challenges.Tumori, , Volume: 107, Issue:5, 2021
Major Clinical Response to Afatinib Monotherapy in Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion Mutation.Clinical lung cancer, , Volume: 22, Issue:1, 2021
Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Successful treatment of an osimertinib-resistant lung adenocarcinoma with an exon 18 EGFR mutation (G719S) with afatinib plus bevacizumab.Investigational new drugs, , Volume: 39, Issue:1, 2021
Severe EGFR inhibitor-induced acneiform eruption responding to dapsone.Dermatology online journal, , Jul-15, Volume: 27, Issue:7, 2021
Feasibility and effectiveness of afatinib for poor performance status patients with EGFR-mutation-positive non-small-cell lung cancer: a retrospective cohort study.BMC cancer, , Jul-27, Volume: 21, Issue:1, 2021
Sequential treatment of afatinib and osimertinib or other regimens in patients with advanced non-small-cell lung cancer harboring EGFR mutations: Results from a real-world study in South Korea.Cancer medicine, , Volume: 10, Issue:17, 2021
An open-label expanded access program of afatinib in EGFR tyrosine kinase inhibitor-naïve patients with locally advanced or metastatic non-small cell lung cancer harboring EGFR mutations.BMC cancer, , Jul-12, Volume: 21, Issue:1, 2021
Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds.BMC pulmonary medicine, , Jul-01, Volume: 21, Issue:1, 2021
Randomized Phase II Study of 3 Months or 2 Years of Adjuvant Afatinib in Patients With Surgically Resected Stage I-III JCO precision oncology, , Volume: 5, 2021
Survival of chemo-naïve patients with EGFR mutation-positive advanced non-small cell lung cancer after treatment with afatinib and bevacizumab: updates from the Okayama Lung Cancer Study Group Trial 1404.Japanese journal of clinical oncology, , Aug-01, Volume: 51, Issue:8, 2021
Drastic antitumor response following administration of afatinib immediately after atezolizumab in a patient with epidermal growth factor receptor tyrosine kinase inhibitor-resistant lung cancer.Thoracic cancer, , Volume: 12, Issue:13, 2021
Effectiveness and Tolerability of First-Line Afatinib for Advanced EGFR-Mutant Non-Small Cell Lung Cancer in Vietnam.Asian Pacific journal of cancer prevention : APJCP, , May-01, Volume: 22, Issue:5, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Successful treatment of triple EGFR mutation T785A/L861Q/H297_E298 with afatinib.Thoracic cancer, , Volume: 12, Issue:13, 2021
Relationship between Epidermal Growth Factor Receptor Mutations and Adverse Events in Non-Small Cell Lung Cancer Patients treated with Afatinib.The journal of medical investigation : JMI, , Volume: 68, Issue:1.2, 2021
A multicenter cohort study of osimertinib compared with afatinib as first-line treatment for EGFR-mutated non-small-cell lung cancer from practical dataset: CJLSG1903.ESMO open, , Volume: 6, Issue:3, 2021
Response to: Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 12, Issue:11, 2021
Limited effect of afatinib in a non-small cell lung cancer patient harboring an epidermal growth factor receptor K860I missense mutation: A case report.Thoracic cancer, , Volume: 12, Issue:11, 2021
Lower starting dose of afatinib for the treatment of metastatic lung adenocarcinoma harboring exon 21 and exon 19 mutations.BMC cancer, , May-03, Volume: 21, Issue:1, 2021
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
An Liquid Chromatography-Tandem Mass Spectrometry Method for the Simultaneous Determination of Afatinib, Alectinib, Ceritinib, Crizotinib, Dacomitinib, Erlotinib, Gefitinib, and Osimertinib in Human Serum.Therapeutic drug monitoring, , 12-01, Volume: 43, Issue:6, 2021
Real-life Effectiveness of Afatinib Anticancer research, , Volume: 41, Issue:4, 2021
Efficacy and dose of afatinib in patients with non-small cell lung cancer after failure of prior gefitinib or erlotinib treatment.Thoracic cancer, , Volume: 12, Issue:10, 2021
Cost-Effectiveness Analysis of Afatinib, Erlotinib, and Gefitinib as First-Line Treatments for EGFR Mutation-Positive Non-Small-Cell Lung Cancer in Ontario, Canada.PharmacoEconomics, , Volume: 39, Issue:5, 2021
Afatinib-loaded inhalable PLGA nanoparticles for localized therapy of non-small cell lung cancer (NSCLC)-development and in-vitro efficacy.Drug delivery and translational research, , Volume: 11, Issue:3, 2021
Afatinib Exerts Immunomodulatory Effects by Targeting the Pyrimidine Biosynthesis Enzyme CAD.Cancer research, , 06-15, Volume: 81, Issue:12, 2021
Differential effects of epidermal growth factor receptor inhibitors in a single patient with neuropathic pain.BMJ case reports, , Mar-26, Volume: 14, Issue:3, 2021
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , 03-18, Volume: 3, 2021
Afatinib as First-Line Treatment in Asian Patients with EGFR Mutation-Positive NSCLC: A Narrative Review of Real-World Evidence.Advances in therapy, , Volume: 38, Issue:5, 2021
Afatinib therapy in case of EGFR G724S emergence as resistance mechanism to osimertinib.Anti-cancer drugs, , 08-01, Volume: 32, Issue:7, 2021
Efficacy of Osimertinib in Afatinib-resistant Lung Cancer Harboring Uncommon EGFR Mutations: Case Report and Literature Review.Clinical lung cancer, , Volume: 22, Issue:3, 2021
Combination therapy with afatinib and bevacizumab in an EGFR-mutated non-small cell lung cancer patient with acquired ERBB2 amplification: A case report.Medicine, , Feb-26, Volume: 100, Issue:8, 2021
A phase II study of first-line afatinib for patients aged ≥75 years with EGFR mutation-positive advanced non-small cell lung cancer: North East Japan Study Group trial NEJ027.BMC cancer, , Mar-01, Volume: 21, Issue:1, 2021
EGFR mutation-guided use of afatinib, erlotinib and gefitinib for advanced non-small-cell lung cancer in Hong Kong - A cost-effectiveness analysis.PloS one, , Volume: 16, Issue:3, 2021
Successful treatment of Afatinib plus Apatinib using for a lung adenocarcinoma patient with HER-2 V659D mutation: a rare case report.Anti-cancer drugs, , 04-01, Volume: 32, Issue:4, 2021
Long-term response to afatinib in an elderly patient with uncommon epidermal growth factor receptor mutation-positive lung adenocarcinoma.Thoracic cancer, , Volume: 12, Issue:6, 2021
Therapeutic Potential of Afatinib in NRG1 Fusion-Driven Solid Tumors: A Case Series.The oncologist, , Volume: 26, Issue:1, 2021
EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios.Cells, , 12-17, Volume: 10, Issue:12, 2021
Drug-induced Hypersensitivity Syndrome by EGFR-TKI in a Patient with Lung Cancer.Internal medicine (Tokyo, Japan), , Volume: 60, Issue:3, 2021
Afatinib for the treatment of advanced non-small-cell lung cancer harboring an epidermal growth factor receptor exon 18 E709_T710delinsD mutation: a case report.Journal of medical case reports, , Nov-22, Volume: 15, Issue:1, 2021
REPORT- Clinical outcomes of using second - versus first-Generation EGFR-tkis for the First-Line treatment of advanced NSCLC patients with EGFR mutations: A meta-analysis.Pakistan journal of pharmaceutical sciences, , Volume: 34, Issue:4, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
Real-world effectiveness of second-line Afatinib versus chemotherapy for the treatment of advanced lung squamous cell carcinoma in immunotherapy-naïve patients.BMC cancer, , Nov-15, Volume: 21, Issue:1, 2021
An elderly advanced non-small cell lung cancer patient harboring rare epidermal growth factor receptor mutations L861R benefited from afatinib: A case report.Medicine, , Nov-12, Volume: 100, Issue:45, 2021
Afatinib and osimertinib in lung adenocarcinoma harbored EGFR T751_I759delinsS mutation: A case report.Thoracic cancer, , Volume: 12, Issue:24, 2021
Comparing survival and treatment response of patients with acquired T790M mutation second-line osimertinib versus sequential treatment of chemotherapy followed by osimertinib: A real-world study.Thoracic cancer, , Volume: 12, Issue:23, 2021
Genetic and treatment profiles of patients with concurrent Epidermal Growth Factor Receptor (EGFR) and Anaplastic Lymphoma Kinase (ALK) mutations.BMC cancer, , Oct-15, Volume: 21, Issue:1, 2021
Sequential afatinib and osimertinib in patients with EGFR mutation-positive NSCLC and acquired T790M: A global non-interventional study (UpSwinG).Lung cancer (Amsterdam, Netherlands), , Volume: 162, 2021
Comparison Between Second- and Third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors as First-line Treatment in Patients With Non-small-cell Lung Cancer: A Retrospective Analysis.Anticancer research, , Volume: 41, Issue:10, 2021
Afatinib treatment response in advanced lung adenocarcinomas harboring uncommon mutations.Thoracic cancer, , Volume: 12, Issue:21, 2021
A prospective, phase II trial of monotherapy with low-dose afatinib for patients with EGFR, mutation-positive, non-small cell lung cancer: Thoracic oncology research group 1632.Lung cancer (Amsterdam, Netherlands), , Volume: 161, 2021
Structure-based classification predicts drug response in EGFR-mutant NSCLC.Nature, , Volume: 597, Issue:7878, 2021
Outcomes of salvage lung resections in advanced EGFR-mutant lung adenocarcinomas under EGFR TKIs.Thoracic cancer, , Volume: 12, Issue:20, 2021
New strategy for suppressing the growth of lung cancer cells harboring mutations in the ATP-binding region of EGFR by targeting the molecular motor MYO1D.Clinical and translational medicine, , Volume: 11, Issue:8, 2021
Overall survival in stage IV EGFR mutation‑positive NSCLC: Comparing first‑, second‑ and third‑generation EGFR‑TKIs (Review).International journal of oncology, , Volume: 58, Issue:2, 2021
Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury.International journal of molecular sciences, , Jan-14, Volume: 22, Issue:2, 2021
Clinical utility of liquid biopsy for EGFR driver, T790M mutation and EGFR amplification in plasma in patients with acquired resistance to afatinib.BMC cancer, , Jan-12, Volume: 21, Issue:1, 2021
Afatinib + bevacizumab combination therapy in EGFR-mutant NSCLC patients with osimertinib resistance: Protocol of an open-label, phase II, multicenter, single-arm trial.Thoracic cancer, , Volume: 11, Issue:8, 2020
Clinical Features and Progression Pattern of Acquired T790M-positive Compared With T790M-negative EGFR Mutant Non-small-cell Lung Cancer: Catching Tumor and Clinical Heterogeneity Over Time Through Liquid Biopsy.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Phase II Study of Low-Dose Afatinib Maintenance Treatment Among Patients with EGFR-Mutated Non-Small Cell Lung Cancer: North Japan Lung Cancer Study Group Trial 1601 (NJLCG1601).The oncologist, , Volume: 25, Issue:10, 2020
[Two cases of EGFR-mutated lung adenocarcinoma treated with bronchial recanalization and first-line therapy with afatinib.]Recenti progressi in medicina, , Volume: 111, Issue:12, 2020
Dissecting the mThe pharmacogenomics journal, , Volume: 20, Issue:2, 2020
Durable Responses to Afatinib as First-line Therapy for HER2-mutated Metastatic Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Photo-induced specific intracellular release EGFR inhibitor from enzyme/ROS-dual sensitive nano-platforms for molecular targeted-photodynamic combinational therapy of non-small cell lung cancer.Journal of materials chemistry. B, , 09-21, Volume: 8, Issue:35, 2020
Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.Clinical lung cancer, , Volume: 21, Issue:3, 2020
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
A randomized, multi-center, open-label study to compare the safety and efficacy between afatinib monotherapy and combination therapy of afatinib and HAD-B1 for the locally advanced or metastatic NSCLC patients with EGFR mutations.Medicine, , 12-04, Volume: 99, Issue:49, 2020
QT interval prolongation related to afatinib treatment in a patient with metastatic non-small-cell lung cancer.Current problems in cancer, , Volume: 44, Issue:6, 2020
Successful treatment of an elderly patient with an uncommon L861Q epidermal growth factor receptor mutation with low-dose afatinib: A case report.Thoracic cancer, , Volume: 11, Issue:2, 2020
ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib.Cancer, , 03-15, Volume: 126, Issue:6, 2020
Comparing the effectiveness of different EGFR-TKIs in patients with EGFR mutant non-small-cell lung cancer: A retrospective cohort study in Taiwan.International journal of cancer, , 08-15, Volume: 147, Issue:4, 2020
Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 11, Issue:8, 2020
New lung-cancer drugs extend survival times.Nature, , Volume: 587, Issue:7834, 2020
Observational Study of Sequential Afatinib and Osimertinib in EGFR Mutation-Positive NSCLC: Patients Treated with a 40-mg Starting Dose of Afatinib.Advances in therapy, , Volume: 37, Issue:2, 2020
Afatinib for the Treatment of NSCLC Harboring Uncommon EGFR Mutations: A Database of 693 Cases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:5, 2020
Role of YES1 amplification in EGFR mutation-positive non-small cell lung cancer: Primary resistance to afatinib in a patient.Thoracic cancer, , Volume: 11, Issue:9, 2020
Quantitative Structure-Mutation-Activity Relationship Tests (QSMART) model for protein kinase inhibitor response prediction.BMC bioinformatics, , Nov-12, Volume: 21, Issue:1, 2020
Nationwide Real-world Cohort Study of First-line Tyrosine Kinase Inhibitor Treatment in Epidermal Growth Factor Receptor-mutated Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:6, 2020
Determination of Somatic Mutations and Tumor Mutation Burden in Plasma by CAPP-Seq during Afatinib Treatment in NSCLC Patients Resistance to Osimertinib.Scientific reports, , 01-20, Volume: 10, Issue:1, 2020
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
Afatinib in patients with advanced non-small cell lung cancer harboring HER2 mutations, previously treated with chemotherapy: A phase II trial.Lung cancer (Amsterdam, Netherlands), , Volume: 147, 2020
Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol cliniMedicine, , Volume: 99, Issue:4, 2020
Lung carcinoma with diffuse cystic lesions misdiagnosed as pulmonary langerhans cell histocytosis: a case report.BMC pulmonary medicine, , Feb-04, Volume: 20, Issue:1, 2020
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.Medicine, , Oct-23, Volume: 99, Issue:43, 2020
Afatinib response in a lung adenocarcinoma with novel compound S720F+L861R mutation in EGFR.Lung cancer (Amsterdam, Netherlands), , Volume: 148, 2020
Differential significance of molecular subtypes which were classified into EGFR exon 19 deletion on the first line afatinib monotherapy.BMC cancer, , Feb-06, Volume: 20, Issue:1, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Healthcare resource utilization and costs associated with patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive NSCLC in the United States.Journal of medical economics, , Volume: 23, Issue:1, 2020
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Complete Response to Immunotherapy Plus Chemotherapy After an Unusual Clinical Response to Afatinib and Stereotactic Radiosurgery in a Patient With Metastatic EGFR-Mutant Non-Small-Cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Emergence of EGFR G724S After Progression on Osimertinib Responded to Afatinib Monotherapy.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:3, 2020
Knockdown of lncRNA BLACAT1 reverses the resistance of afatinib to non-small cell lung cancer via modulating STAT3 signalling.Journal of drug targeting, , Volume: 28, Issue:3, 2020
Site-Specific and Targeted Therapy Based on Molecular Profiling by Next-Generation Sequencing for Cancer of Unknown Primary Site: A Nonrandomized Phase 2 Clinical Trial.JAMA oncology, , Dec-01, Volume: 6, Issue:12, 2020
Retroperitoneal Metastasis, with Marked Fibrosis, of Lung Adenocarcinoma after Afatinib Treatment: An Autopsy Case Report.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 59, Issue:22, 2020
Resolving Resistance to Osimertinib Therapy With Afatinib in an NSCLC Patient With EGFR L718Q Mutation.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Mutation Variants and Co-Mutations as Genomic Modifiers of Response to Afatinib in HER2-Mutant Lung Adenocarcinoma.The oncologist, , Volume: 25, Issue:3, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Osimertinib induced cardiomyopathy: A case report.Medicine, , Sep-25, Volume: 99, Issue:39, 2020
Comparative effectiveness and cost-effectiveness of three first-line EGFR-tyrosine kinase inhibitors: Analysis of real-world data in a tertiary hospital in Taiwan.PloS one, , Volume: 15, Issue:4, 2020
Budget impact of sequential treatment with first-line afatinib versus first-line osimertinib in non-small-cell lung cancer patients with common EGFR mutations.The European journal of health economics : HEPAC : health economics in prevention and care, , Volume: 21, Issue:6, 2020
PLCγ1‑dependent invasion and migration of cells expressing NSCLC‑associated EGFR mutants.International journal of oncology, , Volume: 57, Issue:4, 2020
Uncommon as an Individual, Not That Uncommon as a Whole.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:5, 2020
Afatinib for the first-line treatment of Future oncology (London, England), , Volume: 16, Issue:31, 2020
EGFR L861Q and CDK4 amplification responding to afatinib combined with palbociclib treatment in a patient with advanced lung squamous cell carcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 145, 2020
The efficacy of first-line tyrosine kinase inhibitors combined with co-medications in Asian patients with EGFR mutation non-small cell lung cancer.Scientific reports, , 09-11, Volume: 10, Issue:1, 2020
Simultaneous Single Cell Gene Expression and EGFR Mutation Analysis of Circulating Tumor Cells Reveals Distinct Phenotypes in NSCLC.Advanced biosystems, , Volume: 4, Issue:8, 2020
NRG1 fusion-driven tumors: biology, detection, and the therapeutic role of afatinib and other ErbB-targeting agents.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 31, Issue:12, 2020
Inflammatory changes in actinic keratoses associated with afatinib therapy.Cutis, , Volume: 105, Issue:3, 2020
Durable complete response after afatinib and crizotinib in an advanced non-small cell lung cancer patient with EGFR L861Q mutation and acquired MET amplification: a case report.Annals of palliative medicine, , Volume: 9, Issue:5, 2020
Successful Treatment of a Patient with Lung Adenocarcinoma Harboring Compound EGFR Gene Mutations, G719X and S768I, with Afatinib.The Tokai journal of experimental and clinical medicine, , Sep-20, Volume: 45, Issue:3, 2020
Molecular profiling of afatinib-resistant non-small cell lung cancer cells in vivo derived from mice.Pharmacological research, , Volume: 161, 2020
Cost-effectiveness analysis of first and second-generation EGFR tyrosine kinase inhibitors as first line of treatment for patients with NSCLC harboring EGFR mutations.BMC cancer, , Sep-01, Volume: 20, Issue:1, 2020
Multiple intraventricular metastases from lung adenocarcinoma with EGFR G719X mutation: a case report.BMC pulmonary medicine, , May-11, Volume: 20, Issue:1, 2020
Sequential afatinib and osimertinib in patients with Future oncology (London, England), , Volume: 16, Issue:34, 2020
Real-world assessment of afatinib for patients with EGFR-positive non-small cell lung cancer.Investigational new drugs, , Volume: 38, Issue:6, 2020
Clinical Activity of Afatinib in Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Spanish Retrospective Multicenter Study.Clinical lung cancer, , Volume: 21, Issue:5, 2020
A noteworthy treatment of metastatic small-cell lung cancer with afatinib, followed by subsequent development of rare metastatic lesions in the ascending and sigmoid colon.Cancer reports (Hoboken, N.J.), , Volume: 3, Issue:3, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Prospective exosome-focused translational research for afatinib study of non-small cell lung cancer patients expressing EGFR (EXTRA study).Thoracic cancer, , Volume: 10, Issue:2, 2019
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Development of two different formats of heterogeneous fluorescence immunoassay for bioanalysis of afatinib by employing fluorescence plate reader and KinExA 3200 immunosensor.Scientific reports, , 10-14, Volume: 9, Issue:1, 2019
Palbociclib overcomes afatinib resistance in non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 109, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Successful treatment of a lung adenocarcinoma patient with a novel EGFR exon 20-ins mutation with afatinib: A case report.Medicine, , Volume: 98, Issue:1, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.Advanced healthcare materials, , Volume: 8, Issue:23, 2019
Impact of afatinib dose modification on safety and effectiveness in patients with EGFR mutation-positive advanced NSCLC: Results from a global real-world study (RealGiDo).Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Efficacy of afatinib or osimertinib plus cetuximab combination therapy for non-small-cell lung cancer with EGFR exon 20 insertion mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Cost-effectiveness of afatinib, gefitinib, erlotinib and pemetrexed-based chemotherapy as first-line treatments for advanced non-small cell lung cancer in China.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Responsiveness to Full-Dose Afatinib in a Patient With Lung Adenocarcinoma Harboring EGFR S768I and V769L Mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:2, 2019
Afatinib in patients with metastatic or recurrent HER2-mutant lung cancers: a retrospective international multicentre study.European journal of cancer (Oxford, England : 1990), , Volume: 109, 2019
Survival outcome of tyrosine kinase inhibitors beyond progression in association to radiotherapy in oligoprogressive EGFR-mutant non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:33, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Afatinib-loaded immunoliposomes functionalized with cetuximab: A novel strategy targeting the epidermal growth factor receptor for treatment of non-small-cell lung cancer.International journal of pharmaceutics, , Apr-05, Volume: 560, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
Re-challenge of afatinib after 1st generation EGFR-TKI failure in patients with previously treated non-small cell lung cancer harboring EGFR mutation.Cancer chemotherapy and pharmacology, , Volume: 83, Issue:5, 2019
First-line afatinib vs gefitinib for patients with EGFR mutation-positive NSCLC (LUX-Lung 7): impact of afatinib dose adjustment and analysis of mode of initial progression for patients who continued treatment beyond progression.Journal of cancer research and clinical oncology, , Volume: 145, Issue:6, 2019
Afatinib With Pembrolizumab for Treatment of Patients With Locally Advanced/Metastatic Squamous Cell Carcinoma of the Lung: The LUX-Lung IO/KEYNOTE 497 Study Protocol.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
Acquired EGFR L718V Mutation and Loss of T790M-Mediated Resistance to Osimertinib in a Patient With NSCLC Who Responded to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:12, 2019
Afatinib in NSCLC With HER2 Mutations: Results of the Prospective, Open-Label Phase II NICHE Trial of European Thoracic Oncology Platform (ETOP).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
From Diagnostic-Therapeutic Pathways to Real-World Data: A Multicenter Prospective Study on Upfront Treatment for The oncologist, , Volume: 24, Issue:6, 2019
Afatinib Overcomes Pemetrexed-Acquired Resistance in Non-Small Cell Lung Cancer Cells Harboring an EML4-ALK Rearrangement.Cells, , 11-28, Volume: 8, Issue:12, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.Scientific reports, , 12-03, Volume: 9, Issue:1, 2019
Strategies to overcome acquired resistance to EGFR TKI in the treatment of non-small cell lung cancer.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 21, Issue:10, 2019
Different incidence of interstitial lung disease according to different kinds of EGFR-tyrosine kinase inhibitors administered immediately before and/or after anti-PD-1 antibodies in lung cancer.Thoracic cancer, , Volume: 10, Issue:4, 2019
Phase 1 trial of dasatinib combined with afatinib for epidermal growth factor receptor- (EGFR-) mutated lung cancer with acquired tyrosine kinase inhibitor (TKI) resistance.British journal of cancer, , Volume: 120, Issue:8, 2019
Repeat biopsy procedures and T790M rates after afatinib, gefitinib, or erlotinib therapy in patients with lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 130, 2019
Duration of treatment among patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive non-small-cell lung cancer in the USA.Future oncology (London, England), , Volume: 15, Issue:13, 2019
Identification of a Novel MET Exon 14 Skipping Variant Coexistent with EGFR Mutation in Lung Adenocarcinoma Sensitive to Combined Treatment with Afatinib and Crizotinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:4, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Clinical analysis of EGFR-positive non-small cell lung cancer patients treated with first-line afatinib: A Nagano Lung Cancer Research Group.Thoracic cancer, , Volume: 10, Issue:5, 2019
Clinical significance of monitoring EGFR mutation in plasma using multiplexed digital PCR in EGFR mutated patients treated with afatinib (West Japan Oncology Group 8114LTR study).Lung cancer (Amsterdam, Netherlands), , Volume: 131, 2019
Real-world study of afatinib in first-line or re-challenge settings for patients with EGFR mutant non-small cell lung cancer.Medical oncology (Northwood, London, England), , May-14, Volume: 36, Issue:6, 2019
Efficacy and safety of afatinib in a Chinese population with advanced lung adenocarcinoma with sensitive EGFR mutations.Thoracic cancer, , Volume: 10, Issue:6, 2019
Sequencing of therapy following first-line afatinib in patients with EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 132, 2019
The Evolutionary Difference Between Extracranial Lesions and Leptomeningeal Metastasis in a Patient With Afatinib-Resistant Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Cx32 mediates norepinephrine-promoted EGFR-TKI resistance in a gap junction-independent manner in non-small-cell lung cancer.Journal of cellular physiology, , Volume: 234, Issue:12, 2019
Outcome Differences Between First- and Second-generation EGFR Inhibitors in Advanced EGFR Mutated NSCLC in a Large Population-based Cohort.Clinical lung cancer, , Volume: 20, Issue:5, 2019
Efficacy of afatinib treatment for lung adenocarcinoma harboring exon 18 delE709_T710insD mutation.Japanese journal of clinical oncology, , Aug-01, Volume: 49, Issue:8, 2019
First-line afatinib for advanced EGFRm+ NSCLC: Analysis of long-term responders in the LUX-Lung 3, 6, and 7 trials.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Afatinib is effective in the treatment of lung adenocarcinoma with uncommon EGFR p.L747P and p.L747S mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Cardiac Toxicity From Afatinib in EGFR-Mutated NSCLC: A Rare But Possible Side Effect.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:7, 2019
Monomer Preference of EGFR Tyrosine Kinase Inhibitors Influences the Synergistic Efficacy of Combination Therapy with Cetuximab.Molecular cancer therapeutics, , Volume: 18, Issue:9, 2019
The dual PI3K/mTOR inhibitor BEZ235 restricts the growth of lung cancer tumors regardless of EGFR status, as a potent accompanist in combined therapeutic regimens.Journal of experimental & clinical cancer research : CR, , Jul-01, Volume: 38, Issue:1, 2019
Which Is Better EGFR-TKI Followed by Osimertinib: Afatinib or Gefitinib/Erlotinib?Anticancer research, , Volume: 39, Issue:7, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
Small Cell Lung Cancer Derived from Adenocarcinoma with Mutant Epidermal Growth Factor Receptor Provides a Signature of Transcriptional Alteration in Tumor Cells.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 58, Issue:22, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
A phase Ib study of the combination of afatinib and ruxolitinib in EGFR mutant NSCLC with progression on EGFR-TKIs.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
A phase II study of low starting dose of afatinib as first-line treatment in patients with EGFR mutation-positive non-small-cell lung cancer (KTORG1402).Lung cancer (Amsterdam, Netherlands), , Volume: 135, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
Real-world experience of first-line afatinib in patients with EGFR-mutant advanced NSCLC: a multicenter observational study.BMC cancer, , Sep-09, Volume: 19, Issue:1, 2019
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Acquired Resistance of MET-Amplified Non-small Cell Lung Cancer Cells to the MET Inhibitor Capmatinib.Cancer research and treatment, , Volume: 51, Issue:3, 2019
Cost-utility of afatinib and gefitinib as first-line treatment for EGFR-mutated advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:2, 2019
[Comparison of Effectiveness of Gefitinib, Erlotinib, and Afatinib in Advanced Non-small Cell Lung Cancer Patients with EGFR Mutation Positive in Indonesian Population].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , 09-20, Volume: 22, Issue:9, 2019
Successful Treatment of a Patient With NSCLC Harboring an EGFR Mutation and a Concomitant Met Exon 14 Skipping Mutation Combining Afatinib and Crizotinib.Clinical lung cancer, , Volume: 20, Issue:1, 2019
Fingolimod augments Pemetrexed killing of non-small cell lung cancer and overcomes resistance to ERBB inhibition.Cancer biology & therapy, , Volume: 20, Issue:5, 2019
Durable Response of Low-Dose Afatinib plus Cetuximab in an Adenocarcinoma Patient with a Novel EGFR Exon 20 Insertion Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:10, 2019
Bilateral Ulcerative Keratitis Associated With Afatinib Treatment for Non-Small-cell Lung Carcinoma.Cornea, , Volume: 38, Issue:3, 2019
Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib.Cancer research and treatment, , Volume: 51, Issue:2, 2019
Impact of Exon 19 Deletion Subtypes in EGFR-Mutant Metastatic Non-Small-Cell Lung Cancer Treated With First-Line Tyrosine Kinase Inhibitors.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Potential for afatinib as an optimal treatment for advanced non-small cell lung carcinoma in patients with uncommon EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Dual blockade of EGFR tyrosine kinase using osimertinib and afatinib eradicates EGFR‑mutant Ba/F3 cells.Oncology reports, , Volume: 41, Issue:2, 2019
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Phase 2 Study of Afatinib Alone or Combined With Bevacizumab in Chemonaive Patients With Advanced Non-Small-Cell Lung Cancer Harboring EGFR Mutations: AfaBev-CS Study Protocol.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Afatinib in Osimertinib-Resistant EGFR ex19del/T790M/P794L Mutated NSCLC.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:9, 2018
Effects of secondary EGFR mutations on resistance against upfront osimertinib in cells with EGFR-activating mutations in vitro.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Efficacy of thoracic radiotherapy in patients with stage IIIB-IV epidermal growth factor receptor-mutant lung adenocarcinomas who received and responded to tyrosine kinase inhibitor treatment.Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, , Volume: 129, Issue:1, 2018
Identification of Mutation Accumulation as Resistance Mechanism Emerging in First-Line Osimertinib Treatment.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer.Nature medicine, , Volume: 24, Issue:5, 2018
Afatinib in heavily pretreated advanced NSCLC patients who progressed following prior gefitinib or erlotinib: Compassionate use program in Korea.Lung cancer (Amsterdam, Netherlands), , Volume: 119, 2018
Afatinib as First-line Treatment of Older Patients With EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Subgroup Analyses of the LUX-Lung 3, LUX-Lung 6, and LUX-Lung 7 Trials.Clinical lung cancer, , Volume: 19, Issue:4, 2018
Cost effectiveness analysis of afatinib versus pemetrexed-cisplatin for first-line treatment of locally advanced or metastatic EGFR mutation positive non-small-cell lung cancer from the Singapore healthcare payer's perspective.BMC cancer, , 03-27, Volume: 18, Issue:1, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Mechanisms of acquired resistance to afatinib clarified with liquid biopsy.PloS one, , Volume: 13, Issue:12, 2018
Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 118, 2018
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
Efficacy generated by afatinib in a lung adenocarcinoma patient harboring HER2 S310Y mutation.Cancer biology & therapy, , 06-03, Volume: 19, Issue:6, 2018
Cardiovascular safety of novel non-small cell lung cancer oncotherapy in a patient treated with novel generations of tyrosine kinase inhibitors.Kardiologia polska, , Volume: 76, Issue:3, 2018
Successful treatment with an EGFR tyrosine kinase inhibitor Afatinib in a patient with combined small-cell lung Cancer with EGFR mutation.Investigational new drugs, , Volume: 36, Issue:4, 2018
Therapeutic strategies for afatinib-resistant lung cancer harboring HER2 alterations.Cancer science, , Volume: 109, Issue:5, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Case sharing of a patient re-challenged with afatinib for EGFR-mutated advanced non-small cell lung cancer.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Best Response According to RECIST During First-line EGFR-TKI Treatment Predicts Survival in EGFR Mutation-positive Non-Small-cell Lung Cancer Patients.Clinical lung cancer, , Volume: 19, Issue:3, 2018
The clinical features of squamous cell lung carcinoma with sensitive EGFR mutations.International journal of clinical oncology, , Volume: 23, Issue:3, 2018
A phase I study of afatinib for patients aged 75 or older with advanced non-small cell lung cancer harboring EGFR mutations.Medical oncology (Northwood, London, England), , Feb-08, Volume: 35, Issue:3, 2018
EGFR-mediated interleukin enhancer-binding factor 3 contributes to formation and survival of cancer stem-like tumorspheres as a therapeutic target against EGFR-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 116, 2018
Improvement of erosive pustular dermatosis of the scalp following discontinuation of chemotherapy with afatinib.European journal of dermatology : EJD, , 04-01, Volume: 28, Issue:2, 2018
Global named patient use program of afatinib in advanced non-small-cell lung carcinoma patients who progressed following prior therapies.Future oncology (London, England), , Volume: 14, Issue:15, 2018
Stevens-Johnson syndrome/toxic epidermal necrolysis overlap in a NSCLC patient treated with afatinib.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG, , Volume: 16, Issue:2, 2018
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
A phase I trial of afatinib and bevacizumab in chemo-naïve patients with advanced non-small-cell lung cancer harboring EGFR mutations: Okayama Lung Cancer Study Group Trial 1404.Lung cancer (Amsterdam, Netherlands), , Volume: 115, 2018
Utilization of Molecular Testing and Survival Outcomes of Treatment with First- or Second-line Tyrosine Kinase Inhibitors in Advanced Non-small Cell Lung Cancer in a Dutch Population.Anticancer research, , Volume: 38, Issue:1, 2018
Acquired Resistance to Afatinib Due to T790M-Positive Squamous Progression in EGFR-Mutant Adenosquamous Lung Carcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
Efficacy of Afatinib in a Previously-Treated Patient with Non-Small Cell Lung Cancer Harboring HER2 Mutation: Case Report.Journal of Korean medical science, , Jan-01, Volume: 33, Issue:1, 2018
Does EGFR Mutation Type Influence Patient-Reported Outcomes in Patients with Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer? Analysis of Two Large, Phase III Studies Comparing Afatinib with Chemotherapy (LUX-Lung 3 and LUX-Lung 6).The patient, , Volume: 11, Issue:1, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Therapeutic Potential of Afatinib for Cancers with The oncologist, , Volume: 23, Issue:2, 2018
Afatinib treatment of a squamous lung cancer after tumor progression of nivolumab.Thoracic cancer, , Volume: 9, Issue:1, 2018
[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
Symptom and Quality of Life Improvement in LUX-Lung 8, an Open-Label Phase III Study of Second-Line Afatinib Versus Erlotinib in Patients With Advanced Squamous Cell Carcinoma of the Lung After First-Line Platinum-Based Chemotherapy.Clinical lung cancer, , Volume: 19, Issue:1, 2018
An Evolving Algorithm to Select and Sequence Therapies in EGFR Mutation-positive NSCLC: A Strategic Approach.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Afatinib Decreases P-Glycoprotein Expression to Promote Adriamycin Toxicity of A549T Cells.Journal of cellular biochemistry, , Volume: 119, Issue:1, 2018
Therapeutic Strategies in EGFR Mutant Non-Small Cell Lung Cancer.Current treatment options in oncology, , 09-29, Volume: 19, Issue:11, 2018
A phase II trial of EGFR-TKI readministration with afatinib in advanced non-small-cell lung cancer harboring a sensitive non-T790M EGFR mutation: Okayama Lung Cancer Study Group trial 1403.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
[Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Sep-20, Volume: 21, Issue:9, 2018
Exploration of resistance mechanisms for epidermal growth factor receptor-tyrosine kinase inhibitors based on plasma analysis by digital polymerase chain reaction and next-generation sequencing.Cancer science, , Volume: 109, Issue:12, 2018
Real Clinical Practice of Using Afatinib Therapy in NSCLC Patients with an Acquired Anticancer research, , Volume: 38, Issue:9, 2018
An observational study of the epidermal growth factor receptor-tyrosine kinase inhibitor resistance mechanism in epidermal growth factor receptor gene mutation-positive non-small cell lung cancer.Medicine, , Volume: 97, Issue:40, 2018
Afatinib plus bevacizumab combination after acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant non-small cell lung cancer: Multicenter, single-arm, phase 2 trial (ABC Study).Cancer, , 10-01, Volume: 124, Issue:19, 2018
Ankyrin Repeat Domain 1 Overexpression is Associated with Common Resistance to Afatinib and Osimertinib in EGFR-mutant Lung Cancer.Scientific reports, , 10-05, Volume: 8, Issue:1, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Activity of Afatinib in Heavily Pretreated Patients With ERBB2 Mutation-Positive Advanced NSCLC: Findings From a Global Named Patient Use Program.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Sequential treatment with afatinib and osimertinib in patients with EGFR mutation-positive non-small-cell lung cancer: an observational study.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Phase I Study Evaluating the Combination of Afatinib with Carboplatin and Pemetrexed After First-line EGFR-TKIs.Anticancer research, , Volume: 38, Issue:8, 2018
Overview of the LUX-Lung clinical trial program of afatinib for non-small cell lung cancer.Cancer treatment reviews, , Volume: 69, 2018
Sensitivity of epidermal growth factor receptor with single or double uncommon mutations to afatinib confirmed by a visual assay.Cancer science, , Volume: 109, Issue:11, 2018
Primary Resistance to Afatinib in a Patient with Lung Adenocarcinoma Harboring Uncommon EGFR Mutations: S768I and V769L.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
Afatinib restrains K-RAS-driven lung tumorigenesis.Science translational medicine, , 06-20, Volume: 10, Issue:446, 2018
Irreversible tyrosine kinase inhibition of epidermal growth factor receptor with afatinib in Current oncology (Toronto, Ont.), , Volume: 25, Issue:Suppl 1, 2018
Afatinib and Erlotinib in the treatment of squamous-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 19, Issue:18, 2018
Relationship between Paronychia and Drug Concentrations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.Oncology, , Volume: 95, Issue:4, 2018
In Search of an Oncogene Driver for Squamous Lung Cancer.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Association of ERBB Mutations With Clinical Outcomes of Afatinib- or Erlotinib-Treated Patients With Lung Squamous Cell Carcinoma: Secondary Analysis of the LUX-Lung 8 Randomized Clinical Trial.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Anti-tumor activity of Shikonin against afatinib resistant non-small cell lung cancer via negative regulation of PI3K/Akt signaling pathway.Bioscience reports, , 12-21, Volume: 38, Issue:6, 2018
Economic analysis of osimertinib in previously untreated EGFR-mutant advanced non-small cell lung cancer in Canada.Lung cancer (Amsterdam, Netherlands), , Volume: 125, 2018
Afatinib with subsequent surgery in stage III NSCLC with EGFR mutation: Lessons learned from two clinical experiences.Tumori, , Volume: 104, Issue:6, 2018
Afatinib in advanced pretreated non-small-cell lung cancer- a Canadian experience.Current oncology (Toronto, Ont.), , Volume: 25, Issue:5, 2018
Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the EGFR inhibitors afatinib, erlotinib and osimertinib, the ALK inhibitor crizotinib and the VEGFR inhibitor nintedanib in human plasma from non-small cell lung cancJournal of pharmaceutical and biomedical analysis, , Sep-05, Volume: 158, 2018
Osimertinib for Secondary T790M-Mutation-Positive Squamous Cell Carcinoma Transformation After Afatinib Failure.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Cost-effectiveness of Osimertinib in the First-Line Treatment of Patients With EGFR-Mutated Advanced Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Budget Impact Analysis of Afatinib for First-Line Treatment of Patients with Metastatic Non-Small Cell Lung Cancer with Epidermal Growth Factor Receptor Exon 19 Deletions or Exon 21 Substitution Mutations in a U.S. Health Plan.Journal of managed care & specialty pharmacy, , Volume: 24, Issue:6, 2018
Miliary Adenocarcinoma of the Lung Responds to Gefitinib and Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
EGFR exon 18 DelE709_T710insD as an Acquired Resistance Mechanism to Afatinib in an Advanced EGFR exon 18 E709H Lung Adenocarcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Influence of afatinib dose on outcomes of advanced EGFR-mutant NSCLC patients with brain metastases.BMC cancer, , Dec-03, Volume: 18, Issue:1, 2018
The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.BMC pharmacology & toxicology, , 12-13, Volume: 18, Issue:1, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.Science translational medicine, , Nov-08, Volume: 9, Issue:415, 2017
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Appendix 7: Metastatic non-small-cell lung cancer (1): MCBS eUpdate published online 28 June 2017 (www.esmo.org/Guidelines/Lung-and-Chest-Tumours).Annals of oncology : official journal of the European Society for Medical Oncology, , Jul-01, Volume: 28, Issue:suppl_4, 2017
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.Anticancer research, , Volume: 37, Issue:9, 2017
Overall survival in EGFR mutated non-small-cell lung cancer patients treated with afatinib after EGFR TKI and resistant mechanisms upon disease progression.PloS one, , Volume: 12, Issue:8, 2017
Malignant Pleural Mesothelioma Harboring Both G719C and S768I Mutations of EGFR Successfully Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:9, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
YM155 as an inhibitor of cancer stemness simultaneously inhibits autophosphorylation of epidermal growth factor receptor and G9a-mediated stemness in lung cancer cells.PloS one, , Volume: 12, Issue:8, 2017
Cost-Effectiveness Analysis of Afatinib versus Gefitinib for First-Line Treatment of Advanced EGFR-Mutated Advanced Non-Small Cell Lung Cancers.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:10, 2017
Case series on the association between blood levels and side effects of afatinib maleate.Cancer chemotherapy and pharmacology, , Volume: 80, Issue:3, 2017
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
The Effect of Afatinib Treatment in Non-small Cell Lung Cancer Cells.Anticancer research, , Volume: 37, Issue:7, 2017
Update on afatinib-based combination regimens for the treatment of EGFR mutation-positive non-small-cell lung cancer.Future oncology (London, England), , Volume: 13, Issue:21, 2017
Matrine increases the inhibitory effects of afatinib on H1975 cells via the IL‑6/JAK1/STAT3 signaling pathway.Molecular medicine reports, , Volume: 16, Issue:3, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
A phase Ib trial of continuous once-daily oral afatinib plus sirolimus in patients with epidermal growth factor receptor mutation-positive non-small cell lung cancer and/or disease progression following prior erlotinib or gefitinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Association Between EGFR T790M Status and Progression Patterns During Initial EGFR-TKI Treatment in Patients Harboring EGFR Mutation.Clinical lung cancer, , Volume: 18, Issue:6, 2017
Evaluation of the VeriStratLung cancer (Amsterdam, Netherlands), , Volume: 109, 2017
Purpuric Drug Eruptions Caused by Epidermal Growth Factor Receptor Inhibitors for Non-Small Cell Lung Cancer: A Clinicopathologic Study of 32 Cases.JAMA dermatology, , 09-01, Volume: 153, Issue:9, 2017
Activation of signal transducer and activator of transcription 3 (STAT3) signaling in EGFR mutant non-small-cell lung cancer (NSCLC).Oncotarget, , Jul-18, Volume: 8, Issue:29, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
Second-line therapy of squamous non-small cell lung cancer: an evolving landscape.Expert review of respiratory medicine, , Volume: 11, Issue:6, 2017
Therapeutic Efficacy Comparison of 5 Major EGFR-TKIs in Advanced EGFR-positive Non-Small-cell Lung Cancer: A Network Meta-analysis Based on Head-to-Head Trials.Clinical lung cancer, , Volume: 18, Issue:5, 2017
