osimertinib: an EGFR tyrosine kinase inhibitor
osimertinib : A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treatment of EGFR T790M mutation positive non-small cell lung cancer.
ID Source | ID |
---|---|
PubMed CID | 71496458 |
CHEMBL ID | 3353410 |
CHEBI ID | 90943 |
SCHEMBL ID | 14660911 |
Synonym |
---|
DUYJMQONPNNFPI-UHFFFAOYSA-N |
n-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide |
osimertinib [inn] |
azd9291 , |
1421373-65-0 |
osimertinib |
osimertinib [mi] |
3C06JJ0Z2O , |
osimertinib [usan] |
2-propenamide, n-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl)amino)phenyl)- |
mereletinib |
azd-9291 free base |
osimertinib [who-dd] |
azd-9291 |
S7297 |
HY-15772 |
CS-2018 |
gtpl7719 |
azd 9291 |
n-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide |
mereletinib (obsolete inn) |
mereletinib [inn] |
unii-3c06jj0z2o |
n-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl]amino}phenyl)acrylamide |
osimertinibum |
CHEBI:90943 , |
n-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide |
AKOS025290756 |
SCHEMBL14660911 |
n-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-(4-(1-methyl-1h-indol-3-yl)pyrimidin-2-ylamino)phenyl)acrylamide |
n-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide |
AC-29019 |
n-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide |
DB09330 |
bdbm50029668 |
CHEMBL3353410 |
EX-A314 |
mfcd27988062 |
HMS3653E10 |
NCGC00378622-10 |
osimertinib; azd-9291 |
SW219863-1 |
mereletinibazd-9291,osimertinib |
'osimertinib; azd 9291' |
4714B |
AS-16943 |
n-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide |
BCP08626 |
Q21506464 |
n-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide |
SB22952 |
HMS3672M05 |
AMY9161 |
CCG-264683 |
NCGC00378622-03 |
n(2{[2(dimethylamino)ethyl](methyl)amino}4methoxy5{[4(1methyl1hindol3yl)pyrimidin2yl]amino}phenyl)prop2enamide;osimertinib |
A854509 |
nsc-800812 |
nsc800812 |
nsc779217 |
nsc-781254 |
nsc781254 |
nsc-779217 |
NCGC00378622-04 |
osimertinib (azd9291) |
DTXSID501025961 |
n-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)prop-2-enamide |
l01xe35 |
2-propenamide, n-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-; n-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1h-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide; |
EN300-7382438 |
Osimertinib is a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor used to treat non-small cell lung cancer. It is now a standard-of-care therapy for advanced EGFR mutation-positive non-Small Cell Lung Cancer.
Osimertinib (AZD9291) has an efficacy superior to that of standard EGFR-tyrosine kinase inhibitors for the first-line treatment of patients with cancer. The drug has a favorable safety profile compared to platinum-doublet chemotherapy.
Osimertinib has been approved by the Food and Drug Administration (FDA) of the United States (US) for the treatment of progressive non-small cell lung cancer (NSCLC) that has acquired T790M mutation during treatment with first-line epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKI) The drug has shown promising activity in patients with leptomeningeal metastases (LMs) of EGFR-positive NSCLC.
Excerpt | Reference | Relevance |
---|---|---|
"Osimertinib efficacy was lower than that of other EGFR–tyrosine kinase inhibitors." | ( First-line osimertinib in EGFR mutation-positive non-small cell lung cancer patients with poor performance status. Hakozaki, T; Kato, Y; Kitagawa, S; Okuma, Y; Takamizawa, S; Zenke, Y, 2022) | 1.83 |
Osimertinib is the best treatment choice for patients with epidermal growth factor receptor (EGFR)-mutated advanced non-small-cell lung cancer (NSCLC) The disease progresses on a first- or second-generation EGFR-tyrosine kinase inhibitor due to acquired T790M mutation.
Osimertinib is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) First-line therapy has shown good clinical outcomes in non-small cell lung cancer (NSCLC) Some serious adverse events such as cardiotoxicity have also been reported.
The method was successfully applied in a pharmacokinetic study of osimertinib after oral administration. The aim was to develop a population (pop) pharmacokinetics (PK) model for the drug.
Osimertinib combined with bevacizumab is an appropriate treatment option for patients with LM from EGFRm NSCLC. In AXL-low-expressing EGFRmut-LC cell-derived xenografts, transient IGF-1R inhibition combined with continuous osimert inib treatment could eradicate tumors and prevent regrowth.
17 NLPFs by robust RSM design approach displaying improved response through sensitizing cells to Osimertinib treatment. Improved oral bioavailability of CFM 4.
Osimertinib and dacomitinib combination therapy. Open-label, non-randomized phase 1 study in Taiwan. 13 patients received DS-1205c monotherapy at a dosage of 200, 400, 800, or 1200 mg twice daily for 7 days.