Recent Management of Patients with Advanced Epidermal Growth Factor Receptor Mutation Non-small Cell Lung Cancer: Role of Afatinib and Lesson Learned for Developing Countries.Acta medica Indonesiana, , Volume: 49, Issue:1, 2017
Afatinib versus gefitinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: overall survival data from the phase IIb LUX-Lung 7 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , 02-01, Volume: 28, Issue:2, 2017
Efficacy of continuous EGFR-inhibition and role of Hedgehog in EGFR acquired resistance in human lung cancer cells with activating mutation of EGFR.Oncotarget, , Apr-04, Volume: 8, Issue:14, 2017
Triplet therapy with afatinib, cetuximab, and bevacizumab induces deep remission in lung cancer cells harboring EGFR T790M in vivo.Molecular oncology, , Volume: 11, Issue:6, 2017
Prognostic value of early response assessment using (18F)FDG-PET in patients with advanced non-small cell lung cancer treated with tyrosine-kinase inhibitors.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 65, Issue:5, 2017
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 23, Issue:3, 2017
Phase II Study of the EGFR-TKI Rechallenge With Afatinib in Patients With Advanced NSCLC Harboring Sensitive EGFR Mutation Without T790M: Okayama Lung Cancer Study Group Trial OLCSG 1403.Clinical lung cancer, , Volume: 18, Issue:2, 2017
Variations in EGFR ctDNA Correlates to the Clinical Efficacy of Afatinib in Non Small Cell Lung Cancer with Acquired Resistance.Pathology oncology research : POR, , Volume: 23, Issue:2, 2017
Overcoming EGFR Bypass Signal-Induced Acquired Resistance to ALK Tyrosine Kinase Inhibitors in ALK-Translocated Lung Cancer.Molecular cancer research : MCR, , Volume: 15, Issue:1, 2017
The European Society for Medical Oncology Magnitude of Clinical Benefit Scale (ESMO-MCBS) applied to pivotal phase III randomized-controlled trials of tyrosine kinase inhibitors in first-line for advanced non-small cell lung cancer with activating epidermExpert review of pharmacoeconomics & outcomes research, , Volume: 17, Issue:1, 2017
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Advanced non-small cell lung cancer (NSCLC) with activating EGFR mutations: first-line treatment with afatinib and other EGFR TKIs.Expert review of anticancer therapy, , Volume: 17, Issue:2, 2017
Successful afatinib treatment of advanced non-small-cell lung cancer patients undergoing hemodialysis.Cancer chemotherapy and pharmacology, , Volume: 79, Issue:1, 2017
HER2 Transmembrane Domain (TMD) Mutations (V659/G660) That Stabilize Homo- and Heterodimerization Are Rare Oncogenic Drivers in Lung Adenocarcinoma That Respond to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:3, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer.Molecular cancer therapeutics, , Volume: 16, Issue:2, 2017
Rapid Acquisition of T790M Mutation after Treatment with Afatinib in an NSCLC Patient Harboring EGFR Exon 20 S768I Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:1, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
Risk of Treatment-Related Toxicities from EGFR Tyrosine Kinase Inhibitors: A Meta-analysis of Clinical Trials of Gefitinib, Erlotinib, and Afatinib in Advanced EGFR-Mutated Non-Small Cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.Respiratory investigation, , Volume: 55, Issue:1, 2017
EGFR L858M/L861Q cis Mutations Confer Selective Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
Randomized Phase II Study of Afatinib Plus Simvastatin Versus Afatinib Alone in Previously Treated Patients with Advanced Nonadenocarcinomatous Non-small Cell Lung Cancer.Cancer research and treatment, , Volume: 49, Issue:4, 2017
Novel EGFR Exon 18 (G721R) Mutation in a Patient with Non-Small Cell Lung Carcinoma with Lack of Response to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
[Precision first-line therapy for advanced non-small-cell lung cancer patients harboring EGFR mutation].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Feb-23, Volume: 39, Issue:2, 2017
Chronic myelomonocytic leukemia blast crisis in a patient with advanced non-small cell lung cancer treated with EGFR tyrosine kinase inhibitors.Respiratory investigation, , Volume: 55, Issue:2, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.Clinical drug investigation, , Volume: 37, Issue:6, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells.Molecular carcinogenesis, , Volume: 55, Issue:5, 2016
Tyrosine kinase inhibitors for epidermal growth factor receptor gene mutation-positive non-small cell lung cancers: an update for recent advances in therapeutics.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 22, Issue:3, 2016
Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors.Critical reviews in oncology/hematology, , Volume: 97, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer.Biomedical chromatography : BMC, , Volume: 30, Issue:7, 2016
Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations.Cancer science, , Volume: 107, Issue:1, 2016
Risk of elevated transaminases in non-small cell lung cancer (NSCLC) patients treated with erlotinib, gefitinib and afatinib: a meta-analysis.Expert review of respiratory medicine, , Volume: 10, Issue:2, 2016
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with erlotinib: a case report.Anti-cancer drugs, , Volume: 27, Issue:3, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
Different EGFR Gene Mutations in Exon 18, 19 and 21 as Prognostic and Predictive Markers in NSCLC: A Single Institution Analysis.Molecular diagnosis & therapy, , Volume: 20, Issue:1, 2016
Afatinib beyond progression in patients with non-small-cell lung cancer following chemotherapy, erlotinib/gefitinib and afatinib: phase III randomized LUX-Lung 5 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:3, 2016
Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer.JAMA dermatology, , Volume: 152, Issue:3, 2016
A Phase Ib/II Study of Afatinib in Combination with Nimotuzumab in Non-Small Cell Lung Cancer Patients with Acquired Resistance to Gefitinib or Erlotinib.Clinical cancer research : an official journal of the American Association for Cancer Research, , 05-01, Volume: 22, Issue:9, 2016
Afatinib and chemotherapy in non-small-cell lung cancer.The Lancet. Oncology, , Volume: 17, Issue:2, 2016
Epidermal growth factor receptor tyrosine kinase inhibitors in previously treated advanced non-small-cell lung cancer with wild-type EGFR.Expert opinion on pharmacotherapy, , Volume: 17, Issue:2, 2016
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1, 2016
First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
Resistance mechanisms after tyrosine kinase inhibitors afatinib and crizotinib in non-small cell lung cancer, a review of the literature.Critical reviews in oncology/hematology, , Volume: 100, 2016
The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients.Oncotarget, , Mar-15, Volume: 7, Issue:11, 2016
therascreen® EGFR RGQ PCR Kit: A Companion Diagnostic for Afatinib and Gefitinib in Non-Small Cell Lung Cancer.Molecular diagnosis & therapy, , Volume: 20, Issue:2, 2016
Efficacy and safety of afatinib in Chinese patients with EGFR-mutated metastatic non-small-cell lung cancer (NSCLC) previously responsive to first-generation tyrosine-kinase inhibitors (TKI) and chemotherapy: comparison with historical cohort using erlotiBMC cancer, , Feb-24, Volume: 16, 2016
Afatinib in the first-line treatment of epidermal-growth-factor-receptor mutation-positive non-small cell lung cancer: a review of the clinical evidence.Therapeutic advances in respiratory disease, , Volume: 10, Issue:3, 2016
The afatinib resistance of in vivo generated H1975 lung cancer cell clones is mediated by SRC/ERBB3/c-KIT/c-MET compensatory survival signaling.Oncotarget, , Apr-12, Volume: 7, Issue:15, 2016
Selectivity profile of afatinib for EGFR-mutated non-small-cell lung cancer.Molecular bioSystems, , 04-26, Volume: 12, Issue:5, 2016
Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:6, 2016
Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience.Cancer chemotherapy and pharmacology, , Volume: 77, Issue:5, 2016
Inequalities in lung cancer: a world of EGFR.The European respiratory journal, , Volume: 47, Issue:5, 2016
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Afatinib-associated Stevens-Johnson syndrome in an EGFR-mutated lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 95, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
A Triple Rare E709K and L833V/H835L EGFR Mutation Responsive to an Irreversible Pan-HER Inhibitor: A Case Report of Lung Adenocarcinoma Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:5, 2016
Stevens-Johnson syndrome-like erosive dermatitis possibly related to afatinib.European journal of dermatology : EJD, , Aug-01, Volume: 26, Issue:4, 2016
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , May-25, Issue:5, 2016
Kinases inhibitors in lung cancer: From benchside to bedside.Biochimica et biophysica acta, , Volume: 1866, Issue:1, 2016
Evaluation of assays for drug efficacy in a three-dimensional model of the lung.Journal of cancer research and clinical oncology, , Volume: 142, Issue:9, 2016
[Not Available].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Current status of EGFR/ErbB inhibitors in non-small cell lung carcinoma].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Mechanism of action and preclinical development of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib as first-line therapy in mutation-positive EGFR. Results by type of mutation].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Evidence on afatinib in patients progressing on a first-line treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20, 2016
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:11, 2016
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
The safety of afatinib for the treatment of non-small cell lung cancer.Expert opinion on drug safety, , Volume: 15, Issue:11, 2016
Case report: Durable response to afatinib in a patient with lung cancer harboring two uncommon mutations of EGFR and a KRAS mutation.Lung cancer (Amsterdam, Netherlands), , Volume: 101, 2016
Survival of Lung Adenocarcinoma Patients Predicted from Expression of PD-L1, Galectin-9, and XAGE1 (GAGED2a) on Tumor Cells and Tumor-Infiltrating T Cells.Cancer immunology research, , Volume: 4, Issue:12, 2016
Afatinib: A Review in Advanced Non-Small Cell Lung Cancer.Targeted oncology, , Volume: 11, Issue:6, 2016
Clinical analysis of patients treated with afatinib for advanced non-small cell lung cancer: A Nagano Lung Cancer Research Group observational study.Respiratory investigation, , Volume: 54, Issue:6, 2016
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
[The efficacy of TKIs in treatment of human primary small cell lung cancer xenograft model in vivo].Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology, , Jun-08, Volume: 32, Issue:6, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Prolonged survival with erlotinib followed by afatinib in a caucasian smoker with metastatic, poorly differentiated large cell carcinoma of the lung: a case report.Cancer biology & therapy, , Volume: 16, Issue:10, 2015
Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.The oncologist, , Volume: 20, Issue:8, 2015
Afatinib versus erlotinib as second-line treatment of patients with advanced squamous cell carcinoma of the lung (LUX-Lung 8): an open-label randomised controlled phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:8, 2015
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
Afatinib induces apoptosis in NSCLC without EGFR mutation through Elk-1-mediated suppression of CIP2A.Oncotarget, , Feb-10, Volume: 6, Issue:4, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy, , Volume: 29, Issue:3, 2015
[Is chemotherapy still an option in oncogene-addicted non-small cell lung cancer? No].Bulletin du cancer, , Volume: 102, Issue:6 Suppl 1, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6.The Lancet. Oncology, , Volume: 16, Issue:7, 2015
Successful Afatinib Therapy after Resistance to EGFR-TKI in a Patient with Advanced Adenosquamous Cell Lung Cancer.Oncology research and treatment, , Volume: 38, Issue:6, 2015
Afatinib (Gilotrif) for advanced non-small cell lung cancer.The Medical letter on drugs and therapeutics, , May-25, Volume: 57, Issue:1469, 2015
[Hange-Shashin-to for preventing diarrhea during afatinib therapy].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:5, 2015
Symptom and Quality of Life Improvement in LUX-Lung 6: An Open-Label Phase III Study of Afatinib Versus Cisplatin/Gemcitabine in Asian Patients With EGFR Mutation-Positive Advanced Non-small-cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:6, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in EGFR FISH-positive non-small-cell lung cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:4, 2015
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
Overcoming Resistance Without the Risk of Reaction: Use of Afatinib and Panitumumab in Two Cases of Epidermal Growth Factor Receptor--Mutated Non--Small-Cell Lung Cancer With T790M Mutations.Clinical lung cancer, , Volume: 16, Issue:5, 2015
Risk of fatal pulmonary events in patients with advanced non-small-cell lung cancer treated with EGF receptor tyrosine kinase inhibitors: a comparative meta-analysis.Future oncology (London, England), , Volume: 11, Issue:7, 2015
Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.The oncologist, , Volume: 20, Issue:4, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
[Pharmacological and clinical profile of afatinib (Giotrif®)].Nihon yakurigaku zasshi. Folia pharmacologica Japonica, , Volume: 145, Issue:2, 2015
Afatinib increases sensitivity to radiation in non-small cell lung cancer cells with acquired EGFR T790M mutation.Oncotarget, , Mar-20, Volume: 6, Issue:8, 2015
Optimizing the sequence of anti-EGFR-targeted therapy in EGFR-mutant lung cancer.Molecular cancer therapeutics, , Volume: 14, Issue:2, 2015
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Long progression-free survival with afatinib in a patient with EGFR-unknown lung adenocarcinoma after erlotinib failure: a case report.Tumori, , Apr-28, Volume: 101, Issue:2, 2015
Afatinib resistance in non-small cell lung cancer involves the PI3K/AKT and MAPK/ERK signalling pathways and epithelial-to-mesenchymal transition.Targeted oncology, , Volume: 10, Issue:3, 2015
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.Expert opinion on drug safety, , Volume: 14, Issue:1, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
The combination of irreversible EGFR TKIs and SAHA induces apoptosis and autophagy-mediated cell death to overcome acquired resistance in EGFR T790M-mutated lung cancer.International journal of cancer, , Jun-01, Volume: 136, Issue:11, 2015
CD133-Positive Cells from Non-Small Cell Lung Cancer Show Distinct Sensitivity to Cisplatin and Afatinib.Archivum immunologiae et therapiae experimentalis, , Volume: 63, Issue:3, 2015
Common EGFR-mutated subgroups (Del19/L858R) in advanced non-small-cell lung cancer: chasing better outcomes with tyrosine kinase inhibitors.Future oncology (London, England), , Volume: 11, Issue:8, 2015
Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Afatinib: a second-generation EGF receptor and ErbB tyrosine kinase inhibitor for the treatment of advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 11, Issue:18, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
Managing acquired resistance in EGFR-mutated non-small cell lung cancer.Clinical advances in hematology & oncology : H&O, , Volume: 13, Issue:8, 2015
Afatinib in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations Pretreated With Reversible EGFR Inhibitors.The oncologist, , Volume: 20, Issue:10, 2015
Cost-Effectiveness and Value of Information of Erlotinib, Afatinib, and Cisplatin-Pemetrexed for First-Line Treatment of Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer in the United States.Value in health : the journal of the International Society for Pharmacoeconomics and Outcomes Research, , Volume: 18, Issue:6, 2015
The pan-HER family tyrosine kinase inhibitor afatinib overcomes HER3 ligand heregulin-mediated resistance to EGFR inhibitors in non-small cell lung cancer.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Current and Emerging Options in the Management of EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Considerations in the Elderly.Drugs & aging, , Volume: 32, Issue:11, 2015
[Bufalin reverses hepatocyte growth factor-induced resistance to afatinib in H1975 lung cancer cells].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 37, Issue:7, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.British journal of cancer, , Nov-17, Volume: 113, Issue:10, 2015
HER2 insertion YVMA mutant lung cancer: Long natural history and response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 90, Issue:3, 2015
[Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis].Voprosy onkologii, , Volume: 61, Issue:4, 2015
Effects of cetuximab combined with afatinib on the expression of KDR and AQP1 in lung cancer.Genetics and molecular research : GMR, , Dec-11, Volume: 14, Issue:4, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
EGFR Kinase Domain Duplication (EGFR-KDD) Is a Novel Oncogenic Driver in Lung Cancer That Is Clinically Responsive to Afatinib.Cancer discovery, , Volume: 5, Issue:11, 2015
Cumulative meta-analysis of epidermal growth factor receptor-tyrosine kinase inhibitors as first-line therapy in metastatic non-small-cell lung cancer.Anti-cancer drugs, , Volume: 26, Issue:9, 2015
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
Practical Value of Molecular Pathology in Stage I-III Lung Cancer: Implications for the Clinical Surgeon.Annals of surgical oncology, , Volume: 22, Issue:11, 2015
EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs.Clinical cancer research : an official journal of the American Association for Cancer Research, , Dec-01, Volume: 21, Issue:23, 2015
LUX-Lung: determining the best EGFR inhibitor in NSCLC?The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Acquisition of cancer stem cell-like properties in non-small cell lung cancer with acquired resistance to afatinib.Cancer science, , Volume: 106, Issue:10, 2015
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
[Effect of EGFR-TKI on lymphangiogenesis of lung cancer with EGFR mutation].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:12, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
Next generation tyrosine kinase inhibitor (TKI): afatinib.Recent patents on anti-cancer drug discovery, , Volume: 9, Issue:3, 2014
Ten lessons from EGFR.Respiratory investigation, , Volume: 52, Issue:3, 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Afatinib with concurrent radiotherapy in a patient with metastatic non-small cell lung cancer.Oncology research and treatment, , Volume: 37, Issue:5, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Phase II study of Afatinib as third-line treatment for patients in Korea with stage IIIB/IV non-small cell lung cancer harboring wild-type EGFR.The oncologist, , Volume: 19, Issue:7, 2014
[Afatinib (BIBW 2992)].Revue de pneumologie clinique, , Volume: 70, Issue:5, 2014
Gefitinib and afatinib treatment in an advanced non-small cell lung cancer (NSCLC) patient undergoing hemodialysis.Anticancer research, , Volume: 34, Issue:6, 2014
Afatinib in the treatment of EGFR mutation-positive NSCLC--a network meta-analysis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:2, 2014
Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, , Volume: 47, Issue:11, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
[A new perspective in the treatment of non-small-cell lung cancer (NSCLC). Role of afatinib: An oral and irreversible ErbB family blocker].Bulletin du cancer, , Volume: 101, Issue:6, 2014
Is progression-free survival associated with a better health-related quality of life in patients with lung cancer? Evidence from two randomised trials with afatinib.BMJ open, , Oct-31, Volume: 4, Issue:10, 2014
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Dual ALK and EGFR inhibition targets a mechanism of acquired resistance to the tyrosine kinase inhibitor crizotinib in ALK rearranged lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 83, Issue:1, 2014
Afatinib and lung cancer.Expert review of anticancer therapy, , Volume: 14, Issue:12, 2014
Dual inhibition of EGFR with afatinib and cetuximab in kinase inhibitor-resistant EGFR-mutant lung cancer with and without T790M mutations.Cancer discovery, , Volume: 4, Issue:9, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
The current state of molecularly targeted drugs targeting HGF/Met.Japanese journal of clinical oncology, , Volume: 44, Issue:1, 2014
FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor.Oncotarget, , Aug-15, Volume: 5, Issue:15, 2014
Afatinib: a review of its use in the treatment of advanced non-small cell lung cancer.Drugs, , Volume: 74, Issue:2, 2014
Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib for lung cancer: let there be light?The Lancet. Oncology, , Volume: 15, Issue:2, 2014
β-catenin contributes to lung tumor development induced by EGFR mutations.Cancer research, , Oct-15, Volume: 74, Issue:20, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Reply to F. De Marinis et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22, 2014
Reply to E.R. Haspinger et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Experience with afatinib in patients with non-small cell lung cancer progressing after clinical benefit from gefitinib and erlotinib.The oncologist, , Volume: 19, Issue:10, 2014
Subsequent treatment choices for patients with acquired resistance to EGFR-TKIs in non-small cell lung cancer: restore after a drug holiday or switch to another EGFR-TKI?Asian Pacific journal of cancer prevention : APJCP, , Volume: 15, Issue:1, 2014
Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations.PloS one, , Volume: 9, Issue:2, 2014
Systemic treatment in EGFR-ALK NSCLC patients: second line therapy and beyond.Expert review of anticancer therapy, , Volume: 14, Issue:7, 2014
Afatinib for the treatment of advanced non-small-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 15, Issue:6, 2014
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors.Clinical lung cancer, , Volume: 15, Issue:6, 2014
New therapy targets resistant non-small-cell lung cancers.Journal of the National Cancer Institute, , Volume: 106, Issue:11, 2014
Afatinib use in non-small cell lung cancer previously sensitive to epidermal growth factor receptor inhibitors: the United Kingdom Named Patient Programme.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:10, 2014
LUX-Lung 3: redundancy, toxicity or a major step forward? Afatinib as front-line therapy for patients with metastatic EGFR-mutated lung cancer.Future oncology (London, England), , Volume: 10, Issue:4, 2014
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
Meta-analysis of first-line therapies in advanced non-small-cell lung cancer harboring EGFR-activating mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 9, Issue:6, 2014
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
[About new treatments in thoracic oncology].Revue de pneumologie clinique, , Volume: 69, Issue:2, 2013
Afatinib prolongs survival compared with gefitinib in an epidermal growth factor receptor-driven lung cancer model.Molecular cancer therapeutics, , Volume: 12, Issue:5, 2013
Impact of EGFR inhibitor in non-small cell lung cancer on progression-free and overall survival: a meta-analysis.Journal of the National Cancer Institute, , May-01, Volume: 105, Issue:9, 2013
Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
Clinical perspective of afatinib in non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 81, Issue:2, 2013
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
New kinase inhibitor approved for metastatic lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Aug-15, Volume: 70, Issue:16, 2013
Targeted therapies: Afatinib--new therapy option for EGFR-mutant lung cancer.Nature reviews. Clinical oncology, , Volume: 10, Issue:10, 2013
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Afatinib: first global approval.Drugs, , Volume: 73, Issue:13, 2013
The role of afatinib in the management of non-small cell lung carcinoma.Expert opinion on drug metabolism & toxicology, , Volume: 9, Issue:11, 2013
Afatinib, erlotinib and gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: a review.Onkologie, , Volume: 36, Issue:9, 2013
Afatinib monotherapy in EGFR-mutant lung adenocarcinoma.The Lancet. Oncology, , Volume: 14, Issue:9, 2013
Afatinib for the treatment of patients with EGFR-positive non-small cell lung cancer.Drugs of today (Barcelona, Spain : 1998), , Volume: 49, Issue:9, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Ability of the Met kinase inhibitor crizotinib and new generation EGFR inhibitors to overcome resistance to EGFR inhibitors.PloS one, , Volume: 8, Issue:12, 2013
[Development and biochemical characterization of EGFR/c-Met dual inhibitors].Acta pharmaceutica Hungarica, , Volume: 83, Issue:4, 2013
An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 15, Issue:5, 2013
Symptom and quality of life benefit of afatinib in advanced non-small-cell lung cancer patients previously treated with erlotinib or gefitinib: results of a randomized phase IIb/III trial (LUX-Lung 1).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 8, Issue:2, 2013
Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.Biochemical and biophysical research communications, , Feb-15, Volume: 431, Issue:3, 2013
Strides in personalized medicine.Cancer, , Dec-01, Volume: 118, Issue:23, 2012
Disseminated herpes simplex virus infection following epidermal growth factor tyrosine kinase inhibitor therapy for non-small-cell lung carcinoma.Internal medicine journal, , Volume: 42, Issue:11, 2012
Epidermal growth factor receptor (EGFR) inhibitors and derived treatments.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 23 Suppl 10, 2012
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.Cancer research, , Nov-15, Volume: 72, Issue:22, 2012
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
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Monitoring reversible and irreversible EGFR inhibition with erlotinib and afatinib in a patient with EGFR-mutated non-small cell lung cancer (NSCLC) using sequential [18F]fluorothymidine (FLT-)PET.Lung cancer (Amsterdam, Netherlands), , Volume: 77, Issue:3, 2012
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
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EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
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Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.Lung cancer (Amsterdam, Netherlands), , Volume: 76, Issue:1, 2012
Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab.BMC medicine, , Mar-21, Volume: 10, 2012
A new generation of EGFR tyrosine-kinase inhibitors in NSCLC.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
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Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.Cancer research, , Feb-01, Volume: 70, Issue:3, 2010
The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.Cancer investigation, , Volume: 28, Issue:4, 2010
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EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992.Targeted oncology, , Volume: 5, Issue:4, 2010
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Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy.Proceedings of the National Academy of Sciences of the United States of America, , Jan-13, Volume: 106, Issue:2, 2009
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Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer.The Journal of clinical investigation, , Volume: 119, Issue:10, 2009
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BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.Oncogene, , Aug-07, Volume: 27, Issue:34, 2008
Inhibitory Effects of HangAmDan-B1 (HAD-B1) Combined With Afatinib on H1975 Lung Cancer Cell-Bearing Mice.Integrative cancer therapies, , Volume: 18
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.Integrative cancer therapies, , Volume: 20
Skeletal muscle loss during anti-epidermal growth factor receptor therapy is an independent prognostic factor on non-small cell lung cancer patients survival.Journal of B.U.ON. : official journal of the Balkan Union of Oncology, , Volume: 26, Issue:3
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
Identifying activating mutations in the EGFR gene: prognostic and therapeutic implications in non-small cell lung cancer.Jornal brasileiro de pneumologia : publicacao oficial da Sociedade Brasileira de Pneumologia e Tisilogia, , Volume: 41, Issue:4
Synergistic Effect of HAD-B1 and Afatinib Against Gefitinib Resistance of Non-Small Cell Lung Cancer.Integrative cancer therapies, , Volume: 21
Significance of Polar Charged Amino Acids in Compound Mutations in EGFR-mutated Patients Treated With First-line Afatinib.In vivo (Athens, Greece), , Volume: 36, Issue:4
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Afatinib in the first-line treatment of patients with non-small cell lung cancer: clinical evidence and experience.Therapeutic advances in respiratory disease, , Volume: 12
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.American journal of therapeutics, , Volume: 27, Issue:5
The multi-kinase inhibitor afatinib serves as a novel candidate for the treatment of human uveal melanoma.Cellular oncology (Dordrecht), , Volume: 45, Issue:4, 2022
Inhibiting insulin and mTOR signaling by afatinib and crizotinib combination fosters broad cytotoxic effects in cutaneous malignant melanoma.Cell death & disease, , 10-20, Volume: 11, Issue:10, 2020
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Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Real-life comparison of the afatinib and first-generation tyrosine kinase inhibitors in nonsmall cell lung cancer harboring EGFR exon 19 deletion: a Turk Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 147, Issue:7, 2021
Selective inhibition of stemness through EGFR/FOXA2/SOX9 axis reduces pancreatic cancer metastasis.Oncogene, , Volume: 40, Issue:4, 2021
Targeting human epidermal growth factor receptor 2 enhances radiosensitivity and reduces the metastatic potential of Lewis lung carcinoma cells.Radiation oncology (London, England), , Mar-06, Volume: 15, Issue:1, 2020
Phase 2 study of afatinib among patients with recurrent and/or metastatic esophageal squamous cell carcinoma.Cancer, , 10-15, Volume: 126, Issue:20, 2020
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First-line afatinib for advanced EGFRm+ NSCLC: Analysis of long-term responders in the LUX-Lung 3, 6, and 7 trials.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
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Safety and efficacy of afatinib as add-on to standard therapy of gemcitabine/cisplatin in chemotherapy-naive patients with advanced biliary tract cancer: an open-label, phase I trial with an extensive biomarker program.BMC cancer, , Jan-11, Volume: 19, Issue:1, 2019
The Evolutionary Difference Between Extracranial Lesions and Leptomeningeal Metastasis in a Patient With Afatinib-Resistant Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Cost effectiveness analysis of afatinib versus pemetrexed-cisplatin for first-line treatment of locally advanced or metastatic EGFR mutation positive non-small-cell lung cancer from the Singapore healthcare payer's perspective.BMC cancer, , 03-27, Volume: 18, Issue:1, 2018
Stevens-Johnson syndrome/toxic epidermal necrolysis overlap in a NSCLC patient treated with afatinib.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG, , Volume: 16, Issue:2, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
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Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
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Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
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Afatinib plus vinorelbine versus trastuzumab plus vinorelbine in patients with HER2-overexpressing metastatic breast cancer who had progressed on one previous trastuzumab treatment (LUX-Breast 1): an open-label, randomised, phase 3 trial.The Lancet. Oncology, , Volume: 17, Issue:3, 2016
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Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
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A phase I study of volasertib combined with afatinib, in advanced solid tumors.Cancer chemotherapy and pharmacology, , Volume: 76, Issue:4, 2015
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Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
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Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22, 2014
Randomized Phase II trial of nintedanib, afatinib and sequential combination in castration-resistant prostate cancer.Future oncology (London, England), , Volume: 10, Issue:2, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.Breast cancer research and treatment, , Volume: 134, Issue:3, 2012
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Afatinib in paediatric patients with recurrent/refractory ErbB-dysregulated tumours: Results of a phase I/expansion trial.European journal of cancer (Oxford, England : 1990), , Volume: 188, 2023
Anti-cancer effect of afatinib, dual inhibitor of HER2 and EGFR, on novel mutation HER2 E401G in models of patient-derived cancer.BMC cancer, , Jan-23, Volume: 23, Issue:1, 2023
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Instrumental evaluation sensitively detects subclinical skin changes by the epidermal growth factor receptor inhibitors and risk factors for severe acneiform eruption.The Journal of dermatology, , Volume: 46, Issue:1, 2019
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
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Design, synthesis and biological evaluation of benzoylacrylic acid shikonin ester derivatives as irreversible dual inhibitors of tubulin and EGFR.Bioorganic & medicinal chemistry, , 12-01, Volume: 27, Issue:23, 2019
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Case series showing the efficacy of 5-aminolaevulinic acid photodynamic therapy for epidermal growth factor receptor inhibitor-induced paronychia and pyogenic granuloma-like lesions.The British journal of dermatology, , Volume: 180, Issue:3, 2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.Bioorganic & medicinal chemistry, , 02-01, Volume: 27, Issue:3, 2019
Phase I open-label study of afatinib plus vinorelbine in patients with solid tumours overexpressing EGFR and/or HER2.British journal of cancer, , 02-06, Volume: 118, Issue:3, 2018
Development of a method to determine axitinib, lapatinib and afatinib in plasma by micellar liquid chromatography and validation by the European Medicines Agency guidelines.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , Feb-01, Volume: 1074-1075, 2018
Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.Science signaling, , 09-25, Volume: 11, Issue:549, 2018
Phase Ib Study of High-dose Intermittent Afatinib in Patients With Advanced Solid Tumors.Clinical lung cancer, , Volume: 19, Issue:5, 2018
Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Epidermal growth factor induces STAT1 expression to exacerbate the IFNr-mediated PD-L1 axis in epidermal growth factor receptor-positive cancers.Molecular carcinogenesis, , Volume: 57, Issue:11, 2018
A phase I study of afatinib combined with paclitaxel and bevacizumab in patients with advanced solid tumors.Cancer chemotherapy and pharmacology, , Volume: 79, Issue:1, 2017
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Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
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A novel lead compound CM-118: antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers.Cancer biology & therapy, , Jun-01, Volume: 15, Issue:6, 2014
Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine, , Volume: 54, Issue:6, 2013
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Afatinib demonstrates remarkable activity against HER2-amplified uterine serous endometrial cancer in vitro and in vivo.British journal of cancer, , Oct-28, Volume: 111, Issue:9, 2014
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
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Improving the anticancer effect of afatinib and microRNA by using lipid polymeric nanoparticles conjugated with dual pH-responsive and targeting peptides.Journal of nanobiotechnology, , Aug-19, Volume: 17, Issue:1, 2019
Afatinib treatment for her-2 amplified metastatic colorectal cancer based on patient-derived xenograft models and next generation sequencing.Cancer biology & therapy, , Volume: 20, Issue:4, 2019
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A randomised, open-label phase II trial of afatinib versus cetuximab in patients with metastatic colorectal cancer.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:18, 2014
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Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
Instrumental evaluation sensitively detects subclinical skin changes by the epidermal growth factor receptor inhibitors and risk factors for severe acneiform eruption.The Journal of dermatology, , Volume: 46, Issue:1, 2019
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Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Different incidence of interstitial lung disease according to different kinds of EGFR-tyrosine kinase inhibitors administered immediately before and/or after anti-PD-1 antibodies in lung cancer.Thoracic cancer, , Volume: 10, Issue:4, 2019
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
[Analysis of Time-to-onset of Interstitial Lung Disease after the Administration of Small Molecule Molecularly-targeted Drugs].Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, , Volume: 138, Issue:2, 2018
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Afatinib-Induced Severe Interstitial Lung Disease Successfully Treated with High-Dose Corticosteroid Therapy: A Case Report.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
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Prolonged survival with erlotinib followed by afatinib in a caucasian smoker with metastatic, poorly differentiated large cell carcinoma of the lung: a case report.Cancer biology & therapy, , Volume: 16, Issue:10, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
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"From molecular to clinic": The pivotal role of CDC42 in pathophysiology of human papilloma virus related cancers and a correlated sensitivity of afatinib.Frontiers in immunology, , Volume: 14, 2023
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A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1, 2019
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
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management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
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A noteworthy treatment of metastatic small-cell lung cancer with afatinib, followed by subsequent development of rare metastatic lesions in the ascending and sigmoid colon.Cancer reports (Hoboken, N.J.), , Volume: 3, Issue:3, 2020
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Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
The Evolutionary Difference Between Extracranial Lesions and Leptomeningeal Metastasis in a Patient With Afatinib-Resistant Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
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Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Mechanism of hepatotoxicity of first-line tyrosine kinase inhibitors: Gefitinib and afatinib.Toxicology letters, , Jun-01, Volume: 343, 2021
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
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Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Enhanced antitumor efficacy by combining afatinib with MDV3100 in castration-resistant prostate cancer.Die Pharmazie, , 02-01, Volume: 77, Issue:2, 2022
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Effects of tyrosine kinase inhibitor therapy on skin toxicity and skin-related quality of life in patients with lung cancer: An observational study.Medicine, , Jun-05, Volume: 99, Issue:23, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
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Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
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Phase 1 trial of dasatinib combined with afatinib for epidermal growth factor receptor- (EGFR-) mutated lung cancer with acquired tyrosine kinase inhibitor (TKI) resistance.British journal of cancer, , Volume: 120, Issue:8, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
[Analysis of Time-to-onset of Interstitial Lung Disease after the Administration of Small Molecule Molecularly-targeted Drugs].Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, , Volume: 138, Issue:2, 2018
Afatinib Therapy: Practical Management of Adverse Events With an Oral Agent for Non-Small Cell Lung Cancer Treatment.Clinical journal of oncology nursing, , 10-01, Volume: 22, Issue:5, 2018
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
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Synthesis of novel dual target inhibitors of PARP and EGFR and their antitumor activities in triple negative breast cancers.Bioorganic & medicinal chemistry, , 05-01, Volume: 61, 2022
Neoadjuvant afatinib with paclitaxel for triple-negative breast cancer and the molecular characteristics in responders and non-responders.Journal of the Formosan Medical Association = Taiwan yi zhi, , Volume: 121, Issue:12, 2022
Identification of synergistic drug combinations using breast cancer patient-derived xenografts.Scientific reports, , 01-30, Volume: 10, Issue:1, 2020
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A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.Investigational new drugs, , Volume: 32, Issue:6, 2014
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.American journal of therapeutics, , Volume: 27, Issue:5
Emergence, development, and future of cardio-oncology in China: cardiohypersensitivity, cardiotoxicity and the Kounis syndrome.Chinese medical journal, , 03-20, Volume: 132, Issue:6, 2019
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Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury.International journal of molecular sciences, , Jan-14, Volume: 22, Issue:2, 2021
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Different incidence of interstitial lung disease according to different kinds of EGFR-tyrosine kinase inhibitors administered immediately before and/or after anti-PD-1 antibodies in lung cancer.Thoracic cancer, , Volume: 10, Issue:4, 2019
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
[Analysis of Time-to-onset of Interstitial Lung Disease after the Administration of Small Molecule Molecularly-targeted Drugs].Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, , Volume: 138, Issue:2, 2018
Afatinib-Induced Severe Interstitial Lung Disease Successfully Treated with High-Dose Corticosteroid Therapy: A Case Report.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
Risk of fatal pulmonary events in patients with advanced non-small-cell lung cancer treated with EGF receptor tyrosine kinase inhibitors: a comparative meta-analysis.Future oncology (London, England), , Volume: 11, Issue:7, 2015
Case series showing the efficacy of 5-aminolaevulinic acid photodynamic therapy for epidermal growth factor receptor inhibitor-induced paronychia and pyogenic granuloma-like lesions.The British journal of dermatology, , Volume: 180, Issue:3, 2019
Topical betaxolol for treating relapsing paronychia with pyogenic granuloma-like lesions induced by epidermal growth factor receptor inhibitors.Journal of the American Academy of Dermatology, , Volume: 78, Issue:6, 2018
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Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
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Clinical Features and Progression Pattern of Acquired T790M-positive Compared With T790M-negative EGFR Mutant Non-small-cell Lung Cancer: Catching Tumor and Clinical Heterogeneity Over Time Through Liquid Biopsy.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.Clinical lung cancer, , Volume: 21, Issue:3, 2020
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
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Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Phase 1 trial of dasatinib combined with afatinib for epidermal growth factor receptor- (EGFR-) mutated lung cancer with acquired tyrosine kinase inhibitor (TKI) resistance.British journal of cancer, , Volume: 120, Issue:8, 2019
Afatinib versus methotrexate as second-line treatment in Asian patients with recurrent or metastatic squamous cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 3): an open-label, randomised phase III trialAnnals of oncology : official journal of the European Society for Medical Oncology, , 11-01, Volume: 30, Issue:11, 2019
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Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
From Diagnostic-Therapeutic Pathways to Real-World Data: A Multicenter Prospective Study on Upfront Treatment for The oncologist, , Volume: 24, Issue:6, 2019
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[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
Afatinib treatment of a squamous lung cancer after tumor progression of nivolumab.Thoracic cancer, , Volume: 9, Issue:1, 2018
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A phase Ib trial of continuous once-daily oral afatinib plus sirolimus in patients with epidermal growth factor receptor mutation-positive non-small cell lung cancer and/or disease progression following prior erlotinib or gefitinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Prognostic value of early response assessment using (18F)FDG-PET in patients with advanced non-small cell lung cancer treated with tyrosine-kinase inhibitors.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 65, Issue:5, 2017
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Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:11, 2016
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Afatinib Exerts Immunomodulatory Effects by Targeting the Pyrimidine Biosynthesis Enzyme CAD.Cancer research, , 06-15, Volume: 81, Issue:12, 2021
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"From molecular to clinic": The pivotal role of CDC42 in pathophysiology of human papilloma virus related cancers and a correlated sensitivity of afatinib.Frontiers in immunology, , Volume: 14, 2023
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Small Cell Lung Cancer Derived from Adenocarcinoma with Mutant Epidermal Growth Factor Receptor Provides a Signature of Transcriptional Alteration in Tumor Cells.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 58, Issue:22, 2019
[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
Successful treatment with an EGFR tyrosine kinase inhibitor Afatinib in a patient with combined small-cell lung Cancer with EGFR mutation.Investigational new drugs, , Volume: 36, Issue:4, 2018
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
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Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
The Evolutionary Difference Between Extracranial Lesions and Leptomeningeal Metastasis in a Patient With Afatinib-Resistant Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
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[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Mechanism of hepatotoxicity of first-line tyrosine kinase inhibitors: Gefitinib and afatinib.Toxicology letters, , Jun-01, Volume: 343, 2021
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1, 2016
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
NRG1 promotes tumorigenesis and metastasis and afatinib treatment efficiency is enhanced by NRG1 inhibition in esophageal squamous cell carcinoma.Biochemical pharmacology, , Volume: 218, 2023
NOX4 Signaling Mediates Cancer Development and Therapeutic Resistance through HER3 in Ovarian Cancer Cells.Cells, , 06-30, Volume: 10, Issue:7, 2021
Afatinib, an EGFR inhibitor, decreases EMT and tumorigenesis of Huh‑7 cells by regulating the ERK‑VEGF/MMP9 signaling pathway.Molecular medicine reports, , Volume: 20, Issue:4, 2019
An Evolving Algorithm to Select and Sequence Therapies in EGFR Mutation-positive NSCLC: A Strategic Approach.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Redefining KRAS activation.Nature reviews. Clinical oncology, , Volume: 15, Issue:9, 2018
Afatinib restrains K-RAS-driven lung tumorigenesis.Science translational medicine, , 06-20, Volume: 10, Issue:446, 2018
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miR-124 Regulates the Epithelial-Restricted with Serine Box/Epidermal Growth Factor Receptor Signaling Axis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics, , Volume: 14, Issue:10, 2015
β-catenin contributes to lung tumor development induced by EGFR mutations.Cancer research, , Oct-15, Volume: 74, Issue:20, 2014
Enhanced antitumor efficacy by combining afatinib with MDV3100 in castration-resistant prostate cancer.Die Pharmazie, , 02-01, Volume: 77, Issue:2, 2022
Randomized Phase II trial of nintedanib, afatinib and sequential combination in castration-resistant prostate cancer.Future oncology (London, England), , Volume: 10, Issue:2, 2014
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
Effects of tyrosine kinase inhibitor therapy on skin toxicity and skin-related quality of life in patients with lung cancer: An observational study.Medicine, , Jun-05, Volume: 99, Issue:23, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Safety Profile of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors: A Disproportionality Analysis of FDA Adverse Event Reporting System.Scientific reports, , 03-16, Volume: 10, Issue:1, 2020
Phase 1 trial of dasatinib combined with afatinib for epidermal growth factor receptor- (EGFR-) mutated lung cancer with acquired tyrosine kinase inhibitor (TKI) resistance.British journal of cancer, , Volume: 120, Issue:8, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.Scientific reports, , 12-03, Volume: 9, Issue:1, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
Afatinib Therapy: Practical Management of Adverse Events With an Oral Agent for Non-Small Cell Lung Cancer Treatment.Clinical journal of oncology nursing, , 10-01, Volume: 22, Issue:5, 2018
[Analysis of Time-to-onset of Interstitial Lung Disease after the Administration of Small Molecule Molecularly-targeted Drugs].Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan, , Volume: 138, Issue:2, 2018
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial.The Lancet. Oncology, , Volume: 17, Issue:5, 2016
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
Neoadjuvant afatinib with paclitaxel for triple-negative breast cancer and the molecular characteristics in responders and non-responders.Journal of the Formosan Medical Association = Taiwan yi zhi, , Volume: 121, Issue:12, 2022
Synthesis of novel dual target inhibitors of PARP and EGFR and their antitumor activities in triple negative breast cancers.Bioorganic & medicinal chemistry, , 05-01, Volume: 61, 2022
Identification of a Triple Drug Combination That Is Synergistically Cytotoxic for Triple-Negative Breast Cancer Cells Using a Novel Combination Discovery Approach.SLAS discovery : advancing life sciences R & D, , Volume: 25, Issue:8, 2020
Identification of synergistic drug combinations using breast cancer patient-derived xenografts.Scientific reports, , 01-30, Volume: 10, Issue:1, 2020
Emergence, development, and future of cardio-oncology in China: cardiohypersensitivity, cardiotoxicity and the Kounis syndrome.Chinese medical journal, , 03-20, Volume: 132, Issue:6, 2019
Cardiac Toxicity From Afatinib in EGFR-Mutated NSCLC: A Rare But Possible Side Effect.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:7, 2019
A case of crescentic glomerulonephritis induced by afatinib for lung adenocarcinoma.CEN case reports, , Volume: 12, Issue:2, 2023
Afatinib in Untreated Stage IIIB/IV Lung Adenocarcinoma with Major Uncommon Epidermal Growth Factor Receptor (EGFR) Mutations (G719X/L861Q/S768I): A Multicenter Observational Study in Taiwan.Targeted oncology, , Volume: 18, Issue:2, 2023
Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
A case of multiple primary lung adenocarcinoma with a CD74-NRG1 fusion protein and HER2 mutation benefit from combined target therapy.Thoracic cancer, , Volume: 13, Issue:21, 2022
Long-term survival in a patient with advanced lung adenocarcinoma harboring synchronous EGFR exon 18 G719A and BRAF V600E mutations and treated with afatinib: a case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
The effect of afatinib and radiotherapy on a patient with lung adenocarcinoma with a rare EGFR extracellular domain M277E mutation and high PD-L1 expression.Journal of cancer research and therapeutics, , Volume: 18, Issue:2, 2022
Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.Journal of cancer research and therapeutics, , Volume: 18, Issue:5, 2022
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
Durable clinical benefit from afatinib in a lung adenocarcinoma patient with acquired EGFR L718V mutation-mediated resistance towards osimertinib: a case report and literature review.Annals of palliative medicine, , Volume: 11, Issue:3, 2022
Utilization and costs of epidermal growth factor receptor mutation testing and targeted therapy in Medicare patients with metastatic lung adenocarcinoma.BMC health services research, , Apr-09, Volume: 22, Issue:1, 2022
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
Drug-induced Hypersensitivity Syndrome by EGFR-TKI in a Patient with Lung Cancer.Internal medicine (Tokyo, Japan), , Volume: 60, Issue:3, 2021
Long-term response to afatinib in an elderly patient with uncommon epidermal growth factor receptor mutation-positive lung adenocarcinoma.Thoracic cancer, , Volume: 12, Issue:6, 2021
Afatinib and osimertinib in lung adenocarcinoma harbored EGFR T751_I759delinsS mutation: A case report.Thoracic cancer, , Volume: 12, Issue:24, 2021
Comparing survival and treatment response of patients with acquired T790M mutation second-line osimertinib versus sequential treatment of chemotherapy followed by osimertinib: A real-world study.Thoracic cancer, , Volume: 12, Issue:23, 2021
Successful treatment of Afatinib plus Apatinib using for a lung adenocarcinoma patient with HER-2 V659D mutation: a rare case report.Anti-cancer drugs, , 04-01, Volume: 32, Issue:4, 2021
Successful treatment of an osimertinib-resistant lung adenocarcinoma with an exon 18 EGFR mutation (G719S) with afatinib plus bevacizumab.Investigational new drugs, , Volume: 39, Issue:1, 2021
Afatinib treatment response in advanced lung adenocarcinomas harboring uncommon mutations.Thoracic cancer, , Volume: 12, Issue:21, 2021
Outcomes of salvage lung resections in advanced EGFR-mutant lung adenocarcinomas under EGFR TKIs.Thoracic cancer, , Volume: 12, Issue:20, 2021
Major Clinical Response to Afatinib Monotherapy in Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion Mutation.Clinical lung cancer, , Volume: 22, Issue:1, 2021
Drastic antitumor response following administration of afatinib immediately after atezolizumab in a patient with epidermal growth factor receptor tyrosine kinase inhibitor-resistant lung cancer.Thoracic cancer, , Volume: 12, Issue:13, 2021
Lower starting dose of afatinib for the treatment of metastatic lung adenocarcinoma harboring exon 21 and exon 19 mutations.BMC cancer, , May-03, Volume: 21, Issue:1, 2021
Afatinib response in a lung adenocarcinoma with novel compound S720F+L861R mutation in EGFR.Lung cancer (Amsterdam, Netherlands), , Volume: 148, 2020
Retroperitoneal Metastasis, with Marked Fibrosis, of Lung Adenocarcinoma after Afatinib Treatment: An Autopsy Case Report.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 59, Issue:22, 2020
Multiple intraventricular metastases from lung adenocarcinoma with EGFR G719X mutation: a case report.BMC pulmonary medicine, , May-11, Volume: 20, Issue:1, 2020
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Osimertinib induced cardiomyopathy: A case report.Medicine, , Sep-25, Volume: 99, Issue:39, 2020
Lung carcinoma with diffuse cystic lesions misdiagnosed as pulmonary langerhans cell histocytosis: a case report.BMC pulmonary medicine, , Feb-04, Volume: 20, Issue:1, 2020
[Two cases of EGFR-mutated lung adenocarcinoma treated with bronchial recanalization and first-line therapy with afatinib.]Recenti progressi in medicina, , Volume: 111, Issue:12, 2020
Resolving Resistance to Osimertinib Therapy With Afatinib in an NSCLC Patient With EGFR L718Q Mutation.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Mutation Variants and Co-Mutations as Genomic Modifiers of Response to Afatinib in HER2-Mutant Lung Adenocarcinoma.The oncologist, , Volume: 25, Issue:3, 2020
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
Successful treatment of a lung adenocarcinoma patient with a novel EGFR exon 20-ins mutation with afatinib: A case report.Medicine, , Volume: 98, Issue:1, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Identification of a Novel MET Exon 14 Skipping Variant Coexistent with EGFR Mutation in Lung Adenocarcinoma Sensitive to Combined Treatment with Afatinib and Crizotinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:4, 2019
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib.Journal of visualized experiments : JoVE, , 06-26, Issue:148, 2019
Small Cell Lung Cancer Derived from Adenocarcinoma with Mutant Epidermal Growth Factor Receptor Provides a Signature of Transcriptional Alteration in Tumor Cells.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 58, Issue:22, 2019
Afatinib in patients with metastatic or recurrent HER2-mutant lung cancers: a retrospective international multicentre study.European journal of cancer (Oxford, England : 1990), , Volume: 109, 2019
Afatinib is effective in the treatment of lung adenocarcinoma with uncommon EGFR p.L747P and p.L747S mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Durable Response of Low-Dose Afatinib plus Cetuximab in an Adenocarcinoma Patient with a Novel EGFR Exon 20 Insertion Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:10, 2019
Efficacy of afatinib treatment for lung adenocarcinoma harboring exon 18 delE709_T710insD mutation.Japanese journal of clinical oncology, , Aug-01, Volume: 49, Issue:8, 2019
The EGFR Exon 19 Mutant L747-A750>P Exhibits Distinct Sensitivity to Tyrosine Kinase Inhibitors in Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , 11-01, Volume: 25, Issue:21, 2019
Afatinib restrains K-RAS-driven lung tumorigenesis.Science translational medicine, , 06-20, Volume: 10, Issue:446, 2018
Efficacy generated by afatinib in a lung adenocarcinoma patient harboring HER2 S310Y mutation.Cancer biology & therapy, , 06-03, Volume: 19, Issue:6, 2018
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
Mechanisms of acquired resistance to afatinib clarified with liquid biopsy.PloS one, , Volume: 13, Issue:12, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Afatinib as first-line treatment for advanced lung adenocarcinoma patients harboring HER2 mutation: A case report and review of the literature.Thoracic cancer, , Volume: 9, Issue:12, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Primary Resistance to Afatinib in a Patient with Lung Adenocarcinoma Harboring Uncommon EGFR Mutations: S768I and V769L.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
Efficacy of thoracic radiotherapy in patients with stage IIIB-IV epidermal growth factor receptor-mutant lung adenocarcinomas who received and responded to tyrosine kinase inhibitor treatment.Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, , Volume: 129, Issue:1, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Treatment effectiveness and tolerability of afatinib at different doses in patients with EGFR-mutated lung adenocarcinoma: How low can we go?European journal of cancer (Oxford, England : 1990), , Volume: 103, 2018
EGFR exon 18 DelE709_T710insD as an Acquired Resistance Mechanism to Afatinib in an Advanced EGFR exon 18 E709H Lung Adenocarcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.BMC pharmacology & toxicology, , 12-13, Volume: 18, Issue:1, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
Blocking autophagy improves the anti-tumor activity of afatinib in lung adenocarcinoma with activating EGFR mutations in vitro and in vivo.Scientific reports, , 07-04, Volume: 7, Issue:1, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients.Oncotarget, , Mar-15, Volume: 7, Issue:11, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Survival of Lung Adenocarcinoma Patients Predicted from Expression of PD-L1, Galectin-9, and XAGE1 (GAGED2a) on Tumor Cells and Tumor-Infiltrating T Cells.Cancer immunology research, , Volume: 4, Issue:12, 2016
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Long progression-free survival with afatinib in a patient with EGFR-unknown lung adenocarcinoma after erlotinib failure: a case report.Tumori, , Apr-28, Volume: 101, Issue:2, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
Reply to E.R. Haspinger et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Reply to F. De Marinis et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.Cancer research, , Nov-15, Volume: 72, Issue:22, 2012
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.American journal of therapeutics, , Volume: 27, Issue:5
[Afatinib maintenance therapy does not confer any benefit in the adjuvant treatment of head and neck tumors].Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al], , Volume: 199, Issue:4, 2023
Afatinib maintenance therapy following post-operative radiochemotherapy in head and neck squamous cell carcinoma: Results from the phase III randomised double-blind placebo-controlled study BIB2992ORL (GORTEC 2010-02).European journal of cancer (Oxford, England : 1990), , Volume: 178, 2023
Afatinib and Pembrolizumab for Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (ALPHA Study): A Phase II Study with Biomarker Analysis.Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-14, Volume: 28, Issue:8, 2022
Simultaneously targeting ErbB family kinases and PI3K in HPV-positive head and neck squamous cell carcinoma.Oral oncology, , Volume: 131, 2022
Short-course pembrolizumab and continuous afatinib therapy for recurrent or metastatic head and neck squamous cell carcinoma: a real-world data analysis.BMC cancer, , Nov-28, Volume: 22, Issue:1, 2022
Combinatorial approaches targeting the EGFR family and c-Met in SCCHN.Oral oncology, , Volume: 112, 2021
Afatinib induces pro-survival autophagy and increases sensitivity to apoptosis in stem-like HNSCC cells.Cell death & disease, , 07-22, Volume: 12, Issue:8, 2021
Gefitinib and Afatinib Show Potential Efficacy for Fanconi Anemia-Related Head and Neck Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, , 06-15, Volume: 26, Issue:12, 2020
Rationale for Using Irreversible Epidermal Growth Factor Receptor Inhibitors in Combination with Phosphatidylinositol 3-Kinase Inhibitors for Advanced Head and Neck Squamous Cell Carcinoma.Molecular pharmacology, , Volume: 95, Issue:5, 2019
Afatinib versus methotrexate as second-line treatment in Asian patients with recurrent or metastatic squamous cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 3): an open-label, randomised phase III trialAnnals of oncology : official journal of the European Society for Medical Oncology, , 11-01, Volume: 30, Issue:11, 2019
Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.Oral oncology, , Volume: 97, 2019
Predictive biomarkers and EGFR inhibitors in squamous cell carcinoma of head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Melanoma-associated antigen A11 reduces erlotinib and afatinib efficacy in head and neck cancer.Journal of cranio-maxillo-facial surgery : official publication of the European Association for Cranio-Maxillo-Facial Surgery, , Volume: 46, Issue:3, 2018
Activity and safety of afatinib in a window preoperative EORTC study in patients with squamous cell carcinoma of the head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:8, 2016
Afatinib in squamous cell carcinoma of the head and neck.Expert opinion on pharmacotherapy, , Volume: 17, Issue:9, 2016
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.Targeted oncology, , Volume: 10, Issue:4, 2015
Afatinib versus methotrexate as second-line treatment in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 1): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:5, 2015
Afatinib versus placebo as adjuvant therapy after chemoradiation in a double-blind, phase III study (LUX-Head & Neck 2) in patients with primary unresected, clinically intermediate-to-high-risk head and neck cancer: study protocol for a randomized controlTrials, , Nov-29, Volume: 15, 2014
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.BMC cancer, , Jun-28, Volume: 14, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
Afatinib in the treatment of head and neck squamous cell carcinoma.Expert opinion on investigational drugs, , Volume: 23, Issue:1, 2014
A randomized, phase II study of afatinib versus cetuximab in metastatic or recurrent squamous cell carcinoma of the head and neck.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 25, Issue:9, 2014
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinib.Molecular cancer therapeutics, , Volume: 12, Issue:8, 2013
NRG1 promotes tumorigenesis and metastasis and afatinib treatment efficiency is enhanced by NRG1 inhibition in esophageal squamous cell carcinoma.Biochemical pharmacology, , Volume: 218, 2023
Remarkable inhibition effects of afatinib alone or combining with paclitaxel in esophageal squamous cell carcinoma.Journal of gastroenterology and hepatology, , Volume: 36, Issue:9, 2021
Phase 2 study of afatinib among patients with recurrent and/or metastatic esophageal squamous cell carcinoma.Cancer, , 10-15, Volume: 126, Issue:20, 2020
Mouse avatar models of esophageal squamous cell carcinoma proved the potential for EGFR-TKI afatinib and uncovered Src family kinases involved in acquired resistance.Journal of hematology & oncology, , 08-29, Volume: 11, Issue:1, 2018
A case of crescentic glomerulonephritis induced by afatinib for lung adenocarcinoma.CEN case reports, , Volume: 12, Issue:2, 2023
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Long-term response in a patient with adenocarcinoma harboring both common and uncommon EGFR mutations.Investigational new drugs, , Volume: 40, Issue:6, 2022
AGAPP: efficacy of first-line cisplatin, 5-fluorouracil with afatinib in inoperable gastric and gastroesophageal junction carcinomas. A Hellenic Cooperative Oncology Group study.Acta oncologica (Stockholm, Sweden), , Volume: 60, Issue:6, 2021
Successful Treatment of Afatinib Reversing Epidermal Growth Factor Receptor Exon19Deletion/G724S Mutation Resistance Guided by Protein-Drug Docking.The oncologist, , Volume: 26, Issue:11, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
Successful Treatment of a Patient with Lung Adenocarcinoma Harboring Compound EGFR Gene Mutations, G719X and S768I, with Afatinib.The Tokai journal of experimental and clinical medicine, , Sep-20, Volume: 45, Issue:3, 2020
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Variety Is the Spice of Life, but Maybe Not in Gastroesophageal Adenocarcinomas.Cancer discovery, , Volume: 9, Issue:2, 2019
Responsiveness to Full-Dose Afatinib in a Patient With Lung Adenocarcinoma Harboring EGFR S768I and V769L Mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:2, 2019
Afatinib treatment for her-2 amplified metastatic colorectal cancer based on patient-derived xenograft models and next generation sequencing.Cancer biology & therapy, , Volume: 20, Issue:4, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
Miliary Adenocarcinoma of the Lung Responds to Gefitinib and Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Stevens-Johnson syndrome/toxic epidermal necrolysis overlap in a NSCLC patient treated with afatinib.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG, , Volume: 16, Issue:2, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Therapeutic Potential of Afatinib for Cancers with The oncologist, , Volume: 23, Issue:2, 2018
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.BMC pharmacology & toxicology, , 12-13, Volume: 18, Issue:1, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.Respiratory investigation, , Volume: 55, Issue:1, 2017
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
EGFR L858M/L861Q cis Mutations Confer Selective Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Triplet therapy with afatinib, cetuximab, and bevacizumab induces deep remission in lung cancer cells harboring EGFR T790M in vivo.Molecular oncology, , Volume: 11, Issue:6, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.Anticancer research, , Volume: 37, Issue:9, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients.Oncotarget, , Mar-15, Volume: 7, Issue:11, 2016
Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:6, 2016
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Survival of Lung Adenocarcinoma Patients Predicted from Expression of PD-L1, Galectin-9, and XAGE1 (GAGED2a) on Tumor Cells and Tumor-Infiltrating T Cells.Cancer immunology research, , Volume: 4, Issue:12, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
A Triple Rare E709K and L833V/H835L EGFR Mutation Responsive to an Irreversible Pan-HER Inhibitor: A Case Report of Lung Adenocarcinoma Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:5, 2016
Stevens-Johnson syndrome-like erosive dermatitis possibly related to afatinib.European journal of dermatology : EJD, , Aug-01, Volume: 26, Issue:4, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Afatinib, an Irreversible EGFR Family Inhibitor, Shows Activity Toward Pancreatic Cancer Cells, Alone and in Combination with Radiotherapy, Independent of KRAS Status.Targeted oncology, , Volume: 11, Issue:3, 2016
Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.The Lancet. Oncology, , Volume: 16, Issue:2, 2015
LUX-Lung: determining the best EGFR inhibitor in NSCLC?The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
Long progression-free survival with afatinib in a patient with EGFR-unknown lung adenocarcinoma after erlotinib failure: a case report.Tumori, , Apr-28, Volume: 101, Issue:2, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
[Is chemotherapy still an option in oncogene-addicted non-small cell lung cancer? No].Bulletin du cancer, , Volume: 102, Issue:6 Suppl 1, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
A randomised, open-label phase II trial of afatinib versus cetuximab in patients with metastatic colorectal cancer.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:18, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
Is progression-free survival associated with a better health-related quality of life in patients with lung cancer? Evidence from two randomised trials with afatinib.BMJ open, , Oct-31, Volume: 4, Issue:10, 2014
Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Reply to E.R. Haspinger et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Reply to F. De Marinis et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Afatinib monotherapy in EGFR-mutant lung adenocarcinoma.The Lancet. Oncology, , Volume: 14, Issue:9, 2013
Afatinib, erlotinib and gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: a review.Onkologie, , Volume: 36, Issue:9, 2013
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Symptom and quality of life benefit of afatinib in advanced non-small-cell lung cancer patients previously treated with erlotinib or gefitinib: results of a randomized phase IIb/III trial (LUX-Lung 1).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 8, Issue:2, 2013
Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
A new generation of EGFR tyrosine-kinase inhibitors in NSCLC.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.Lung cancer (Amsterdam, Netherlands), , Volume: 76, Issue:1, 2012
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.Molecular cancer therapeutics, , Volume: 11, Issue:3, 2012
EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.Cancer research, , Nov-15, Volume: 72, Issue:22, 2012
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
Monitoring reversible and irreversible EGFR inhibition with erlotinib and afatinib in a patient with EGFR-mutated non-small cell lung cancer (NSCLC) using sequential [18F]fluorothymidine (FLT-)PET.Lung cancer (Amsterdam, Netherlands), , Volume: 77, Issue:3, 2012
The LUX-Lung clinical trial program of afatinib for non-small-cell lung cancer.Expert review of anticancer therapy, , Volume: 11, Issue:5, 2011
Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Nov-15, Volume: 14, Issue:22, 2008
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
Synergistic Blockade of EGFR and HER2 by New-Generation EGFR Tyrosine Kinase Inhibitor Enhances Radiation Effect in Bladder Cancer Cells.Molecular cancer therapeutics, , Volume: 14, Issue:3, 2015
Targeting epidermal growth factor receptor/human epidermal growth factor receptor 2 signalling pathway by a dual receptor tyrosine kinase inhibitor afatinib for radiosensitisation in murine bladder carcinoma.European journal of cancer (Oxford, England : 1990), , Volume: 49, Issue:6, 2013
TSC1 involvement in bladder cancer: diverse effects and therapeutic implications.The Journal of pathology, , Volume: 230, Issue:1, 2013
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs.Thoracic cancer, , Volume: 14, Issue:32, 2023
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Efficacy of tyrosine kinase inhibitors for the treatment of patients with HER2-positive breast cancer with brain metastases: a systematic review and meta-analysis.ESMO open, , Volume: 7, Issue:3, 2022
Androgen Receptor Activation in Glioblastoma Can Be Achieved by Ligand-Independent Signaling through EGFR-A Potential Therapeutic Target.International journal of molecular sciences, , Oct-11, Volume: 22, Issue:20, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Afatinib and radiotherapy, with or without temozolomide, in patients with newly diagnosed glioblastoma: results of a phase I trial.Journal of neuro-oncology, , Volume: 155, Issue:3, 2021
The NRG3/ERBB4 signaling cascade as a novel therapeutic target for canine glioma.Experimental cell research, , 03-15, Volume: 400, Issue:2, 2021
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Multiple intraventricular metastases from lung adenocarcinoma with EGFR G719X mutation: a case report.BMC pulmonary medicine, , May-11, Volume: 20, Issue:1, 2020
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
Efficacy of EGFR plus TNF inhibition in a preclinical model of temozolomide-resistant glioblastoma.Neuro-oncology, , 12-17, Volume: 21, Issue:12, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
First-line afatinib vs gefitinib for patients with EGFR mutation-positive NSCLC (LUX-Lung 7): impact of afatinib dose adjustment and analysis of mode of initial progression for patients who continued treatment beyond progression.Journal of cancer research and clinical oncology, , Volume: 145, Issue:6, 2019
Afatinib and Temozolomide combination inhibits tumorigenesis by targeting EGFRvIII-cMet signaling in glioblastoma cells.Journal of experimental & clinical cancer research : CR, , Jun-18, Volume: 38, Issue:1, 2019
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Influence of afatinib dose on outcomes of advanced EGFR-mutant NSCLC patients with brain metastases.BMC cancer, , Dec-03, Volume: 18, Issue:1, 2018
Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer.Cancer treatment reviews, , Volume: 67, 2018
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Clinical Efficacy of Afatinib Treatment for a Patient with Leptomeningeal Carcinomatosis.Chemotherapy, , Volume: 62, Issue:3, 2017
First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with erlotinib: a case report.Anti-cancer drugs, , Volume: 27, Issue:3, 2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20, 2016
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
Better treatments needed for breast cancer brain metastases.The Lancet. Oncology, , Volume: 16, Issue:16, 2015
Afatinib, an irreversible ErbB family blocker, with protracted temozolomide in recurrent glioblastoma: a case report.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Phase I/randomized phase II study of afatinib, an irreversible ErbB family blocker, with or without protracted temozolomide in adults with recurrent glioblastoma.Neuro-oncology, , Volume: 17, Issue:3, 2015
Afatinib alone or afatinib plus vinorelbine versus investigator's choice of treatment for HER2-positive breast cancer with progressive brain metastases after trastuzumab, lapatinib, or both (LUX-Breast 3): a randomised, open-label, multicentre, phase 2 trThe Lancet. Oncology, , Volume: 16, Issue:16, 2015
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
ErbB4-mediated regulation of vasculogenic mimicry capability in breast cancer cells.Cancer science, , Volume: 113, Issue:3, 2022
Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Efficacy of tyrosine kinase inhibitors for the treatment of patients with HER2-positive breast cancer with brain metastases: a systematic review and meta-analysis.ESMO open, , Volume: 7, Issue:3, 2022
Neoadjuvant afatinib with paclitaxel for triple-negative breast cancer and the molecular characteristics in responders and non-responders.Journal of the Formosan Medical Association = Taiwan yi zhi, , Volume: 121, Issue:12, 2022
Phase II Study of Afatinib in Patients With Tumors With Human Epidermal Growth Factor Receptor 2-Activating Mutations: Results From the National Cancer Institute-Molecular Analysis for Therapy Choice ECOG-ACRIN Trial (EAY131) Subprotocol EAY131-B.JCO precision oncology, , Volume: 6, 2022
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.Bioorganic & medicinal chemistry, , 09-15, Volume: 28, Issue:18, 2020
HER-targeted tyrosine kinase inhibitors enhance response to trastuzumab and pertuzumab in HER2-positive breast cancer.Investigational new drugs, , Volume: 37, Issue:3, 2019
Tyrosine kinase inhibitors for brain metastases in HER2-positive breast cancer.Cancer treatment reviews, , Volume: 67, 2018
Phase I trial of afatinib and 3-weekly trastuzumab with optimal anti-diarrheal management in patients with HER2-positive metastatic cancer.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
An Acquired Cancer discovery, , Volume: 7, Issue:6, 2017
Neratinib resistance and cross-resistance to other HER2-targeted drugs due to increased activity of metabolism enzyme cytochrome P4503A4.British journal of cancer, , Feb-28, Volume: 116, Issue:5, 2017
Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines.Scientific reports, , 06-21, Volume: 7, Issue:1, 2017
Ethacrynic acid improves the antitumor effects of irreversible epidermal growth factor receptor tyrosine kinase inhibitors in breast cancer.Oncotarget, , Sep-06, Volume: 7, Issue:36, 2016
Afatinib plus vinorelbine versus trastuzumab plus vinorelbine in patients with HER2-overexpressing metastatic breast cancer who had progressed on one previous trastuzumab treatment (LUX-Breast 1): an open-label, randomised, phase 3 trial.The Lancet. Oncology, , Volume: 17, Issue:3, 2016
HER Specific TKIs Exert Their Antineoplastic Effects on Breast Cancer Cell Lines through the Involvement of STAT5 and JNK.PloS one, , Volume: 11, Issue:1, 2016
Afatinib alone or afatinib plus vinorelbine versus investigator's choice of treatment for HER2-positive breast cancer with progressive brain metastases after trastuzumab, lapatinib, or both (LUX-Breast 3): a randomised, open-label, multicentre, phase 2 trThe Lancet. Oncology, , Volume: 16, Issue:16, 2015
Better treatments needed for breast cancer brain metastases.The Lancet. Oncology, , Volume: 16, Issue:16, 2015
Phase I trial of afatinib plus vinorelbine in Japanese patients with advanced solid tumors, including breast cancer.Cancer chemotherapy and pharmacology, , Volume: 76, Issue:4, 2015
Label-free LC-MS analysis of HER2+ breast cancer cell line response to HER2 inhibitor treatment.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences, , Aug-04, Volume: 23, 2015
Dual Blockade with AFatinib and Trastuzumab as NEoadjuvant Treatment for Patients with Locally Advanced or Operable Breast Cancer Receiving Taxane-Anthracycline Containing Chemotherapy-DAFNE (GBG-70).Clinical cancer research : an official journal of the American Association for Cancer Research, , Jul-01, Volume: 21, Issue:13, 2015
A neoadjuvant, randomized, open-label phase II trial of afatinib versus trastuzumab versus lapatinib in patients with locally advanced HER2-positive breast cancer.Clinical breast cancer, , Volume: 15, Issue:2, 2015
Phase I Study to Assess the Combination of Afatinib with Trastuzumab in Patients with Advanced or Metastatic HER2-Positive Breast Cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jun-15, Volume: 21, Issue:12, 2015
HER2 aberrations in cancer: implications for therapy.Cancer treatment reviews, , Volume: 40, Issue:6, 2014
Afatinib in the treatment of breast cancer.Expert opinion on investigational drugs, , Volume: 23, Issue:7, 2014
A systematic review of dual targeting in HER2-positive breast cancer.Cancer treatment reviews, , Volume: 40, Issue:2, 2014
New protein kinase inhibitors in breast cancer: afatinib and neratinib.Expert opinion on pharmacotherapy, , Volume: 15, Issue:9, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
[HER2-positive breast cancer: available targeted agents and biomarkers for therapy response].Magyar onkologia, , Volume: 57, Issue:3, 2013
A gene expression profile indicative of early stage HER2 targeted therapy response.Molecular cancer, , Jul-01, Volume: 12, 2013
Sensitivity and kinase activity of epidermal growth factor receptor (EGFR) exon 19 and others to EGFR-tyrosine kinase inhibitors.Cancer science, , Volume: 104, Issue:5, 2013
Dual human epidermal growth factor receptor 2 blockade: another step forward in treating patients with human epidermal growth factor receptor 2-positive breast cancer.Current opinion in oncology, , Volume: 24, Issue:6, 2012
A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.Breast cancer research and treatment, , Volume: 134, Issue:3, 2012
A phase II study of afatinib (BIBW 2992), an irreversible ErbB family blocker, in patients with HER2-positive metastatic breast cancer progressing after trastuzumab.Breast cancer research and treatment, , Volume: 133, Issue:3, 2012
New therapies in HER2-positive breast cancer: a major step towards a cure of the disease?Cancer treatment reviews, , Volume: 38, Issue:5, 2012
Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.Cancer treatment reviews, , Volume: 35, Issue:8, 2009
Short-course pembrolizumab and continuous afatinib therapy for recurrent or metastatic head and neck squamous cell carcinoma: a real-world data analysis.BMC cancer, , Nov-28, Volume: 22, Issue:1, 2022
In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.Drug design, development and therapy, , Volume: 10, 2016
Sustained Inhibition of HER3 and EGFR Is Necessary to Induce Regression of HER2-Amplified Gastrointestinal Carcinomas.Clinical cancer research : an official journal of the American Association for Cancer Research, , Dec-15, Volume: 21, Issue:24, 2015
Afatinib in combination with GEMOX chemotherapy as the adjuvant treatment in patients with ErbB pathway mutated, resectable gallbladder cancer: study protocol for a ctDNA-based, multicentre, open-label, randomised, controlled, phase II trial.BMJ open, , 02-28, Volume: 13, Issue:2, 2023
Real-life comparison of afatinib and erlotinib in non-small cell lung cancer with rare EGFR exon 18 and exon 20 mutations: a Turkish Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 149, Issue:2, 2023
All EGFR mutations are (not) created equal: focus on uncommon EGFR mutations.Journal of cancer research and clinical oncology, , Volume: 149, Issue:4, 2023
Neoadjuvant Afatinib for stage III EGFR-mutant non-small cell lung cancer: a phase II study.Nature communications, , 08-03, Volume: 14, Issue:1, 2023
Flashback Foreword: Afatinib for the Treatment of Epidermal Growth Factor Receptor Mutation-Positive Non-Small-Cell Lung Cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , 06-01, Volume: 41, Issue:16, 2023
Comprehensive assessment of pretreatment sarcopenia impacts on patients with EGFR-mutated NSCLC treated with afatinib.Thoracic cancer, , Volume: 14, Issue:25, 2023
Final Report on Real-World Effectiveness of Sequential Afatinib and Osimertinib in EGFR-Positive Advanced Non-Small Cell Lung Cancer: Updated Analysis of the RESET Study.Cancer research and treatment, , Volume: 55, Issue:4, 2023
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 181, 2023
Non-small cell lung cancer with EGFR (L858R and E709X) and CNNB1 mutations responded to afatinib.Thoracic cancer, , Volume: 14, Issue:4, 2023
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
The second-generation tyrosine kinase inhibitor afatinib inhibits IL-1β secretion via blocking assembly of NLRP3 inflammasome independent of epidermal growth factor receptor signaling in macrophage.Molecular immunology, , Volume: 153, 2023
A randomized phase II study of afatinib alone or combined with bevacizumab for treating chemo-naïve patients with non-small cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 184, 2023
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
A real-world study of Afatinib plus ramucirumab in treatment-naïve, EGFR-mutated, non-small cell lung cancer.BMC cancer, , May-08, Volume: 23, Issue:1, 2023
Clinical Outcomes of Afatinib Versus Osimertinib in Patients With Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: A Pooled Analysis.The oncologist, , 06-02, Volume: 28, Issue:6, 2023
Survival outcomes of east Asian patients with advanced non-small cell lung cancer treated with first-line EGFR tyrosine kinase inhibitors: A network meta-analysis of real-world evidence.Thoracic cancer, , Volume: 14, Issue:32, 2023
The Use of Cytotoxic Drugs as First Line Chemotherapy for EGFR (+) Nonsquamous NSCLC: A Network Meta-Analysis.Disease markers, , Volume: 2023, 2023
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs.Thoracic cancer, , Volume: 14, Issue:32, 2023
Determining plasma and cerebrospinal fluid concentrations of EGFR-TKI in lung cancer patients.Analytical biochemistry, , 05-15, Volume: 669, 2023
Monitoring of T790M in plasma ctDNA of advanced EGFR-mutant NSCLC patients on first- or second-generation tyrosine kinase inhibitors.BMC cancer, , Mar-13, Volume: 23, Issue:1, 2023
NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity.European journal of pharmacology, , May-05, Volume: 946, 2023
Epidermal growth factor receptor tyrosine kinase inhibitors for non-small cell lung cancer harboring uncommon EGFR mutations: Real-world data from Taiwan.Thoracic cancer, , Volume: 14, Issue:1, 2023
Afatinib for the Treatment of NSCLC with Uncommon EGFR Mutations: A Narrative Review.Current oncology (Toronto, Ont.), , 05-28, Volume: 30, Issue:6, 2023
Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
Treatment outcomes of non-small cell lung cancers treated with EGFR tyrosine kinase inhibitors: a real-world cohort study.Acta oncologica (Stockholm, Sweden), , Volume: 62, Issue:12, 2023
Absence of copy number gain of EGFR: A possible predictive marker of long-term response to afatinib.Cancer science, , Volume: 114, Issue:3, 2023
Alternating Therapy With Osimertinib and Afatinib Blockades EGFR Secondary Mutation in EGFR-Mutant Lung Cancer: A Single-Arm Phase II Trial.Clinical lung cancer, , Volume: 24, Issue:6, 2023
Older patients with EGFR mutation-positive non-small cell lung cancer treated with afatinib in clinical practice: A subset analysis of the non-interventional GIDEON study.Journal of geriatric oncology, , Volume: 14, Issue:1, 2023
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.Neoplasia (New York, N.Y.), , Volume: 43, 2023
Afatinib plus osimertinib in the treatment of osimertinib-resistant non-small cell lung carcinoma: a phase I clinical trial.BMC cancer, , Jan-03, Volume: 23, Issue:1, 2023
The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Effects of targeted lung cancer drugs on cardiomyocytes studied by atomic force microscopy.Analytical methods : advancing methods and applications, , 08-24, Volume: 15, Issue:33, 2023
Afatinib triggers a NiFundamental & clinical pharmacology, , Volume: 37, Issue:2, 2023
Natural Cyclophilin A Inhibitors Suppress the Growth of Cancer Stem Cells in Non-Small Cell Lung Cancer by Disrupting Crosstalk between CypA/CD147 and EGFR.International journal of molecular sciences, , May-29, Volume: 24, Issue:11, 2023
Metabolic complete tumor response in a patient with The Journal of international medical research, , Volume: 50, Issue:3, 2022
Preclinical assessment of combination therapy of EGFR tyrosine kinase inhibitors in a highly heterogeneous tumor model.Oncogene, , Volume: 41, Issue:17, 2022
Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Real-world Afatinib Outcomes in Advanced Non-small Cell Lung Cancer Harboring Anticancer research, , Volume: 42, Issue:4, 2022
Durable clinical benefit from afatinib in a lung adenocarcinoma patient with acquired EGFR L718V mutation-mediated resistance towards osimertinib: a case report and literature review.Annals of palliative medicine, , Volume: 11, Issue:3, 2022
Utilization and costs of epidermal growth factor receptor mutation testing and targeted therapy in Medicare patients with metastatic lung adenocarcinoma.BMC health services research, , Apr-09, Volume: 22, Issue:1, 2022
Development and validation of a new liquid chromatography-tandem mass spectrometry assay for the simultaneous quantification of afatinib, dacomitinib, osimertinib, and the active metabolites of osimertinib in human serum.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , May-30, Volume: 1199, 2022
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L).Lung cancer (Amsterdam, Netherlands), , Volume: 168, 2022
Epidermal growth factor receptor tyrosine kinase inhibitors for de novo T790M mutation: A retrospective study of 44 patients.Thoracic cancer, , Volume: 13, Issue:13, 2022
A Phase 2 Trial of Afatinib in Patients with Solid Tumors that Harbor Genomic Aberrations in the HER family: The MOBILITY3 Basket Study.Targeted oncology, , Volume: 17, Issue:3, 2022
The effect of afatinib and radiotherapy on a patient with lung adenocarcinoma with a rare EGFR extracellular domain M277E mutation and high PD-L1 expression.Journal of cancer research and therapeutics, , Volume: 18, Issue:2, 2022
Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