Role | Description |
---|---|
antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
epidermal growth factor receptor antagonist | An antagonist at the epidermal growth factor receptor. |
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Class | Description |
---|---|
indoles | Any compound containing an indole skeleton. |
aminopyrimidine | A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives. |
biaryl | An organic aromatic compound whose structure contains two aromatic rings or ring systems, joined to each other by a single bond. |
secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
monomethoxybenzene | Compounds containing a benzene skeleton substituted with one methoxy group. |
acrylamides | An enamide which is acrylamide or a derivative of acrylamide obtained by replacement of one or more of its hydrogens. |
substituted aniline | |
secondary carboxamide | A carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1). |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Pathway | Proteins | Compounds |
---|---|---|
Disease | 1278 | 231 |
Diseases of signal transduction by growth factor receptors and second messengers | 262 | 31 |
Signaling by ERBB2 in Cancer | 16 | 10 |
Drug resistance in ERBB2 KD mutants | 4 | 6 |
Resistance of ERBB2 KD mutants to osimertinib | 3 | 1 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
PPM1D protein | Homo sapiens (human) | Potency | 8.2891 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 10.6840 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
G | Vesicular stomatitis virus | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 23.9185 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
Interferon beta | Homo sapiens (human) | Potency | 12.9261 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 2.5359 | 0.0096 | 10.5250 | 35.4813 | AID1479145; AID1479148 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 26.8370 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Bone morphogenetic protein receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.1413 | 3.7000 | AID1424922 |
Membrane-associated progesterone receptor component 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2040 | 0.2040 | 0.2040 | AID1425109 |
Serine/threonine-protein kinase PLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.5144 | 9.0000 | AID1425121 |
ATP-dependent RNA helicase DDX3X | Homo sapiens (human) | Kd | 30.0000 | 0.4350 | 0.4350 | 0.4350 | AID1424975 |
Pyridoxal kinase | Homo sapiens (human) | Kd | 30.0000 | 0.2860 | 5.0765 | 16.4040 | AID1425106 |
Citron Rho-interacting kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 3.0646 | 48.8760 | AID1424954 |
Serine/threonine-protein kinase Chk1 | Homo sapiens (human) | Kd | 30.0000 | 0.0028 | 1.4744 | 8.7000 | AID1424953 |
Aurora kinase A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.7342 | 9.3000 | AID1424917 |
Cyclin-G-associated kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 0.9086 | 28.6510 | AID1425009 |
Ephrin type-B receptor 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0768 | 9.0000 | AID1424995 |
Peroxisomal acyl-coenzyme A oxidase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.3140 | 2.6020 | AID1424896 |
Receptor-interacting serine/threonine-protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6212 | 11.4330 | AID1425155 |
Mitotic checkpoint serine/threonine-protein kinase BUB1 | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 1.3910 | 3.5070 | AID1424926 |
Dynamin-like 120 kDa protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 0.3610 | 0.7050 | AID1425097 |
Putative nucleoside diphosphate kinase | Homo sapiens (human) | Kd | 30.0000 | 0.8620 | 0.8620 | 0.8620 | AID1425092 |
Eukaryotic translation initiation factor 5B | Homo sapiens (human) | Kd | 30.0000 | 0.2320 | 0.2320 | 0.2320 | AID1424986 |
Rho-associated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7105 | 56.0660 | AID1425158 |
Serine/threonine-protein kinase ULK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.8410 | 23.2730 | AID1425208 |
Serine/threonine-protein kinase/endoribonuclease IRE1 | Homo sapiens (human) | Kd | 30.0000 | 0.0057 | 2.0095 | 12.2010 | AID1424997 |
Ribosomal protein S6 kinase alpha-5 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 1.9737 | 29.9570 | AID1425162 |
U5 small nuclear ribonucleoprotein 200 kDa helicase | Homo sapiens (human) | Kd | 30.0000 | 1.3820 | 1.3820 | 1.3820 | AID1425174 |
Ribosomal protein S6 kinase alpha-4 | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.6396 | 7.2000 | AID1425161 |
Serine/threonine-protein kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.2483 | 9.9690 | AID1425179 |
Cyclin-dependent kinase-like 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.4788 | 7.3000 | AID1424951 |
Serine/threonine-protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 2.9234 | 57.4530 | AID1425177 |
Serine/threonine-protein kinase D3 | Homo sapiens (human) | Kd | 30.0000 | 0.0089 | 2.2738 | 23.3410 | AID1425137 |
Structural maintenance of chromosomes protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.2090 | 0.6575 | 1.1060 | AID1425173 |
Mitogen-activated protein kinase kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 1.5781 | 8.0000 | AID1425050 |
Mitogen-activated protein kinase kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0082 | 2.3645 | 62.7720 | AID1425054 |
Serine/threonine-protein kinase LATS1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 1.8393 | 10.7330 | AID1425033 |
Serine/threonine-protein kinase PAK 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0027 | 2.5694 | 30.3710 | AID1425100 |
Tyrosine-protein kinase ABL1 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 1.0411 | 13.4530 | AID1424890 |
Epidermal growth factor receptor | Homo sapiens (human) | EC50 (µMol) | 1.1610 | 0.0020 | 0.9902 | 7.9300 | AID1441913; AID1441914; AID1481350; AID1481351; AID1583839; AID1583840; AID1583841; AID1583844; AID1583845; AID1583851; AID1583855; AID1583862; AID1583870; AID1807693; AID1807694; AID1807698; AID1807699; AID1807700; AID1880122; AID1880123 |
Epidermal growth factor receptor | Homo sapiens (human) | Kd | 0.1550 | 0.0001 | 1.3514 | 20.8270 | AID1424983 |
Receptor tyrosine-protein kinase erbB-2 | Homo sapiens (human) | EC50 (µMol) | 0.1220 | 0.0020 | 0.1293 | 0.6900 | AID1880133 |
High affinity nerve growth factor receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.3484 | 9.2000 | AID1425094 |
Guanine nucleotide-binding protein G(i) subunit alpha-2 | Homo sapiens (human) | Kd | 30.0000 | 0.1840 | 0.1840 | 0.1840 | AID1425011 |
ADP/ATP translocase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.4510 | 0.4510 | 0.4510 | AID1425169 |
Protein kinase C beta type | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 2.7081 | 26.3240 | AID1425130 |
Insulin receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 1.0823 | 7.9060 | AID1425026 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1174 | 24.2210 | AID1425034 |
Tyrosine-protein kinase Fyn | Homo sapiens (human) | Kd | 30.0000 | 0.0008 | 1.4238 | 8.4000 | AID1425008 |
Cyclin-dependent kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.2880 | 1.4952 | 3.0490 | AID1424937 |
Glycogen phosphorylase, liver form | Homo sapiens (human) | Kd | 30.0000 | 2.1210 | 2.1210 | 2.1210 | AID1425146 |
Tyrosine-protein kinase Fes/Fps | Homo sapiens (human) | Kd | 30.0000 | 0.0048 | 1.0986 | 7.4000 | AID1425003 |
Adenine phosphoribosyltransferase | Homo sapiens (human) | Kd | 30.0000 | 0.0290 | 0.0290 | 0.0290 | AID1424914 |
Tyrosine-protein kinase Yes | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.3708 | 17.1520 | AID1425212 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0485 | 5.7000 | AID1425037 |
Proto-oncogene tyrosine-protein kinase receptor Ret | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 0.8642 | 27.5420 | AID1425154 |
Insulin-like growth factor 1 receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9211 | 19.2170 | AID1425022 |
Signal recognition particle receptor subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 0.0080 | 0.0080 | AID1425176 |
Cytochrome c1, heme protein, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2020 | 0.2020 | 0.2020 | AID1424969 |
Tyrosine-protein kinase HCK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0343 | 15.9930 | AID1425017 |
Platelet-derived growth factor receptor beta | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.0050 | 11.1070 | AID1425104 |
Serine/threonine-protein kinase A-Raf | Homo sapiens (human) | Kd | 30.0000 | 0.0470 | 9.6832 | 33.6550 | AID1424915 |
Glycogen phosphorylase, brain form | Homo sapiens (human) | Kd | 30.0000 | 3.5690 | 3.5690 | 3.5690 | AID1425145 |
Breakpoint cluster region protein | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2196 | 17.3640 | AID1424919 |
Serine/threonine-protein kinase pim-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1393 | 19.3160 | AID1425111 |
Fibroblast growth factor receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5581 | 6.2000 | AID1425004 |
DNA topoisomerase 2-alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0640 | 0.2750 | 0.4860 | AID1425202 |
Cyclin-dependent kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0033 | 1.6050 | 8.6000 | AID1424946 |
ADP/ATP translocase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.2505 | 0.4950 | AID1425170 |
Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.5077 | 9.6000 | AID1425175 |
cAMP-dependent protein kinase type II-alpha regulatory subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0520 | 1.7535 | 3.4550 | AID1425128 |
Serine/threonine-protein kinase B-raf | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6258 | 26.0180 | AID1424924 |
Phosphorylase b kinase gamma catalytic chain, liver/testis isoform | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.0569 | 9.5000 | AID1425110 |
Ribosyldihydronicotinamide dehydrogenase [quinone] | Homo sapiens (human) | Kd | 3.6580 | 0.0040 | 6.7556 | 88.9030 | AID1425093 |
Tyrosine-protein kinase Fer | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 1.3604 | 8.8000 | AID1425002 |
Protein kinase C alpha type | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7922 | 21.3520 | AID1425129 |
cAMP-dependent protein kinase catalytic subunit alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 2.9479 | 23.2450 | AID1425123 |
General transcription and DNA repair factor IIH helicase subunit XPD | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6906 | 12.0220 | AID1424996 |
Casein kinase II subunit alpha' | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5309 | 28.8720 | AID1424968 |
Ras-related protein Rab-6A | Homo sapiens (human) | Kd | 30.0000 | 0.0330 | 0.0330 | 0.0330 | AID1425150 |
Ephrin type-A receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0041 | 1.8000 | 9.8000 | AID1424987 |
Multifunctional protein ADE2 | Homo sapiens (human) | Kd | 30.0000 | 5.4810 | 5.4810 | 5.4810 | AID1425098 |
Nucleoside diphosphate kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.1420 | 0.1420 | 0.1420 | AID1425091 |
cAMP-dependent protein kinase catalytic subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 8.5577 | 49.2780 | AID1425125 |
cAMP-dependent protein kinase catalytic subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 0.7408 | 4.1000 | AID1425124 |
Ferrochelatase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.2430 | 6.4343 | 67.9140 | AID1425001 |
Ribosomal protein S6 kinase beta-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 1.1805 | 4.8000 | AID1425164 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 1.2166 | 7.8000 | AID1425030 |
Cyclin-dependent kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.5179 | 10.4870 | AID1424944 |
Beta-adrenergic receptor kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.5791 | 22.4940 | AID1424908 |
Probable ATP-dependent RNA helicase DDX6 | Homo sapiens (human) | Kd | 30.0000 | 4.1030 | 4.1030 | 4.1030 | AID1424977 |
Mitogen-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.4300 | 5.2743 | 9.8000 | AID1425061 |
MAP/microtubule affinity-regulating kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.9689 | 58.2400 | AID1425069 |
Deoxycytidine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 1.0875 | 2.1630 | AID1424970 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.7441 | 7.3000 | AID1425056 |
Ephrin type-A receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.0752 | 8.1980 | AID1424988 |
Ephrin type-B receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 3.1536 | 53.1980 | AID1424992 |
Non-receptor tyrosine-protein kinase TYK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.5575 | 8.7000 | AID1425207 |
UMP-CMP kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1424959 |
Phosphatidylethanolamine-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1425107 |
Wee1-like protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0014 | 3.5389 | 65.1580 | AID1425210 |
Heme oxygenase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.1190 | 0.1190 | 0.1190 | AID1425018 |
DnaJ homolog subfamily A member 1 | Homo sapiens (human) | Kd | 30.0000 | 0.9620 | 0.9620 | 0.9620 | AID1424980 |
RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0006 | 1.0621 | 4.4000 | AID1424910 |
RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0021 | 1.6196 | 8.7000 | AID1424911 |
DNA replication licensing factor MCM4 | Homo sapiens (human) | Kd | 30.0000 | 0.6290 | 0.6290 | 0.6290 | AID1425072 |
Myosin-10 | Homo sapiens (human) | Kd | 30.0000 | 0.2290 | 0.4935 | 0.7580 | AID1425079 |
Dual specificity mitogen-activated protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0039 | 1.6429 | 9.6000 | AID1425039 |
Receptor-type tyrosine-protein kinase FLT3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 0.9559 | 9.9000 | AID1425006 |