Application of afatinib combined with np regimen in the treatment of stage iv non-small cell lung cancer and its effect on patient survival.Pakistan journal of pharmaceutical sciences, , Volume: 35, Issue:2(Special), 2022
Survival benefits from afatinib compared with gefitinib and erlotinib among patients with common EGFR mutation in first-line setting.Thoracic cancer, , Volume: 13, Issue:14, 2022
Audit of Molecular Mechanisms of Primary and Secondary Resistance to Various Generations of Tyrosine Kinase Inhibitors in Known Epidermal Growth Factor Receptor-Mutant Non-small Cell Lung Cancer Patients in a Tertiary Centre.Clinical oncology (Royal College of Radiologists (Great Britain)), , Volume: 34, Issue:11, 2022
The EGFR-STYK1-FGF1 axis sustains functional drug tolerance to EGFR inhibitors in EGFR-mutant non-small cell lung cancer.Cell death & disease, , 07-15, Volume: 13, Issue:7, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
Efficacy of Combined Use of Everolimus and Second-Generation Pan-EGRF Inhibitors in International journal of molecular sciences, , Jul-14, Volume: 23, Issue:14, 2022
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Non-small cell lung cancer harboring EGFR G724S mutation and exon 19 deletion responded to afatinib monotherapy after multiple lines of target therapies.Anti-cancer drugs, , 10-01, Volume: 33, Issue:9, 2022
Rare EGFR E709-T710delinsX: Molecular characteristics and superior response to afatinib treatment in NSCLC patients.Lung cancer (Amsterdam, Netherlands), , Volume: 172, 2022
Efficacy and potential resistance mechanisms of afatinib in advanced non-small cell lung cancer patients with EGFR G719X/L861Q/S768I.Cancer, , 11-01, Volume: 128, Issue:21, 2022
A case of multiple primary lung adenocarcinoma with a CD74-NRG1 fusion protein and HER2 mutation benefit from combined target therapy.Thoracic cancer, , Volume: 13, Issue:21, 2022
Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 155, 2022
Early-Onset Pulmonary Events with Combined Brigatinib and Afatinib Treatment of L858/cisT790M/cisC797S NSCLC: A Case Report.The American journal of case reports, , Sep-23, Volume: 23, 2022
Afatinib Targeted Therapy Affects the Immune Function and Serum Levels of EGFR and Gastrin-Releasing Peptide Precursor (pro-GRP) in Patients with Non-Small-Cell Lung Cancer (NSCLC).Disease markers, , Volume: 2022, 2022
The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
Elucidation of the inhibitory potential of flavonoids against PKP1 protein in non-small cell lung cancer.Cellular and molecular biology (Noisy-le-Grand, France), , Nov-30, Volume: 68, Issue:11, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Hypotension from afatinib in epidermal growth factor receptor-mutated non-small cell lung cancer: a case report and literature review.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Advanced Lung Cancer Patients' Use of EGFR Tyrosine Kinase Inhibitors and Overall Survival: Real-World Evidence from Quebec, Canada.Current oncology (Toronto, Ont.), , 10-26, Volume: 29, Issue:11, 2022
Real-world data with afatinib in Spanish patients with treatment-naïve non-small-cell lung cancer harboring exon 19 deletions in epidermal growth factor receptor (Del19 EGFR): Clinical experience of the Galician Lung Cancer Group.Cancer treatment and research communications, , Volume: 33, 2022
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.Investigational new drugs, , Volume: 40, Issue:2, 2022
Prevalence, Treatment Patterns, and Outcomes of Individuals with Current oncology (Toronto, Ont.), , 09-30, Volume: 29, Issue:10, 2022
Cost-effectiveness analysis of the first-line EGFR-TKIs in patients with advanced EGFR-mutated non-small-cell lung cancer.Expert review of pharmacoeconomics & outcomes research, , Volume: 22, Issue:4, 2022
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
Application of several machine learning algorithms for the prediction of afatinib treatment outcome in advanced-stage EGFR-mutated non-small-cell lung cancer.Thoracic cancer, , Volume: 13, Issue:23, 2022
Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.Journal of cancer research and therapeutics, , Volume: 18, Issue:5, 2022
Durable response to afatinib rechallenge in a long-term survivor of non-small cell lung cancer harboring EGFR L858R and L747V mutations.Thoracic cancer, , Volume: 13, Issue:22, 2022
Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.European journal of cancer (Oxford, England : 1990), , Volume: 160, 2022
Successful erlotinib rechallenge in an EGFR-mutant metastatic non-small cell lung cancer patient with afatinib-induced drug rash with eosinophilia and systemic symptoms: A case report.Thoracic cancer, , Volume: 13, Issue:3, 2022
Liquid biopsy for detecting epidermal growth factor receptor mutation among patients with non-small cell lung cancer treated with afatinib: a multicenter prospective study.BMC cancer, , Oct-04, Volume: 22, Issue:1, 2022
Drug Repurposing against KRAS Mutant G12C: A Machine Learning, Molecular Docking, and Molecular Dynamics Study.International journal of molecular sciences, , Dec-30, Volume: 24, Issue:1, 2022
The EPICAL trial, a phase Ib study combining first line afatinib with anti-EGF vaccination in EGFR-mutant metastatic NSCLC.Lung cancer (Amsterdam, Netherlands), , Volume: 164, 2022
Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry.Clinica chimica acta; international journal of clinical chemistry, , Feb-15, Volume: 527, 2022
Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
Determination of Afatinib in Human Plasma by 2-Dimensional Liquid Chromatography.Pharmacology, , Volume: 107, Issue:5-6, 2022
Classification and regression tree for estimating predictive markers to detect T790M mutations after acquired resistance to first line EGFR-TKI: HOPE-002.Investigational new drugs, , Volume: 40, Issue:2, 2022
First-line Afatinib in Patients With Non-small-cell Lung Cancer With Uncommon EGFR Mutations in South Korea.Anticancer research, , Volume: 42, Issue:3, 2022
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
Afatinib-loaded inhalable PLGA nanoparticles for localized therapy of non-small cell lung cancer (NSCLC)-development and in-vitro efficacy.Drug delivery and translational research, , Volume: 11, Issue:3, 2021
Cost-Effectiveness Analysis of Afatinib, Erlotinib, and Gefitinib as First-Line Treatments for EGFR Mutation-Positive Non-Small-Cell Lung Cancer in Ontario, Canada.PharmacoEconomics, , Volume: 39, Issue:5, 2021
Efficacy and dose of afatinib in patients with non-small cell lung cancer after failure of prior gefitinib or erlotinib treatment.Thoracic cancer, , Volume: 12, Issue:10, 2021
Real-life Effectiveness of Afatinib Anticancer research, , Volume: 41, Issue:4, 2021
Limited effect of afatinib in a non-small cell lung cancer patient harboring an epidermal growth factor receptor K860I missense mutation: A case report.Thoracic cancer, , Volume: 12, Issue:11, 2021
Response to: Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 12, Issue:11, 2021
A multicenter cohort study of osimertinib compared with afatinib as first-line treatment for EGFR-mutated non-small-cell lung cancer from practical dataset: CJLSG1903.ESMO open, , Volume: 6, Issue:3, 2021
Relationship between Epidermal Growth Factor Receptor Mutations and Adverse Events in Non-Small Cell Lung Cancer Patients treated with Afatinib.The journal of medical investigation : JMI, , Volume: 68, Issue:1.2, 2021
Successful treatment of triple EGFR mutation T785A/L861Q/H297_E298 with afatinib.Thoracic cancer, , Volume: 12, Issue:13, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Effectiveness and Tolerability of First-Line Afatinib for Advanced EGFR-Mutant Non-Small Cell Lung Cancer in Vietnam.Asian Pacific journal of cancer prevention : APJCP, , May-01, Volume: 22, Issue:5, 2021
Survival of chemo-naïve patients with EGFR mutation-positive advanced non-small cell lung cancer after treatment with afatinib and bevacizumab: updates from the Okayama Lung Cancer Study Group Trial 1404.Japanese journal of clinical oncology, , Aug-01, Volume: 51, Issue:8, 2021
Randomized Phase II Study of 3 Months or 2 Years of Adjuvant Afatinib in Patients With Surgically Resected Stage I-III JCO precision oncology, , Volume: 5, 2021
Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds.BMC pulmonary medicine, , Jul-01, Volume: 21, Issue:1, 2021
An open-label expanded access program of afatinib in EGFR tyrosine kinase inhibitor-naïve patients with locally advanced or metastatic non-small cell lung cancer harboring EGFR mutations.BMC cancer, , Jul-12, Volume: 21, Issue:1, 2021
Sequential treatment of afatinib and osimertinib or other regimens in patients with advanced non-small-cell lung cancer harboring EGFR mutations: Results from a real-world study in South Korea.Cancer medicine, , Volume: 10, Issue:17, 2021
Feasibility and effectiveness of afatinib for poor performance status patients with EGFR-mutation-positive non-small-cell lung cancer: a retrospective cohort study.BMC cancer, , Jul-27, Volume: 21, Issue:1, 2021
Severe EGFR inhibitor-induced acneiform eruption responding to dapsone.Dermatology online journal, , Jul-15, Volume: 27, Issue:7, 2021
Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Therapeutic Potential of Afatinib in NRG1 Fusion-Driven Solid Tumors: A Case Series.The oncologist, , Volume: 26, Issue:1, 2021
EGFR tyrosine kinase inhibitors in non-small cell lung cancer: treatment paradigm, current evidence, and challenges.Tumori, , Volume: 107, Issue:5, 2021
Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells.International journal of radiation biology, , Volume: 97, Issue:2, 2021
Does metformin improve the efficacy of standard epidermal growth factor receptor-tyrosine kinase inhibitor treatment for patients with advanced non-small-cell lung cancer?Interactive cardiovascular and thoracic surgery, , 01-01, Volume: 32, Issue:1, 2021
Celastrol acts synergistically with afatinib to suppress non-small cell lung cancer cell proliferation by inducing paraptosis.Journal of cellular physiology, , Volume: 236, Issue:6, 2021
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.The oncologist, , Volume: 26, Issue:4, 2021
New strategy for suppressing the growth of lung cancer cells harboring mutations in the ATP-binding region of EGFR by targeting the molecular motor MYO1D.Clinical and translational medicine, , Volume: 11, Issue:8, 2021
HER2 amplification as a potential mechanism of acquired resistance to afatinib in an advanced non-small-cell lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 151, 2021
Synergy between vinorelbine and afatinib in the inhibition of non-small cell lung cancer progression by EGFR and p53 signaling pathways.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 134, 2021
Afatinib in EGFR TKI-naïve patients with locally advanced or metastatic EGFR mutation-positive non-small cell lung cancer: Interim analysis of a Phase 3b study.Lung cancer (Amsterdam, Netherlands), , Volume: 152, 2021
Structure-based classification predicts drug response in EGFR-mutant NSCLC.Nature, , Volume: 597, Issue:7878, 2021
A prospective, phase II trial of monotherapy with low-dose afatinib for patients with EGFR, mutation-positive, non-small cell lung cancer: Thoracic oncology research group 1632.Lung cancer (Amsterdam, Netherlands), , Volume: 161, 2021
Comparison Between Second- and Third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors as First-line Treatment in Patients With Non-small-cell Lung Cancer: A Retrospective Analysis.Anticancer research, , Volume: 41, Issue:10, 2021
Real-life comparison of the afatinib and first-generation tyrosine kinase inhibitors in nonsmall cell lung cancer harboring EGFR exon 19 deletion: a Turk Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 147, Issue:7, 2021
Clinical utility of liquid biopsy for EGFR driver, T790M mutation and EGFR amplification in plasma in patients with acquired resistance to afatinib.BMC cancer, , Jan-12, Volume: 21, Issue:1, 2021
Sequential afatinib and osimertinib in patients with EGFR mutation-positive NSCLC and acquired T790M: A global non-interventional study (UpSwinG).Lung cancer (Amsterdam, Netherlands), , Volume: 162, 2021
Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury.International journal of molecular sciences, , Jan-14, Volume: 22, Issue:2, 2021
An elderly advanced non-small cell lung cancer patient harboring rare epidermal growth factor receptor mutations L861R benefited from afatinib: A case report.Medicine, , Nov-12, Volume: 100, Issue:45, 2021
Overall survival in stage IV EGFR mutation‑positive NSCLC: Comparing first‑, second‑ and third‑generation EGFR‑TKIs (Review).International journal of oncology, , Volume: 58, Issue:2, 2021
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
REPORT- Clinical outcomes of using second - versus first-Generation EGFR-tkis for the First-Line treatment of advanced NSCLC patients with EGFR mutations: A meta-analysis.Pakistan journal of pharmaceutical sciences, , Volume: 34, Issue:4, 2021
Afatinib for the treatment of advanced non-small-cell lung cancer harboring an epidermal growth factor receptor exon 18 E709_T710delinsD mutation: a case report.Journal of medical case reports, , Nov-22, Volume: 15, Issue:1, 2021
Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).Thoracic cancer, , Volume: 12, Issue:8, 2021
EGFR mutation-guided use of afatinib, erlotinib and gefitinib for advanced non-small-cell lung cancer in Hong Kong - A cost-effectiveness analysis.PloS one, , Volume: 16, Issue:3, 2021
A phase II study of first-line afatinib for patients aged ≥75 years with EGFR mutation-positive advanced non-small cell lung cancer: North East Japan Study Group trial NEJ027.BMC cancer, , Mar-01, Volume: 21, Issue:1, 2021
Combination therapy with afatinib and bevacizumab in an EGFR-mutated non-small cell lung cancer patient with acquired ERBB2 amplification: A case report.Medicine, , Feb-26, Volume: 100, Issue:8, 2021
Afatinib therapy in case of EGFR G724S emergence as resistance mechanism to osimertinib.Anti-cancer drugs, , 08-01, Volume: 32, Issue:7, 2021
Afatinib as First-Line Treatment in Asian Patients with EGFR Mutation-Positive NSCLC: A Narrative Review of Real-World Evidence.Advances in therapy, , Volume: 38, Issue:5, 2021
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , 03-18, Volume: 3, 2021
Incremental cost-effectiveness analysis of tyrosine kinase inhibitors in advanced non-small cell lung cancer with mutations of the epidermal growth factor receptor in Colombia.Expert review of pharmacoeconomics & outcomes research, , Volume: 21, Issue:4, 2021
Afatinib Exerts Immunomodulatory Effects by Targeting the Pyrimidine Biosynthesis Enzyme CAD.Cancer research, , 06-15, Volume: 81, Issue:12, 2021
Nationwide Real-world Cohort Study of First-line Tyrosine Kinase Inhibitor Treatment in Epidermal Growth Factor Receptor-mutated Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:6, 2020
Phase II Study of Low-Dose Afatinib Maintenance Treatment Among Patients with EGFR-Mutated Non-Small Cell Lung Cancer: North Japan Lung Cancer Study Group Trial 1601 (NJLCG1601).The oncologist, , Volume: 25, Issue:10, 2020
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 11, Issue:8, 2020
QT interval prolongation related to afatinib treatment in a patient with metastatic non-small-cell lung cancer.Current problems in cancer, , Volume: 44, Issue:6, 2020
Effects of tyrosine kinase inhibitor therapy on skin toxicity and skin-related quality of life in patients with lung cancer: An observational study.Medicine, , Jun-05, Volume: 99, Issue:23, 2020
ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib.Cancer, , 03-15, Volume: 126, Issue:6, 2020
Comparing the effectiveness of different EGFR-TKIs in patients with EGFR mutant non-small-cell lung cancer: A retrospective cohort study in Taiwan.International journal of cancer, , 08-15, Volume: 147, Issue:4, 2020
Observational Study of Sequential Afatinib and Osimertinib in EGFR Mutation-Positive NSCLC: Patients Treated with a 40-mg Starting Dose of Afatinib.Advances in therapy, , Volume: 37, Issue:2, 2020
Determination of Somatic Mutations and Tumor Mutation Burden in Plasma by CAPP-Seq during Afatinib Treatment in NSCLC Patients Resistance to Osimertinib.Scientific reports, , 01-20, Volume: 10, Issue:1, 2020
Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol cliniMedicine, , Volume: 99, Issue:4, 2020
Cost-effectiveness analysis of first and second-generation EGFR tyrosine kinase inhibitors as first line of treatment for patients with NSCLC harboring EGFR mutations.BMC cancer, , Sep-01, Volume: 20, Issue:1, 2020
Molecular profiling of afatinib-resistant non-small cell lung cancer cells in vivo derived from mice.Pharmacological research, , Volume: 161, 2020
Comparative effectiveness and cost-effectiveness of three first-line EGFR-tyrosine kinase inhibitors: Analysis of real-world data in a tertiary hospital in Taiwan.PloS one, , Volume: 15, Issue:4, 2020
NRG1 fusion-driven tumors: biology, detection, and the therapeutic role of afatinib and other ErbB-targeting agents.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 31, Issue:12, 2020
The efficacy of first-line tyrosine kinase inhibitors combined with co-medications in Asian patients with EGFR mutation non-small cell lung cancer.Scientific reports, , 09-11, Volume: 10, Issue:1, 2020
Afatinib for the first-line treatment of Future oncology (London, England), , Volume: 16, Issue:31, 2020
Budget impact of sequential treatment with first-line afatinib versus first-line osimertinib in non-small-cell lung cancer patients with common EGFR mutations.The European journal of health economics : HEPAC : health economics in prevention and care, , Volume: 21, Issue:6, 2020
PLCγ1‑dependent invasion and migration of cells expressing NSCLC‑associated EGFR mutants.International journal of oncology, , Volume: 57, Issue:4, 2020
Treatment of Patients With Non-small-cell Lung Cancer With Uncommon Anticancer research, , Volume: 40, Issue:10, 2020
Complete Response to Immunotherapy Plus Chemotherapy After an Unusual Clinical Response to Afatinib and Stereotactic Radiosurgery in a Patient With Metastatic EGFR-Mutant Non-Small-Cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Clinical Features and Progression Pattern of Acquired T790M-positive Compared With T790M-negative EGFR Mutant Non-small-cell Lung Cancer: Catching Tumor and Clinical Heterogeneity Over Time Through Liquid Biopsy.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Knockdown of lncRNA BLACAT1 reverses the resistance of afatinib to non-small cell lung cancer via modulating STAT3 signalling.Journal of drug targeting, , Volume: 28, Issue:3, 2020
Sequential afatinib and osimertinib in patients with Future oncology (London, England), , Volume: 16, Issue:34, 2020
Site-Specific and Targeted Therapy Based on Molecular Profiling by Next-Generation Sequencing for Cancer of Unknown Primary Site: A Nonrandomized Phase 2 Clinical Trial.JAMA oncology, , Dec-01, Volume: 6, Issue:12, 2020
Healthcare resource utilization and costs associated with patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive NSCLC in the United States.Journal of medical economics, , Volume: 23, Issue:1, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Photo-induced specific intracellular release EGFR inhibitor from enzyme/ROS-dual sensitive nano-platforms for molecular targeted-photodynamic combinational therapy of non-small cell lung cancer.Journal of materials chemistry. B, , 09-21, Volume: 8, Issue:35, 2020
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.Medicine, , Oct-23, Volume: 99, Issue:43, 2020
Dissecting the mThe pharmacogenomics journal, , Volume: 20, Issue:2, 2020
Role of YES1 amplification in EGFR mutation-positive non-small cell lung cancer: Primary resistance to afatinib in a patient.Thoracic cancer, , Volume: 11, Issue:9, 2020
Quantitative Structure-Mutation-Activity Relationship Tests (QSMART) model for protein kinase inhibitor response prediction.BMC bioinformatics, , Nov-12, Volume: 21, Issue:1, 2020
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
New lung-cancer drugs extend survival times.Nature, , Volume: 587, Issue:7834, 2020
Durable Responses to Afatinib as First-line Therapy for HER2-mutated Metastatic Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Afatinib in patients with advanced non-small cell lung cancer harboring HER2 mutations, previously treated with chemotherapy: A phase II trial.Lung cancer (Amsterdam, Netherlands), , Volume: 147, 2020
A randomized, multi-center, open-label study to compare the safety and efficacy between afatinib monotherapy and combination therapy of afatinib and HAD-B1 for the locally advanced or metastatic NSCLC patients with EGFR mutations.Medicine, , 12-04, Volume: 99, Issue:49, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
Real-world assessment of afatinib for patients with EGFR-positive non-small cell lung cancer.Investigational new drugs, , Volume: 38, Issue:6, 2020
Clinical Activity of Afatinib in Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Spanish Retrospective Multicenter Study.Clinical lung cancer, , Volume: 21, Issue:5, 2020
Afatinib + bevacizumab combination therapy in EGFR-mutant NSCLC patients with osimertinib resistance: Protocol of an open-label, phase II, multicenter, single-arm trial.Thoracic cancer, , Volume: 11, Issue:8, 2020
Simultaneous Single Cell Gene Expression and EGFR Mutation Analysis of Circulating Tumor Cells Reveals Distinct Phenotypes in NSCLC.Advanced biosystems, , Volume: 4, Issue:8, 2020
Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.Clinical lung cancer, , Volume: 21, Issue:3, 2020
Successful treatment of an elderly patient with an uncommon L861Q epidermal growth factor receptor mutation with low-dose afatinib: A case report.Thoracic cancer, , Volume: 11, Issue:2, 2020
Differential significance of molecular subtypes which were classified into EGFR exon 19 deletion on the first line afatinib monotherapy.BMC cancer, , Feb-06, Volume: 20, Issue:1, 2020
Inflammatory changes in actinic keratoses associated with afatinib therapy.Cutis, , Volume: 105, Issue:3, 2020
Durable complete response after afatinib and crizotinib in an advanced non-small cell lung cancer patient with EGFR L861Q mutation and acquired MET amplification: a case report.Annals of palliative medicine, , Volume: 9, Issue:5, 2020
Propensity score analysis of overall survival between first- and second-generation EGFR-TKIs using real-world data.Cancer science, , Volume: 111, Issue:10, 2020
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.Scientific reports, , 12-03, Volume: 9, Issue:1, 2019
[Comparison of Effectiveness of Gefitinib, Erlotinib, and Afatinib in Advanced Non-small Cell Lung Cancer Patients with EGFR Mutation Positive in Indonesian Population].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , 09-20, Volume: 22, Issue:9, 2019
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in non-small cell lung cancer harboring uncommon EGFR mutations: Focus on afatinib.Seminars in oncology, , Volume: 46, Issue:3, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
Successful Treatment of a Patient With NSCLC Harboring an EGFR Mutation and a Concomitant Met Exon 14 Skipping Mutation Combining Afatinib and Crizotinib.Clinical lung cancer, , Volume: 20, Issue:1, 2019
Cost-utility of afatinib and gefitinib as first-line treatment for EGFR-mutated advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:2, 2019
A phase Ib study of the combination of afatinib and ruxolitinib in EGFR mutant NSCLC with progression on EGFR-TKIs.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Acquired Resistance of MET-Amplified Non-small Cell Lung Cancer Cells to the MET Inhibitor Capmatinib.Cancer research and treatment, , Volume: 51, Issue:3, 2019
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Development of two different formats of heterogeneous fluorescence immunoassay for bioanalysis of afatinib by employing fluorescence plate reader and KinExA 3200 immunosensor.Scientific reports, , 10-14, Volume: 9, Issue:1, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
Which Is Better EGFR-TKI Followed by Osimertinib: Afatinib or Gefitinib/Erlotinib?Anticancer research, , Volume: 39, Issue:7, 2019
The dual PI3K/mTOR inhibitor BEZ235 restricts the growth of lung cancer tumors regardless of EGFR status, as a potent accompanist in combined therapeutic regimens.Journal of experimental & clinical cancer research : CR, , Jul-01, Volume: 38, Issue:1, 2019
Monomer Preference of EGFR Tyrosine Kinase Inhibitors Influences the Synergistic Efficacy of Combination Therapy with Cetuximab.Molecular cancer therapeutics, , Volume: 18, Issue:9, 2019
Cardiac Toxicity From Afatinib in EGFR-Mutated NSCLC: A Rare But Possible Side Effect.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:7, 2019
First-line afatinib for advanced EGFRm+ NSCLC: Analysis of long-term responders in the LUX-Lung 3, 6, and 7 trials.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Outcome Differences Between First- and Second-generation EGFR Inhibitors in Advanced EGFR Mutated NSCLC in a Large Population-based Cohort.Clinical lung cancer, , Volume: 20, Issue:5, 2019
Cx32 mediates norepinephrine-promoted EGFR-TKI resistance in a gap junction-independent manner in non-small-cell lung cancer.Journal of cellular physiology, , Volume: 234, Issue:12, 2019
Sequencing of therapy following first-line afatinib in patients with EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 132, 2019
Efficacy and safety of afatinib in a Chinese population with advanced lung adenocarcinoma with sensitive EGFR mutations.Thoracic cancer, , Volume: 10, Issue:6, 2019
Real-world study of afatinib in first-line or re-challenge settings for patients with EGFR mutant non-small cell lung cancer.Medical oncology (Northwood, London, England), , May-14, Volume: 36, Issue:6, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
Clinical significance of monitoring EGFR mutation in plasma using multiplexed digital PCR in EGFR mutated patients treated with afatinib (West Japan Oncology Group 8114LTR study).Lung cancer (Amsterdam, Netherlands), , Volume: 131, 2019
Clinical analysis of EGFR-positive non-small cell lung cancer patients treated with first-line afatinib: A Nagano Lung Cancer Research Group.Thoracic cancer, , Volume: 10, Issue:5, 2019
Tyrosine Kinase Inhibitor Gold Nanoconjugates for the Treatment of Non-Small Cell Lung Cancer.ACS applied materials & interfaces, , May-08, Volume: 11, Issue:18, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
A phase II study of low starting dose of afatinib as first-line treatment in patients with EGFR mutation-positive non-small-cell lung cancer (KTORG1402).Lung cancer (Amsterdam, Netherlands), , Volume: 135, 2019
Duration of treatment among patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive non-small-cell lung cancer in the USA.Future oncology (London, England), , Volume: 15, Issue:13, 2019
Repeat biopsy procedures and T790M rates after afatinib, gefitinib, or erlotinib therapy in patients with lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 130, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
Strategies to overcome acquired resistance to EGFR TKI in the treatment of non-small cell lung cancer.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 21, Issue:10, 2019
PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.Advanced healthcare materials, , Volume: 8, Issue:23, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
From Diagnostic-Therapeutic Pathways to Real-World Data: A Multicenter Prospective Study on Upfront Treatment for The oncologist, , Volume: 24, Issue:6, 2019
Secreted Phosphoprotein 1 (SPP1) Contributes to Second-Generation EGFR Tyrosine Kinase Inhibitor Resistance in Non-Small Cell Lung Cancer.Oncology research, , Aug-08, Volume: 27, Issue:8, 2019
Afatinib in NSCLC With HER2 Mutations: Results of the Prospective, Open-Label Phase II NICHE Trial of European Thoracic Oncology Platform (ETOP).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Survival outcome of tyrosine kinase inhibitors beyond progression in association to radiotherapy in oligoprogressive EGFR-mutant non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:33, 2019
First-line afatinib vs gefitinib for patients with EGFR mutation-positive NSCLC (LUX-Lung 7): impact of afatinib dose adjustment and analysis of mode of initial progression for patients who continued treatment beyond progression.Journal of cancer research and clinical oncology, , Volume: 145, Issue:6, 2019
Re-challenge of afatinib after 1st generation EGFR-TKI failure in patients with previously treated non-small cell lung cancer harboring EGFR mutation.Cancer chemotherapy and pharmacology, , Volume: 83, Issue:5, 2019
Afatinib-loaded immunoliposomes functionalized with cetuximab: A novel strategy targeting the epidermal growth factor receptor for treatment of non-small-cell lung cancer.International journal of pharmaceutics, , Apr-05, Volume: 560, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
Cost-effectiveness of afatinib, gefitinib, erlotinib and pemetrexed-based chemotherapy as first-line treatments for advanced non-small cell lung cancer in China.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Efficacy of afatinib or osimertinib plus cetuximab combination therapy for non-small-cell lung cancer with EGFR exon 20 insertion mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Impact of afatinib dose modification on safety and effectiveness in patients with EGFR mutation-positive advanced NSCLC: Results from a global real-world study (RealGiDo).Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
HER2 exon 20 insertions in non-small-cell lung cancer are sensitive to the irreversible pan-HER receptor tyrosine kinase inhibitor pyrotinib.Annals of oncology : official journal of the European Society for Medical Oncology, , 03-01, Volume: 30, Issue:3, 2019
Palbociclib overcomes afatinib resistance in non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 109, 2019
Acquired EGFR L718V Mutation and Loss of T790M-Mediated Resistance to Osimertinib in a Patient With NSCLC Who Responded to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:12, 2019
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Prospective exosome-focused translational research for afatinib study of non-small cell lung cancer patients expressing EGFR (EXTRA study).Thoracic cancer, , Volume: 10, Issue:2, 2019
Phase 2 Study of Afatinib Alone or Combined With Bevacizumab in Chemonaive Patients With Advanced Non-Small-Cell Lung Cancer Harboring EGFR Mutations: AfaBev-CS Study Protocol.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Dual blockade of EGFR tyrosine kinase using osimertinib and afatinib eradicates EGFR‑mutant Ba/F3 cells.Oncology reports, , Volume: 41, Issue:2, 2019
Real-world experience of first-line afatinib in patients with EGFR-mutant advanced NSCLC: a multicenter observational study.BMC cancer, , Sep-09, Volume: 19, Issue:1, 2019
Afatinib Overcomes Pemetrexed-Acquired Resistance in Non-Small Cell Lung Cancer Cells Harboring an EML4-ALK Rearrangement.Cells, , 11-28, Volume: 8, Issue:12, 2019
Potential for afatinib as an optimal treatment for advanced non-small cell lung carcinoma in patients with uncommon EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Impact of Exon 19 Deletion Subtypes in EGFR-Mutant Metastatic Non-Small-Cell Lung Cancer Treated With First-Line Tyrosine Kinase Inhibitors.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib.Cancer research and treatment, , Volume: 51, Issue:2, 2019
Bilateral Ulcerative Keratitis Associated With Afatinib Treatment for Non-Small-cell Lung Carcinoma.Cornea, , Volume: 38, Issue:3, 2019
Fingolimod augments Pemetrexed killing of non-small cell lung cancer and overcomes resistance to ERBB inhibition.Cancer biology & therapy, , Volume: 20, Issue:5, 2019
Therapeutic Strategies in EGFR Mutant Non-Small Cell Lung Cancer.Current treatment options in oncology, , 09-29, Volume: 19, Issue:11, 2018
Overview of the LUX-Lung clinical trial program of afatinib for non-small cell lung cancer.Cancer treatment reviews, , Volume: 69, 2018
Phase I Study Evaluating the Combination of Afatinib with Carboplatin and Pemetrexed After First-line EGFR-TKIs.Anticancer research, , Volume: 38, Issue:8, 2018
Sequential treatment with afatinib and osimertinib in patients with EGFR mutation-positive non-small-cell lung cancer: an observational study.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Activity of Afatinib in Heavily Pretreated Patients With ERBB2 Mutation-Positive Advanced NSCLC: Findings From a Global Named Patient Use Program.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
An Evolving Algorithm to Select and Sequence Therapies in EGFR Mutation-positive NSCLC: A Strategic Approach.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Afatinib plus bevacizumab combination after acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant non-small cell lung cancer: Multicenter, single-arm, phase 2 trial (ABC Study).Cancer, , 10-01, Volume: 124, Issue:19, 2018
Real Clinical Practice of Using Afatinib Therapy in NSCLC Patients with an Acquired Anticancer research, , Volume: 38, Issue:9, 2018
Ankyrin Repeat Domain 1 Overexpression is Associated with Common Resistance to Afatinib and Osimertinib in EGFR-mutant Lung Cancer.Scientific reports, , 10-05, Volume: 8, Issue:1, 2018
An observational study of the epidermal growth factor receptor-tyrosine kinase inhibitor resistance mechanism in epidermal growth factor receptor gene mutation-positive non-small cell lung cancer.Medicine, , Volume: 97, Issue:40, 2018
[Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Sep-20, Volume: 21, Issue:9, 2018
Exploration of resistance mechanisms for epidermal growth factor receptor-tyrosine kinase inhibitors based on plasma analysis by digital polymerase chain reaction and next-generation sequencing.Cancer science, , Volume: 109, Issue:12, 2018
Afatinib Therapy: Practical Management of Adverse Events With an Oral Agent for Non-Small Cell Lung Cancer Treatment.Clinical journal of oncology nursing, , 10-01, Volume: 22, Issue:5, 2018
A phase II trial of EGFR-TKI readministration with afatinib in advanced non-small-cell lung cancer harboring a sensitive non-T790M EGFR mutation: Okayama Lung Cancer Study Group trial 1403.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
Sensitivity of epidermal growth factor receptor with single or double uncommon mutations to afatinib confirmed by a visual assay.Cancer science, , Volume: 109, Issue:11, 2018
Does EGFR Mutation Type Influence Patient-Reported Outcomes in Patients with Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer? Analysis of Two Large, Phase III Studies Comparing Afatinib with Chemotherapy (LUX-Lung 3 and LUX-Lung 6).The patient, , Volume: 11, Issue:1, 2018
Efficacy of Afatinib in a Previously-Treated Patient with Non-Small Cell Lung Cancer Harboring HER2 Mutation: Case Report.Journal of Korean medical science, , Jan-01, Volume: 33, Issue:1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
Utilization of Molecular Testing and Survival Outcomes of Treatment with First- or Second-line Tyrosine Kinase Inhibitors in Advanced Non-small Cell Lung Cancer in a Dutch Population.Anticancer research, , Volume: 38, Issue:1, 2018
A phase I trial of afatinib and bevacizumab in chemo-naïve patients with advanced non-small-cell lung cancer harboring EGFR mutations: Okayama Lung Cancer Study Group Trial 1404.Lung cancer (Amsterdam, Netherlands), , Volume: 115, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Optimizing outcomes in EGFR mutation-positive NSCLC: which tyrosine kinase inhibitor and when?Future oncology (London, England), , Volume: 14, Issue:11, 2018
Global named patient use program of afatinib in advanced non-small-cell lung carcinoma patients who progressed following prior therapies.Future oncology (London, England), , Volume: 14, Issue:15, 2018
Improvement of erosive pustular dermatosis of the scalp following discontinuation of chemotherapy with afatinib.European journal of dermatology : EJD, , 04-01, Volume: 28, Issue:2, 2018
EGFR-mediated interleukin enhancer-binding factor 3 contributes to formation and survival of cancer stem-like tumorspheres as a therapeutic target against EGFR-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 116, 2018
A phase I study of afatinib for patients aged 75 or older with advanced non-small cell lung cancer harboring EGFR mutations.Medical oncology (Northwood, London, England), , Feb-08, Volume: 35, Issue:3, 2018
Best Response According to RECIST During First-line EGFR-TKI Treatment Predicts Survival in EGFR Mutation-positive Non-Small-cell Lung Cancer Patients.Clinical lung cancer, , Volume: 19, Issue:3, 2018
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Case sharing of a patient re-challenged with afatinib for EGFR-mutated advanced non-small cell lung cancer.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Therapeutic strategies for afatinib-resistant lung cancer harboring HER2 alterations.Cancer science, , Volume: 109, Issue:5, 2018
Cardiovascular safety of novel non-small cell lung cancer oncotherapy in a patient treated with novel generations of tyrosine kinase inhibitors.Kardiologia polska, , Volume: 76, Issue:3, 2018
Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 118, 2018
Cost effectiveness analysis of afatinib versus pemetrexed-cisplatin for first-line treatment of locally advanced or metastatic EGFR mutation positive non-small-cell lung cancer from the Singapore healthcare payer's perspective.BMC cancer, , 03-27, Volume: 18, Issue:1, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Afatinib as First-line Treatment of Older Patients With EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Subgroup Analyses of the LUX-Lung 3, LUX-Lung 6, and LUX-Lung 7 Trials.Clinical lung cancer, , Volume: 19, Issue:4, 2018
Afatinib in heavily pretreated advanced NSCLC patients who progressed following prior gefitinib or erlotinib: Compassionate use program in Korea.Lung cancer (Amsterdam, Netherlands), , Volume: 119, 2018
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer.Nature medicine, , Volume: 24, Issue:5, 2018
Afatinib in Osimertinib-Resistant EGFR ex19del/T790M/P794L Mutated NSCLC.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:9, 2018
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Effects of secondary EGFR mutations on resistance against upfront osimertinib in cells with EGFR-activating mutations in vitro.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Influence of afatinib dose on outcomes of advanced EGFR-mutant NSCLC patients with brain metastases.BMC cancer, , Dec-03, Volume: 18, Issue:1, 2018
Budget Impact Analysis of Afatinib for First-Line Treatment of Patients with Metastatic Non-Small Cell Lung Cancer with Epidermal Growth Factor Receptor Exon 19 Deletions or Exon 21 Substitution Mutations in a U.S. Health Plan.Journal of managed care & specialty pharmacy, , Volume: 24, Issue:6, 2018
Cost-effectiveness of Osimertinib in the First-Line Treatment of Patients With EGFR-Mutated Advanced Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the EGFR inhibitors afatinib, erlotinib and osimertinib, the ALK inhibitor crizotinib and the VEGFR inhibitor nintedanib in human plasma from non-small cell lung cancJournal of pharmaceutical and biomedical analysis, , Sep-05, Volume: 158, 2018
Afatinib with subsequent surgery in stage III NSCLC with EGFR mutation: Lessons learned from two clinical experiences.Tumori, , Volume: 104, Issue:6, 2018
Afatinib in advanced pretreated non-small-cell lung cancer- a Canadian experience.Current oncology (Toronto, Ont.), , Volume: 25, Issue:5, 2018
Economic analysis of osimertinib in previously untreated EGFR-mutant advanced non-small cell lung cancer in Canada.Lung cancer (Amsterdam, Netherlands), , Volume: 125, 2018
Anti-tumor activity of Shikonin against afatinib resistant non-small cell lung cancer via negative regulation of PI3K/Akt signaling pathway.Bioscience reports, , 12-21, Volume: 38, Issue:6, 2018
Relationship between Paronychia and Drug Concentrations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.Oncology, , Volume: 95, Issue:4, 2018
Irreversible tyrosine kinase inhibition of epidermal growth factor receptor with afatinib in Current oncology (Toronto, Ont.), , Volume: 25, Issue:Suppl 1, 2018
Advanced non-small cell lung cancer (NSCLC) with activating EGFR mutations: first-line treatment with afatinib and other EGFR TKIs.Expert review of anticancer therapy, , Volume: 17, Issue:2, 2017
The European Society for Medical Oncology Magnitude of Clinical Benefit Scale (ESMO-MCBS) applied to pivotal phase III randomized-controlled trials of tyrosine kinase inhibitors in first-line for advanced non-small cell lung cancer with activating epidermExpert review of pharmacoeconomics & outcomes research, , Volume: 17, Issue:1, 2017
Variations in EGFR ctDNA Correlates to the Clinical Efficacy of Afatinib in Non Small Cell Lung Cancer with Acquired Resistance.Pathology oncology research : POR, , Volume: 23, Issue:2, 2017
Phase II Study of the EGFR-TKI Rechallenge With Afatinib in Patients With Advanced NSCLC Harboring Sensitive EGFR Mutation Without T790M: Okayama Lung Cancer Study Group Trial OLCSG 1403.Clinical lung cancer, , Volume: 18, Issue:2, 2017
Prognostic value of early response assessment using (18F)FDG-PET in patients with advanced non-small cell lung cancer treated with tyrosine-kinase inhibitors.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 65, Issue:5, 2017
Treatment Paradigms for Advanced Non-Small Cell Lung Cancer at Academic Medical Centers: Involvement in Clinical Trial Endpoint Design.The oncologist, , Volume: 22, Issue:6, 2017
Efficacy of continuous EGFR-inhibition and role of Hedgehog in EGFR acquired resistance in human lung cancer cells with activating mutation of EGFR.Oncotarget, , Apr-04, Volume: 8, Issue:14, 2017
Afatinib versus gefitinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: overall survival data from the phase IIb LUX-Lung 7 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , 02-01, Volume: 28, Issue:2, 2017
Recent Management of Patients with Advanced Epidermal Growth Factor Receptor Mutation Non-small Cell Lung Cancer: Role of Afatinib and Lesson Learned for Developing Countries.Acta medica Indonesiana, , Volume: 49, Issue:1, 2017
Therapeutic Efficacy Comparison of 5 Major EGFR-TKIs in Advanced EGFR-positive Non-Small-cell Lung Cancer: A Network Meta-analysis Based on Head-to-Head Trials.Clinical lung cancer, , Volume: 18, Issue:5, 2017
Activation of signal transducer and activator of transcription 3 (STAT3) signaling in EGFR mutant non-small-cell lung cancer (NSCLC).Oncotarget, , Jul-18, Volume: 8, Issue:29, 2017
Purpuric Drug Eruptions Caused by Epidermal Growth Factor Receptor Inhibitors for Non-Small Cell Lung Cancer: A Clinicopathologic Study of 32 Cases.JAMA dermatology, , 09-01, Volume: 153, Issue:9, 2017
Association Between EGFR T790M Status and Progression Patterns During Initial EGFR-TKI Treatment in Patients Harboring EGFR Mutation.Clinical lung cancer, , Volume: 18, Issue:6, 2017
A phase Ib trial of continuous once-daily oral afatinib plus sirolimus in patients with epidermal growth factor receptor mutation-positive non-small cell lung cancer and/or disease progression following prior erlotinib or gefitinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
HER2 regulates cancer stem-like cell phenotype in ALK translocated NSCLC.International journal of oncology, , Volume: 51, Issue:2, 2017
Matrine increases the inhibitory effects of afatinib on H1975 cells via the IL‑6/JAK1/STAT3 signaling pathway.Molecular medicine reports, , Volume: 16, Issue:3, 2017
Update on afatinib-based combination regimens for the treatment of EGFR mutation-positive non-small-cell lung cancer.Future oncology (London, England), , Volume: 13, Issue:21, 2017
The Effect of Afatinib Treatment in Non-small Cell Lung Cancer Cells.Anticancer research, , Volume: 37, Issue:7, 2017
Treatment in EGFR-mutated non-small cell lung cancer: how to block the receptor and overcome resistance mechanisms.Tumori, , Jul-31, Volume: 103, Issue:4, 2017
Case series on the association between blood levels and side effects of afatinib maleate.Cancer chemotherapy and pharmacology, , Volume: 80, Issue:3, 2017
Significance of neutrophil-to-lymphocyte ratio in Western advanced EGFR-mutated non-small cell lung cancer receiving a targeted therapy.Tumori, , Sep-18, Volume: 103, Issue:5, 2017
Cerebrospinal Fluid Penetration Rate and Efficacy of Afatinib in Patients with EGFR Mutation-positive Non-small Cell Lung Cancer with Leptomeningeal Carcinomatosis: A Multicenter Prospective Study.Anticancer research, , Volume: 37, Issue:8, 2017
Cost-Effectiveness Analysis of Afatinib versus Gefitinib for First-Line Treatment of Advanced EGFR-Mutated Advanced Non-Small Cell Lung Cancers.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:10, 2017
Overall survival in EGFR mutated non-small-cell lung cancer patients treated with afatinib after EGFR TKI and resistant mechanisms upon disease progression.PloS one, , Volume: 12, Issue:8, 2017
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.Anticancer research, , Volume: 37, Issue:9, 2017
Appendix 7: Metastatic non-small-cell lung cancer (1): MCBS eUpdate published online 28 June 2017 (www.esmo.org/Guidelines/Lung-and-Chest-Tumours).Annals of oncology : official journal of the European Society for Medical Oncology, , Jul-01, Volume: 28, Issue:suppl_4, 2017
Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 23, Issue:3, 2017
Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.Science translational medicine, , Nov-08, Volume: 9, Issue:415, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.Clinical drug investigation, , Volume: 37, Issue:6, 2017
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
Chronic myelomonocytic leukemia blast crisis in a patient with advanced non-small cell lung cancer treated with EGFR tyrosine kinase inhibitors.Respiratory investigation, , Volume: 55, Issue:2, 2017
[Precision first-line therapy for advanced non-small-cell lung cancer patients harboring EGFR mutation].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Feb-23, Volume: 39, Issue:2, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Novel EGFR Inhibitors in Non-small Cell Lung Cancer: Current Status of Afatinib.Current oncology reports, , Volume: 19, Issue:1, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
Novel EGFR Exon 18 (G721R) Mutation in a Patient with Non-Small Cell Lung Carcinoma with Lack of Response to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
Randomized Phase II Study of Afatinib Plus Simvastatin Versus Afatinib Alone in Previously Treated Patients with Advanced Nonadenocarcinomatous Non-small Cell Lung Cancer.Cancer research and treatment, , Volume: 49, Issue:4, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
Clinical Efficacy of Afatinib Treatment for a Patient with Leptomeningeal Carcinomatosis.Chemotherapy, , Volume: 62, Issue:3, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Risk of Treatment-Related Toxicities from EGFR Tyrosine Kinase Inhibitors: A Meta-analysis of Clinical Trials of Gefitinib, Erlotinib, and Afatinib in Advanced EGFR-Mutated Non-Small Cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
Rapid Acquisition of T790M Mutation after Treatment with Afatinib in an NSCLC Patient Harboring EGFR Exon 20 S768I Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:1, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
HER2 Transmembrane Domain (TMD) Mutations (V659/G660) That Stabilize Homo- and Heterodimerization Are Rare Oncogenic Drivers in Lung Adenocarcinoma That Respond to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:3, 2017
Successful afatinib treatment of advanced non-small-cell lung cancer patients undergoing hemodialysis.Cancer chemotherapy and pharmacology, , Volume: 79, Issue:1, 2017
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Clinical analysis of patients treated with afatinib for advanced non-small cell lung cancer: A Nagano Lung Cancer Research Group observational study.Respiratory investigation, , Volume: 54, Issue:6, 2016
Afatinib: A Review in Advanced Non-Small Cell Lung Cancer.Targeted oncology, , Volume: 11, Issue:6, 2016
Case report: Durable response to afatinib in a patient with lung cancer harboring two uncommon mutations of EGFR and a KRAS mutation.Lung cancer (Amsterdam, Netherlands), , Volume: 101, 2016
The safety of afatinib for the treatment of non-small cell lung cancer.Expert opinion on drug safety, , Volume: 15, Issue:11, 2016
Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:11, 2016
Non-small Cell Lung Cancer in South Wales: Are Exon 19 Deletions and L858R Different?Anticancer research, , Volume: 36, Issue:8, 2016
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20, 2016
[Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Evidence on afatinib in patients progressing on a first-line treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib as first-line therapy in mutation-positive EGFR. Results by type of mutation].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Mechanism of action and preclinical development of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Current status of EGFR/ErbB inhibitors in non-small cell lung carcinoma].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Not Available].Medicina clinica, , Volume: 146 Suppl 1, 2016
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , May-25, Issue:5, 2016
Tyrosine kinase inhibitors for epidermal growth factor receptor gene mutation-positive non-small cell lung cancers: an update for recent advances in therapeutics.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 22, Issue:3, 2016
Epidermal growth factor receptor tyrosine kinase inhibitors in previously treated advanced non-small-cell lung cancer with wild-type EGFR.Expert opinion on pharmacotherapy, , Volume: 17, Issue:2, 2016
Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations.Cancer science, , Volume: 107, Issue:1, 2016
Risk of elevated transaminases in non-small cell lung cancer (NSCLC) patients treated with erlotinib, gefitinib and afatinib: a meta-analysis.Expert review of respiratory medicine, , Volume: 10, Issue:2, 2016
Detection of T790M, the Acquired Resistance EGFR Mutation, by Tumor Biopsy versus Noninvasive Blood-Based Analyses.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-01, Volume: 22, Issue:5, 2016
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1, 2016
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with erlotinib: a case report.Anti-cancer drugs, , Volume: 27, Issue:3, 2016
First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
Resistance mechanisms after tyrosine kinase inhibitors afatinib and crizotinib in non-small cell lung cancer, a review of the literature.Critical reviews in oncology/hematology, , Volume: 100, 2016
Different EGFR Gene Mutations in Exon 18, 19 and 21 as Prognostic and Predictive Markers in NSCLC: A Single Institution Analysis.Molecular diagnosis & therapy, , Volume: 20, Issue:1, 2016
Afatinib beyond progression in patients with non-small-cell lung cancer following chemotherapy, erlotinib/gefitinib and afatinib: phase III randomized LUX-Lung 5 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:3, 2016
therascreen® EGFR RGQ PCR Kit: A Companion Diagnostic for Afatinib and Gefitinib in Non-Small Cell Lung Cancer.Molecular diagnosis & therapy, , Volume: 20, Issue:2, 2016
Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer.JAMA dermatology, , Volume: 152, Issue:3, 2016
Efficacy and safety of afatinib in Chinese patients with EGFR-mutated metastatic non-small-cell lung cancer (NSCLC) previously responsive to first-generation tyrosine-kinase inhibitors (TKI) and chemotherapy: comparison with historical cohort using erlotiBMC cancer, , Feb-24, Volume: 16, 2016
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Afatinib in the first-line treatment of epidermal-growth-factor-receptor mutation-positive non-small cell lung cancer: a review of the clinical evidence.Therapeutic advances in respiratory disease, , Volume: 10, Issue:3, 2016
Selectivity profile of afatinib for EGFR-mutated non-small-cell lung cancer.Molecular bioSystems, , 04-26, Volume: 12, Issue:5, 2016
Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors.Critical reviews in oncology/hematology, , Volume: 97, 2016
Functionalized gold nanoparticles improve afatinib delivery into cancer cells.Expert opinion on drug delivery, , Volume: 13, Issue:1, 2016
Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience.Cancer chemotherapy and pharmacology, , Volume: 77, Issue:5, 2016
A Phase Ib/II Study of Afatinib in Combination with Nimotuzumab in Non-Small Cell Lung Cancer Patients with Acquired Resistance to Gefitinib or Erlotinib.Clinical cancer research : an official journal of the American Association for Cancer Research, , 05-01, Volume: 22, Issue:9, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer.Biomedical chromatography : BMC, , Volume: 30, Issue:7, 2016
Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial.The Lancet. Oncology, , Volume: 17, Issue:5, 2016
Afatinib and chemotherapy in non-small-cell lung cancer.The Lancet. Oncology, , Volume: 17, Issue:2, 2016
Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells.Molecular carcinogenesis, , Volume: 55, Issue:5, 2016
[The efficacy of TKIs in treatment of human primary small cell lung cancer xenograft model in vivo].Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology, , Jun-08, Volume: 32, Issue:6, 2016
Phase II study of afatinib, an irreversible ErbB family blocker, in EGFR FISH-positive non-small-cell lung cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:4, 2015
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
Afatinib induces apoptosis in NSCLC without EGFR mutation through Elk-1-mediated suppression of CIP2A.Oncotarget, , Feb-10, Volume: 6, Issue:4, 2015
Afatinib (Gilotrif) for advanced non-small cell lung cancer.The Medical letter on drugs and therapeutics, , May-25, Volume: 57, Issue:1469, 2015
Current and Emerging Options in the Management of EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Considerations in the Elderly.Drugs & aging, , Volume: 32, Issue:11, 2015
E-Cadherin and EpCAM expression by NSCLC tumour cells associate with normal fibroblast activation through a pathway initiated by integrin αvβ6 and maintained through TGFβ signalling.Oncogene, , Feb-05, Volume: 34, Issue:6, 2015
[Hange-Shashin-to for preventing diarrhea during afatinib therapy].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:5, 2015
Cumulative meta-analysis of epidermal growth factor receptor-tyrosine kinase inhibitors as first-line therapy in metastatic non-small-cell lung cancer.Anti-cancer drugs, , Volume: 26, Issue:9, 2015
Symptom and Quality of Life Improvement in LUX-Lung 6: An Open-Label Phase III Study of Afatinib Versus Cisplatin/Gemcitabine in Asian Patients With EGFR Mutation-Positive Advanced Non-small-cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:6, 2015
[Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis].Voprosy onkologii, , Volume: 61, Issue:4, 2015
Afatinib is especially effective against non-small cell lung cancer carrying an EGFR exon 19 deletion.Anticancer research, , Volume: 35, Issue:4, 2015
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
Afatinib in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations Pretreated With Reversible EGFR Inhibitors.The oncologist, , Volume: 20, Issue:10, 2015
Acquisition of cancer stem cell-like properties in non-small cell lung cancer with acquired resistance to afatinib.Cancer science, , Volume: 106, Issue:10, 2015
Treatment approaches for EGFR-inhibitor-resistant patients with non-small-cell lung cancer.The Lancet. Oncology, , Volume: 16, Issue:9, 2015
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.The oncologist, , Volume: 20, Issue:8, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
CD133-Positive Cells from Non-Small Cell Lung Cancer Show Distinct Sensitivity to Cisplatin and Afatinib.Archivum immunologiae et therapiae experimentalis, , Volume: 63, Issue:3, 2015
Common EGFR-mutated subgroups (Del19/L858R) in advanced non-small-cell lung cancer: chasing better outcomes with tyrosine kinase inhibitors.Future oncology (London, England), , Volume: 11, Issue:8, 2015
Afatinib resistance in non-small cell lung cancer involves the PI3K/AKT and MAPK/ERK signalling pathways and epithelial-to-mesenchymal transition.Targeted oncology, , Volume: 10, Issue:3, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Overcoming Resistance Without the Risk of Reaction: Use of Afatinib and Panitumumab in Two Cases of Epidermal Growth Factor Receptor--Mutated Non--Small-Cell Lung Cancer With T790M Mutations.Clinical lung cancer, , Volume: 16, Issue:5, 2015
Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.The oncologist, , Volume: 20, Issue:4, 2015
Afatinib: a second-generation EGF receptor and ErbB tyrosine kinase inhibitor for the treatment of advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 11, Issue:18, 2015
Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy, , Volume: 29, Issue:3, 2015
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.Expert opinion on drug safety, , Volume: 14, Issue:1, 2015
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.British journal of cancer, , Nov-17, Volume: 113, Issue:10, 2015
[Is chemotherapy still an option in oncogene-addicted non-small cell lung cancer? No].Bulletin du cancer, , Volume: 102, Issue:6 Suppl 1, 2015
Afatinib increases sensitivity to radiation in non-small cell lung cancer cells with acquired EGFR T790M mutation.Oncotarget, , Mar-20, Volume: 6, Issue:8, 2015
Cost-Effectiveness and Value of Information of Erlotinib, Afatinib, and Cisplatin-Pemetrexed for First-Line Treatment of Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer in the United States.Value in health : the journal of the International Society for Pharmacoeconomics and Outcomes Research, , Volume: 18, Issue:6, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
Risk of fatal pulmonary events in patients with advanced non-small-cell lung cancer treated with EGF receptor tyrosine kinase inhibitors: a comparative meta-analysis.Future oncology (London, England), , Volume: 11, Issue:7, 2015
[Pharmacological and clinical profile of afatinib (Giotrif®)].Nihon yakurigaku zasshi. Folia pharmacologica Japonica, , Volume: 145, Issue:2, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
Managing acquired resistance in EGFR-mutated non-small cell lung cancer.Clinical advances in hematology & oncology : H&O, , Volume: 13, Issue:8, 2015
The pan-HER family tyrosine kinase inhibitor afatinib overcomes HER3 ligand heregulin-mediated resistance to EGFR inhibitors in non-small cell lung cancer.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6.The Lancet. Oncology, , Volume: 16, Issue:7, 2015
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
Subsequent treatment choices for patients with acquired resistance to EGFR-TKIs in non-small cell lung cancer: restore after a drug holiday or switch to another EGFR-TKI?Asian Pacific journal of cancer prevention : APJCP, , Volume: 15, Issue:1, 2014
Afatinib for lung cancer: let there be light?The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib: a review of its use in the treatment of advanced non-small cell lung cancer.Drugs, , Volume: 74, Issue:2, 2014
The current state of molecularly targeted drugs targeting HGF/Met.Japanese journal of clinical oncology, , Volume: 44, Issue:1, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors.Clinical lung cancer, , Volume: 15, Issue:6, 2014
Dual ALK and EGFR inhibition targets a mechanism of acquired resistance to the tyrosine kinase inhibitor crizotinib in ALK rearranged lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 83, Issue:1, 2014
Experience with afatinib in patients with non-small cell lung cancer progressing after clinical benefit from gefitinib and erlotinib.The oncologist, , Volume: 19, Issue:10, 2014
Patients with exon 19 deletion were associated with longer progression-free survival compared to those with L858R mutation after first-line EGFR-TKIs for advanced non-small cell lung cancer: a meta-analysis.PloS one, , Volume: 9, Issue:9, 2014
β-catenin contributes to lung tumor development induced by EGFR mutations.Cancer research, , Oct-15, Volume: 74, Issue:20, 2014
FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor.Oncotarget, , Aug-15, Volume: 5, Issue:15, 2014
[A new perspective in the treatment of non-small-cell lung cancer (NSCLC). Role of afatinib: An oral and irreversible ErbB family blocker].Bulletin du cancer, , Volume: 101, Issue:6, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
Afatinib in the treatment of EGFR mutation-positive NSCLC--a network meta-analysis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:2, 2014
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, , Volume: 47, Issue:11, 2014
Gefitinib and afatinib treatment in an advanced non-small cell lung cancer (NSCLC) patient undergoing hemodialysis.Anticancer research, , Volume: 34, Issue:6, 2014
[Afatinib (BIBW 2992)].Revue de pneumologie clinique, , Volume: 70, Issue:5, 2014
Phase II study of Afatinib as third-line treatment for patients in Korea with stage IIIB/IV non-small cell lung cancer harboring wild-type EGFR.The oncologist, , Volume: 19, Issue:7, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Afatinib with concurrent radiotherapy in a patient with metastatic non-small cell lung cancer.Oncology research and treatment, , Volume: 37, Issue:5, 2014
Next generation tyrosine kinase inhibitor (TKI): afatinib.Recent patents on anti-cancer drug discovery, , Volume: 9, Issue:3, 2014
Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22, 2014
Meta-analysis of first-line therapies in advanced non-small-cell lung cancer harboring EGFR-activating mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 9, Issue:6, 2014
LUX-Lung 3: redundancy, toxicity or a major step forward? Afatinib as front-line therapy for patients with metastatic EGFR-mutated lung cancer.Future oncology (London, England), , Volume: 10, Issue:4, 2014
Afatinib use in non-small cell lung cancer previously sensitive to epidermal growth factor receptor inhibitors: the United Kingdom Named Patient Programme.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:10, 2014
Afatinib and lung cancer.Expert review of anticancer therapy, , Volume: 14, Issue:12, 2014
Afatinib for the treatment of advanced non-small-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 15, Issue:6, 2014
New therapy targets resistant non-small-cell lung cancers.Journal of the National Cancer Institute, , Volume: 106, Issue:11, 2014
Systemic treatment in EGFR-ALK NSCLC patients: second line therapy and beyond.Expert review of anticancer therapy, , Volume: 14, Issue:7, 2014
Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations.PloS one, , Volume: 9, Issue:2, 2014
Afatinib for the treatment of patients with EGFR-positive non-small cell lung cancer.Drugs of today (Barcelona, Spain : 1998), , Volume: 49, Issue:9, 2013
Afatinib: first global approval.Drugs, , Volume: 73, Issue:13, 2013
Targeted therapies: Afatinib--new therapy option for EGFR-mutant lung cancer.Nature reviews. Clinical oncology, , Volume: 10, Issue:10, 2013
New kinase inhibitor approved for metastatic lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Aug-15, Volume: 70, Issue:16, 2013
Glycolysis inhibition sensitizes non-small cell lung cancer with T790M mutation to irreversible EGFR inhibitors via translational suppression of Mcl-1 by AMPK activation.Molecular cancer therapeutics, , Volume: 12, Issue:10, 2013
Clinical perspective of afatinib in non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 81, Issue:2, 2013
Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
Impact of EGFR inhibitor in non-small cell lung cancer on progression-free and overall survival: a meta-analysis.Journal of the National Cancer Institute, , May-01, Volume: 105, Issue:9, 2013
Synergistic effect of afatinib with su11274 in non-small cell lung cancer cells resistant to gefitinib or erlotinib.PloS one, , Volume: 8, Issue:3, 2013
An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 15, Issue:5, 2013
Symptom and quality of life benefit of afatinib in advanced non-small-cell lung cancer patients previously treated with erlotinib or gefitinib: results of a randomized phase IIb/III trial (LUX-Lung 1).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 8, Issue:2, 2013
Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.Biochemical and biophysical research communications, , Feb-15, Volume: 431, Issue:3, 2013
[Development and biochemical characterization of EGFR/c-Met dual inhibitors].Acta pharmaceutica Hungarica, , Volume: 83, Issue:4, 2013
Disseminated herpes simplex virus infection following epidermal growth factor tyrosine kinase inhibitor therapy for non-small-cell lung carcinoma.Internal medicine journal, , Volume: 42, Issue:11, 2012
Epidermal growth factor receptor (EGFR) inhibitors and derived treatments.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 23 Suppl 10, 2012
Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation.Molecular cancer therapeutics, , Volume: 11, Issue:10, 2012
Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab.BMC medicine, , Mar-21, Volume: 10, 2012
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence.Critical reviews in oncology/hematology, , Volume: 83, Issue:3, 2012
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.Molecular cancer therapeutics, , Volume: 11, Issue:3, 2012
Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4).Cancer chemotherapy and pharmacology, , Volume: 69, Issue:4, 2012
Afatinib (BIBW 2992) development in non-small-cell lung cancer.Future oncology (London, England), , Volume: 7, Issue:7, 2011
The LUX-Lung clinical trial program of afatinib for non-small-cell lung cancer.Expert review of anticancer therapy, , Volume: 11, Issue:5, 2011
The search for improved systemic therapy of non-small cell lung cancer--what are today's options?Lung cancer (Amsterdam, Netherlands), , Volume: 72, Issue:3, 2011
BIBW 2992 in non-small cell lung cancer.Expert opinion on investigational drugs, , Volume: 20, Issue:3, 2011
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.Expert opinion on investigational drugs, , Volume: 19, Issue:12, 2010
EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992.Targeted oncology, , Volume: 5, Issue:4, 2010
Enhanced anticancer effect of the combination of BIBW2992 and thymidylate synthase-targeted agents in non-small cell lung cancer with the T790M mutation of epidermal growth factor receptor.Molecular cancer therapeutics, , Volume: 9, Issue:6, 2010
The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.Cancer investigation, , Volume: 28, Issue:4, 2010
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.Cancer research, , Feb-01, Volume: 70, Issue:3, 2010
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.Clinical lung cancer, , Volume: 10, Issue:4, 2009
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.Oncogene, , Aug-07, Volume: 27, Issue:34, 2008
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Significance of Polar Charged Amino Acids in Compound Mutations in EGFR-mutated Patients Treated With First-line Afatinib.In vivo (Athens, Greece), , Volume: 36, Issue:4
Skeletal muscle loss during anti-epidermal growth factor receptor therapy is an independent prognostic factor on non-small cell lung cancer patients survival.Journal of B.U.ON. : official journal of the Balkan Union of Oncology, , Volume: 26, Issue:3
Identifying activating mutations in the EGFR gene: prognostic and therapeutic implications in non-small cell lung cancer.Jornal brasileiro de pneumologia : publicacao oficial da Sociedade Brasileira de Pneumologia e Tisilogia, , Volume: 41, Issue:4
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.Integrative cancer therapies, , Volume: 20
Synergistic Effect of HAD-B1 and Afatinib Against Gefitinib Resistance of Non-Small Cell Lung Cancer.Integrative cancer therapies, , Volume: 21
Afatinib in the first-line treatment of patients with non-small cell lung cancer: clinical evidence and experience.Therapeutic advances in respiratory disease, , Volume: 12
"From molecular to clinic": The pivotal role of CDC42 in pathophysiology of human papilloma virus related cancers and a correlated sensitivity of afatinib.Frontiers in immunology, , Volume: 14, 2023
Afatinib maintenance therapy following post-operative radiochemotherapy in head and neck squamous cell carcinoma: Results from the phase III randomised double-blind placebo-controlled study BIB2992ORL (GORTEC 2010-02).European journal of cancer (Oxford, England : 1990), , Volume: 178, 2023
NRG1 promotes tumorigenesis and metastasis and afatinib treatment efficiency is enhanced by NRG1 inhibition in esophageal squamous cell carcinoma.Biochemical pharmacology, , Volume: 218, 2023
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
Afatinib and Pembrolizumab for Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (ALPHA Study): A Phase II Study with Biomarker Analysis.Clinical cancer research : an official journal of the American Association for Cancer Research, , 04-14, Volume: 28, Issue:8, 2022
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Phase II study of afatinib plus pembrolizumab in patients with squamous cell carcinoma of the lung following progression during or after first-line chemotherapy (LUX-Lung-IO).Lung cancer (Amsterdam, Netherlands), , Volume: 166, 2022
Real-world effectiveness of second-line Afatinib versus chemotherapy for the treatment of advanced lung squamous cell carcinoma in immunotherapy-naïve patients.BMC cancer, , Nov-15, Volume: 21, Issue:1, 2021
Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).Thoracic cancer, , Volume: 12, Issue:8, 2021
EGFR L861Q and CDK4 amplification responding to afatinib combined with palbociclib treatment in a patient with advanced lung squamous cell carcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 145, 2020
Establishment and characterization of patient-derived xenografts as paraclinical models for head and neck cancer.BMC cancer, , Apr-15, Volume: 20, Issue:1, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Afatinib With Pembrolizumab for Treatment of Patients With Locally Advanced/Metastatic Squamous Cell Carcinoma of the Lung: The LUX-Lung IO/KEYNOTE 497 Study Protocol.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1, 2019
Emergence, development, and future of cardio-oncology in China: cardiohypersensitivity, cardiotoxicity and the Kounis syndrome.Chinese medical journal, , 03-20, Volume: 132, Issue:6, 2019
Afatinib treatment of a squamous lung cancer after tumor progression of nivolumab.Thoracic cancer, , Volume: 9, Issue:1, 2018
Acquired Resistance to Afatinib Due to T790M-Positive Squamous Progression in EGFR-Mutant Adenosquamous Lung Carcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:1, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Predictive biomarkers and EGFR inhibitors in squamous cell carcinoma of head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
The clinical features of squamous cell lung carcinoma with sensitive EGFR mutations.International journal of clinical oncology, , Volume: 23, Issue:3, 2018
Symptom and Quality of Life Improvement in LUX-Lung 8, an Open-Label Phase III Study of Second-Line Afatinib Versus Erlotinib in Patients With Advanced Squamous Cell Carcinoma of the Lung After First-Line Platinum-Based Chemotherapy.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Phase I study of induction chemotherapy with afatinib, ribavirin, and weekly carboplatin and paclitaxel for stage IVA/IVB human papillomavirus-associated oropharyngeal squamous cell cancer.Head & neck, , Volume: 40, Issue:2, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Osimertinib for Secondary T790M-Mutation-Positive Squamous Cell Carcinoma Transformation After Afatinib Failure.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Perspectives on window of opportunity trials in head and neck cancer: lessons from the EORTC 90111-24111-NOCI-HNCG study.European journal of cancer (Oxford, England : 1990), , Volume: 104, 2018
Association of ERBB Mutations With Clinical Outcomes of Afatinib- or Erlotinib-Treated Patients With Lung Squamous Cell Carcinoma: Secondary Analysis of the LUX-Lung 8 Randomized Clinical Trial.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
In Search of an Oncogene Driver for Squamous Lung Cancer.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Afatinib and Erlotinib in the treatment of squamous-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 19, Issue:18, 2018
Second-line therapy of squamous non-small cell lung cancer: an evolving landscape.Expert review of respiratory medicine, , Volume: 11, Issue:6, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Afatinib radiosensitizes head and neck squamous cell carcinoma cells by targeting cancer stem cells.Oncotarget, , Mar-28, Volume: 8, Issue:13, 2017
Evaluation of the VeriStratLung cancer (Amsterdam, Netherlands), , Volume: 109, 2017
Overview of Current Treatment Options and Investigational Targeted Therapies for Locally Advanced Squamous Cell Carcinoma of the Head and Neck.American journal of clinical oncology, , Volume: 39, Issue:4, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
Afatinib in squamous cell carcinoma of the head and neck.Expert opinion on pharmacotherapy, , Volume: 17, Issue:9, 2016
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The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
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HER2 activating mutations are targets for colorectal cancer treatment.Cancer discovery, , Volume: 5, Issue:8, 2015
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Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine, , Volume: 54, Issue:6, 2013
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Severe EGFR inhibitor-induced acneiform eruption responding to dapsone.Dermatology online journal, , Jul-15, Volume: 27, Issue:7, 2021
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Stevens-Johnson syndrome-like erosive dermatitis possibly related to afatinib.European journal of dermatology : EJD, , Aug-01, Volume: 26, Issue:4, 2016
Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer.JAMA dermatology, , Volume: 152, Issue:3, 2016
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New strategy for suppressing the growth of lung cancer cells harboring mutations in the ATP-binding region of EGFR by targeting the molecular motor MYO1D.Clinical and translational medicine, , Volume: 11, Issue:8, 2021
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Afatinib is active in osteosarcoma in osteosarcoma cell lines.Journal of cancer research and clinical oncology, , Volume: 146, Issue:7, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Intestinal epithelial potassium channels and CFTR chloride channels activated in ErbB tyrosine kinase inhibitor diarrhea.JCI insight, , 02-21, Volume: 4, Issue:4, 2019
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Mouse avatar models of esophageal squamous cell carcinoma proved the potential for EGFR-TKI afatinib and uncovered Src family kinases involved in acquired resistance.Journal of hematology & oncology, , 08-29, Volume: 11, Issue:1, 2018
Blocking autophagy improves the anti-tumor activity of afatinib in lung adenocarcinoma with activating EGFR mutations in vitro and in vivo.Scientific reports, , 07-04, Volume: 7, Issue:1, 2017
Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
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A phase II study of first-line afatinib for patients aged ≥75 years with EGFR mutation-positive advanced non-small cell lung cancer: North East Japan Study Group trial NEJ027.BMC cancer, , Mar-01, Volume: 21, Issue:1, 2021
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Afatinib and radiotherapy, with or without temozolomide, in patients with newly diagnosed glioblastoma: results of a phase I trial.Journal of neuro-oncology, , Volume: 155, Issue:3, 2021
Androgen Receptor Activation in Glioblastoma Can Be Achieved by Ligand-Independent Signaling through EGFR-A Potential Therapeutic Target.International journal of molecular sciences, , Oct-11, Volume: 22, Issue:20, 2021
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Boswellic acid has anti-inflammatory effects and enhances the anticancer activities of Temozolomide and Afatinib, an irreversible ErbB family blocker, in human glioblastoma cells.Phytotherapy research : PTR, , Volume: 33, Issue:6, 2019
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[Afatinib maintenance therapy does not confer any benefit in the adjuvant treatment of head and neck tumors].Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al], , Volume: 199, Issue:4, 2023
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Afatinib induces pro-survival autophagy and increases sensitivity to apoptosis in stem-like HNSCC cells.Cell death & disease, , 07-22, Volume: 12, Issue:8, 2021
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Chordoma: A Case Report and Review of Literature.The American journal of case reports, , Jan-23, Volume: 21, 2020
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Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.Oral oncology, , Volume: 97, 2019
Rationale for Using Irreversible Epidermal Growth Factor Receptor Inhibitors in Combination with Phosphatidylinositol 3-Kinase Inhibitors for Advanced Head and Neck Squamous Cell Carcinoma.Molecular pharmacology, , Volume: 95, Issue:5, 2019
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Activity and safety of afatinib in a window preoperative EORTC study in patients with squamous cell carcinoma of the head and neck (SCCHN).Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4, 2018
Biomarkers predict enhanced clinical outcomes with afatinib versus methotrexate in patients with second-line recurrent and/or metastatic head and neck cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
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Afatinib against Esophageal or Head-and-Neck Squamous Cell Carcinoma: Significance of Activating Oncogenic HER4 Mutations in HNSCC.Molecular cancer therapeutics, , Volume: 15, Issue:8, 2016
Afatinib versus methotrexate in older patients with second-line recurrent and/or metastatic head and neck squamous cell carcinoma: subgroup analysis of the LUX-Head & Neck 1 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:8, 2016
Overview of Current Treatment Options and Investigational Targeted Therapies for Locally Advanced Squamous Cell Carcinoma of the Head and Neck.American journal of clinical oncology, , Volume: 39, Issue:4, 2016
A phase I study afatinib/carboplatin/paclitaxel induction chemotherapy followed by standard chemoradiation in HPV-negative or high-risk HPV-positive locally advanced stage III/IVa/IVb head and neck squamous cell carcinoma.Oral oncology, , Volume: 53, 2016
Co-treatment of wild-type EGFR head and neck cancer cell lines with afatinib and cisplatin.Molecular medicine reports, , Volume: 13, Issue:3, 2016
Research Progress in Head and Neck Squamous Cell Carcinoma: Best Abstracts of ICHNO 2015.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2015
Afatinib efficacy against squamous cell carcinoma of the head and neck cell lines in vitro and in vivo.Targeted oncology, , Volume: 10, Issue:4, 2015
Afatinib versus methotrexate as second-line treatment in patients with recurrent or metastatic squamous-cell carcinoma of the head and neck progressing on or after platinum-based therapy (LUX-Head & Neck 1): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:5, 2015
miR-124 Regulates the Epithelial-Restricted with Serine Box/Epidermal Growth Factor Receptor Signaling Axis in Head and Neck Squamous Cell Carcinoma.Molecular cancer therapeutics, , Volume: 14, Issue:10, 2015
Rationale and design of LUX-Head & Neck 1: a randomised, Phase III trial of afatinib versus methotrexate in patients with recurrent and/or metastatic head and neck squamous cell carcinoma who progressed after platinum-based therapy.BMC cancer, , Jun-28, Volume: 14, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
A randomized, phase II study of afatinib versus cetuximab in metastatic or recurrent squamous cell carcinoma of the head and neck.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 25, Issue:9, 2014
Afatinib in the treatment of head and neck squamous cell carcinoma.Expert opinion on investigational drugs, , Volume: 23, Issue:1, 2014
Afatinib versus placebo as adjuvant therapy after chemoradiation in a double-blind, phase III study (LUX-Head & Neck 2) in patients with primary unresected, clinically intermediate-to-high-risk head and neck cancer: study protocol for a randomized controlTrials, , Nov-29, Volume: 15, 2014
Genetic and chemical targeting of epithelial-restricted with serine box reduces EGF receptor and potentiates the efficacy of afatinib.Molecular cancer therapeutics, , Volume: 12, Issue:8, 2013
Ethoxy-erianin phosphate and afatinib synergistically inhibit liver tumor growth and angiogenesis via regulating VEGF and EGFR signaling pathways.Toxicology and applied pharmacology, , 03-01, Volume: 438, 2022
Afatinib, an EGFR inhibitor, decreases EMT and tumorigenesis of Huh‑7 cells by regulating the ERK‑VEGF/MMP9 signaling pathway.Molecular medicine reports, , Volume: 20, Issue:4, 2019
Intranasal delivery of a small-molecule ErbB inhibitor promotes recovery from acute and late-stage CNS inflammation.JCI insight, , 04-08, Volume: 7, Issue:7, 2022
Anti-inflammatory effect of afatinib (an EGFR-TKI) on OGD-induced neuroinflammation.Scientific reports, , 02-21, Volume: 9, Issue:1, 2019
Ethoxy-erianin phosphate and afatinib synergistically inhibit liver tumor growth and angiogenesis via regulating VEGF and EGFR signaling pathways.Toxicology and applied pharmacology, , 03-01, Volume: 438, 2022
Afatinib, an EGFR inhibitor, decreases EMT and tumorigenesis of Huh‑7 cells by regulating the ERK‑VEGF/MMP9 signaling pathway.Molecular medicine reports, , Volume: 20, Issue:4, 2019
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Real-life comparison of afatinib and erlotinib in non-small cell lung cancer with rare EGFR exon 18 and exon 20 mutations: a Turkish Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 149, Issue:2, 2023
All EGFR mutations are (not) created equal: focus on uncommon EGFR mutations.Journal of cancer research and clinical oncology, , Volume: 149, Issue:4, 2023
A case of crescentic glomerulonephritis induced by afatinib for lung adenocarcinoma.CEN case reports, , Volume: 12, Issue:2, 2023
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Older patients with EGFR mutation-positive non-small cell lung cancer treated with afatinib in clinical practice: A subset analysis of the non-interventional GIDEON study.Journal of geriatric oncology, , Volume: 14, Issue:1, 2023
Absence of copy number gain of EGFR: A possible predictive marker of long-term response to afatinib.Cancer science, , Volume: 114, Issue:3, 2023
Epidermal growth factor receptor tyrosine kinase inhibitors for non-small cell lung cancer harboring uncommon EGFR mutations: Real-world data from Taiwan.Thoracic cancer, , Volume: 14, Issue:1, 2023
The second-generation tyrosine kinase inhibitor afatinib inhibits IL-1β secretion via blocking assembly of NLRP3 inflammasome independent of epidermal growth factor receptor signaling in macrophage.Molecular immunology, , Volume: 153, 2023
Non-small cell lung cancer with EGFR (L858R and E709X) and CNNB1 mutations responded to afatinib.Thoracic cancer, , Volume: 14, Issue:4, 2023
The Role of Brain Radiotherapy before First-Line Afatinib Therapy, Compared to Gefitinib or Erlotinib, in Patients with EGFR-Mutant Non-Small Cell Lung Cancer.Cancer research and treatment, , Volume: 55, Issue:2, 2023
Afatinib plus osimertinib in the treatment of osimertinib-resistant non-small cell lung carcinoma: a phase I clinical trial.BMC cancer, , Jan-03, Volume: 23, Issue:1, 2023
Afatinib in Untreated Stage IIIB/IV Lung Adenocarcinoma with Major Uncommon Epidermal Growth Factor Receptor (EGFR) Mutations (G719X/L861Q/S768I): A Multicenter Observational Study in Taiwan.Targeted oncology, , Volume: 18, Issue:2, 2023
Bruceine D and afatinib combination inhibits ovarian cancer cells proliferation and migration through DNA damage repair and EGFR pathway.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 71, Issue:5, 2023
NEP010, a novel compound with minor structural modification from afatinib, exhibited significantly improved antitumor activity.European journal of pharmacology, , May-05, Volume: 946, 2023
Monitoring of T790M in plasma ctDNA of advanced EGFR-mutant NSCLC patients on first- or second-generation tyrosine kinase inhibitors.BMC cancer, , Mar-13, Volume: 23, Issue:1, 2023
Determining plasma and cerebrospinal fluid concentrations of EGFR-TKI in lung cancer patients.Analytical biochemistry, , 05-15, Volume: 669, 2023
The Use of Cytotoxic Drugs as First Line Chemotherapy for EGFR (+) Nonsquamous NSCLC: A Network Meta-Analysis.Disease markers, , Volume: 2023, 2023
Clinical Outcomes of Afatinib Versus Osimertinib in Patients With Non-Small Cell Lung Cancer With Uncommon EGFR Mutations: A Pooled Analysis.The oncologist, , 06-02, Volume: 28, Issue:6, 2023
A real-world study of Afatinib plus ramucirumab in treatment-naïve, EGFR-mutated, non-small cell lung cancer.BMC cancer, , May-08, Volume: 23, Issue:1, 2023
Front-line therapy for brain metastases and non-brain metastases in advanced epidermal growth factor receptor-mutated non-small cell lung cancer: a network meta-analysis.Chinese medical journal, , Nov-05, Volume: 136, Issue:21, 2023
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 181, 2023
Final Report on Real-World Effectiveness of Sequential Afatinib and Osimertinib in EGFR-Positive Advanced Non-Small Cell Lung Cancer: Updated Analysis of the RESET Study.Cancer research and treatment, , Volume: 55, Issue:4, 2023
Flashback Foreword: Afatinib for the Treatment of Epidermal Growth Factor Receptor Mutation-Positive Non-Small-Cell Lung Cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , 06-01, Volume: 41, Issue:16, 2023
Natural Cyclophilin A Inhibitors Suppress the Growth of Cancer Stem Cells in Non-Small Cell Lung Cancer by Disrupting Crosstalk between CypA/CD147 and EGFR.International journal of molecular sciences, , May-29, Volume: 24, Issue:11, 2023
Alternating Therapy With Osimertinib and Afatinib Blockades EGFR Secondary Mutation in EGFR-Mutant Lung Cancer: A Single-Arm Phase II Trial.Clinical lung cancer, , Volume: 24, Issue:6, 2023
Afatinib for the Treatment of NSCLC with Uncommon EGFR Mutations: A Narrative Review.Current oncology (Toronto, Ont.), , 05-28, Volume: 30, Issue:6, 2023
Comprehensive assessment of pretreatment sarcopenia impacts on patients with EGFR-mutated NSCLC treated with afatinib.Thoracic cancer, , Volume: 14, Issue:25, 2023
Neoadjuvant Afatinib for stage III EGFR-mutant non-small cell lung cancer: a phase II study.Nature communications, , 08-03, Volume: 14, Issue:1, 2023
Effects of targeted lung cancer drugs on cardiomyocytes studied by atomic force microscopy.Analytical methods : advancing methods and applications, , 08-24, Volume: 15, Issue:33, 2023
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.Neoplasia (New York, N.Y.), , Volume: 43, 2023
Durable response to afatinib in advanced lung adenocarcinoma harboring a novel NPTN-NRG1 fusion: a case report.World journal of surgical oncology, , Aug-16, Volume: 21, Issue:1, 2023
A randomized phase II study of afatinib alone or combined with bevacizumab for treating chemo-naïve patients with non-small cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 184, 2023
Survival outcomes of east Asian patients with advanced non-small cell lung cancer treated with first-line EGFR tyrosine kinase inhibitors: A network meta-analysis of real-world evidence.Thoracic cancer, , Volume: 14, Issue:32, 2023
Do patient characteristics affect EGFR tyrosine kinase inhibitor treatment outcomes? A network meta-analysis of real-world survival outcomes of East Asian patients with advanced non-small cell lung cancer treated with first-line EGFR-TKIs.Thoracic cancer, , Volume: 14, Issue:32, 2023
Treatment outcomes of non-small cell lung cancers treated with EGFR tyrosine kinase inhibitors: a real-world cohort study.Acta oncologica (Stockholm, Sweden), , Volume: 62, Issue:12, 2023
Brain metastasis, EGFR mutation subtype and generation of EGFR-TKI jointly influence the treatment outcome of patient with EGFR-mutant NSCLC.Scientific reports, , Nov-21, Volume: 13, Issue:1, 2023
Afatinib in the treatment of brain metastases of lung cancer with one rare EGFR mutation: a two-case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
The Clinical Outcomes of Different First-Line EGFR-TKIs Plus Bevacizumab in Advanced EGFR-Mutant Lung Adenocarcinoma.Cancer research and treatment, , Volume: 54, Issue:2, 2022
Long-term survival in a patient with advanced lung adenocarcinoma harboring synchronous EGFR exon 18 G719A and BRAF V600E mutations and treated with afatinib: a case report.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Hypotension from afatinib in epidermal growth factor receptor-mutated non-small cell lung cancer: a case report and literature review.Anti-cancer drugs, , 01-01, Volume: 33, Issue:1, 2022
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.Investigational new drugs, , Volume: 40, Issue:2, 2022
Cost-effectiveness analysis of the first-line EGFR-TKIs in patients with advanced EGFR-mutated non-small-cell lung cancer.Expert review of pharmacoeconomics & outcomes research, , Volume: 22, Issue:4, 2022
Combination treatment with bevacizumab plus erlotinib for meningeal carcinomatosis of afatinib-resistant EGFR mutated lung cancer without T790M mutation: a case report.Annals of palliative medicine, , Volume: 11, Issue:8, 2022
Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.European journal of cancer (Oxford, England : 1990), , Volume: 160, 2022
Complete Remission to Afatinib in a Patient Harboring a Novel Epidermal Growth Factor Mutation in De Novo Small-Cell Lung Cancer: A Case Report: Clinical Lung Cancer.Clinical lung cancer, , Volume: 23, Issue:4, 2022
Successful erlotinib rechallenge in an EGFR-mutant metastatic non-small cell lung cancer patient with afatinib-induced drug rash with eosinophilia and systemic symptoms: A case report.Thoracic cancer, , Volume: 13, Issue:3, 2022
The EPICAL trial, a phase Ib study combining first line afatinib with anti-EGF vaccination in EGFR-mutant metastatic NSCLC.Lung cancer (Amsterdam, Netherlands), , Volume: 164, 2022
Simultaneous quantitative detection of afatinib, erlotinib, gefitinib, icotinib, osimertinib and their metabolites in plasma samples of patients with non-small cell lung cancer using liquid chromatography-tandem mass spectrometry.Clinica chimica acta; international journal of clinical chemistry, , Feb-15, Volume: 527, 2022
Potential applications of clickable probes in EGFR activity visualization and prediction of EGFR-TKI therapy response for NSCLC patients.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