Bone morphogenetic protein receptor type-1A | Homo sapiens (human) | Kd | 30.0000 | 0.0600 | 1.5010 | 7.0000 | AID1424921 |
Activin receptor type-1B | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.5110 | 15.2580 | AID1424901 |
TGF-beta receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.2785 | 9.6000 | AID1425196 |
Electron transfer flavoprotein subunit beta | Homo sapiens (human) | Kd | 30.0000 | 0.0120 | 0.0120 | 0.0120 | AID1424999 |
Tyrosine-protein kinase CSK | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 3.4578 | 39.5530 | AID1424960 |
Glycine--tRNA ligase | Homo sapiens (human) | Kd | 30.0000 | 0.0400 | 0.0400 | 0.0400 | AID1425010 |
Protein kinase C iota type | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 9.3316 | 51.0180 | AID1425133 |
Exosome RNA helicase MTR4 | Homo sapiens (human) | Kd | 30.0000 | 2.6070 | 2.6070 | 2.6070 | AID1425168 |
Tyrosine-protein kinase Tec | Homo sapiens (human) | Kd | 0.3210 | 0.0010 | 1.0095 | 8.7000 | AID1425193 |
Tyrosine-protein kinase ABL2 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1249 | 14.9240 | AID1424891 |
Tyrosine-protein kinase FRK | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.2424 | 10.8370 | AID1425007 |
G protein-coupled receptor kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 1.1890 | 1.4020 | 1.6150 | AID1425012 |
Tyrosine-protein kinase SYK | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 2.0052 | 9.2260 | AID1425188 |
26S proteasome regulatory subunit 6B | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 0.0050 | 0.0050 | AID1425141 |
Mitogen-activated protein kinase 8 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 2.0965 | 26.0590 | AID1425063 |
Mitogen-activated protein kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4596 | 8.1000 | AID1425064 |
Dual specificity mitogen-activated protein kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 2.0462 | 6.6000 | AID1425040 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.2080 | 3.6125 | 7.0170 | AID1425113 |
Casein kinase I isoform alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 2.5756 | 19.3520 | AID1424961 |
Casein kinase I isoform delta | Homo sapiens (human) | Kd | 30.0000 | 0.0150 | 2.2270 | 18.3960 | AID1424962 |
MAP kinase-activated protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.0274 | 14.7420 | AID1425065 |
Elongation factor Tu, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.4640 | 0.4640 | 0.4640 | AID1425206 |
Cysteine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 0.0120 | 0.0120 | 0.3320 | 0.6520 | AID1424932 |
Casein kinase I isoform epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.4086 | 12.4090 | AID1424963 |
Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.6890 | 1.6890 | 1.6890 | AID1424894 |
Dual specificity protein kinase CLK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.8791 | 29.8810 | AID1424955 |
Dual specificity protein kinase CLK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.1384 | 6.5000 | AID1424956 |
Dual specificity protein kinase CLK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.4499 | 9.0000 | AID1424957 |
Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 2.4754 | 22.5430 | AID1425013 |
Glycogen synthase kinase-3 beta | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.0057 | 6.1680 | AID1425014 |
Cyclin-dependent kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.6783 | 7.7000 | AID1424949 |
Cyclin-dependent kinase 9 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6166 | 9.9010 | AID1424950 |
Ras-related protein Rab-27A | Homo sapiens (human) | Kd | 30.0000 | 4.4930 | 4.4930 | 4.4930 | AID1425149 |
Interleukin-1 receptor-associated kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0061 | 1.5252 | 8.5000 | AID1425027 |
Ribosomal protein S6 kinase alpha-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0170 | 2.8896 | 37.6050 | AID1425160 |
Serine/threonine-protein kinase Nek2 | Homo sapiens (human) | Kd | 30.0000 | 0.1100 | 1.5649 | 6.5000 | AID1425086 |
Serine/threonine-protein kinase Nek3 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 5.9368 | 38.0880 | AID1425087 |
Dual specificity mitogen-activated protein kinase kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0034 | 2.3943 | 6.5000 | AID1425043 |
LIM domain kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0260 | 1.7840 | 21.0890 | AID1425035 |
LIM domain kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.9717 | 52.0560 | AID1425036 |
Mitogen-activated protein kinase 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.6354 | 5.9000 | AID1425057 |
Tyrosine--tRNA ligase, cytoplasmic | Homo sapiens (human) | Kd | 30.0000 | 3.3160 | 3.3160 | 3.3160 | AID1425211 |
5'-AMP-activated protein kinase subunit gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.4681 | 10.2120 | AID1425126 |
Ephrin type-B receptor 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0069 | 2.1713 | 6.4100 | AID1424993 |
Ephrin type-A receptor 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.2100 | 5.9000 | AID1424990 |
Ephrin type-B receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 2.1678 | 26.3990 | AID1424994 |
Ephrin type-A receptor 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 3.1525 | 43.9420 | AID1424989 |
Adenylate kinase 2, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 1.0360 | 1.0360 | 1.0360 | AID1424909 |
Adenosine kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0130 | 1.8368 | 3.4930 | AID1424907 |
Ras-related protein Rab-10 | Homo sapiens (human) | Kd | 30.0000 | 1.3480 | 1.3480 | 1.3480 | AID1425148 |
Actin-related protein 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0360 | 2.7735 | 5.5110 | AID1424899 |
Actin-related protein 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 0.0040 | 0.0040 | AID1424898 |
GTP-binding nuclear protein Ran | Homo sapiens (human) | Kd | 30.0000 | 0.7590 | 0.7590 | 0.7590 | AID1425153 |
Casein kinase I isoform gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0460 | 1.4506 | 6.6000 | AID1424965 |
Cyclin-dependent kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 3.0602 | 63.6140 | AID1424945 |
Cyclin-dependent kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.2007 | 3.3560 | AID1424948 |
Cyclin-dependent-like kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0430 | 1.3757 | 8.3000 | AID1424947 |
Cyclin-dependent kinase 16 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.5855 | 10.0000 | AID1424941 |
Cyclin-dependent kinase 17 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.8233 | 5.6000 | AID1424942 |
ATP-dependent 6-phosphofructokinase, platelet type | Homo sapiens (human) | Kd | 30.0000 | 0.9830 | 0.9830 | 0.9830 | AID1425108 |
Dual specificity mitogen-activated protein kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1386 | 8.7730 | AID1425038 |
DNA topoisomerase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.1480 | 1.2270 | 2.5970 | AID1425203 |