A Phase IIIb Open-Label, Single-Arm Study of Afatinib in EGFR TKI-Naïve Patients with EGFRm+ NSCLC: Final Analysis, with a Focus on Patients Enrolled at Sites in China.Targeted oncology, , Volume: 17, Issue:1, 2022
Determination of Afatinib in Human Plasma by 2-Dimensional Liquid Chromatography.Pharmacology, , Volume: 107, Issue:5-6, 2022
Classification and regression tree for estimating predictive markers to detect T790M mutations after acquired resistance to first line EGFR-TKI: HOPE-002.Investigational new drugs, , Volume: 40, Issue:2, 2022
First-line Afatinib in Patients With Non-small-cell Lung Cancer With Uncommon EGFR Mutations in South Korea.Anticancer research, , Volume: 42, Issue:3, 2022
Afatinib, an effective treatment for patient with lung squamous cell carcinoma harboring uncommon EGFR G719A and R776C co-mutations.Journal of cancer research and clinical oncology, , Volume: 148, Issue:5, 2022
Phase II study of afatinib plus pembrolizumab in patients with squamous cell carcinoma of the lung following progression during or after first-line chemotherapy (LUX-Lung-IO).Lung cancer (Amsterdam, Netherlands), , Volume: 166, 2022
Metabolic complete tumor response in a patient with The Journal of international medical research, , Volume: 50, Issue:3, 2022
Preclinical assessment of combination therapy of EGFR tyrosine kinase inhibitors in a highly heterogeneous tumor model.Oncogene, , Volume: 41, Issue:17, 2022
Pyrotinib for HER2-amplified non-small cell lung cancer patient after progression to Afatinib: a case report.Anti-cancer drugs, , 06-01, Volume: 33, Issue:5, 2022
Real-world Afatinib Outcomes in Advanced Non-small Cell Lung Cancer Harboring Anticancer research, , Volume: 42, Issue:4, 2022
Durable clinical benefit from afatinib in a lung adenocarcinoma patient with acquired EGFR L718V mutation-mediated resistance towards osimertinib: a case report and literature review.Annals of palliative medicine, , Volume: 11, Issue:3, 2022
Utilization and costs of epidermal growth factor receptor mutation testing and targeted therapy in Medicare patients with metastatic lung adenocarcinoma.BMC health services research, , Apr-09, Volume: 22, Issue:1, 2022
Plain language summary of publication: new information for the potential role of afatinib in treating people with Future oncology (London, England), , Volume: 18, Issue:18, 2022
Development and validation of a new liquid chromatography-tandem mass spectrometry assay for the simultaneous quantification of afatinib, dacomitinib, osimertinib, and the active metabolites of osimertinib in human serum.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences, , May-30, Volume: 1199, 2022
The Difference in Clinical Outcomes Between Osimertinib and Afatinib for First-Line Treatment in Patients with Advanced and Recurrent EGFR-Mutant Non-Small Cell Lung Cancer in Taiwan.Targeted oncology, , Volume: 17, Issue:3, 2022
Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L).Lung cancer (Amsterdam, Netherlands), , Volume: 168, 2022
Epidermal growth factor receptor tyrosine kinase inhibitors for de novo T790M mutation: A retrospective study of 44 patients.Thoracic cancer, , Volume: 13, Issue:13, 2022
A Phase 2 Trial of Afatinib in Patients with Solid Tumors that Harbor Genomic Aberrations in the HER family: The MOBILITY3 Basket Study.Targeted oncology, , Volume: 17, Issue:3, 2022
The effect of afatinib and radiotherapy on a patient with lung adenocarcinoma with a rare EGFR extracellular domain M277E mutation and high PD-L1 expression.Journal of cancer research and therapeutics, , Volume: 18, Issue:2, 2022
Dacomitinib overcomes afatinib-refractory carcinomatous meningitis in a lung cancer patient harbouring EGFR Ex.19 deletion and G724S mutation; a case report.Investigational new drugs, , Volume: 40, Issue:5, 2022
Application of afatinib combined with np regimen in the treatment of stage iv non-small cell lung cancer and its effect on patient survival.Pakistan journal of pharmaceutical sciences, , Volume: 35, Issue:2(Special), 2022
Survival benefits from afatinib compared with gefitinib and erlotinib among patients with common EGFR mutation in first-line setting.Thoracic cancer, , Volume: 13, Issue:14, 2022
Ad hoc afatinib in an eldery lung cancer patient with EGFR exon 19 deletion L747-A750>P.Advances in respiratory medicine, , Volume: 90, Issue:3, 2022
Structural dynamics and kinase inhibitory activity of three generations of tyrosine kinase inhibitors against wild-type, L858R/T790M, and L858R/T790M/C797S forms of EGFR.Computers in biology and medicine, , Volume: 147, 2022
Audit of Molecular Mechanisms of Primary and Secondary Resistance to Various Generations of Tyrosine Kinase Inhibitors in Known Epidermal Growth Factor Receptor-Mutant Non-small Cell Lung Cancer Patients in a Tertiary Centre.Clinical oncology (Royal College of Radiologists (Great Britain)), , Volume: 34, Issue:11, 2022
The EGFR-STYK1-FGF1 axis sustains functional drug tolerance to EGFR inhibitors in EGFR-mutant non-small cell lung cancer.Cell death & disease, , 07-15, Volume: 13, Issue:7, 2022
Treatment Considerations for Patients With Advanced Squamous Cell Carcinoma of the Lung.Clinical lung cancer, , Volume: 23, Issue:6, 2022
Plain language summary of NRG1 fusions in cancer: current knowledge and treatment with afatinib and other drugs.Future oncology (London, England), , Volume: 18, Issue:26, 2022
Efficacy of Combined Use of Everolimus and Second-Generation Pan-EGRF Inhibitors in International journal of molecular sciences, , Jul-14, Volume: 23, Issue:14, 2022
Plain language summary of outcomes in people treated for lung squamous cell cancer with afatinib after receiving pembrolizumab with chemotherapy.Future oncology (London, England), , Volume: 18, Issue:28, 2022
Non-small cell lung cancer harboring EGFR G724S mutation and exon 19 deletion responded to afatinib monotherapy after multiple lines of target therapies.Anti-cancer drugs, , 10-01, Volume: 33, Issue:9, 2022
Rare EGFR E709-T710delinsX: Molecular characteristics and superior response to afatinib treatment in NSCLC patients.Lung cancer (Amsterdam, Netherlands), , Volume: 172, 2022
Efficacy and potential resistance mechanisms of afatinib in advanced non-small cell lung cancer patients with EGFR G719X/L861Q/S768I.Cancer, , 11-01, Volume: 128, Issue:21, 2022
A case of multiple primary lung adenocarcinoma with a CD74-NRG1 fusion protein and HER2 mutation benefit from combined target therapy.Thoracic cancer, , Volume: 13, Issue:21, 2022
Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 155, 2022
Early-Onset Pulmonary Events with Combined Brigatinib and Afatinib Treatment of L858/cisT790M/cisC797S NSCLC: A Case Report.The American journal of case reports, , Sep-23, Volume: 23, 2022
Long-term response in a patient with adenocarcinoma harboring both common and uncommon EGFR mutations.Investigational new drugs, , Volume: 40, Issue:6, 2022
Afatinib Targeted Therapy Affects the Immune Function and Serum Levels of EGFR and Gastrin-Releasing Peptide Precursor (pro-GRP) in Patients with Non-Small-Cell Lung Cancer (NSCLC).Disease markers, , Volume: 2022, 2022
Liquid biopsy for detecting epidermal growth factor receptor mutation among patients with non-small cell lung cancer treated with afatinib: a multicenter prospective study.BMC cancer, , Oct-04, Volume: 22, Issue:1, 2022
Durable response to afatinib rechallenge in a long-term survivor of non-small cell lung cancer harboring EGFR L858R and L747V mutations.Thoracic cancer, , Volume: 13, Issue:22, 2022
Afatinib treatment in a lung adenocarcinoma patient harboring a rare EGFR L747P mutation.Journal of cancer research and therapeutics, , Volume: 18, Issue:5, 2022
Study on the prognosis, immune and drug resistance of m6A-related genes in lung cancer.BMC bioinformatics, , Oct-19, Volume: 23, Issue:1, 2022
Application of several machine learning algorithms for the prediction of afatinib treatment outcome in advanced-stage EGFR-mutated non-small-cell lung cancer.Thoracic cancer, , Volume: 13, Issue:23, 2022
[Multidisciplinary Treatment for Postoperative Recurrent Patients-Report of a Long-Term Survivor].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 49, Issue:10, 2022
Prevalence, Treatment Patterns, and Outcomes of Individuals with Current oncology (Toronto, Ont.), , 09-30, Volume: 29, Issue:10, 2022
Real-world data with afatinib in Spanish patients with treatment-naïve non-small-cell lung cancer harboring exon 19 deletions in epidermal growth factor receptor (Del19 EGFR): Clinical experience of the Galician Lung Cancer Group.Cancer treatment and research communications, , Volume: 33, 2022
Advanced Lung Cancer Patients' Use of EGFR Tyrosine Kinase Inhibitors and Overall Survival: Real-World Evidence from Quebec, Canada.Current oncology (Toronto, Ont.), , 10-26, Volume: 29, Issue:11, 2022
Drug Repurposing against KRAS Mutant G12C: A Machine Learning, Molecular Docking, and Molecular Dynamics Study.International journal of molecular sciences, , Dec-30, Volume: 24, Issue:1, 2022
Elucidation of the inhibitory potential of flavonoids against PKP1 protein in non-small cell lung cancer.Cellular and molecular biology (Noisy-le-Grand, France), , Nov-30, Volume: 68, Issue:11, 2022
Molecular and Clinical Features of EGFR-TKI-Associated Lung Injury.International journal of molecular sciences, , Jan-14, Volume: 22, Issue:2, 2021
Overall survival in stage IV EGFR mutation‑positive NSCLC: Comparing first‑, second‑ and third‑generation EGFR‑TKIs (Review).International journal of oncology, , Volume: 58, Issue:2, 2021
Drug-induced Hypersensitivity Syndrome by EGFR-TKI in a Patient with Lung Cancer.Internal medicine (Tokyo, Japan), , Volume: 60, Issue:3, 2021
Long-term response to afatinib in an elderly patient with uncommon epidermal growth factor receptor mutation-positive lung adenocarcinoma.Thoracic cancer, , Volume: 12, Issue:6, 2021
Successful treatment of Afatinib plus Apatinib using for a lung adenocarcinoma patient with HER-2 V659D mutation: a rare case report.Anti-cancer drugs, , 04-01, Volume: 32, Issue:4, 2021
EGFR mutation-guided use of afatinib, erlotinib and gefitinib for advanced non-small-cell lung cancer in Hong Kong - A cost-effectiveness analysis.PloS one, , Volume: 16, Issue:3, 2021
A phase II study of first-line afatinib for patients aged ≥75 years with EGFR mutation-positive advanced non-small cell lung cancer: North East Japan Study Group trial NEJ027.BMC cancer, , Mar-01, Volume: 21, Issue:1, 2021
Combination therapy with afatinib and bevacizumab in an EGFR-mutated non-small cell lung cancer patient with acquired ERBB2 amplification: A case report.Medicine, , Feb-26, Volume: 100, Issue:8, 2021
Afatinib therapy in case of EGFR G724S emergence as resistance mechanism to osimertinib.Anti-cancer drugs, , 08-01, Volume: 32, Issue:7, 2021
Afatinib as First-Line Treatment in Asian Patients with EGFR Mutation-Positive NSCLC: A Narrative Review of Real-World Evidence.Advances in therapy, , Volume: 38, Issue:5, 2021
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , 03-18, Volume: 3, 2021
Therapeutic Potential of Afatinib in NRG1 Fusion-Driven Solid Tumors: A Case Series.The oncologist, , Volume: 26, Issue:1, 2021
Differential effects of epidermal growth factor receptor inhibitors in a single patient with neuropathic pain.BMJ case reports, , Mar-26, Volume: 14, Issue:3, 2021
Afatinib Exerts Immunomodulatory Effects by Targeting the Pyrimidine Biosynthesis Enzyme CAD.Cancer research, , 06-15, Volume: 81, Issue:12, 2021
Cost-Effectiveness Analysis of Afatinib, Erlotinib, and Gefitinib as First-Line Treatments for EGFR Mutation-Positive Non-Small-Cell Lung Cancer in Ontario, Canada.PharmacoEconomics, , Volume: 39, Issue:5, 2021
Efficacy and dose of afatinib in patients with non-small cell lung cancer after failure of prior gefitinib or erlotinib treatment.Thoracic cancer, , Volume: 12, Issue:10, 2021
Real-life Effectiveness of Afatinib Anticancer research, , Volume: 41, Issue:4, 2021
An Liquid Chromatography-Tandem Mass Spectrometry Method for the Simultaneous Determination of Afatinib, Alectinib, Ceritinib, Crizotinib, Dacomitinib, Erlotinib, Gefitinib, and Osimertinib in Human Serum.Therapeutic drug monitoring, , 12-01, Volume: 43, Issue:6, 2021
Ring-opening of five-membered heterocycles conjugated 4-isopropylresorcinol scaffold-based benzamides as HSP90 inhibitors suppressing tumor growth in vitro and in vivo.European journal of medicinal chemistry, , Jul-05, Volume: 219, 2021
Lower starting dose of afatinib for the treatment of metastatic lung adenocarcinoma harboring exon 21 and exon 19 mutations.BMC cancer, , May-03, Volume: 21, Issue:1, 2021
Limited effect of afatinib in a non-small cell lung cancer patient harboring an epidermal growth factor receptor K860I missense mutation: A case report.Thoracic cancer, , Volume: 12, Issue:11, 2021
Response to: Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 12, Issue:11, 2021
A multicenter cohort study of osimertinib compared with afatinib as first-line treatment for EGFR-mutated non-small-cell lung cancer from practical dataset: CJLSG1903.ESMO open, , Volume: 6, Issue:3, 2021
Relationship between Epidermal Growth Factor Receptor Mutations and Adverse Events in Non-Small Cell Lung Cancer Patients treated with Afatinib.The journal of medical investigation : JMI, , Volume: 68, Issue:1.2, 2021
Successful treatment of triple EGFR mutation T785A/L861Q/H297_E298 with afatinib.Thoracic cancer, , Volume: 12, Issue:13, 2021
Osimertinib versus afatinib in patients with T790M-positive, non-small-cell lung cancer and multiple central nervous system metastases after failure of initial EGFR-TKI treatment.BMC pulmonary medicine, , May-19, Volume: 21, Issue:1, 2021
Effectiveness and Tolerability of First-Line Afatinib for Advanced EGFR-Mutant Non-Small Cell Lung Cancer in Vietnam.Asian Pacific journal of cancer prevention : APJCP, , May-01, Volume: 22, Issue:5, 2021
Drastic antitumor response following administration of afatinib immediately after atezolizumab in a patient with epidermal growth factor receptor tyrosine kinase inhibitor-resistant lung cancer.Thoracic cancer, , Volume: 12, Issue:13, 2021
Survival of chemo-naïve patients with EGFR mutation-positive advanced non-small cell lung cancer after treatment with afatinib and bevacizumab: updates from the Okayama Lung Cancer Study Group Trial 1404.Japanese journal of clinical oncology, , Aug-01, Volume: 51, Issue:8, 2021
Randomized Phase II Study of 3 Months or 2 Years of Adjuvant Afatinib in Patients With Surgically Resected Stage I-III JCO precision oncology, , Volume: 5, 2021
Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds.BMC pulmonary medicine, , Jul-01, Volume: 21, Issue:1, 2021
An open-label expanded access program of afatinib in EGFR tyrosine kinase inhibitor-naïve patients with locally advanced or metastatic non-small cell lung cancer harboring EGFR mutations.BMC cancer, , Jul-12, Volume: 21, Issue:1, 2021
Sequential treatment of afatinib and osimertinib or other regimens in patients with advanced non-small-cell lung cancer harboring EGFR mutations: Results from a real-world study in South Korea.Cancer medicine, , Volume: 10, Issue:17, 2021
Feasibility and effectiveness of afatinib for poor performance status patients with EGFR-mutation-positive non-small-cell lung cancer: a retrospective cohort study.BMC cancer, , Jul-27, Volume: 21, Issue:1, 2021
Severe EGFR inhibitor-induced acneiform eruption responding to dapsone.Dermatology online journal, , Jul-15, Volume: 27, Issue:7, 2021
New strategy for suppressing the growth of lung cancer cells harboring mutations in the ATP-binding region of EGFR by targeting the molecular motor MYO1D.Clinical and translational medicine, , Volume: 11, Issue:8, 2021
Outcomes of salvage lung resections in advanced EGFR-mutant lung adenocarcinomas under EGFR TKIs.Thoracic cancer, , Volume: 12, Issue:20, 2021
Structure-based classification predicts drug response in EGFR-mutant NSCLC.Nature, , Volume: 597, Issue:7878, 2021
A prospective, phase II trial of monotherapy with low-dose afatinib for patients with EGFR, mutation-positive, non-small cell lung cancer: Thoracic oncology research group 1632.Lung cancer (Amsterdam, Netherlands), , Volume: 161, 2021
Afatinib treatment response in advanced lung adenocarcinomas harboring uncommon mutations.Thoracic cancer, , Volume: 12, Issue:21, 2021
Comparison Between Second- and Third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors as First-line Treatment in Patients With Non-small-cell Lung Cancer: A Retrospective Analysis.Anticancer research, , Volume: 41, Issue:10, 2021
Sequential afatinib and osimertinib in patients with EGFR mutation-positive NSCLC and acquired T790M: A global non-interventional study (UpSwinG).Lung cancer (Amsterdam, Netherlands), , Volume: 162, 2021
Genetic and treatment profiles of patients with concurrent Epidermal Growth Factor Receptor (EGFR) and Anaplastic Lymphoma Kinase (ALK) mutations.BMC cancer, , Oct-15, Volume: 21, Issue:1, 2021
Comparing survival and treatment response of patients with acquired T790M mutation second-line osimertinib versus sequential treatment of chemotherapy followed by osimertinib: A real-world study.Thoracic cancer, , Volume: 12, Issue:23, 2021
Afatinib and osimertinib in lung adenocarcinoma harbored EGFR T751_I759delinsS mutation: A case report.Thoracic cancer, , Volume: 12, Issue:24, 2021
An elderly advanced non-small cell lung cancer patient harboring rare epidermal growth factor receptor mutations L861R benefited from afatinib: A case report.Medicine, , Nov-12, Volume: 100, Issue:45, 2021
Real-world effectiveness of second-line Afatinib versus chemotherapy for the treatment of advanced lung squamous cell carcinoma in immunotherapy-naïve patients.BMC cancer, , Nov-15, Volume: 21, Issue:1, 2021
Efficacy of Osimertinib in Afatinib-resistant Lung Cancer Harboring Uncommon EGFR Mutations: Case Report and Literature Review.Clinical lung cancer, , Volume: 22, Issue:3, 2021
Afatinib combined with anlotinib in the treatment of lung adenocarcinoma patient with novel HER2 mutation: a case report and review of the literature.World journal of surgical oncology, , Nov-18, Volume: 19, Issue:1, 2021
Association between oligo-residual disease and patterns of failure during EGFR-TKI treatment in EGFR-mutated non-small cell lung cancer: a retrospective study.BMC cancer, , Nov-19, Volume: 21, Issue:1, 2021
REPORT- Clinical outcomes of using second - versus first-Generation EGFR-tkis for the First-Line treatment of advanced NSCLC patients with EGFR mutations: A meta-analysis.Pakistan journal of pharmaceutical sciences, , Volume: 34, Issue:4, 2021
Afatinib for the treatment of advanced non-small-cell lung cancer harboring an epidermal growth factor receptor exon 18 E709_T710delinsD mutation: a case report.Journal of medical case reports, , Nov-22, Volume: 15, Issue:1, 2021
EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios.Cells, , 12-17, Volume: 10, Issue:12, 2021
Afatinib-loaded inhalable PLGA nanoparticles for localized therapy of non-small cell lung cancer (NSCLC)-development and in-vitro efficacy.Drug delivery and translational research, , Volume: 11, Issue:3, 2021
Successful treatment of an osimertinib-resistant lung adenocarcinoma with an exon 18 EGFR mutation (G719S) with afatinib plus bevacizumab.Investigational new drugs, , Volume: 39, Issue:1, 2021
Incremental cost-effectiveness analysis of tyrosine kinase inhibitors in advanced non-small cell lung cancer with mutations of the epidermal growth factor receptor in Colombia.Expert review of pharmacoeconomics & outcomes research, , Volume: 21, Issue:4, 2021
Successful Treatment with Afatinib after Osimertinib-induced Interstitial Lung Disease in a Patient with EGFR-mutant Non-small-cell Lung Cancer.Internal medicine (Tokyo, Japan), , Feb-15, Volume: 60, Issue:4, 2021
Major Clinical Response to Afatinib Monotherapy in Lung Adenocarcinoma Harboring EGFR Exon 20 Insertion Mutation.Clinical lung cancer, , Volume: 22, Issue:1, 2021
EGFR tyrosine kinase inhibitors in non-small cell lung cancer: treatment paradigm, current evidence, and challenges.Tumori, , Volume: 107, Issue:5, 2021
Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells.International journal of radiation biology, , Volume: 97, Issue:2, 2021
Celastrol acts synergistically with afatinib to suppress non-small cell lung cancer cell proliferation by inducing paraptosis.Journal of cellular physiology, , Volume: 236, Issue:6, 2021
Phase II open-label multicenter study to assess the antitumor activity of afatinib in lung cancer patients with activating epidermal growth factor receptor mutation from circulating tumor DNA: Liquid-Lung-A.Thoracic cancer, , Volume: 12, Issue:4, 2021
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.The oncologist, , Volume: 26, Issue:4, 2021
HER2 amplification as a potential mechanism of acquired resistance to afatinib in an advanced non-small-cell lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 151, 2021
Synergy between vinorelbine and afatinib in the inhibition of non-small cell lung cancer progression by EGFR and p53 signaling pathways.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 134, 2021
Afatinib in EGFR TKI-naïve patients with locally advanced or metastatic EGFR mutation-positive non-small cell lung cancer: Interim analysis of a Phase 3b study.Lung cancer (Amsterdam, Netherlands), , Volume: 152, 2021
Real-life comparison of the afatinib and first-generation tyrosine kinase inhibitors in nonsmall cell lung cancer harboring EGFR exon 19 deletion: a Turk Oncology Group (TOG) study.Journal of cancer research and clinical oncology, , Volume: 147, Issue:7, 2021
Clinical utility of liquid biopsy for EGFR driver, T790M mutation and EGFR amplification in plasma in patients with acquired resistance to afatinib.BMC cancer, , Jan-12, Volume: 21, Issue:1, 2021
Advanced lung adenocarcinoma with coexistent HER2 mutation and amplification and response to afatinib: a case report.Annals of palliative medicine, , Volume: 9, Issue:2, 2020
Sequential afatinib and osimertinib in patients with Future oncology (London, England), , Volume: 16, Issue:34, 2020
Survival analysis of afatinib versus erlotinib for individuals with advanced del19 lung adenocarcinoma with asymptomatic brain metastasis after pemetrexed-cisplatin chemotherapy: a retrospective study.The Journal of international medical research, , Volume: 48, Issue:8, 2020
Photo-induced specific intracellular release EGFR inhibitor from enzyme/ROS-dual sensitive nano-platforms for molecular targeted-photodynamic combinational therapy of non-small cell lung cancer.Journal of materials chemistry. B, , 09-21, Volume: 8, Issue:35, 2020
Role of YES1 amplification in EGFR mutation-positive non-small cell lung cancer: Primary resistance to afatinib in a patient.Thoracic cancer, , Volume: 11, Issue:9, 2020
Afatinib in patients with advanced non-small cell lung cancer harboring HER2 mutations, previously treated with chemotherapy: A phase II trial.Lung cancer (Amsterdam, Netherlands), , Volume: 147, 2020
Discovery of 4,6-pyrimidinediamine derivatives as novel dual EGFR/FGFR inhibitors aimed EGFR/FGFR1-positive NSCLC.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.European journal of medicinal chemistry, , Mar-15, Volume: 190, 2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFREuropean journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Retroperitoneal Metastasis, with Marked Fibrosis, of Lung Adenocarcinoma after Afatinib Treatment: An Autopsy Case Report.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 59, Issue:22, 2020
Knockdown of lncRNA BLACAT1 reverses the resistance of afatinib to non-small cell lung cancer via modulating STAT3 signalling.Journal of drug targeting, , Volume: 28, Issue:3, 2020
Simultaneous Single Cell Gene Expression and EGFR Mutation Analysis of Circulating Tumor Cells Reveals Distinct Phenotypes in NSCLC.Advanced biosystems, , Volume: 4, Issue:8, 2020
Healthcare resource utilization and costs associated with patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive NSCLC in the United States.Journal of medical economics, , Volume: 23, Issue:1, 2020
A noteworthy treatment of metastatic small-cell lung cancer with afatinib, followed by subsequent development of rare metastatic lesions in the ascending and sigmoid colon.Cancer reports (Hoboken, N.J.), , Volume: 3, Issue:3, 2020
Afatinib response in a lung adenocarcinoma with novel compound S720F+L861R mutation in EGFR.Lung cancer (Amsterdam, Netherlands), , Volume: 148, 2020
Lung carcinoma with diffuse cystic lesions misdiagnosed as pulmonary langerhans cell histocytosis: a case report.BMC pulmonary medicine, , Feb-04, Volume: 20, Issue:1, 2020
Durable complete response after afatinib and crizotinib in an advanced non-small cell lung cancer patient with EGFR L861Q mutation and acquired MET amplification: a case report.Annals of palliative medicine, , Volume: 9, Issue:5, 2020
Therapeutic Changes in Bilateral Choroidal Metastasis from Non-Small Cell Lung Cancer with Response to Afatinib: A Case Report.Ocular immunology and inflammation, , Aug-17, Volume: 28, Issue:6, 2020
Nationwide Real-world Cohort Study of First-line Tyrosine Kinase Inhibitor Treatment in Epidermal Growth Factor Receptor-mutated Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:6, 2020
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1, 2020
Phase II Study of Low-Dose Afatinib Maintenance Treatment Among Patients with EGFR-Mutated Non-Small Cell Lung Cancer: North Japan Lung Cancer Study Group Trial 1601 (NJLCG1601).The oncologist, , Volume: 25, Issue:10, 2020
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.Investigational new drugs, , Volume: 38, Issue:6, 2020
Successful afatinib rechallenge in a patient with non-small cell lung cancer harboring EGFR G719C and S768I mutations.Thoracic cancer, , Volume: 11, Issue:8, 2020
QT interval prolongation related to afatinib treatment in a patient with metastatic non-small-cell lung cancer.Current problems in cancer, , Volume: 44, Issue:6, 2020
Afatinib + bevacizumab combination therapy in EGFR-mutant NSCLC patients with osimertinib resistance: Protocol of an open-label, phase II, multicenter, single-arm trial.Thoracic cancer, , Volume: 11, Issue:8, 2020
Clinical Activity of Afatinib in Patients With Non-Small-Cell Lung Cancer Harboring Uncommon EGFR Mutations: A Spanish Retrospective Multicenter Study.Clinical lung cancer, , Volume: 21, Issue:5, 2020
Real-world assessment of afatinib for patients with EGFR-positive non-small cell lung cancer.Investigational new drugs, , Volume: 38, Issue:6, 2020
Multiple intraventricular metastases from lung adenocarcinoma with EGFR G719X mutation: a case report.BMC pulmonary medicine, , May-11, Volume: 20, Issue:1, 2020
Inflammatory changes in actinic keratoses associated with afatinib therapy.Cutis, , Volume: 105, Issue:3, 2020
EGFR L861Q and CDK4 amplification responding to afatinib combined with palbociclib treatment in a patient with advanced lung squamous cell carcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 145, 2020
Uncommon as an Individual, Not That Uncommon as a Whole.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:5, 2020
Differential significance of molecular subtypes which were classified into EGFR exon 19 deletion on the first line afatinib monotherapy.BMC cancer, , Feb-06, Volume: 20, Issue:1, 2020
Budget impact of sequential treatment with first-line afatinib versus first-line osimertinib in non-small-cell lung cancer patients with common EGFR mutations.The European journal of health economics : HEPAC : health economics in prevention and care, , Volume: 21, Issue:6, 2020
Comparative effectiveness and cost-effectiveness of three first-line EGFR-tyrosine kinase inhibitors: Analysis of real-world data in a tertiary hospital in Taiwan.PloS one, , Volume: 15, Issue:4, 2020
Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Clinical Features and Progression Pattern of Acquired T790M-positive Compared With T790M-negative EGFR Mutant Non-small-cell Lung Cancer: Catching Tumor and Clinical Heterogeneity Over Time Through Liquid Biopsy.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Dissecting the mThe pharmacogenomics journal, , Volume: 20, Issue:2, 2020
Durable Responses to Afatinib as First-line Therapy for HER2-mutated Metastatic Non-small-cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:1, 2020
Mutation Variants and Co-Mutations as Genomic Modifiers of Response to Afatinib in HER2-Mutant Lung Adenocarcinoma.The oncologist, , Volume: 25, Issue:3, 2020
Resolving Resistance to Osimertinib Therapy With Afatinib in an NSCLC Patient With EGFR L718Q Mutation.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Incidence of T790M in Patients With NSCLC Progressed to Gefitinib, Erlotinib, and Afatinib: A Study on Circulating Cell-free DNA.Clinical lung cancer, , Volume: 21, Issue:3, 2020
Successful treatment of an elderly patient with an uncommon L861Q epidermal growth factor receptor mutation with low-dose afatinib: A case report.Thoracic cancer, , Volume: 11, Issue:2, 2020
Emergence of EGFR G724S After Progression on Osimertinib Responded to Afatinib Monotherapy.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:3, 2020
ERK inhibition effectively overcomes acquired resistance of epidermal growth factor receptor-mutant non-small cell lung cancer cells to osimertinib.Cancer, , 03-15, Volume: 126, Issue:6, 2020
Comparing the effectiveness of different EGFR-TKIs in patients with EGFR mutant non-small-cell lung cancer: A retrospective cohort study in Taiwan.International journal of cancer, , 08-15, Volume: 147, Issue:4, 2020
Observational Study of Sequential Afatinib and Osimertinib in EGFR Mutation-Positive NSCLC: Patients Treated with a 40-mg Starting Dose of Afatinib.Advances in therapy, , Volume: 37, Issue:2, 2020
Afatinib for the Treatment of NSCLC Harboring Uncommon EGFR Mutations: A Database of 693 Cases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 15, Issue:5, 2020
Complete Response to Immunotherapy Plus Chemotherapy After an Unusual Clinical Response to Afatinib and Stereotactic Radiosurgery in a Patient With Metastatic EGFR-Mutant Non-Small-Cell Lung Cancer.Clinical lung cancer, , Volume: 21, Issue:4, 2020
Determination of Somatic Mutations and Tumor Mutation Burden in Plasma by CAPP-Seq during Afatinib Treatment in NSCLC Patients Resistance to Osimertinib.Scientific reports, , 01-20, Volume: 10, Issue:1, 2020
Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol cliniMedicine, , Volume: 99, Issue:4, 2020
Cost-effectiveness analysis of first and second-generation EGFR tyrosine kinase inhibitors as first line of treatment for patients with NSCLC harboring EGFR mutations.BMC cancer, , Sep-01, Volume: 20, Issue:1, 2020
Molecular profiling of afatinib-resistant non-small cell lung cancer cells in vivo derived from mice.Pharmacological research, , Volume: 161, 2020
Successful Treatment of a Patient with Lung Adenocarcinoma Harboring Compound EGFR Gene Mutations, G719X and S768I, with Afatinib.The Tokai journal of experimental and clinical medicine, , Sep-20, Volume: 45, Issue:3, 2020
NRG1 fusion-driven tumors: biology, detection, and the therapeutic role of afatinib and other ErbB-targeting agents.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 31, Issue:12, 2020
The efficacy of first-line tyrosine kinase inhibitors combined with co-medications in Asian patients with EGFR mutation non-small cell lung cancer.Scientific reports, , 09-11, Volume: 10, Issue:1, 2020
Afatinib for the first-line treatment of Future oncology (London, England), , Volume: 16, Issue:31, 2020
PLCγ1‑dependent invasion and migration of cells expressing NSCLC‑associated EGFR mutants.International journal of oncology, , Volume: 57, Issue:4, 2020
Osimertinib induced cardiomyopathy: A case report.Medicine, , Sep-25, Volume: 99, Issue:39, 2020
Site-Specific and Targeted Therapy Based on Molecular Profiling by Next-Generation Sequencing for Cancer of Unknown Primary Site: A Nonrandomized Phase 2 Clinical Trial.JAMA oncology, , Dec-01, Volume: 6, Issue:12, 2020
Long-term response to second-line afatinib treatment for advanced squamous cell carcinoma non-small cell lung cancer: a rare case report.The Journal of international medical research, , Volume: 48, Issue:10, 2020
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.Medicine, , Oct-23, Volume: 99, Issue:43, 2020
Quantitative Structure-Mutation-Activity Relationship Tests (QSMART) model for protein kinase inhibitor response prediction.BMC bioinformatics, , Nov-12, Volume: 21, Issue:1, 2020
New lung-cancer drugs extend survival times.Nature, , Volume: 587, Issue:7834, 2020
A randomized, multi-center, open-label study to compare the safety and efficacy between afatinib monotherapy and combination therapy of afatinib and HAD-B1 for the locally advanced or metastatic NSCLC patients with EGFR mutations.Medicine, , 12-04, Volume: 99, Issue:49, 2020
[Two cases of EGFR-mutated lung adenocarcinoma treated with bronchial recanalization and first-line therapy with afatinib.]Recenti progressi in medicina, , Volume: 111, Issue:12, 2020
Successful Treatment of a Patient With NSCLC Harboring an EGFR Mutation and a Concomitant Met Exon 14 Skipping Mutation Combining Afatinib and Crizotinib.Clinical lung cancer, , Volume: 20, Issue:1, 2019
Cost-utility of afatinib and gefitinib as first-line treatment for EGFR-mutated advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:2, 2019
Acquired Resistance of MET-Amplified Non-small Cell Lung Cancer Cells to the MET Inhibitor Capmatinib.Cancer research and treatment, , Volume: 51, Issue:3, 2019
Multi-disciplinary proactive follow-up algorithm for patients with advanced NSCLC receiving afatinib.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, , Volume: 27, Issue:3, 2019
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.Journal of medicinal chemistry, , 11-27, Volume: 62, Issue:22, 2019
A phase Ib study of the combination of afatinib and ruxolitinib in EGFR mutant NSCLC with progression on EGFR-TKIs.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 134, 2019
Afatinib helped overcome subsequent resistance to osimertinib in a patient with NSCLC having leptomeningeal metastasis baring acquired EGFR L718Q mutation: a case report.BMC cancer, , Jul-17, Volume: 19, Issue:1, 2019
Small Cell Lung Cancer Derived from Adenocarcinoma with Mutant Epidermal Growth Factor Receptor Provides a Signature of Transcriptional Alteration in Tumor Cells.Internal medicine (Tokyo, Japan), , Nov-15, Volume: 58, Issue:22, 2019
Long-term efficacy of afatinib in a patient with squamous cell carcinoma of the lung and multiple ERBB family aberrations: afatinib in ERBB+ lung squamous cell carcinoma.Anti-cancer drugs, , Volume: 30, Issue:8, 2019
Which Is Better EGFR-TKI Followed by Osimertinib: Afatinib or Gefitinib/Erlotinib?Anticancer research, , Volume: 39, Issue:7, 2019
The dual PI3K/mTOR inhibitor BEZ235 restricts the growth of lung cancer tumors regardless of EGFR status, as a potent accompanist in combined therapeutic regimens.Journal of experimental & clinical cancer research : CR, , Jul-01, Volume: 38, Issue:1, 2019
Monomer Preference of EGFR Tyrosine Kinase Inhibitors Influences the Synergistic Efficacy of Combination Therapy with Cetuximab.Molecular cancer therapeutics, , Volume: 18, Issue:9, 2019
Cardiac Toxicity From Afatinib in EGFR-Mutated NSCLC: A Rare But Possible Side Effect.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:7, 2019
Afatinib is effective in the treatment of lung adenocarcinoma with uncommon EGFR p.L747P and p.L747S mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
First-line afatinib for advanced EGFRm+ NSCLC: Analysis of long-term responders in the LUX-Lung 3, 6, and 7 trials.Lung cancer (Amsterdam, Netherlands), , Volume: 133, 2019
Efficacy of afatinib treatment for lung adenocarcinoma harboring exon 18 delE709_T710insD mutation.Japanese journal of clinical oncology, , Aug-01, Volume: 49, Issue:8, 2019
Outcome Differences Between First- and Second-generation EGFR Inhibitors in Advanced EGFR Mutated NSCLC in a Large Population-based Cohort.Clinical lung cancer, , Volume: 20, Issue:5, 2019
Cx32 mediates norepinephrine-promoted EGFR-TKI resistance in a gap junction-independent manner in non-small-cell lung cancer.Journal of cellular physiology, , Volume: 234, Issue:12, 2019
The Evolutionary Difference Between Extracranial Lesions and Leptomeningeal Metastasis in a Patient With Afatinib-Resistant Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Sequencing of therapy following first-line afatinib in patients with EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 132, 2019
Efficacy and safety of afatinib in a Chinese population with advanced lung adenocarcinoma with sensitive EGFR mutations.Thoracic cancer, , Volume: 10, Issue:6, 2019
Real-world study of afatinib in first-line or re-challenge settings for patients with EGFR mutant non-small cell lung cancer.Medical oncology (Northwood, London, England), , May-14, Volume: 36, Issue:6, 2019
Clinical significance of monitoring EGFR mutation in plasma using multiplexed digital PCR in EGFR mutated patients treated with afatinib (West Japan Oncology Group 8114LTR study).Lung cancer (Amsterdam, Netherlands), , Volume: 131, 2019
Clinical analysis of EGFR-positive non-small cell lung cancer patients treated with first-line afatinib: A Nagano Lung Cancer Research Group.Thoracic cancer, , Volume: 10, Issue:5, 2019
Real-world treatment of over 1600 Japanese patients with EGFR mutation-positive non-small cell lung cancer with daily afatinib.International journal of clinical oncology, , Volume: 24, Issue:8, 2019
Intracranial Responses to Afatinib at Different Doses in Patients With EGFR-mutated Non-small-cell Lung Carcinoma and Brain Metastases.Clinical lung cancer, , Volume: 20, Issue:3, 2019
Identification of a Novel MET Exon 14 Skipping Variant Coexistent with EGFR Mutation in Lung Adenocarcinoma Sensitive to Combined Treatment with Afatinib and Crizotinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:4, 2019
Duration of treatment among patients prescribed afatinib or erlotinib as first-line therapy for EGFR mutation-positive non-small-cell lung cancer in the USA.Future oncology (London, England), , Volume: 15, Issue:13, 2019
Repeat biopsy procedures and T790M rates after afatinib, gefitinib, or erlotinib therapy in patients with lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 130, 2019
Phase 1 trial of dasatinib combined with afatinib for epidermal growth factor receptor- (EGFR-) mutated lung cancer with acquired tyrosine kinase inhibitor (TKI) resistance.British journal of cancer, , Volume: 120, Issue:8, 2019
Different incidence of interstitial lung disease according to different kinds of EGFR-tyrosine kinase inhibitors administered immediately before and/or after anti-PD-1 antibodies in lung cancer.Thoracic cancer, , Volume: 10, Issue:4, 2019
Strategies to overcome acquired resistance to EGFR TKI in the treatment of non-small cell lung cancer.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 21, Issue:10, 2019
Optimal Sequence of Local and EGFR-TKI Therapy for EGFR-Mutant Non-Small Cell Lung Cancer With Brain Metastases Stratified by Number of Brain Metastases.International journal of radiation oncology, biology, physics, , 07-01, Volume: 104, Issue:3, 2019
From Diagnostic-Therapeutic Pathways to Real-World Data: A Multicenter Prospective Study on Upfront Treatment for The oncologist, , Volume: 24, Issue:6, 2019
Afatinib in NSCLC With HER2 Mutations: Results of the Prospective, Open-Label Phase II NICHE Trial of European Thoracic Oncology Platform (ETOP).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:6, 2019
Next-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors for Leptomeningeal Carcinomatosis: Review of 2 Cases.The neurologist, , Volume: 24, Issue:2, 2019
Afatinib With Pembrolizumab for Treatment of Patients With Locally Advanced/Metastatic Squamous Cell Carcinoma of the Lung: The LUX-Lung IO/KEYNOTE 497 Study Protocol.Clinical lung cancer, , Volume: 20, Issue:3, 2019
First-line afatinib vs gefitinib for patients with EGFR mutation-positive NSCLC (LUX-Lung 7): impact of afatinib dose adjustment and analysis of mode of initial progression for patients who continued treatment beyond progression.Journal of cancer research and clinical oncology, , Volume: 145, Issue:6, 2019
Re-challenge of afatinib after 1st generation EGFR-TKI failure in patients with previously treated non-small cell lung cancer harboring EGFR mutation.Cancer chemotherapy and pharmacology, , Volume: 83, Issue:5, 2019
Afatinib-loaded immunoliposomes functionalized with cetuximab: A novel strategy targeting the epidermal growth factor receptor for treatment of non-small-cell lung cancer.International journal of pharmaceutics, , Apr-05, Volume: 560, 2019
Long-lasting response to afatinib that persisted after treatment discontinuation in a case of BMJ case reports, , Jan-31, Volume: 12, Issue:1, 2019
Clinical efficacy of concurrent bevacizumab for malignant ascites in nonsquamous cell carcinoma of the lung.Asia-Pacific journal of clinical oncology, , Volume: 15, Issue:5, 2019
Afatinib in patients with metastatic or recurrent HER2-mutant lung cancers: a retrospective international multicentre study.European journal of cancer (Oxford, England : 1990), , Volume: 109, 2019
Responsiveness to Full-Dose Afatinib in a Patient With Lung Adenocarcinoma Harboring EGFR S768I and V769L Mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:2, 2019
Cost-effectiveness of afatinib, gefitinib, erlotinib and pemetrexed-based chemotherapy as first-line treatments for advanced non-small cell lung cancer in China.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Efficacy of afatinib or osimertinib plus cetuximab combination therapy for non-small-cell lung cancer with EGFR exon 20 insertion mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Impact of afatinib dose modification on safety and effectiveness in patients with EGFR mutation-positive advanced NSCLC: Results from a global real-world study (RealGiDo).Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Successful treatment of a lung adenocarcinoma patient with a novel EGFR exon 20-ins mutation with afatinib: A case report.Medicine, , Volume: 98, Issue:1, 2019
Successful Treatment of Lung Adenocarcinoma with Epidermal Growth Factor Receptor Compound Mutations Involving Exon 19 Deletion and Exon 20 Insertion by Afatinib.Internal medicine (Tokyo, Japan), , Volume: 58, Issue:1, 2019
Palbociclib overcomes afatinib resistance in non-small cell lung cancer.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 109, 2019
Liquid-Biopsy-Based Identification of EGFR T790M Mutation-Mediated Resistance to Afatinib Treatment in Patients with Advanced EGFR Mutation-Positive NSCLC, and Subsequent Response to Osimertinib.Targeted oncology, , Volume: 14, Issue:1, 2019
Prospective exosome-focused translational research for afatinib study of non-small cell lung cancer patients expressing EGFR (EXTRA study).Thoracic cancer, , Volume: 10, Issue:2, 2019
Phase 2 Study of Afatinib Alone or Combined With Bevacizumab in Chemonaive Patients With Advanced Non-Small-Cell Lung Cancer Harboring EGFR Mutations: AfaBev-CS Study Protocol.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Clinical outcomes and secondary epidermal growth factor receptor (EGFR) T790M mutation among first-line gefitinib, erlotinib and afatinib-treated non-small cell lung cancer patients with activating EGFR mutations.International journal of cancer, , 06-01, Volume: 144, Issue:11, 2019
Dual blockade of EGFR tyrosine kinase using osimertinib and afatinib eradicates EGFR‑mutant Ba/F3 cells.Oncology reports, , Volume: 41, Issue:2, 2019
Potential for afatinib as an optimal treatment for advanced non-small cell lung carcinoma in patients with uncommon EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 127, 2019
Impact of Exon 19 Deletion Subtypes in EGFR-Mutant Metastatic Non-Small-Cell Lung Cancer Treated With First-Line Tyrosine Kinase Inhibitors.Clinical lung cancer, , Volume: 20, Issue:2, 2019
Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib.Cancer research and treatment, , Volume: 51, Issue:2, 2019
Bilateral Ulcerative Keratitis Associated With Afatinib Treatment for Non-Small-cell Lung Carcinoma.Cornea, , Volume: 38, Issue:3, 2019
Fingolimod augments Pemetrexed killing of non-small cell lung cancer and overcomes resistance to ERBB inhibition.Cancer biology & therapy, , Volume: 20, Issue:5, 2019
Non-small cell lung cancer harbouring non-resistant uncommon EGFR mutations: Mutation patterns, effectiveness of epidermal growth factor receptor-tyrosine kinase inhibitors and prognostic factors.European journal of cancer (Oxford, England : 1990), , Volume: 119, 2019
A phase II study of low starting dose of afatinib as first-line treatment in patients with EGFR mutation-positive non-small-cell lung cancer (KTORG1402).Lung cancer (Amsterdam, Netherlands), , Volume: 135, 2019
Real-world experience of first-line afatinib in patients with EGFR-mutant advanced NSCLC: a multicenter observational study.BMC cancer, , Sep-09, Volume: 19, Issue:1, 2019
[Comparison of Effectiveness of Gefitinib, Erlotinib, and Afatinib in Advanced Non-small Cell Lung Cancer Patients with EGFR Mutation Positive in Indonesian Population].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , 09-20, Volume: 22, Issue:9, 2019
Durable Response of Low-Dose Afatinib plus Cetuximab in an Adenocarcinoma Patient with a Novel EGFR Exon 20 Insertion Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:10, 2019
Development of two different formats of heterogeneous fluorescence immunoassay for bioanalysis of afatinib by employing fluorescence plate reader and KinExA 3200 immunosensor.Scientific reports, , 10-14, Volume: 9, Issue:1, 2019
Clinical factors associated with treatment outcomes in EGFR mutant non-small cell lung cancer patients with brain metastases: a case-control observational study.BMC cancer, , Oct-26, Volume: 19, Issue:1, 2019
PLGA Porous Microspheres Dry Powders for Codelivery of Afatinib-Loaded Solid Lipid Nanoparticles and Paclitaxel: Novel Therapy for EGFR Tyrosine Kinase Inhibitors Resistant Nonsmall Cell Lung Cancer.Advanced healthcare materials, , Volume: 8, Issue:23, 2019
Survival outcome of tyrosine kinase inhibitors beyond progression in association to radiotherapy in oligoprogressive EGFR-mutant non-small-cell lung cancer.Future oncology (London, England), , Volume: 15, Issue:33, 2019
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.Lung cancer (Amsterdam, Netherlands), , Volume: 138, 2019
Acquired EGFR L718V Mutation and Loss of T790M-Mediated Resistance to Osimertinib in a Patient With NSCLC Who Responded to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 14, Issue:12, 2019
Afatinib Overcomes Pemetrexed-Acquired Resistance in Non-Small Cell Lung Cancer Cells Harboring an EML4-ALK Rearrangement.Cells, , 11-28, Volume: 8, Issue:12, 2019
Population pharmacokinetics of afatinib and exposure-safety relationships in Japanese patients with EGFR mutation-positive non-small cell lung cancer.Scientific reports, , 12-03, Volume: 9, Issue:1, 2019
Overview of the LUX-Lung clinical trial program of afatinib for non-small cell lung cancer.Cancer treatment reviews, , Volume: 69, 2018
Phase I Study Evaluating the Combination of Afatinib with Carboplatin and Pemetrexed After First-line EGFR-TKIs.Anticancer research, , Volume: 38, Issue:8, 2018
Sequential treatment with afatinib and osimertinib in patients with EGFR mutation-positive non-small-cell lung cancer: an observational study.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Activity of Afatinib in Heavily Pretreated Patients With ERBB2 Mutation-Positive Advanced NSCLC: Findings From a Global Named Patient Use Program.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
An EGFR-mutated Lung Adenocarcinoma Undergoing Squamous Cell Carcinoma Transformation Exhibited a Durable Response to Afatinib.Internal medicine (Tokyo, Japan), , Dec-01, Volume: 57, Issue:23, 2018
Afatinib plus bevacizumab combination after acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutant non-small cell lung cancer: Multicenter, single-arm, phase 2 trial (ABC Study).Cancer, , 10-01, Volume: 124, Issue:19, 2018
Ankyrin Repeat Domain 1 Overexpression is Associated with Common Resistance to Afatinib and Osimertinib in EGFR-mutant Lung Cancer.Scientific reports, , 10-05, Volume: 8, Issue:1, 2018
Real Clinical Practice of Using Afatinib Therapy in NSCLC Patients with an Acquired Anticancer research, , Volume: 38, Issue:9, 2018
An observational study of the epidermal growth factor receptor-tyrosine kinase inhibitor resistance mechanism in epidermal growth factor receptor gene mutation-positive non-small cell lung cancer.Medicine, , Volume: 97, Issue:40, 2018
[Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Sep-20, Volume: 21, Issue:9, 2018
Exploration of resistance mechanisms for epidermal growth factor receptor-tyrosine kinase inhibitors based on plasma analysis by digital polymerase chain reaction and next-generation sequencing.Cancer science, , Volume: 109, Issue:12, 2018
A phase II trial of EGFR-TKI readministration with afatinib in advanced non-small-cell lung cancer harboring a sensitive non-T790M EGFR mutation: Okayama Lung Cancer Study Group trial 1403.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
Response to afatinib in treatment-naïve patients with advanced mutant epidermal growth factor receptor lung adenocarcinoma with brain metastases.Expert review of anticancer therapy, , Volume: 18, Issue:1, 2018
Afatinib Decreases P-Glycoprotein Expression to Promote Adriamycin Toxicity of A549T Cells.Journal of cellular biochemistry, , Volume: 119, Issue:1, 2018
An Evolving Algorithm to Select and Sequence Therapies in EGFR Mutation-positive NSCLC: A Strategic Approach.Clinical lung cancer, , Volume: 19, Issue:1, 2018
Symptom and Quality of Life Improvement in LUX-Lung 8, an Open-Label Phase III Study of Second-Line Afatinib Versus Erlotinib in Patients With Advanced Squamous Cell Carcinoma of the Lung After First-Line Platinum-Based Chemotherapy.Clinical lung cancer, , Volume: 19, Issue:1, 2018
[Hyponatremia in a 58-year-old female patient with EGFR-positive lung adenocarcinoma].Der Internist, , Volume: 59, Issue:4, 2018
Afatinib treatment of a squamous lung cancer after tumor progression of nivolumab.Thoracic cancer, , Volume: 9, Issue:1, 2018
Therapeutic Potential of Afatinib for Cancers with The oncologist, , Volume: 23, Issue:2, 2018
Does EGFR Mutation Type Influence Patient-Reported Outcomes in Patients with Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer? Analysis of Two Large, Phase III Studies Comparing Afatinib with Chemotherapy (LUX-Lung 3 and LUX-Lung 6).The patient, , Volume: 11, Issue:1, 2018
Efficacy of Afatinib in a Previously-Treated Patient with Non-Small Cell Lung Cancer Harboring HER2 Mutation: Case Report.Journal of Korean medical science, , Jan-01, Volume: 33, Issue:1, 2018
The Effectiveness of Afatinib in a Patient with Advanced Lung Adenocarcinoma Harboring Rare G719X and S768I Mutations.Internal medicine (Tokyo, Japan), , Apr-01, Volume: 57, Issue:7, 2018
Acquired Resistance to Afatinib Due to T790M-Positive Squamous Progression in EGFR-Mutant Adenosquamous Lung Carcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:1, 2018
Utilization of Molecular Testing and Survival Outcomes of Treatment with First- or Second-line Tyrosine Kinase Inhibitors in Advanced Non-small Cell Lung Cancer in a Dutch Population.Anticancer research, , Volume: 38, Issue:1, 2018
A phase I trial of afatinib and bevacizumab in chemo-naïve patients with advanced non-small-cell lung cancer harboring EGFR mutations: Okayama Lung Cancer Study Group Trial 1404.Lung cancer (Amsterdam, Netherlands), , Volume: 115, 2018
A Retrospective Comparison of the Clinical Efficacy of Gefitinib, Erlotinib, and Afatinib in Japanese Patients With Non-Small Cell Lung Cancer.Oncology research, , Aug-23, Volume: 26, Issue:7, 2018
EGFR-TKI-Associated Interstitial Pneumonitis in Nivolumab-Treated Patients With Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Stevens-Johnson syndrome/toxic epidermal necrolysis overlap in a NSCLC patient treated with afatinib.Journal der Deutschen Dermatologischen Gesellschaft = Journal of the German Society of Dermatology : JDDG, , Volume: 16, Issue:2, 2018
Global named patient use program of afatinib in advanced non-small-cell lung carcinoma patients who progressed following prior therapies.Future oncology (London, England), , Volume: 14, Issue:15, 2018
Improvement of erosive pustular dermatosis of the scalp following discontinuation of chemotherapy with afatinib.European journal of dermatology : EJD, , 04-01, Volume: 28, Issue:2, 2018
EGFR-mediated interleukin enhancer-binding factor 3 contributes to formation and survival of cancer stem-like tumorspheres as a therapeutic target against EGFR-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 116, 2018
A phase I study of afatinib for patients aged 75 or older with advanced non-small cell lung cancer harboring EGFR mutations.Medical oncology (Northwood, London, England), , Feb-08, Volume: 35, Issue:3, 2018
The clinical features of squamous cell lung carcinoma with sensitive EGFR mutations.International journal of clinical oncology, , Volume: 23, Issue:3, 2018
Best Response According to RECIST During First-line EGFR-TKI Treatment Predicts Survival in EGFR Mutation-positive Non-Small-cell Lung Cancer Patients.Clinical lung cancer, , Volume: 19, Issue:3, 2018
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Case sharing of a patient re-challenged with afatinib for EGFR-mutated advanced non-small cell lung cancer.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Afatinib for an EGFR exon 20 insertion mutation: A case report of progressive stage IV metastatic lung adenocarcinoma with 54 months' survival.Asia-Pacific journal of clinical oncology, , Volume: 14 Suppl 1, 2018
Therapeutic strategies for afatinib-resistant lung cancer harboring HER2 alterations.Cancer science, , Volume: 109, Issue:5, 2018
Successful treatment with an EGFR tyrosine kinase inhibitor Afatinib in a patient with combined small-cell lung Cancer with EGFR mutation.Investigational new drugs, , Volume: 36, Issue:4, 2018
Cardiovascular safety of novel non-small cell lung cancer oncotherapy in a patient treated with novel generations of tyrosine kinase inhibitors.Kardiologia polska, , Volume: 76, Issue:3, 2018
Efficacy generated by afatinib in a lung adenocarcinoma patient harboring HER2 S310Y mutation.Cancer biology & therapy, , 06-03, Volume: 19, Issue:6, 2018
[Metastatic Brain Tumor from Lung Adenocarcinoma Presenting a Unique Radiographic Pattern during Afatinib Treatment:A Case Report].No shinkei geka. Neurological surgery, , Volume: 46, Issue:3, 2018
Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 118, 2018
Mechanisms of acquired resistance to afatinib clarified with liquid biopsy.PloS one, , Volume: 13, Issue:12, 2018
Cost effectiveness analysis of afatinib versus pemetrexed-cisplatin for first-line treatment of locally advanced or metastatic EGFR mutation positive non-small-cell lung cancer from the Singapore healthcare payer's perspective.BMC cancer, , 03-27, Volume: 18, Issue:1, 2018
Afatinib in the Treatment of Advanced Non-Small Cell Lung Cancer with Rare EGFR (in exon 18-T179X) Mutation - a Case Report.Klinicka onkologie : casopis Ceske a Slovenske onkologicke spolecnosti, ,Fall, Volume: 31, Issue:5, 2018
Afatinib as First-line Treatment of Older Patients With EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Subgroup Analyses of the LUX-Lung 3, LUX-Lung 6, and LUX-Lung 7 Trials.Clinical lung cancer, , Volume: 19, Issue:4, 2018
Afatinib in heavily pretreated advanced NSCLC patients who progressed following prior gefitinib or erlotinib: Compassionate use program in Korea.Lung cancer (Amsterdam, Netherlands), , Volume: 119, 2018
Mechanisms and clinical activity of an EGFR and HER2 exon 20-selective kinase inhibitor in non-small cell lung cancer.Nature medicine, , Volume: 24, Issue:5, 2018
Identification of Mutation Accumulation as Resistance Mechanism Emerging in First-Line Osimertinib Treatment.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
Efficacy of thoracic radiotherapy in patients with stage IIIB-IV epidermal growth factor receptor-mutant lung adenocarcinomas who received and responded to tyrosine kinase inhibitor treatment.Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, , Volume: 129, Issue:1, 2018
A phase II study of afatinib treatment for elderly patients with previously untreated advanced non-small-cell lung cancer harboring EGFR mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
Afatinib in Osimertinib-Resistant EGFR ex19del/T790M/P794L Mutated NSCLC.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:9, 2018
Effects of secondary EGFR mutations on resistance against upfront osimertinib in cells with EGFR-activating mutations in vitro.Lung cancer (Amsterdam, Netherlands), , Volume: 126, 2018
EGFR exon 18 DelE709_T710insD as an Acquired Resistance Mechanism to Afatinib in an Advanced EGFR exon 18 E709H Lung Adenocarcinoma.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Influence of afatinib dose on outcomes of advanced EGFR-mutant NSCLC patients with brain metastases.BMC cancer, , Dec-03, Volume: 18, Issue:1, 2018
Miliary Adenocarcinoma of the Lung Responds to Gefitinib and Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:6, 2018
Budget Impact Analysis of Afatinib for First-Line Treatment of Patients with Metastatic Non-Small Cell Lung Cancer with Epidermal Growth Factor Receptor Exon 19 Deletions or Exon 21 Substitution Mutations in a U.S. Health Plan.Journal of managed care & specialty pharmacy, , Volume: 24, Issue:6, 2018
Cost-effectiveness of Osimertinib in the First-Line Treatment of Patients With EGFR-Mutated Advanced Non-Small Cell Lung Cancer.JAMA oncology, , 08-01, Volume: 4, Issue:8, 2018
Cost-effectiveness of afatinib and erlotinib as second-line treatments for advanced squamous cell carcinoma of the lung.Future oncology (London, England), , Volume: 14, Issue:27, 2018
Liquid chromatography-tandem mass spectrometric assay for therapeutic drug monitoring of the EGFR inhibitors afatinib, erlotinib and osimertinib, the ALK inhibitor crizotinib and the VEGFR inhibitor nintedanib in human plasma from non-small cell lung cancJournal of pharmaceutical and biomedical analysis, , Sep-05, Volume: 158, 2018
Osimertinib for Secondary T790M-Mutation-Positive Squamous Cell Carcinoma Transformation After Afatinib Failure.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:12, 2018
Afatinib with subsequent surgery in stage III NSCLC with EGFR mutation: Lessons learned from two clinical experiences.Tumori, , Volume: 104, Issue:6, 2018
Afatinib in advanced pretreated non-small-cell lung cancer- a Canadian experience.Current oncology (Toronto, Ont.), , Volume: 25, Issue:5, 2018
Economic analysis of osimertinib in previously untreated EGFR-mutant advanced non-small cell lung cancer in Canada.Lung cancer (Amsterdam, Netherlands), , Volume: 125, 2018
Association of ERBB Mutations With Clinical Outcomes of Afatinib- or Erlotinib-Treated Patients With Lung Squamous Cell Carcinoma: Secondary Analysis of the LUX-Lung 8 Randomized Clinical Trial.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Anti-tumor activity of Shikonin against afatinib resistant non-small cell lung cancer via negative regulation of PI3K/Akt signaling pathway.Bioscience reports, , 12-21, Volume: 38, Issue:6, 2018
In Search of an Oncogene Driver for Squamous Lung Cancer.JAMA oncology, , 09-01, Volume: 4, Issue:9, 2018
Relationship between Paronychia and Drug Concentrations of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors.Oncology, , Volume: 95, Issue:4, 2018
Irreversible tyrosine kinase inhibition of epidermal growth factor receptor with afatinib in Current oncology (Toronto, Ont.), , Volume: 25, Issue:Suppl 1, 2018
Afatinib and Erlotinib in the treatment of squamous-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 19, Issue:18, 2018
Afatinib restrains K-RAS-driven lung tumorigenesis.Science translational medicine, , 06-20, Volume: 10, Issue:446, 2018
Primary Resistance to Afatinib in a Patient with Lung Adenocarcinoma Harboring Uncommon EGFR Mutations: S768I and V769L.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 13, Issue:7, 2018
Sensitivity of epidermal growth factor receptor with single or double uncommon mutations to afatinib confirmed by a visual assay.Cancer science, , Volume: 109, Issue:11, 2018
Therapeutic Strategies in EGFR Mutant Non-Small Cell Lung Cancer.Current treatment options in oncology, , 09-29, Volume: 19, Issue:11, 2018
Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Quantitative Tyrosine Phosphoproteomics of Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor-treated Lung Adenocarcinoma Cells Reveals Potential Novel Biomarkers of Therapeutic Response.Molecular & cellular proteomics : MCP, , Volume: 16, Issue:5, 2017
Prognostic value of early response assessment using (18F)FDG-PET in patients with advanced non-small cell lung cancer treated with tyrosine-kinase inhibitors.Journal of investigative medicine : the official publication of the American Federation for Clinical Research, , Volume: 65, Issue:5, 2017
Triplet therapy with afatinib, cetuximab, and bevacizumab induces deep remission in lung cancer cells harboring EGFR T790M in vivo.Molecular oncology, , Volume: 11, Issue:6, 2017
Efficacy of continuous EGFR-inhibition and role of Hedgehog in EGFR acquired resistance in human lung cancer cells with activating mutation of EGFR.Oncotarget, , Apr-04, Volume: 8, Issue:14, 2017
Afatinib versus gefitinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: overall survival data from the phase IIb LUX-Lung 7 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , 02-01, Volume: 28, Issue:2, 2017
Recent Management of Patients with Advanced Epidermal Growth Factor Receptor Mutation Non-small Cell Lung Cancer: Role of Afatinib and Lesson Learned for Developing Countries.Acta medica Indonesiana, , Volume: 49, Issue:1, 2017
Therapeutic Efficacy Comparison of 5 Major EGFR-TKIs in Advanced EGFR-positive Non-Small-cell Lung Cancer: A Network Meta-analysis Based on Head-to-Head Trials.Clinical lung cancer, , Volume: 18, Issue:5, 2017
Second-line therapy of squamous non-small cell lung cancer: an evolving landscape.Expert review of respiratory medicine, , Volume: 11, Issue:6, 2017
Durable Response to Afatinib in Lung Adenocarcinoma Harboring NRG1 Gene Fusions.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:8, 2017
Activation of signal transducer and activator of transcription 3 (STAT3) signaling in EGFR mutant non-small-cell lung cancer (NSCLC).Oncotarget, , Jul-18, Volume: 8, Issue:29, 2017
Purpuric Drug Eruptions Caused by Epidermal Growth Factor Receptor Inhibitors for Non-Small Cell Lung Cancer: A Clinicopathologic Study of 32 Cases.JAMA dermatology, , 09-01, Volume: 153, Issue:9, 2017
Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.Clinical drug investigation, , Volume: 37, Issue:6, 2017
Evaluation of the VeriStratLung cancer (Amsterdam, Netherlands), , Volume: 109, 2017
Association Between EGFR T790M Status and Progression Patterns During Initial EGFR-TKI Treatment in Patients Harboring EGFR Mutation.Clinical lung cancer, , Volume: 18, Issue:6, 2017
Comparison of gefitinib, erlotinib and afatinib in non-small cell lung cancer: A meta-analysis.International journal of cancer, , 06-15, Volume: 140, Issue:12, 2017
A phase Ib trial of continuous once-daily oral afatinib plus sirolimus in patients with epidermal growth factor receptor mutation-positive non-small cell lung cancer and/or disease progression following prior erlotinib or gefitinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Distinct Afatinib Resistance Mechanisms Identified in Lung Adenocarcinoma Harboring an EGFR Mutation.Molecular cancer research : MCR, , Volume: 15, Issue:7, 2017
EGFR exon 18 delE709_T710insD mutated stage IV lung adenocarcinoma with response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 108, 2017
Chronic myelomonocytic leukemia blast crisis in a patient with advanced non-small cell lung cancer treated with EGFR tyrosine kinase inhibitors.Respiratory investigation, , Volume: 55, Issue:2, 2017
Matrine increases the inhibitory effects of afatinib on H1975 cells via the IL‑6/JAK1/STAT3 signaling pathway.Molecular medicine reports, , Volume: 16, Issue:3, 2017
Update on afatinib-based combination regimens for the treatment of EGFR mutation-positive non-small-cell lung cancer.Future oncology (London, England), , Volume: 13, Issue:21, 2017
[Precision first-line therapy for advanced non-small-cell lung cancer patients harboring EGFR mutation].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Feb-23, Volume: 39, Issue:2, 2017
The Effect of Afatinib Treatment in Non-small Cell Lung Cancer Cells.Anticancer research, , Volume: 37, Issue:7, 2017
Monitoring of somatic mutations in circulating cell-free DNA by digital PCR and next-generation sequencing during afatinib treatment in patients with lung adenocarcinoma positive for EGFR activating mutations.Annals of oncology : official journal of the European Society for Medical Oncology, , 01-01, Volume: 28, Issue:1, 2017
Comparing the effects of afatinib with gefitinib or Erlotinib in patients with advanced-stage lung adenocarcinoma harboring non-classical epidermal growth factor receptor mutations.Lung cancer (Amsterdam, Netherlands), , Volume: 110, 2017
ERBB2-Mutated Metastatic Non-Small Cell Lung Cancer: Response and Resistance to Targeted Therapies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Case series on the association between blood levels and side effects of afatinib maleate.Cancer chemotherapy and pharmacology, , Volume: 80, Issue:3, 2017
Cost-Effectiveness Analysis of Afatinib versus Gefitinib for First-Line Treatment of Advanced EGFR-Mutated Advanced Non-Small Cell Lung Cancers.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:10, 2017
An unexpected response to second line EGFR inhibitor in relapsing leptomeningeal carcinomatosis from lung adenocarcinoma raises questions on differential mechanisms of action of these agents.Bulletin du cancer, , Volume: 104, Issue:4, 2017
YM155 as an inhibitor of cancer stemness simultaneously inhibits autophosphorylation of epidermal growth factor receptor and G9a-mediated stemness in lung cancer cells.PloS one, , Volume: 12, Issue:8, 2017
Novel EGFR Exon 18 (G721R) Mutation in a Patient with Non-Small Cell Lung Carcinoma with Lack of Response to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:2, 2017
[A Case of Lung Adenocarcinoma Presenting with Leptomeningeal Carcinomatosis Successfully Treated with Afatinib after Erlotinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 44, Issue:7, 2017
Randomized Phase II Study of Afatinib Plus Simvastatin Versus Afatinib Alone in Previously Treated Patients with Advanced Nonadenocarcinomatous Non-small Cell Lung Cancer.Cancer research and treatment, , Volume: 49, Issue:4, 2017
Malignant Pleural Mesothelioma Harboring Both G719C and S768I Mutations of EGFR Successfully Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:9, 2017
Overall survival in EGFR mutated non-small-cell lung cancer patients treated with afatinib after EGFR TKI and resistant mechanisms upon disease progression.PloS one, , Volume: 12, Issue:8, 2017
Genomic Profiling of Circulating Tumor DNA in Relapsed EGFR-mutated Lung Adenocarcinoma Reveals an Acquired FGFR3-TACC3 Fusion.Clinical lung cancer, , Volume: 18, Issue:3, 2017
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.Anticancer research, , Volume: 37, Issue:9, 2017
Appendix 7: Metastatic non-small-cell lung cancer (1): MCBS eUpdate published online 28 June 2017 (www.esmo.org/Guidelines/Lung-and-Chest-Tumours).Annals of oncology : official journal of the European Society for Medical Oncology, , Jul-01, Volume: 28, Issue:suppl_4, 2017
EGFR L858M/L861Q cis Mutations Confer Selective Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:5, 2017
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21, 2017
An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.Respiratory investigation, , Volume: 55, Issue:1, 2017
Successful targeting of the NRG1 pathway indicates novel treatment strategy for metastatic cancer.Annals of oncology : official journal of the European Society for Medical Oncology, , Dec-01, Volume: 28, Issue:12, 2017
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
Dual MET and ERBB inhibition overcomes intratumor plasticity in osimertinib-resistant-advanced non-small-cell lung cancer (NSCLC).Annals of oncology : official journal of the European Society for Medical Oncology, , Oct-01, Volume: 28, Issue:10, 2017
Risk of Treatment-Related Toxicities from EGFR Tyrosine Kinase Inhibitors: A Meta-analysis of Clinical Trials of Gefitinib, Erlotinib, and Afatinib in Advanced EGFR-Mutated Non-Small Cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
EGFR mutation detection in circulating cell-free DNA of lung adenocarcinoma patients: analysis of LUX-Lung 3 and 6.British journal of cancer, , Jan-17, Volume: 116, Issue:2, 2017
Continued use of afatinib with the addition of cetuximab after progression on afatinib in patients with EGFR mutation-positive non-small-cell lung cancer and acquired resistance to gefitinib or erlotinib.Lung cancer (Amsterdam, Netherlands), , Volume: 113, 2017
Stress hormones promote EGFR inhibitor resistance in NSCLC: Implications for combinations with β-blockers.Science translational medicine, , Nov-08, Volume: 9, Issue:415, 2017
Afatinib successfully treated leptomeningeal metastasis during erlotinib treatment in a patient with EGFR-mutant (Exon18:G719S) lung adenocarcinoma as a second-line chemotherapy.Asia-Pacific journal of clinical oncology, , Volume: 13, Issue:5, 2017
Sequential occurrence of small cell and non-small lung cancer in a male patient: Is it a transformation?Cancer biology & therapy, , Dec-02, Volume: 18, Issue:12, 2017
Rapid Acquisition of T790M Mutation after Treatment with Afatinib in an NSCLC Patient Harboring EGFR Exon 20 S768I Mutation.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:1, 2017
Surgical resection of advanced non-small cell lung cancer after a response to EGFR-TKI: presentation of two cases and a literature review.Journal of cardiothoracic surgery, , Nov-23, Volume: 12, Issue:1, 2017
Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer.Molecular cancer therapeutics, , Volume: 16, Issue:2, 2017
A Case of Invasive Mucinous Pulmonary Adenocarcinoma with a CD74-NRG1 Fusion Protein Targeted with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:12, 2017
Epidermal Growth Factor Receptor Mutated Advanced Non-Small Cell Lung Cancer: A Changing Treatment Paradigm.Hematology/oncology clinics of North America, , Volume: 31, Issue:1, 2017
HER2 Transmembrane Domain (TMD) Mutations (V659/G660) That Stabilize Homo- and Heterodimerization Are Rare Oncogenic Drivers in Lung Adenocarcinoma That Respond to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:3, 2017
Successful afatinib treatment of advanced non-small-cell lung cancer patients undergoing hemodialysis.Cancer chemotherapy and pharmacology, , Volume: 79, Issue:1, 2017
Advanced non-small cell lung cancer (NSCLC) with activating EGFR mutations: first-line treatment with afatinib and other EGFR TKIs.Expert review of anticancer therapy, , Volume: 17, Issue:2, 2017
The clinical efficacy of Afatinib 30 mg daily as starting dose may not be inferior to Afatinib 40 mg daily in patients with stage IV lung Adenocarcinoma harboring exon 19 or exon 21 mutations.BMC pharmacology & toxicology, , 12-13, Volume: 18, Issue:1, 2017
Successful Use of Afatinib After Erlotinib-induced Pneumonitis in a Patient With Epidermal Growth Factor Receptor-mutant Lung Cancer.Clinical lung cancer, , Volume: 18, Issue:1, 2017
The European Society for Medical Oncology Magnitude of Clinical Benefit Scale (ESMO-MCBS) applied to pivotal phase III randomized-controlled trials of tyrosine kinase inhibitors in first-line for advanced non-small cell lung cancer with activating epidermExpert review of pharmacoeconomics & outcomes research, , Volume: 17, Issue:1, 2017
Overcoming EGFR Bypass Signal-Induced Acquired Resistance to ALK Tyrosine Kinase Inhibitors in ALK-Translocated Lung Cancer.Molecular cancer research : MCR, , Volume: 15, Issue:1, 2017
Variations in EGFR ctDNA Correlates to the Clinical Efficacy of Afatinib in Non Small Cell Lung Cancer with Acquired Resistance.Pathology oncology research : POR, , Volume: 23, Issue:2, 2017
Phase II Study of the EGFR-TKI Rechallenge With Afatinib in Patients With Advanced NSCLC Harboring Sensitive EGFR Mutation Without T790M: Okayama Lung Cancer Study Group Trial OLCSG 1403.Clinical lung cancer, , Volume: 18, Issue:2, 2017
Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 23, Issue:3, 2017
Stevens-Johnson syndrome-like erosive dermatitis possibly related to afatinib.European journal of dermatology : EJD, , Aug-01, Volume: 26, Issue:4, 2016
Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Case report: Durable response to afatinib in a patient with lung cancer harboring two uncommon mutations of EGFR and a KRAS mutation.Lung cancer (Amsterdam, Netherlands), , Volume: 101, 2016
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.Respiratory investigation, , Volume: 54, Issue:6, 2016
Clinical analysis of patients treated with afatinib for advanced non-small cell lung cancer: A Nagano Lung Cancer Research Group observational study.Respiratory investigation, , Volume: 54, Issue:6, 2016
Afatinib: A Review in Advanced Non-Small Cell Lung Cancer.Targeted oncology, , Volume: 11, Issue:6, 2016
Survival of Lung Adenocarcinoma Patients Predicted from Expression of PD-L1, Galectin-9, and XAGE1 (GAGED2a) on Tumor Cells and Tumor-Infiltrating T Cells.Cancer immunology research, , Volume: 4, Issue:12, 2016
The safety of afatinib for the treatment of non-small cell lung cancer.Expert opinion on drug safety, , Volume: 15, Issue:11, 2016
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11, 2016
Promising Effects of Afatinib on Leptomeningeal Carcinomatosis Derived from Erlotinib-resistant Lung Adenocarcinoma.Internal medicine (Tokyo, Japan), , Volume: 55, Issue:17, 2016
Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:11, 2016
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.Investigational new drugs, , Volume: 34, Issue:6, 2016
Complete remissions in afatinib-treated non-small-cell lung cancer patients with symptomatic brain metastases.Anti-cancer drugs, , Volume: 27, Issue:9, 2016
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20, 2016
[Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib in patients with squamous cell carcinoma of the lung: current context and the option of oral treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Evidence on afatinib in patients progressing on a first-line treatment].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Afatinib as first-line therapy in mutation-positive EGFR. Results by type of mutation].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Mechanism of action and preclinical development of afatinib].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Current status of EGFR/ErbB inhibitors in non-small cell lung carcinoma].Medicina clinica, , Volume: 146 Suppl 1, 2016
[Not Available].Medicina clinica, , Volume: 146 Suppl 1, 2016
Evaluation of assays for drug efficacy in a three-dimensional model of the lung.Journal of cancer research and clinical oncology, , Volume: 142, Issue:9, 2016
Kinases inhibitors in lung cancer: From benchside to bedside.Biochimica et biophysica acta, , Volume: 1866, Issue:1, 2016
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer.The Cochrane database of systematic reviews, , May-25, Issue:5, 2016
A Triple Rare E709K and L833V/H835L EGFR Mutation Responsive to an Irreversible Pan-HER Inhibitor: A Case Report of Lung Adenocarcinoma Treated with Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:5, 2016
[The efficacy of TKIs in treatment of human primary small cell lung cancer xenograft model in vivo].Zhongguo ying yong sheng li xue za zhi = Zhongguo yingyong shenglixue zazhi = Chinese journal of applied physiology, , Jun-08, Volume: 32, Issue:6, 2016
Choroidal metastasis as a presenting manifestation of a lung adenocarcinoma with response to afatinib.Archivos de la Sociedad Espanola de Oftalmologia, , Volume: 91, Issue:11, 2016
Afatinib-associated Stevens-Johnson syndrome in an EGFR-mutated lung cancer patient.Lung cancer (Amsterdam, Netherlands), , Volume: 95, 2016
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.The journal of medical investigation : JMI, , Volume: 63, Issue:1-2, 2016
Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial.Targeted oncology, , Volume: 11, Issue:5, 2016
Inequalities in lung cancer: a world of EGFR.The European respiratory journal, , Volume: 47, Issue:5, 2016
Development of a skin rash within the first week and the therapeutic effect in afatinib monotherapy for EGFR-mutant non-small cell lung cancer (NSCLC): Okayama Lung Cancer Study Group experience.Cancer chemotherapy and pharmacology, , Volume: 77, Issue:5, 2016
Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:6, 2016
Selectivity profile of afatinib for EGFR-mutated non-small-cell lung cancer.Molecular bioSystems, , 04-26, Volume: 12, Issue:5, 2016
The afatinib resistance of in vivo generated H1975 lung cancer cell clones is mediated by SRC/ERBB3/c-KIT/c-MET compensatory survival signaling.Oncotarget, , Apr-12, Volume: 7, Issue:15, 2016
Efficacy and safety of afatinib in Chinese patients with EGFR-mutated metastatic non-small-cell lung cancer (NSCLC) previously responsive to first-generation tyrosine-kinase inhibitors (TKI) and chemotherapy: comparison with historical cohort using erlotiBMC cancer, , Feb-24, Volume: 16, 2016
therascreen® EGFR RGQ PCR Kit: A Companion Diagnostic for Afatinib and Gefitinib in Non-Small Cell Lung Cancer.Molecular diagnosis & therapy, , Volume: 20, Issue:2, 2016
The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients.Oncotarget, , Mar-15, Volume: 7, Issue:11, 2016
Resistance mechanisms after tyrosine kinase inhibitors afatinib and crizotinib in non-small cell lung cancer, a review of the literature.Critical reviews in oncology/hematology, , Volume: 100, 2016
First-Line Afatinib versus Chemotherapy in Patients with Non-Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:3, 2016
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1, 2016
Epidermal growth factor receptor tyrosine kinase inhibitors in previously treated advanced non-small-cell lung cancer with wild-type EGFR.Expert opinion on pharmacotherapy, , Volume: 17, Issue:2, 2016
Afatinib and chemotherapy in non-small-cell lung cancer.The Lancet. Oncology, , Volume: 17, Issue:2, 2016
A Phase Ib/II Study of Afatinib in Combination with Nimotuzumab in Non-Small Cell Lung Cancer Patients with Acquired Resistance to Gefitinib or Erlotinib.Clinical cancer research : an official journal of the American Association for Cancer Research, , 05-01, Volume: 22, Issue:9, 2016
Comparison of Skin Toxic Effects Associated With Gefitinib, Erlotinib, or Afatinib Treatment for Non-Small Cell Lung Cancer.JAMA dermatology, , Volume: 152, Issue:3, 2016
Afatinib beyond progression in patients with non-small-cell lung cancer following chemotherapy, erlotinib/gefitinib and afatinib: phase III randomized LUX-Lung 5 trial.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:3, 2016
Different EGFR Gene Mutations in Exon 18, 19 and 21 as Prognostic and Predictive Markers in NSCLC: A Single Institution Analysis.Molecular diagnosis & therapy, , Volume: 20, Issue:1, 2016
Lung cancer patients with HER2 mutations treated with chemotherapy and HER2-targeted drugs: results from the European EUHER2 cohort.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:2, 2016
Tyrosine kinase inhibitors for epidermal growth factor receptor gene mutation-positive non-small cell lung cancers: an update for recent advances in therapeutics.Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 22, Issue:3, 2016
Small Molecule T315 Promotes Casitas B-Lineage Lymphoma-Dependent Degradation of Epidermal Growth Factor Receptor via Y1045 Autophosphorylation.American journal of respiratory and critical care medicine, , Apr-01, Volume: 193, Issue:7, 2016
Afatinib-refractory brain metastases from EGFR-mutant non-small-cell lung cancer successfully controlled with erlotinib: a case report.Anti-cancer drugs, , Volume: 27, Issue:3, 2016
Risk of elevated transaminases in non-small cell lung cancer (NSCLC) patients treated with erlotinib, gefitinib and afatinib: a meta-analysis.Expert review of respiratory medicine, , Volume: 10, Issue:2, 2016
Antitumor effect of afatinib, as a human epidermal growth factor receptor 2-targeted therapy, in lung cancers harboring HER2 oncogene alterations.Cancer science, , Volume: 107, Issue:1, 2016
Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer.Biomedical chromatography : BMC, , Volume: 30, Issue:7, 2016
Afatinib in the first-line treatment of epidermal-growth-factor-receptor mutation-positive non-small cell lung cancer: a review of the clinical evidence.Therapeutic advances in respiratory disease, , Volume: 10, Issue:3, 2016
Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Jan-15, Volume: 22, Issue:2, 2016
Afatinib: An overview of its clinical development in non-small-cell lung cancer and other tumors.Critical reviews in oncology/hematology, , Volume: 97, 2016
Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells.Molecular carcinogenesis, , Volume: 55, Issue:5, 2016
Risk of interstitial lung disease associated with EGFR-TKIs in advanced non-small-cell lung cancer: a meta-analysis of 24 phase III clinical trials.Journal of chemotherapy (Florence, Italy), , Volume: 27, Issue:1, 2015
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Afatinib resistance in non-small cell lung cancer involves the PI3K/AKT and MAPK/ERK signalling pathways and epithelial-to-mesenchymal transition.Targeted oncology, , Volume: 10, Issue:3, 2015
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.Expert opinion on drug safety, , Volume: 14, Issue:1, 2015
Overcoming Resistance Without the Risk of Reaction: Use of Afatinib and Panitumumab in Two Cases of Epidermal Growth Factor Receptor--Mutated Non--Small-Cell Lung Cancer With T790M Mutations.Clinical lung cancer, , Volume: 16, Issue:5, 2015
The combination of irreversible EGFR TKIs and SAHA induces apoptosis and autophagy-mediated cell death to overcome acquired resistance in EGFR T790M-mutated lung cancer.International journal of cancer, , Jun-01, Volume: 136, Issue:11, 2015
Optimizing the sequence of anti-EGFR-targeted therapy in EGFR-mutant lung cancer.Molecular cancer therapeutics, , Volume: 14, Issue:2, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in EGFR FISH-positive non-small-cell lung cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:4, 2015
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
Afatinib induces apoptosis in NSCLC without EGFR mutation through Elk-1-mediated suppression of CIP2A.Oncotarget, , Feb-10, Volume: 6, Issue:4, 2015
LUX-Lung: determining the best EGFR inhibitor in NSCLC?The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials.The Lancet. Oncology, , Volume: 16, Issue:2, 2015
Common EGFR-mutated subgroups (Del19/L858R) in advanced non-small-cell lung cancer: chasing better outcomes with tyrosine kinase inhibitors.Future oncology (London, England), , Volume: 11, Issue:8, 2015
CD133-Positive Cells from Non-Small Cell Lung Cancer Show Distinct Sensitivity to Cisplatin and Afatinib.Archivum immunologiae et therapiae experimentalis, , Volume: 63, Issue:3, 2015
Phase II study of afatinib, an irreversible ErbB family blocker, in demographically and genotypically defined lung adenocarcinoma.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
Effects of cetuximab combined with afatinib on the expression of KDR and AQP1 in lung cancer.Genetics and molecular research : GMR, , Dec-11, Volume: 14, Issue:4, 2015
Long progression-free survival with afatinib in a patient with EGFR-unknown lung adenocarcinoma after erlotinib failure: a case report.Tumori, , Apr-28, Volume: 101, Issue:2, 2015
[Gefitinib therapy in advanced non-small cell lung cancer in patients with EGFR mutations: cost-effectiveness analysis].Voprosy onkologii, , Volume: 61, Issue:4, 2015
HER2 insertion YVMA mutant lung cancer: Long natural history and response to afatinib.Lung cancer (Amsterdam, Netherlands), , Volume: 90, Issue:3, 2015
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1, 2015
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.British journal of cancer, , Nov-17, Volume: 113, Issue:10, 2015
Afatinib in Treatment-Naive Patients With EGFR-Mutated Lung Adenocarcinoma With Brain Metastasis: A Case Series.Medicine, , Volume: 94, Issue:41, 2015
[Bufalin reverses hepatocyte growth factor-induced resistance to afatinib in H1975 lung cancer cells].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 37, Issue:7, 2015
Current and Emerging Options in the Management of EGFR Mutation-Positive Non-Small-Cell Lung Cancer: Considerations in the Elderly.Drugs & aging, , Volume: 32, Issue:11, 2015
The pan-HER family tyrosine kinase inhibitor afatinib overcomes HER3 ligand heregulin-mediated resistance to EGFR inhibitors in non-small cell lung cancer.Oncotarget, , Oct-20, Volume: 6, Issue:32, 2015
Cost-Effectiveness and Value of Information of Erlotinib, Afatinib, and Cisplatin-Pemetrexed for First-Line Treatment of Advanced EGFR Mutation-Positive Non-Small-Cell Lung Cancer in the United States.Value in health : the journal of the International Society for Pharmacoeconomics and Outcomes Research, , Volume: 18, Issue:6, 2015
Afatinib increases sensitivity to radiation in non-small cell lung cancer cells with acquired EGFR T790M mutation.Oncotarget, , Mar-20, Volume: 6, Issue:8, 2015
Afatinib in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations Pretreated With Reversible EGFR Inhibitors.The oncologist, , Volume: 20, Issue:10, 2015
Managing acquired resistance in EGFR-mutated non-small cell lung cancer.Clinical advances in hematology & oncology : H&O, , Volume: 13, Issue:8, 2015
[Pharmacological and clinical profile of afatinib (Giotrif®)].Nihon yakurigaku zasshi. Folia pharmacologica Japonica, , Volume: 145, Issue:2, 2015
[Retrospective Analysis of the Afatinib Clinical Pathway during the 28-Day Introductory Period-The Japanese Style of Collaborative Drug Therapy Management(J-CDTM)].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:8, 2015
Afatinib: a second-generation EGF receptor and ErbB tyrosine kinase inhibitor for the treatment of advanced non-small-cell lung cancer.Future oncology (London, England), , Volume: 11, Issue:18, 2015
EGFR Kinase Domain Duplication (EGFR-KDD) Is a Novel Oncogenic Driver in Lung Cancer That Is Clinically Responsive to Afatinib.Cancer discovery, , Volume: 5, Issue:11, 2015
Cumulative meta-analysis of epidermal growth factor receptor-tyrosine kinase inhibitors as first-line therapy in metastatic non-small-cell lung cancer.Anti-cancer drugs, , Volume: 26, Issue:9, 2015
Practical Value of Molecular Pathology in Stage I-III Lung Cancer: Implications for the Clinical Surgeon.Annals of surgical oncology, , Volume: 22, Issue:11, 2015
EGFR Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs.Clinical cancer research : an official journal of the American Association for Cancer Research, , Dec-01, Volume: 21, Issue:23, 2015
Acquisition of cancer stem cell-like properties in non-small cell lung cancer with acquired resistance to afatinib.Cancer science, , Volume: 106, Issue:10, 2015
RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer.Nature communications, , Mar-11, Volume: 6, 2015
Prolonged survival with erlotinib followed by afatinib in a caucasian smoker with metastatic, poorly differentiated large cell carcinoma of the lung: a case report.Cancer biology & therapy, , Volume: 16, Issue:10, 2015
Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.The oncologist, , Volume: 20, Issue:8, 2015
Afatinib versus erlotinib as second-line treatment of patients with advanced squamous cell carcinoma of the lung (LUX-Lung 8): an open-label randomised controlled phase 3 trial.The Lancet. Oncology, , Volume: 16, Issue:8, 2015
Discordant HER2 Exon 20 Mutation Status Determines a Differential Sensitivity to Afatinib.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:7, 2015
Clinical Utility of Patient-Derived Xenografts to Determine Biomarkers of Prognosis and Map Resistance Pathways in EGFR-Mutant Lung Adenocarcinoma.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Aug-01, Volume: 33, Issue:22, 2015
Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.The oncologist, , Volume: 20, Issue:4, 2015
Next-Generation Covalent Irreversible Kinase Inhibitors in NSCLC: Focus on Afatinib.BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy, , Volume: 29, Issue:3, 2015
[Is chemotherapy still an option in oncogene-addicted non-small cell lung cancer? No].Bulletin du cancer, , Volume: 102, Issue:6 Suppl 1, 2015
Afatinib versus cisplatin plus pemetrexed in Japanese patients with advanced non-small cell lung cancer harboring activating EGFR mutations: Subgroup analysis of LUX-Lung 3.Cancer science, , Volume: 106, Issue:9, 2015
Risk of fatal pulmonary events in patients with advanced non-small-cell lung cancer treated with EGF receptor tyrosine kinase inhibitors: a comparative meta-analysis.Future oncology (London, England), , Volume: 11, Issue:7, 2015
Clinical activity of afatinib in patients with advanced non-small-cell lung cancer harbouring uncommon EGFR mutations: a combined post-hoc analysis of LUX-Lung 2, LUX-Lung 3, and LUX-Lung 6.The Lancet. Oncology, , Volume: 16, Issue:7, 2015
Successful Afatinib Therapy after Resistance to EGFR-TKI in a Patient with Advanced Adenosquamous Cell Lung Cancer.Oncology research and treatment, , Volume: 38, Issue:6, 2015
Afatinib (Gilotrif) for advanced non-small cell lung cancer.The Medical letter on drugs and therapeutics, , May-25, Volume: 57, Issue:1469, 2015
[Hange-Shashin-to for preventing diarrhea during afatinib therapy].Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 42, Issue:5, 2015
Symptom and Quality of Life Improvement in LUX-Lung 6: An Open-Label Phase III Study of Afatinib Versus Cisplatin/Gemcitabine in Asian Patients With EGFR Mutation-Positive Advanced Non-small-cell Lung Cancer.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:6, 2015
Acquired resistance of EGFR-mutant lung adenocarcinomas to afatinib plus cetuximab is associated with activation of mTORC1.Cell reports, , May-22, Volume: 7, Issue:4, 2014
Meta-analysis of first-line therapies in advanced non-small-cell lung cancer harboring EGFR-activating mutations.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 9, Issue:6, 2014
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
LUX-Lung 3: redundancy, toxicity or a major step forward? Afatinib as front-line therapy for patients with metastatic EGFR-mutated lung cancer.Future oncology (London, England), , Volume: 10, Issue:4, 2014