Protein kinase C theta type | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.6140 | 7.2000 | AID1425134 |
Activin receptor type-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 1.4853 | 16.1210 | AID1424900 |
Macrophage-stimulating protein receptor | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 2.0718 | 8.4000 | AID1425078 |
Focal adhesion kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.2255 | 13.0390 | AID1425142 |
Protein kinase C delta type | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.1261 | 9.2060 | AID1425131 |
Tyrosine-protein kinase BTK | Homo sapiens (human) | Kd | 0.5250 | 0.0006 | 1.5299 | 10.1530 | AID1424925 |
Activated CDC42 kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.7138 | 9.6000 | AID1425201 |
Epithelial discoidin domain-containing receptor 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.6314 | 71.4840 | AID1424972 |
Mitogen-activated protein kinase kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 1.4681 | 14.0430 | AID1425052 |
Serine/threonine-protein kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.7120 | 25.9020 | AID1425185 |
5'-AMP-activated protein kinase catalytic subunit alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0037 | 1.8913 | 15.3890 | AID1425122 |
Dual specificity mitogen-activated protein kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.6590 | 65.6770 | AID1425042 |
Mitogen-activated protein kinase 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0420 | 2.0073 | 9.9000 | AID1425062 |
Serine/threonine-protein kinase PAK 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0031 | 2.3045 | 6.0000 | AID1425099 |
Serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 1.8602 | 17.5260 | AID1425182 |
Mitogen-activated protein kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.5995 | 12.4730 | AID1425044 |
Integrin-linked protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0200 | 0.4603 | 1.3290 | AID1425024 |
Rho-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.7555 | 13.4620 | AID1425157 |
Non-receptor tyrosine-protein kinase TNK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.0064 | 11.2690 | AID1425200 |
Calcium/calmodulin-dependent protein kinase type II subunit gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.0209 | 7.8000 | AID1424929 |
Calcium/calmodulin-dependent protein kinase type II subunit delta | Homo sapiens (human) | Kd | 30.0000 | 0.0003 | 1.5044 | 20.3010 | AID1424928 |
Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 2.1016 | 40.2910 | AID1424981 |
Activin receptor type-2B | Homo sapiens (human) | Kd | 30.0000 | 0.0076 | 2.7328 | 9.9000 | AID1424902 |
Bone morphogenetic protein receptor type-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0190 | 2.5917 | 14.3770 | AID1424923 |
Protein-tyrosine kinase 6 | Homo sapiens (human) | Kd | 30.0000 | 0.0043 | 1.7430 | 9.0000 | AID1425144 |
cGMP-dependent protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0016 | 0.7072 | 3.8000 | AID1425138 |
Cyclin-dependent kinase 13 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.2571 | 4.5180 | AID1424940 |
Inhibitor of nuclear factor kappa-B kinase subunit epsilon | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.1093 | 8.3000 | AID1425023 |
Protein-tyrosine kinase 2-beta | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.9450 | 30.4140 | AID1425143 |
Maternal embryonic leucine zipper kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 2.2835 | 29.9330 | AID1425074 |
Structural maintenance of chromosomes protein 1A | Homo sapiens (human) | Kd | 30.0000 | 0.3650 | 0.3650 | 0.3650 | AID1425172 |
Chromodomain-helicase-DNA-binding protein 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1424952 |
Peroxisomal acyl-coenzyme A oxidase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0140 | 0.1425 | 0.2710 | AID1424895 |
Serine/threonine-protein kinase 38 | Homo sapiens (human) | Kd | 30.0000 | 0.0560 | 1.5651 | 9.4000 | AID1425183 |
Ephrin type-A receptor 7 | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.4445 | 6.5000 | AID1424991 |
Delta(24)-sterol reductase | Homo sapiens (human) | Kd | 30.0000 | 0.4320 | 0.4320 | 0.4320 | AID1424978 |
Ribosomal protein S6 kinase alpha-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0280 | 2.5286 | 22.7260 | AID1425159 |
Myosin light chain kinase, smooth muscle | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2088 | 7.9000 | AID1425081 |
Mitogen-activated protein kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.4610 | 3.7430 | AID1425058 |
Serine/threonine-protein kinase STK11 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.9949 | 5.9000 | AID1425178 |
Serine/threonine-protein kinase N1 | Homo sapiens (human) | Kd | 30.0000 | 0.0013 | 3.1729 | 49.8130 | AID1425117 |
Serine/threonine-protein kinase N2 | Homo sapiens (human) | Kd | 30.0000 | 0.0018 | 1.7527 | 9.9000 | AID1425118 |
Mitogen-activated protein kinase 14 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 0.5036 | 8.5000 | AID1425059 |
Calcium/calmodulin-dependent protein kinase type IV | Homo sapiens (human) | Kd | 30.0000 | 0.0300 | 1.9215 | 5.4600 | AID1424930 |
Mitogen-activated protein kinase kinase kinase 11 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.5639 | 17.9840 | AID1425045 |
MAP kinase-activated protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0170 | 0.0260 | AID1425066 |
Discoidin domain-containing receptor 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.9888 | 42.2800 | AID1424973 |
AP2-associated protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3707 | 13.7110 | AID1424889 |
Myosin light chain kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.6184 | 10.4240 | AID1425082 |
Putative heat shock protein HSP 90-beta 2 | Homo sapiens (human) | Kd | 30.0000 | 2.5660 | 2.5660 | 2.5660 | AID1425019 |
Serine/threonine-protein kinase MRCK alpha | Homo sapiens (human) | Kd | 30.0000 | 0.0570 | 4.5547 | 14.0200 | AID1424933 |
Serine/threonine-protein kinase MRCK gamma | Homo sapiens (human) | Kd | 30.0000 | 0.0370 | 1.9625 | 9.5000 | AID1424935 |
Acyl-CoA dehydrogenase family member 10 | Homo sapiens (human) | Kd | 30.0000 | 0.0780 | 1.6997 | 3.9570 | AID1424892 |
Serine/threonine-protein kinase N3 | Homo sapiens (human) | Kd | 30.0000 | 0.0990 | 0.7365 | 1.3740 | AID1425119 |
Serine/threonine-protein kinase ULK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0012 | 1.3350 | 9.9000 | AID1425209 |
Uncharacterized protein FLJ45252 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 1.2292 | 9.3110 | AID1425147 |
Serine/threonine-protein kinase/endoribonuclease IRE2 | Homo sapiens (human) | Kd | 30.0000 | 0.1160 | 0.7604 | 1.5000 | AID1424998 |
Serine/threonine-protein kinase MARK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 1.8425 | 11.1030 | AID1425068 |
ATP-dependent RNA helicase DHX30 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 0.0060 | 0.0060 | AID1424979 |
Serine/threonine-protein kinase TAO1 | Homo sapiens (human) | Kd | 30.0000 | 0.0004 | 2.1612 | 18.7570 | AID1425189 |
STE20-related kinase adapter protein alpha | Homo sapiens (human) | Kd | 30.0000 | 0.3160 | 1.7208 | 3.6720 | AID1425186 |
AarF domain-containing protein kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0230 | 3.1137 | 22.7470 | AID1424904 |
Mitogen-activated protein kinase kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0051 | 1.6413 | 15.4350 | AID1425053 |
MAP kinase-activated protein kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0080 | 1.1241 | 3.1180 | AID1425067 |
Eukaryotic peptide chain release factor GTP-binding subunit ERF3B | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0030 | 0.0030 | AID1425015 |
Misshapen-like kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.1425 | 8.9000 | AID1425077 |
Atypical kinase COQ8A, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0940 | 5.1673 | 65.3020 | AID1424905 |
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma | Homo sapiens (human) | Kd | 2.9730 | 0.0030 | 2.7522 | 8.8000 | AID1425115 |
Mitogen-activated protein kinase 15 | Homo sapiens (human) | Kd | 30.0000 | 0.0049 | 0.6880 | 4.5000 | AID1425060 |
Serine/threonine-protein kinase Nek9 | Homo sapiens (human) | Kd | 30.0000 | 0.0160 | 2.7428 | 19.6170 | AID1425089 |
Serine/threonine-protein kinase Nek7 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 3.6719 | 8.7000 | AID1425088 |
ATP-dependent RNA helicase DDX1 | Homo sapiens (human) | Kd | 30.0000 | 0.0860 | 0.0860 | 0.0860 | AID1424974 |
Mitogen-activated protein kinase kinase kinase kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 0.9378 | 5.5000 | AID1425051 |
Aurora kinase B | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.0614 | 22.8520 | AID1424918 |
MAP/microtubule affinity-regulating kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0054 | 1.1029 | 4.9000 | AID1425070 |
Calcium/calmodulin-dependent protein kinase type 1G | Homo sapiens (human) | Kd | 30.0000 | 0.0010 | 1.9148 | 6.8000 | AID1424927 |
Serine/threonine-protein kinase Nek1 | Homo sapiens (human) | Kd | 30.0000 | 0.1700 | 2.4294 | 8.3000 | AID1425085 |
Calcium/calmodulin-dependent protein kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.2331 | 52.8470 | AID1424931 |
EKC/KEOPS complex subunit TP53RK | Homo sapiens (human) | Kd | 30.0000 | 0.3110 | 1.9519 | 3.8400 | AID1425204 |
Dual specificity testis-specific protein kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 0.0020 | 0.0020 | AID1425195 |
Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0440 | 0.9285 | 2.9000 | AID1425116 |
Mitogen-activated protein kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0700 | 6.5647 | 50.5360 | AID1425049 |
Mitogen-activated protein kinase kinase kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.5331 | 9.9000 | AID1425047 |
Eukaryotic translation initiation factor 2-alpha kinase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0580 | 1.9224 | 4.8360 | AID1424984 |
Nucleolar GTP-binding protein 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0090 | 4.1035 | 8.1980 | AID1425016 |
Serine/threonine-protein kinase D2 | Homo sapiens (human) | Kd | 30.0000 | 0.0081 | 2.3723 | 25.0190 | AID1425136 |
NUAK family SNF1-like kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0001 | 0.6774 | 4.6000 | AID1425095 |
RNA cytidine acetyltransferase | Homo sapiens (human) | Kd | 30.0000 | 1.2400 | 1.2400 | 1.2400 | AID1425083 |
Serine/threonine-protein kinase SIK2 | Homo sapiens (human) | Kd | 30.0000 | 0.0011 | 1.8165 | 41.7950 | AID1425166 |
STE20-like serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0000 | 3.8573 | 99.2320 | AID1425171 |
Serine/threonine-protein kinase TAO3 | Homo sapiens (human) | Kd | 30.0000 | 0.0002 | 2.7131 | 14.1960 | AID1425191 |
dCTP pyrophosphatase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.5730 | 1.7403 | 3.0540 | AID1424971 |
Dual specificity protein kinase CLK4 | Homo sapiens (human) | Kd | 30.0000 | 0.0020 | 1.4122 | 8.3000 | AID1424958 |
Echinoderm microtubule-associated protein-like 4 | Homo sapiens (human) | EC50 (µMol) | 1.7480 | 0.0260 | 2.5324 | 6.2580 | AID1583842 |
Casein kinase I isoform gamma-1 | Homo sapiens (human) | Kd | 30.0000 | 0.0530 | 2.0622 | 5.7000 | AID1424964 |
Phenylalanine--tRNA ligase beta subunit | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0045 | 0.0060 | AID1425000 |
Isoleucine--tRNA ligase, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 0.0110 | 0.0110 | AID1425020 |
BMP-2-inducible protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0022 | 2.4097 | 56.0320 | AID1424920 |
Obg-like ATPase 1 | Homo sapiens (human) | Kd | 30.0000 | 0.0030 | 0.0050 | 0.0070 | AID1425096 |
Interleukin-1 receptor-associated kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0017 | 3.4719 | 34.1450 | AID1425029 |
Mitogen-activated protein kinase kinase kinase 20 | Homo sapiens (human) | Kd | 30.0000 | 0.0023 | 1.7034 | 13.6380 | AID1425213 |
Cyclin-dependent kinase 12 | Homo sapiens (human) | Kd | 30.0000 | 0.0320 | 1.8032 | 5.6350 | AID1424939 |
NADH dehydrogenase [ubiquinone] 1 alpha subcomplex subunit 13 | Homo sapiens (human) | Kd | 30.0000 | 3.9200 | 3.9200 | 3.9200 | AID1425084 |
Serine/threonine-protein kinase 26 | Homo sapiens (human) | Kd | 30.0000 | 0.0074 | 1.7380 | 8.3000 | AID1425181 |
Succinate--CoA ligase [ADP-forming] subunit beta, mitochondrial | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 0.0070 | 0.0070 | AID1425187 |
Serine/threonine-protein kinase NLK | Homo sapiens (human) | Kd | 30.0000 | 0.0060 | 1.0226 | 4.4000 | AID1425090 |
5'-AMP-activated protein kinase subunit gamma-2 | Homo sapiens (human) | Kd | 30.0000 | 0.0050 | 1.1581 | 9.1280 | AID1425127 |
Serine/threonine-protein kinase TBK1 | Homo sapiens (human) | Kd | 30.0000 | 0.0009 | 1.7674 | 49.6010 | AID1425192 |
Septin-9 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 0.2430 | 0.6350 | AID1425165 |
Ribosomal protein S6 kinase alpha-6 | Homo sapiens (human) | Kd | 30.0000 | 0.0040 | 2.4153 | 23.7620 | AID1425163 |
TRAF2 and NCK-interacting protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0047 | 1.3935 | 10.0000 | AID1425199 |
Serine/threonine-protein kinase TAO2 | Homo sapiens (human) | Kd | 30.0000 | 0.0100 | 2.0176 | 12.9420 | AID1425190 |
ALK tyrosine kinase receptor | Homo sapiens (human) | EC50 (µMol) | 1.7480 | 0.0005 | 1.9984 | 6.2580 | AID1583842 |
Serine/threonine-protein kinase ICK | Homo sapiens (human) | Kd | 30.0000 | 0.0007 | 1.4717 | 9.3000 | AID1425021 |
RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Kd | 30.0000 | 0.0025 | 1.7646 | 6.2000 | AID1424912 |
Serine/threonine-protein kinase SIK3 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.5086 | 10.3180 | AID1425167 |
Mitogen-activated protein kinase kinase kinase 2 | Homo sapiens (human) | Kd | 30.0000 | 0.0024 | 1.3298 | 6.9000 | AID1425046 |