Afatinib use in non-small cell lung cancer previously sensitive to epidermal growth factor receptor inhibitors: the United Kingdom Named Patient Programme.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:10, 2014
Afatinib for the treatment of advanced non-small-cell lung cancer.Expert opinion on pharmacotherapy, , Volume: 15, Issue:6, 2014
Systemic treatment in EGFR-ALK NSCLC patients: second line therapy and beyond.Expert review of anticancer therapy, , Volume: 14, Issue:7, 2014
Network meta-analysis of erlotinib, gefitinib, afatinib and icotinib in patients with advanced non-small-cell lung cancer harboring EGFR mutations.PloS one, , Volume: 9, Issue:2, 2014
Subsequent treatment choices for patients with acquired resistance to EGFR-TKIs in non-small cell lung cancer: restore after a drug holiday or switch to another EGFR-TKI?Asian Pacific journal of cancer prevention : APJCP, , Volume: 15, Issue:1, 2014
Reply to E.R. Haspinger et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Reply to F. De Marinis et al.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib-related nonhematologic adverse events: is common evaluation enough for now?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Do we really need another epidermal growth factor receptor tyrosine kinase inhibitor in first-line treatment for patients with non-small-cell lung cancer and EGFR mutations?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Mar-10, Volume: 32, Issue:8, 2014
Afatinib for lung cancer: let there be light?The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial.The Lancet. Oncology, , Volume: 15, Issue:2, 2014
Afatinib: a review of its use in the treatment of advanced non-small cell lung cancer.Drugs, , Volume: 74, Issue:2, 2014
The current state of molecularly targeted drugs targeting HGF/Met.Japanese journal of clinical oncology, , Volume: 44, Issue:1, 2014
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Preclinical and clinical development of afatinib: a focus on breast cancer and squamous cell carcinoma of the head and neck.Future oncology (London, England), , Volume: 10, Issue:1, 2014
Dual ALK and EGFR inhibition targets a mechanism of acquired resistance to the tyrosine kinase inhibitor crizotinib in ALK rearranged lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 83, Issue:1, 2014
Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical data.Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas, , Volume: 47, Issue:11, 2014
Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22, 2014
Is progression-free survival associated with a better health-related quality of life in patients with lung cancer? Evidence from two randomised trials with afatinib.BMJ open, , Oct-31, Volume: 4, Issue:10, 2014
Afatinib and lung cancer.Expert review of anticancer therapy, , Volume: 14, Issue:12, 2014
New therapy targets resistant non-small-cell lung cancers.Journal of the National Cancer Institute, , Volume: 106, Issue:11, 2014
[Efficacy of first-line afatinib versus chemotherapy in EGFR mutation positive pulmonary adenocarcinoma].Magyar onkologia, , Volume: 58, Issue:4, 2014
[Effect of EGFR-TKI on lymphangiogenesis of lung cancer with EGFR mutation].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:12, 2014
Activity of the EGFR-HER2 dual inhibitor afatinib in EGFR-mutant lung cancer patients with acquired resistance to reversible EGFR tyrosine kinase inhibitors.Clinical lung cancer, , Volume: 15, Issue:6, 2014
Experience with afatinib in patients with non-small cell lung cancer progressing after clinical benefit from gefitinib and erlotinib.The oncologist, , Volume: 19, Issue:10, 2014
β-catenin contributes to lung tumor development induced by EGFR mutations.Cancer research, , Oct-15, Volume: 74, Issue:20, 2014
FGFR1 activation is an escape mechanism in human lung cancer cells resistant to afatinib, a pan-EGFR family kinase inhibitor.Oncotarget, , Aug-15, Volume: 5, Issue:15, 2014
Dual inhibition of EGFR with afatinib and cetuximab in kinase inhibitor-resistant EGFR-mutant lung cancer with and without T790M mutations.Cancer discovery, , Volume: 4, Issue:9, 2014
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
[A new perspective in the treatment of non-small-cell lung cancer (NSCLC). Role of afatinib: An oral and irreversible ErbB family blocker].Bulletin du cancer, , Volume: 101, Issue:6, 2014
management of nonhematologic toxicities associated with different EGFR-TKIs in advanced NSCLC: a comparison analysis.Clinical lung cancer, , Volume: 15, Issue:4, 2014
Afatinib in the treatment of EGFR mutation-positive NSCLC--a network meta-analysis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:2, 2014
Gefitinib and afatinib treatment in an advanced non-small cell lung cancer (NSCLC) patient undergoing hemodialysis.Anticancer research, , Volume: 34, Issue:6, 2014
[Afatinib (BIBW 2992)].Revue de pneumologie clinique, , Volume: 70, Issue:5, 2014
Phase II study of Afatinib as third-line treatment for patients in Korea with stage IIIB/IV non-small cell lung cancer harboring wild-type EGFR.The oncologist, , Volume: 19, Issue:7, 2014
Management and future directions in non-small cell lung cancer with known activating mutations.American Society of Clinical Oncology educational book. American Society of Clinical Oncology. Annual Meeting, , 2014
Afatinib with concurrent radiotherapy in a patient with metastatic non-small cell lung cancer.Oncology research and treatment, , Volume: 37, Issue:5, 2014
Ten lessons from EGFR.Respiratory investigation, , Volume: 52, Issue:3, 2014
Next generation tyrosine kinase inhibitor (TKI): afatinib.Recent patents on anti-cancer drug discovery, , Volume: 9, Issue:3, 2014
Combination of BIBW2992 and ARQ 197 is effective against erlotinib-resistant human lung cancer cells with the EGFR T790M mutation.Oncology reports, , Volume: 32, Issue:1, 2014
Successful treatment of a patient with Li-Fraumeni syndrome and metastatic lung adenocarcinoma harboring synchronous EGFR L858R and ERBB2 extracellular domain S310F mutations with the pan-HER inhibitor afatinib.Cancer biology & therapy, , Volume: 15, Issue:8, 2014
An update on molecularly targeted therapies in second- and third-line treatment in non-small cell lung cancer: focus on EGFR inhibitors and anti-angiogenic agents.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico, , Volume: 15, Issue:5, 2013
Symptom and quality of life benefit of afatinib in advanced non-small-cell lung cancer patients previously treated with erlotinib or gefitinib: results of a randomized phase IIb/III trial (LUX-Lung 1).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 8, Issue:2, 2013
Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.Biochemical and biophysical research communications, , Feb-15, Volume: 431, Issue:3, 2013
[Development and biochemical characterization of EGFR/c-Met dual inhibitors].Acta pharmaceutica Hungarica, , Volume: 83, Issue:4, 2013
Ability of the Met kinase inhibitor crizotinib and new generation EGFR inhibitors to overcome resistance to EGFR inhibitors.PloS one, , Volume: 8, Issue:12, 2013
[Tumor microenvironment elicits primary resistance to afatinib through HGF secretion].Zhonghua zhong liu za zhi [Chinese journal of oncology], , Volume: 35, Issue:10, 2013
Afatinib for the treatment of patients with EGFR-positive non-small cell lung cancer.Drugs of today (Barcelona, Spain : 1998), , Volume: 49, Issue:9, 2013
Afatinib monotherapy in EGFR-mutant lung adenocarcinoma.The Lancet. Oncology, , Volume: 14, Issue:9, 2013
Afatinib, erlotinib and gefitinib in the first-line therapy of EGFR mutation-positive lung adenocarcinoma: a review.Onkologie, , Volume: 36, Issue:9, 2013
The role of afatinib in the management of non-small cell lung carcinoma.Expert opinion on drug metabolism & toxicology, , Volume: 9, Issue:11, 2013
Afatinib: first global approval.Drugs, , Volume: 73, Issue:13, 2013
Epidermal growth factor receptor inhibition in mutation-positive non-small-cell lung cancer: is afatinib better or simply newer?Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Targeted therapies: Afatinib--new therapy option for EGFR-mutant lung cancer.Nature reviews. Clinical oncology, , Volume: 10, Issue:10, 2013
New kinase inhibitor approved for metastatic lung cancer.American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Aug-15, Volume: 70, Issue:16, 2013
Symptom control and quality of life in LUX-Lung 3: a phase III study of afatinib or cisplatin/pemetrexed in patients with advanced lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
LUX-Lung 4: a phase II trial of afatinib in patients with advanced non-small-cell lung cancer who progressed during prior treatment with erlotinib, gefitinib, or both.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27, 2013
Clinical perspective of afatinib in non-small cell lung cancer.Lung cancer (Amsterdam, Netherlands), , Volume: 81, Issue:2, 2013
Lung cancer that harbors an HER2 mutation: epidemiologic characteristics and therapeutic perspectives.Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Jun-01, Volume: 31, Issue:16, 2013
Impact of EGFR inhibitor in non-small cell lung cancer on progression-free and overall survival: a meta-analysis.Journal of the National Cancer Institute, , May-01, Volume: 105, Issue:9, 2013
Afatinib prolongs survival compared with gefitinib in an epidermal growth factor receptor-driven lung cancer model.Molecular cancer therapeutics, , Volume: 12, Issue:5, 2013
[About new treatments in thoracic oncology].Revue de pneumologie clinique, , Volume: 69, Issue:2, 2013
Strides in personalized medicine.Cancer, , Dec-01, Volume: 118, Issue:23, 2012
Disseminated herpes simplex virus infection following epidermal growth factor tyrosine kinase inhibitor therapy for non-small-cell lung carcinoma.Internal medicine journal, , Volume: 42, Issue:11, 2012
Epidermal growth factor receptor (EGFR) inhibitors and derived treatments.Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 23 Suppl 10, 2012
Temporal molecular and biological assessment of an erlotinib-resistant lung adenocarcinoma model reveals markers of tumor progression and treatment response.Cancer research, , Nov-15, Volume: 72, Issue:22, 2012
HER2 amplification: a potential mechanism of acquired resistance to EGFR inhibition in EGFR-mutant lung cancers that lack the second-site EGFRT790M mutation.Cancer discovery, , Volume: 2, Issue:10, 2012
Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation.Molecular cancer therapeutics, , Volume: 11, Issue:10, 2012
Monitoring reversible and irreversible EGFR inhibition with erlotinib and afatinib in a patient with EGFR-mutated non-small cell lung cancer (NSCLC) using sequential [18F]fluorothymidine (FLT-)PET.Lung cancer (Amsterdam, Netherlands), , Volume: 77, Issue:3, 2012
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Afatinib for patients with lung adenocarcinoma and epidermal growth factor receptor mutations (LUX-Lung 2): a phase 2 trial.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
A new generation of EGFR tyrosine-kinase inhibitors in NSCLC.The Lancet. Oncology, , Volume: 13, Issue:5, 2012
Targeting the epidermal growth factor receptor in non-small cell lung cancer cells: the effect of combining RNA interference with tyrosine kinase inhibitors or cetuximab.BMC medicine, , Mar-21, Volume: 10, 2012
Clinical activity of afatinib (BIBW 2992) in patients with lung adenocarcinoma with mutations in the kinase domain of HER2/neu.Lung cancer (Amsterdam, Netherlands), , Volume: 76, Issue:1, 2012
Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence.Critical reviews in oncology/hematology, , Volume: 83, Issue:3, 2012
The EGFR T790M mutation in acquired resistance to an irreversible second-generation EGFR inhibitor.Molecular cancer therapeutics, , Volume: 11, Issue:3, 2012
EGFR exon 19 insertions: a new family of sensitizing EGFR mutations in lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-15, Volume: 18, Issue:6, 2012
Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4).Cancer chemotherapy and pharmacology, , Volume: 69, Issue:4, 2012
Afatinib (BIBW 2992) development in non-small-cell lung cancer.Future oncology (London, England), , Volume: 7, Issue:7, 2011
The LUX-Lung clinical trial program of afatinib for non-small-cell lung cancer.Expert review of anticancer therapy, , Volume: 11, Issue:5, 2011
The search for improved systemic therapy of non-small cell lung cancer--what are today's options?Lung cancer (Amsterdam, Netherlands), , Volume: 72, Issue:3, 2011
BIBW 2992 in non-small cell lung cancer.Expert opinion on investigational drugs, , Volume: 20, Issue:3, 2011
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.Expert opinion on investigational drugs, , Volume: 19, Issue:12, 2010
EGFR inhibitors in non-small cell lung cancer (NSCLC): the emerging role of the dual irreversible EGFR/HER2 inhibitor BIBW 2992.Targeted oncology, , Volume: 5, Issue:4, 2010
Enhanced anticancer effect of the combination of BIBW2992 and thymidylate synthase-targeted agents in non-small cell lung cancer with the T790M mutation of epidermal growth factor receptor.Molecular cancer therapeutics, , Volume: 9, Issue:6, 2010
The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.Cancer investigation, , Volume: 28, Issue:4, 2010
Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation.Cancer research, , Feb-01, Volume: 70, Issue:3, 2010
Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer.The Journal of clinical investigation, , Volume: 119, Issue:10, 2009
Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.Clinical lung cancer, , Volume: 10, Issue:4, 2009
HER2YVMA drives rapid development of adenosquamous lung tumors in mice that are sensitive to BIBW2992 and rapamycin combination therapy.Proceedings of the National Academy of Sciences of the United States of America, , Jan-13, Volume: 106, Issue:2, 2009
BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.Oncogene, , Aug-07, Volume: 27, Issue:34, 2008
Acquired resistance to epidermal growth factor receptor kinase inhibitors associated with a novel T854A mutation in a patient with EGFR-mutant lung adenocarcinoma.Clinical cancer research : an official journal of the American Association for Cancer Research, , Nov-15, Volume: 14, Issue:22, 2008
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
Skeletal muscle loss during anti-epidermal growth factor receptor therapy is an independent prognostic factor on non-small cell lung cancer patients survival.Journal of B.U.ON. : official journal of the Balkan Union of Oncology, , Volume: 26, Issue:3
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.Integrative cancer therapies, , Volume: 20
Inhibitory Effects of HangAmDan-B1 (HAD-B1) Combined With Afatinib on H1975 Lung Cancer Cell-Bearing Mice.Integrative cancer therapies, , Volume: 18
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in Integrative cancer therapies, , Volume: 21
Significance of Polar Charged Amino Acids in Compound Mutations in EGFR-mutated Patients Treated With First-line Afatinib.In vivo (Athens, Greece), , Volume: 36, Issue:4
Afatinib in the first-line treatment of patients with non-small cell lung cancer: clinical evidence and experience.Therapeutic advances in respiratory disease, , Volume: 12
Synergistic Effect of HAD-B1 and Afatinib Against Gefitinib Resistance of Non-Small Cell Lung Cancer.Integrative cancer therapies, , Volume: 21
Identifying activating mutations in the EGFR gene: prognostic and therapeutic implications in non-small cell lung cancer.Jornal brasileiro de pneumologia : publicacao oficial da Sociedade Brasileira de Pneumologia e Tisilogia, , Volume: 41, Issue:4
Afatinib Achieved Remarkable Disease Control in a Chinese Patient With Lung Adenocarcinoma Harboring Rare EGFR Exon 18-25 Kinase Domain Duplication.American journal of therapeutics, , Volume: 27, Issue:5
Clinical Outcome of ALK-Positive Non-Small Cell Lung Cancer (NSCLC) Patients with De Novo EGFR or KRAS Co-Mutations Receiving Tyrosine Kinase Inhibitors (TKIs).Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 12, Issue:4, 2017
The role of surgery in patients with advanced gynaecological cancers participating in phase I clinical trials.European journal of gynaecological oncology, , Volume: 33, Issue:2, 2012
Overcoming T790M-driven acquired resistance to EGFR-TKIs in NSCLC with afatinib: a case report.Tumori, , Volume: 100, Issue:1
The multi-kinase inhibitor afatinib serves as a novel candidate for the treatment of human uveal melanoma.Cellular oncology (Dordrecht), , Volume: 45, Issue:4, 2022
Inhibiting insulin and mTOR signaling by afatinib and crizotinib combination fosters broad cytotoxic effects in cutaneous malignant melanoma.Cell death & disease, , 10-20, Volume: 11, Issue:10, 2020
Combining ERBB family and MET inhibitors is an effective therapeutic strategy in cutaneous malignant melanoma independent of BRAF/NRAS mutation status.Cell death & disease, , 09-10, Volume: 10, Issue:9, 2019
Strides in personalized medicine.Cancer, , Dec-01, Volume: 118, Issue:23, 2012
Efficacy of afatinib for pulmonary adenocarcinoma with leptomeningeal metastases harboring an epidermal growth factor receptor complex mutation (exon 19del+K754E): A case report.Medicine, , Oct-23, Volume: 99, Issue:43, 2020
Efficacy of the irreversible ErbB family blocker afatinib in epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI)-pretreated non-small-cell lung cancer patients with brain metastases or leptomeningeal disease.Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 10, Issue:1, 2015
Afatinib combined with cetuximab for lung adenocarcinoma with leptomeningeal carcinomatosis.Lung cancer (Amsterdam, Netherlands), , Volume: 85, Issue:3, 2014
Simultaneous Single Cell Gene Expression and EGFR Mutation Analysis of Circulating Tumor Cells Reveals Distinct Phenotypes in NSCLC.Advanced biosystems, , Volume: 4, Issue:8, 2020
Detection of T790M, the Acquired Resistance EGFR Mutation, by Tumor Biopsy versus Noninvasive Blood-Based Analyses.Clinical cancer research : an official journal of the American Association for Cancer Research, , Mar-01, Volume: 22, Issue:5, 2016
Targeting human epidermal growth factor receptor 2 enhances radiosensitivity and reduces the metastatic potential of Lewis lung carcinoma cells.Radiation oncology (London, England), , Mar-06, Volume: 15, Issue:1, 2020
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Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
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Minocycline prevents and repairs the skin disorder associated with afatinib, one of the epidermal growth factor receptor-tyrosine kinase inhibitors for non-small cell lung cancer.BMC cancer, , Apr-06, Volume: 20, Issue:1, 2020
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4, 2019
Randomized, open-label trial evaluating the preventive effect of tetracycline on afatinib induced-skin toxicities in non-small cell lung cancer patients.Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:3, 2015
Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors.Investigational new drugs, , Volume: 31, Issue:3, 2013
Inflammatory changes in actinic keratoses associated with afatinib therapy.Cutis, , Volume: 105, Issue:3, 2020
Inhibiting insulin and mTOR signaling by afatinib and crizotinib combination fosters broad cytotoxic effects in cutaneous malignant melanoma.Cell death & disease, , 10-20, Volume: 11, Issue:10, 2020
Combining ERBB family and MET inhibitors is an effective therapeutic strategy in cutaneous malignant melanoma independent of BRAF/NRAS mutation status.Cell death & disease, , 09-10, Volume: 10, Issue:9, 2019
Oxidative stress and autophagy-mediated immune patterns and tumor microenvironment infiltration characterization in gastric cancer.Aging, , 11-09, Volume: 15, Issue:21, 2023
Enhancing vulnerability of Afatinib using Erastin via xCT-mediated ROS/P38MAPK signaling feedback loop in gastric cancer cells.Gene, , Jul-15, Volume: 873, 2023
Knockdown of CALM2 increases the sensitivity to afatinib in HER2-amplified gastric cancer cells by regulating the Akt/FoxO3a/Puma axis.Toxicology in vitro : an international journal published in association with BIBRA, , Volume: 87, 2023
Feasibility of Gastric Tumor Xenograft (GTX)-derived Cell Lines for Individualized Anti-cancer Drug Screening.Anticancer research, , Volume: 42, Issue:6, 2022
Combining gene expression analysis of gastric cancer cell lines and tumor specimens to identify biomarkers for anti-HER therapies-the role of HAS2, SHB and HBEGF.BMC cancer, , Mar-09, Volume: 22, Issue:1, 2022
Determining the effects of trastuzumab, cetuximab and afatinib by phosphoprotein, gene expression and phenotypic analysis in gastric cancer cell lines.BMC cancer, , Oct-28, Volume: 20, Issue:1, 2020
EPHA2 blockade reverses acquired resistance to afatinib induced by EPHA2-mediated MAPK pathway activation in gastric cancer cells and avatar mice.International journal of cancer, , 11-01, Volume: 145, Issue:9, 2019
MET as resistance factor for afatinib therapy and motility driver in gastric cancer cells.PloS one, , Volume: 14, Issue:9, 2019
Efficacy of Afatinib and Lapatinib Against Anticancer research, , Volume: 39, Issue:11, 2019
Acquired resistance mechanisms to afatinib in HER2-amplified gastric cancer cells.Cancer science, , Volume: 110, Issue:8, 2019
Effects of trastuzumab and afatinib on kinase activity in gastric cancer cell lines.Molecular oncology, , Volume: 12, Issue:4, 2018
Phase I trial of afatinib and 3-weekly trastuzumab with optimal anti-diarrheal management in patients with HER2-positive metastatic cancer.Cancer chemotherapy and pharmacology, , Volume: 82, Issue:6, 2018
A novel lead compound CM-118: antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers.Cancer biology & therapy, , Jun-01, Volume: 15, Issue:6, 2014
Monitoring afatinib treatment in HER2-positive gastric cancer with 18F-FDG and 89Zr-trastuzumab PET.Journal of nuclear medicine : official publication, Society of Nuclear Medicine, , Volume: 54, Issue:6, 2013
Skin Rash Can Be a Useful Marker for Afatinib Efficacy.Anticancer research, , Volume: 38, Issue:3, 2018
Management of the adverse events of afatinib: a consensus of the recommendations of the Spanish expert panel.Future oncology (London, England), , Volume: 11, Issue:2, 2015
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4, 2014
HER2 regulates cancer stem-like cell phenotype in ALK translocated NSCLC.International journal of oncology, , Volume: 51, Issue:2, 2017
Overcoming EGFR Bypass Signal-Induced Acquired Resistance to ALK Tyrosine Kinase Inhibitors in ALK-Translocated Lung Cancer.Molecular cancer research : MCR, , Volume: 15, Issue:1, 2017
Singapore Cancer Network (SCAN) Guidelines for the Use of Systemic Therapy in Advanced Non-Small Cell Lung Cancer.Annals of the Academy of Medicine, Singapore, , Volume: 44, Issue:10, 2015
Objective, domain-specific HER2 measurement in uterine and ovarian serous carcinomas and its clinical significance.Gynecologic oncology, , Volume: 145, Issue:1, 2017
Afatinib demonstrates remarkable activity against HER2-amplified uterine serous endometrial cancer in vitro and in vivo.British journal of cancer, , Oct-28, Volume: 111, Issue:9, 2014
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.The oncologist, , Volume: 26, Issue:4, 2021
One Atom Makes All the Difference: Getting a Foot in the Door between SOS1 and KRAS.Journal of medicinal chemistry, , 05-27, Volume: 64, Issue:10, 2021
BRAF mutant colorectal cancer: ErbB2 expression levels as predictive factor for the response to combined BRAF/ErbB inhibitors.BMC cancer, , Feb-17, Volume: 20, Issue:1, 2020
Afatinib treatment for her-2 amplified metastatic colorectal cancer based on patient-derived xenograft models and next generation sequencing.Cancer biology & therapy, , Volume: 20, Issue:4, 2019
Combined targeting of HER-2 and HER-3 represents a promising therapeutic strategy in colorectal cancer.BMC cancer, , Sep-05, Volume: 19, Issue:1, 2019
Improving the anticancer effect of afatinib and microRNA by using lipid polymeric nanoparticles conjugated with dual pH-responsive and targeting peptides.Journal of nanobiotechnology, , Aug-19, Volume: 17, Issue:1, 2019
Preclinical and clinical studies on afatinib in monotherapy and in combination regimens: Potential impact in colorectal cancer.Pharmacology & therapeutics, , Volume: 166, 2016
HER2 activating mutations are targets for colorectal cancer treatment.Cancer discovery, , Volume: 5, Issue:8, 2015
Effect of KRAS exon 2 mutations on antitumor activity of afatinib and gefitinib.Anti-cancer drugs, , Volume: 26, Issue:4, 2015
A randomised, open-label phase II trial of afatinib versus cetuximab in patients with metastatic colorectal cancer.European journal of cancer (Oxford, England : 1990), , Volume: 50, Issue:18, 2014
Afatinib and its encapsulated polymeric micelles inhibits HER2-overexpressed colorectal tumor cell growth in vitro and in vivo.Oncotarget, , Jul-15, Volume: 5, Issue:13, 2014
EGFR- and VEGF(R)-targeted small molecules show synergistic activity in colorectal cancer models refractory to combinations of monoclonal antibodies.Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 17, Issue:20, 2011
Phase II trial of weekly alternating sequential BIBF 1120 and afatinib for advanced colorectal cancer.Anticancer research, , Volume: 31, Issue:6, 2011
Growth response of human colorectal tumour cell lines to treatment with afatinib (BIBW2992), an irreversible erbB family blocker, and its association with expression of HER family members.International journal of oncology, , Volume: 39, Issue:2, 2011
Safety/Toxicity (47)
| Article | Year |
|---|
A randomized, open-label, two-cycle, two-crossover phase I clinical trial comparing the bioequivalence and safety of afatinib and Giotrif
Journal of cancer research and clinical oncology, , Volume: 149, Issue:6 | 2023 |
Efficacy of Prophylactic Traditional Chinese Medicine on Skin Toxicity of Afatinib in
Integrative cancer therapies, , Volume: 21 | |
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.
Investigational new drugs, , Volume: 40, Issue:2 | 2022 |
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.
Integrative cancer therapies, , Volume: 20 | |
Relationship between Epidermal Growth Factor Receptor Mutations and Adverse Events in Non-Small Cell Lung Cancer Patients treated with Afatinib.
The journal of medical investigation : JMI, , Volume: 68, Issue:1.2 | 2021 |
Treatment outcomes and safety of afatinib in advanced squamous cell lung cancer progressed after platinum-based doublet chemotherapy and immunotherapy (SPACE study).
Thoracic cancer, , Volume: 12, Issue:8 | 2021 |
Mechanism of hepatotoxicity of first-line tyrosine kinase inhibitors: Gefitinib and afatinib.
Toxicology letters, , Jun-01, Volume: 343 | 2021 |
A randomized, multi-center, open-label study to compare the safety and efficacy between afatinib monotherapy and combination therapy of afatinib and HAD-B1 for the locally advanced or metastatic NSCLC patients with EGFR mutations.
Medicine, , 12-04, Volume: 99, Issue:49 | 2020 |
Safety and efficacy of afatinib for the treatment of non-small-cell lung cancer following osimertinib-induced interstitial lung disease: A retrospective study.
Investigational new drugs, , Volume: 38, Issue:6 | 2020 |
Effects of tyrosine kinase inhibitor therapy on skin toxicity and skin-related quality of life in patients with lung cancer: An observational study.
Medicine, , Jun-05, Volume: 99, Issue:23 | 2020 |
Safety Profile of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors: A Disproportionality Analysis of FDA Adverse Event Reporting System.
Scientific reports, , 03-16, Volume: 10, Issue:1 | 2020 |
Multi-center, randomized, double-blind, placebo-controlled, exploratory study to evaluate the efficacy and safety of HAD-B1 for dose-finding in EGFR positive and locally advanced or metastatic NSCLC subjects who need Afatinib therapy: Study protocol clini
Medicine, , Volume: 99, Issue:4 | 2020 |
The rate of occurrence, healthcare resource use and costs of adverse events among metastatic non-small cell lung cancer patients treated with first- and second-generation epidermal growth factor receptor tyrosine kinase inhibitors.
Lung cancer (Amsterdam, Netherlands), , Volume: 138 | 2019 |
Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.
Oral oncology, , Volume: 97 | 2019 |
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.
Lung cancer (Amsterdam, Netherlands), , Volume: 134 | 2019 |
Efficacy and safety of afatinib in a Chinese population with advanced lung adenocarcinoma with sensitive EGFR mutations.
Thoracic cancer, , Volume: 10, Issue:6 | 2019 |
Pharmacist-led patient education and adverse event management in patients with non-small cell lung cancer receiving afatinib in a community-based, real-world clinical setting.
Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 26, Issue:1 | 2020 |
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.
CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4 | 2019 |
Impact of afatinib dose modification on safety and effectiveness in patients with EGFR mutation-positive advanced NSCLC: Results from a global real-world study (RealGiDo).
Lung cancer (Amsterdam, Netherlands), , Volume: 127 | 2019 |
Safety and efficacy of afatinib as add-on to standard therapy of gemcitabine/cisplatin in chemotherapy-naive patients with advanced biliary tract cancer: an open-label, phase I trial with an extensive biomarker program.
BMC cancer, , Jan-11, Volume: 19, Issue:1 | 2019 |
Cryoprotectant toxicity in Caenorhabditis elegans.
Cryobiology, , Volume: 86 | 2019 |
Afatinib Therapy: Practical Management of Adverse Events With an Oral Agent for Non-Small Cell Lung Cancer Treatment.
Clinical journal of oncology nursing, , 10-01, Volume: 22, Issue:5 | 2018 |
Efficacy and Safety of Afatinib for EGFR-mutant Non-small Cell Lung Cancer, Compared with Gefitinib or Erlotinib.
Cancer research and treatment, , Volume: 51, Issue:2 | 2019 |
Activity and safety of afatinib in a window preoperative EORTC study in patients with squamous cell carcinoma of the head and neck (SCCHN).
Annals of oncology : official journal of the European Society for Medical Oncology, , 04-01, Volume: 29, Issue:4 | 2018 |
Afatinib Therapy for Brain Metastases Aggravated by a Reduction in the Dose of Erlotinib Due to the Development of Hepatotoxicity.
Internal medicine (Tokyo, Japan), , Nov-01, Volume: 56, Issue:21 | 2017 |
Tyrosine kinase inhibitors as modulators of trastuzumab-mediated antibody-dependent cell-mediated cytotoxicity in breast cancer cell lines.
Cellular immunology, , Volume: 319 | 2017 |
Case series on the association between blood levels and side effects of afatinib maleate.
Cancer chemotherapy and pharmacology, , Volume: 80, Issue:3 | 2017 |
An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.
Respiratory investigation, , Volume: 55, Issue:1 | 2017 |
The safety of afatinib for the treatment of non-small cell lung cancer.
Expert opinion on drug safety, , Volume: 15, Issue:11 | 2016 |
Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.
Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 27, Issue:11 | 2016 |
Successful treatment with afatinib after gefitinib- and erlotinib-induced hepatotoxicity.
Investigational new drugs, , Volume: 34, Issue:6 | 2016 |
[Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].
Medicina clinica, , Volume: 146 Suppl 1 | 2016 |
Safe and successful treatment with afatinib in three postoperative non-small cell lung cancer patients with recurrences following gefitinib/erlotinib-induced hepatotoxicity.
The journal of medical investigation : JMI, , Volume: 63, Issue:1-2 | 2016 |
Efficacy and safety of afatinib in Chinese patients with EGFR-mutated metastatic non-small-cell lung cancer (NSCLC) previously responsive to first-generation tyrosine-kinase inhibitors (TKI) and chemotherapy: comparison with historical cohort using erloti
BMC cancer, , Feb-24, Volume: 16 | 2016 |
[Successful Treatment of Non-Small Cell Lung Cancer with Afatinib after Gefitinib-Induced Hepatotoxicity].
Gan to kagaku ryoho. Cancer & chemotherapy, , Volume: 43, Issue:1 | 2016 |
Renal toxicity of anticancer agents targeting HER2 and EGFR.
Journal of nephrology, , Volume: 28, Issue:6 | 2015 |
Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.
The oncologist, , Volume: 20, Issue:8 | 2015 |
Gefitinib and erlotinib in metastatic non-small cell lung cancer: a meta-analysis of toxicity and efficacy of randomized clinical trials.
The oncologist, , Volume: 20, Issue:4 | 2015 |
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.
Lung cancer (Amsterdam, Netherlands), , Volume: 88, Issue:1 | 2015 |
Synergistic cytotoxicity of afatinib and cetuximab against EGFR T790M involves Rab11-dependent EGFR recycling.
Biochemical and biophysical research communications, , Dec-12, Volume: 455, Issue:3-4 | 2014 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23 | 2014 |
Class act: safety comparison of approved tyrosine kinase inhibitors for non-small-cell lung carcinoma.
Expert opinion on drug safety, , Volume: 14, Issue:1 | 2015 |
Management of the adverse events of afatinib: a consensus of the recommendations of the Spanish expert panel.
Future oncology (London, England), , Volume: 11, Issue:2 | 2015 |
[Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].
Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Volume: 17, Issue:4 | 2014 |
Dermatologic adverse events associated with afatinib: an oral ErbB family blocker.
Expert review of anticancer therapy, , Volume: 13, Issue:6 | 2013 |
A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors.
Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 24, Issue:5 | 2013 |
A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.
Breast cancer research and treatment, , Volume: 134, Issue:3 | 2012 |
Pharmacokinetics (13)
| Article | Year |
|---|
Pharmacokinetic and Safety Comparison of 2 Afatinib Dimaleate Tablets in Healthy Chinese Volunteers Under Fasted Conditions: A Randomized, Open-Label, 2-Period, Single-Dose Crossover Study.
Clinical pharmacology in drug development, , Volume: 11, Issue:10 | 2022 |
Pharmacokinetic and pharmacogenomic analysis of low-dose afatinib treatment in elderly patients with EGFR mutation-positive non-small cell lung cancer.
European journal of cancer (Oxford, England : 1990), , Volume: 160 | 2022 |
Effects of pharmacokinetics-related genetic polymorphisms on the side effect profile of afatinib in patients with non-small cell lung cancer.
Lung cancer (Amsterdam, Netherlands), , Volume: 134 | 2019 |
Clinical Pharmacokinetics and Pharmacodynamics of Afatinib.
Clinical pharmacokinetics, , Volume: 56, Issue:3 | 2017 |
Development of a novel noncapillary plasma microsampling device for ultra-low volume of blood collection.
Bioanalysis, , Volume: 8, Issue:9 | 2016 |
The role of extrahepatic metabolism in the pharmacokinetics of the targeted covalent inhibitors afatinib, ibrutinib, and neratinib.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 43, Issue:3 | 2015 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23 | 2014 |
Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment.
Cancer chemotherapy and pharmacology, , Volume: 74, Issue:2 | 2014 |
Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 73, Issue:4 | 2014 |
Pharmacokinetic drug interactions of afatinib with rifampicin and ritonavir.
Clinical drug investigation, , Volume: 34, Issue:3 | 2014 |
Phase II, open-label trial to assess QTcF effects, pharmacokinetics and antitumor activity of afatinib in patients with relapsed or refractory solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 72, Issue:6 | 2013 |
Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Clinical pharmacokinetics, , Volume: 52, Issue:12 | 2013 |
Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers.
Cancer chemotherapy and pharmacology, , Volume: 69, Issue:4 | 2012 |
Bioavailability (10)
| Article | Year |
|---|
Influence of esomeprazole on the bioavailability of afatinib: A pharmacokinetic cross-over study in patients with non-small cell lung cancer.
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, , Volume: 155 | 2022 |
Afatinib-loaded inhalable PLGA nanoparticles for localized therapy of non-small cell lung cancer (NSCLC)-development and in-vitro efficacy.
Drug delivery and translational research, , Volume: 11, Issue:3 | 2021 |
Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors.
Journal of medicinal chemistry, , 06-27, Volume: 62, Issue:12 | 2019 |
Tyrosine Kinase Inhibitor Gold Nanoconjugates for the Treatment of Non-Small Cell Lung Cancer.
ACS applied materials & interfaces, , May-08, Volume: 11, Issue:18 | 2019 |
[Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].
Zhongguo fei ai za zhi = Chinese journal of lung cancer, , Sep-20, Volume: 21, Issue:9 | 2018 |
Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.
European journal of medicinal chemistry, , Sep-18, Volume: 102 | 2015 |
A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles.
Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23 | 2014 |
Afatinib in the treatment of breast cancer.
Expert opinion on investigational drugs, , Volume: 23, Issue:7 | 2014 |
Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 73, Issue:4 | 2014 |
Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, , Sep-20, Volume: 31, Issue:27 | 2013 |
Dosage (27)
| Article | Year |
|---|
Medication adjustment of afatinib and combination therapy with sitagliptin for alleviating afatinib-induced diarrhea in rats.
Neoplasia (New York, N.Y.), , Volume: 43 | 2023 |
Early-Onset Pulmonary Events with Combined Brigatinib and Afatinib Treatment of L858/cisT790M/cisC797S NSCLC: A Case Report.
The American journal of case reports, , Sep-23, Volume: 23 | 2022 |
Multi-Center, Randomized, Double-Blind, Placebo-Controlled, Exploratory Study to Evaluate the Efficacy and Safety of HAD-B1 for Dose-Finding in EGFR Mutation Positive and Locally Advanced or Metastatic NSCLC Subjects Who Need Afatinib Therapy.
Integrative cancer therapies, , Volume: 20 | |
Phase I Study of Afatinib and Selumetinib in Patients with KRAS-Mutated Colorectal, Non-Small Cell Lung, and Pancreatic Cancer.
The oncologist, , Volume: 26, Issue:4 | 2021 |
Modeling Exposure-Driven Adverse Event Time Courses in Oncology Exemplified by Afatinib.
CPT: pharmacometrics & systems pharmacology, , Volume: 8, Issue:4 | 2019 |
Chemotherapeutic agents eligible for prior dosing in pancreatic cancer patients requiring hemodialysis: a systematic review
.
Clinical nephrology, , Volume: 90, Issue:2 | 2018 |
A phase I trial of afatinib and bevacizumab in chemo-naïve patients with advanced non-small-cell lung cancer harboring EGFR mutations: Okayama Lung Cancer Study Group Trial 1404.
Lung cancer (Amsterdam, Netherlands), , Volume: 115 | 2018 |
Phase I study of induction chemotherapy with afatinib, ribavirin, and weekly carboplatin and paclitaxel for stage IVA/IVB human papillomavirus-associated oropharyngeal squamous cell cancer.
Head & neck, , Volume: 40, Issue:2 | 2018 |
Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.
Anticancer research, , Volume: 37, Issue:9 | 2017 |
Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.
Clinical drug investigation, , Volume: 37, Issue:6 | 2017 |
Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.
Respiratory investigation, , Volume: 54, Issue:6 | 2016 |
The safety of afatinib for the treatment of non-small cell lung cancer.
Expert opinion on drug safety, , Volume: 15, Issue:11 | 2016 |
Clinical Pharmacokinetics and Pharmacodynamics of Afatinib.
Clinical pharmacokinetics, , Volume: 56, Issue:3 | 2017 |
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity.
Clinical cancer research : an official journal of the American Association for Cancer Research, , Oct-15, Volume: 22, Issue:20 | 2016 |
Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.
Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, , Volume: 11, Issue:6 | 2016 |
Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.
Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, , Volume: 23, Issue:3 | 2017 |
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.
British journal of cancer, , Nov-17, Volume: 113, Issue:10 | 2015 |
A phase I study of daily afatinib, an irreversible ErbB family blocker, in combination with weekly paclitaxel in patients with advanced solid tumours.
European journal of cancer (Oxford, England : 1990), , Volume: 51, Issue:16 | 2015 |
Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.
American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists, , Nov-15, Volume: 71, Issue:22 | 2014 |
Phase I/randomized phase II study of afatinib, an irreversible ErbB family blocker, with or without protracted temozolomide in adults with recurrent glioblastoma.
Neuro-oncology, , Volume: 17, Issue:3 | 2015 |
A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.
Investigational new drugs, , Volume: 32, Issue:6 | 2014 |
Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment.
Cancer chemotherapy and pharmacology, , Volume: 74, Issue:2 | 2014 |
A novel lead compound CM-118: antitumor activity and new insight into the molecular mechanism and combination therapy strategy in c-Met- and ALK-dependent cancers.
Cancer biology & therapy, , Jun-01, Volume: 15, Issue:6 | 2014 |
Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 73, Issue:4 | 2014 |
Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Clinical pharmacokinetics, , Volume: 52, Issue:12 | 2013 |
A Phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors.
Investigational new drugs, , Volume: 31, Issue:2 | 2013 |
Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers.
Cancer chemotherapy and pharmacology, , Volume: 69, Issue:4 | 2012 |
Interactions (22)
| Article | Year |
|---|
Afatinib in combination with GEMOX chemotherapy as the adjuvant treatment in patients with ErbB pathway mutated, resectable gallbladder cancer: study protocol for a ctDNA-based, multicentre, open-label, randomised, controlled, phase II trial.
BMJ open, , 02-28, Volume: 13, Issue:2 | 2023 |
Application of afatinib combined with np regimen in the treatment of stage iv non-small cell lung cancer and its effect on patient survival.
Pakistan journal of pharmaceutical sciences, , Volume: 35, Issue:2(Special) | 2022 |
Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer.
Investigational new drugs, , Volume: 40, Issue:2 | 2022 |
Drug combination screening as a translational approach toward an improved drug therapy for chordoma.
Cellular oncology (Dordrecht), , Volume: 44, Issue:6 | 2021 |
The efficacy of first-line tyrosine kinase inhibitors combined with co-medications in Asian patients with EGFR mutation non-small cell lung cancer.
Scientific reports, , 09-11, Volume: 10, Issue:1 | 2020 |
Identification of a Triple Drug Combination That Is Synergistically Cytotoxic for Triple-Negative Breast Cancer Cells Using a Novel Combination Discovery Approach.
SLAS discovery : advancing life sciences R & D, , Volume: 25, Issue:8 | 2020 |
Identification of synergistic drug combinations using breast cancer patient-derived xenografts.
Scientific reports, , 01-30, Volume: 10, Issue:1 | 2020 |
A Phase 1 Study of Afatinib in Combination with Postoperative Radiation Therapy with and Without Weekly Docetaxel in Intermediate- and High-Risk Patients with Resected Squamous Cell Carcinoma of the Head and Neck.
International journal of radiation oncology, biology, physics, , 09-01, Volume: 105, Issue:1 | 2019 |
Inhibitory Effects of HangAmDan-B1 (HAD-B1) Combined With Afatinib on H1975 Lung Cancer Cell-Bearing Mice.
Integrative cancer therapies, , Volume: 18 | |
Synergistic effects of various Her inhibitors in combination with IGF-1R, C-MET and Src targeting agents in breast cancer cell lines.
Scientific reports, , 06-21, Volume: 7, Issue:1 | 2017 |
In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.
Drug design, development and therapy, , Volume: 10 | 2016 |
Effects of cetuximab combined with afatinib on the expression of KDR and AQP1 in lung cancer.
Genetics and molecular research : GMR, , Dec-11, Volume: 14, Issue:4 | 2015 |
Afatinib, an Irreversible EGFR Family Inhibitor, Shows Activity Toward Pancreatic Cancer Cells, Alone and in Combination with Radiotherapy, Independent of KRAS Status.
Targeted oncology, , Volume: 11, Issue:3 | 2016 |
Phase I study of afatinib combined with nintedanib in patients with advanced solid tumours.
British journal of cancer, , Nov-17, Volume: 113, Issue:10 | 2015 |
A phase I study of volasertib combined with afatinib, in advanced solid tumors.
Cancer chemotherapy and pharmacology, , Volume: 76, Issue:4 | 2015 |
A phase I study of daily afatinib, an irreversible ErbB family blocker, in combination with weekly paclitaxel in patients with advanced solid tumours.
European journal of cancer (Oxford, England : 1990), , Volume: 51, Issue:16 | 2015 |
A Phase I dose-escalation study of afatinib combined with nintedanib in patients with advanced solid tumors.
Future oncology (London, England), , Volume: 11, Issue:10 | 2015 |
A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.
Investigational new drugs, , Volume: 32, Issue:6 | 2014 |
Pharmacokinetic drug interactions of afatinib with rifampicin and ritonavir.
Clinical drug investigation, , Volume: 34, Issue:3 | 2014 |
A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors.
Annals of oncology : official journal of the European Society for Medical Oncology, , Volume: 24, Issue:5 | 2013 |
Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.
Biochemical and biophysical research communications, , Feb-15, Volume: 431, Issue:3 | 2013 |
Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors.
Investigational new drugs, , Volume: 31, Issue:3 | 2013 |