Thyroid hormone receptor-associated protein 3 | Homo sapiens (human) | Kd | 30.0000 | 2.7460 | 2.7460 | 2.7460 | AID1425198 |
Mitogen-activated protein kinase kinase kinase kinase 5 | Homo sapiens (human) | Kd | 30.0000 | 0.0005 | 1.9494 | 50.2140 | AID1425055 |
Receptor-interacting serine/threonine-protein kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0110 | 1.4797 | 6.7000 | AID1425156 |
Serine/threonine-protein kinase MRCK beta | Homo sapiens (human) | Kd | 30.0000 | 0.0340 | 3.6252 | 50.0050 | AID1424934 |
Interleukin-1 receptor-associated kinase 3 | Homo sapiens (human) | Kd | 30.0000 | 0.0070 | 1.7137 | 25.5810 | AID1425028 |
Casein kinase I isoform gamma-3 | Homo sapiens (human) | Kd | 30.0000 | 0.0970 | 2.3978 | 8.7000 | AID1424966 |
Mitogen-activated protein kinase kinase kinase 4 | Homo sapiens (human) | Kd | 30.0000 | 0.0390 | 2.3970 | 8.4000 | AID1425048 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Epidermal growth factor receptor | Homo sapiens (human) | DC50 | 2.0000 | 0.0117 | 0.0139 | 0.0223 | AID1691144; AID1691145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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 | The target landscape of clinical kinase drugs. |
AID1848538 | Selectivity index, ratio of IC50 for N-terminal GST-tagged human recombinant wild type EGFR (695 to end residues) expressed in baculovirus-infected Sf9 cells to IC50 for N-terminal GST-tagged human recombinant EGFR T790M/L858R mutant (695 to end residues) | |||
AID1458988 | Efflux ratio of apparent permeability from basolateral side to apical side over apical side to basolateral side over in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1585323 | Toxicity in castrated nude mouse xenografted with human PC9 cells assessed as body weight loss at 10 mg/kg, po daily for 14 consecutive days relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1167104 | Lipophilicity, log D of the compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1815230 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1730481 | Intrinsic clearance in human liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1519431 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 0.462 uM after 24 hrs by propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 22.24 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1434570 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR |
AID1424954 | 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 | The target landscape of clinical kinase drugs. |
AID1483368 | Inhibition of EGFR L858R mutant (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1730490 | Drug metabolism in cynomolgus monkey liver microsomes assessed as AZ5104 metabolite levels preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1872388 | Inhibition of cell growth in human Lymphoma cell line bearing wildtype EZH2 | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
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 | The target landscape of clinical kinase drugs. |
AID1617468 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1583855 | Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay in presence of ceritinib | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1391283 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1815814 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1580126 | Inhibition of recombinant human GST-tagged EGFR L858R mutant expressed in baculovirus expression system using Tyr 04 as substrate incubated for 1 hr by Z'-LYTE assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1703392 | Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1708233 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1824071 | Induction of cell cycle arrest in human NCI-H1975 cells assessed as accumulation at G2/M phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 43.1%) | |||
AID1585919 | Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1585923 | Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1865642 | Selectivity ratio of Kinact/Ki for human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant to Kinact/Ki for human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) (unknown origin) | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1585934 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 1 uM after 72 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1771693 | Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
AID1461713 | Selectivity index, ratio of IC50 for wild type EGFR (unknown origin) to IC50 for EGFR L858R/T790M double mutant (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1484435 | Selectivity ratio of IC50 for human recombinant cytoplasmic GST-tagged EGFR (668 to 1210 residues) to IC50 for human recombinant cytoplasmic GST-tagged EGFR T790M/L858R double mutant (668 to 1210 residues) | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1740135 | Inhibition of wild type EGFR in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1616559 | Inhibition of GST-tagged human EGFR A763_Y764insFHEA mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
AID1909240 | Inhibition of EGFR 19 del/T790M/C797S mutant (unknown origin) by ELISA | |||
AID1583865 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM by Western blot analysis | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1717441 | Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay | |||
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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1730447 | Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system at 0.01 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1865380 | Inhibition of wild type EGFR expressed in human A-431 cells | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1484448 | Half life in human hepatocytes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1599834 | Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR |
AID1865639 | Inhibition of recombinant human N-terminal GST-tagged HER2 wild type (679 to 1255 residues) expressed in baculovirus infected Sf9 insect cells assessed as Kinact using AQT0794 as substrate measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1424930 | 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 | The target landscape of clinical kinase drugs. |
AID1391284 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
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 | The target landscape of clinical kinase drugs. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1730527 | Cmax in Sprague-Dawley rat assessed as AZ5104 at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1424931 | 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 | The target landscape of clinical kinase drugs. |
AID1425107 | 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 | The target landscape of clinical kinase drugs. |
AID1481371 | Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1425172 | 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 | The target landscape of clinical kinase drugs. |
AID1481437 | Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as caspase3 cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1688933 | Induction of apoptosis in human HCC827 cells assessed as late apoptotic cells at 1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 18.02%) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1458979 | Selectivity ratio of IC50 for wild type N-terminal GST-fused human EGFR cytoplasmic domain to IC50 for human recombinant GST-tagged EGFR L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1656714 | Inhibition of EGFR L858R/T790M (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1497685 | Induction of apoptosis in human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34 to 1.67%) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1740144 | Inhibition of wild type EGFR in human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1291334 | Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1708246 | Selectivity ratio of IC50 for HLF cells to IC50 for antiproliferative activity against human NCI-H1975 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1425113 | 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 | The target landscape of clinical kinase drugs. |
AID1497686 | Induction of apoptosis in human HCC827 cells harboring EGFR E746 to A750 deletion mutant assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 23.66 to 27.14%) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
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 | 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 | The Ascension of Targeted Covalent Inhibitors. |
AID1896793 | Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1425012 | 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 | The target landscape of clinical kinase drugs. |
AID1857184 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1167101 | Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1445479 | Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin incubated for 2 to 90 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1703388 | Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1740137 | Inhibition of TEL-fused EGFR L858R mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1861556 | Selectivity ratio IC50 for human NCI-H1299 cells expressing wild type EGFR to human NCI-H1975 cells expressing EGFR L858R/T790M | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1390663 | Inhibition of recombinant human full length His-tagged ABL1 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
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 | The target landscape of clinical kinase drugs. |
AID1382533 | Inhibition of wild type EGFR L858R mutant (unknown origin) using Poly (Glu, Tyr) as substrate after 40 mins by kinase-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1425094 | 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 | The target landscape of clinical kinase drugs. |
AID1709317 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1861586 | Induction of apoptosis in human NCI-H1299 cells assessed as necrotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.24 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1904338 | Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
AID1876328 | Antiviral activity against SARS-CoV-2 inoculated in african green monkey Vero E6 cells expressing ACE2 assessed as reduction of cytopathic effect measured after 72 hrs by CellTitre-Glo based plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
AID1291353 | Clearance in patient with EGFR TKI-resistant NSCLC at 20 to 240 mg, po qd | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1585930 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 0.1 uM after 48 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1756966 | Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1483366 | Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1585290 | Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1585312 | Antitumor activity against human HCC827 cells harboring EGFR exon-19 del mutant xenografted in castrated nude mouse assessed as tumor growth inhibition at 10 mg/kg, po daily for 14 consecutive days measured on day 15 relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1730446 | Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system at 0.1 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1425054 | 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 | The target landscape of clinical kinase drugs. |
AID1585931 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 0.1 uM after 72 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1599833 | Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR |
AID1167122 | Intrinsic clearance in human hepatocytes measured per 10'6 cells | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1481348 | Inhibition of Tel-fused INSR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1882661 | Inhibition of wildtype EGFR (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 | Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy. |
AID1865635 | Inhibition of recombinant human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) expressed in baculovirus infected Sf21 insect cells assessed as Kinact/Ki ratio using AQT0734 as substrate measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1771671 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay | |||
AID1730479 | Intrinsic clearance in Beagle dog liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1861574 | Induction of apoptosis in human NCI-H1975 cells assessed as early apoptotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.11 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1824058 | Induction of cell cycle arrest in human NCI-H1299 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 70.2%) | |||
AID1412320 | Selectivity ratio of IC50 for human NCI-H1975 cells to IC50 for human A549 cells | |||
AID1424945 | 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 | The target landscape of clinical kinase drugs. |
AID1709334 | AUC (0 to 8 hrs) in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1484457 | MRT in Sprague-Dawley rat at 10 mg/kg, po administered via gavage by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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 | The target landscape of clinical kinase drugs. |
AID1484455 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 10 mg/kg, po administered via gavage by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1760295 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1580131 | Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
AID1772778 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in phosphorylation of EGFR L858R/T790M mutant at 0.5 to 1 uM incubated for 48 hrs incubated by western blot analysis | |||
AID1425211 | 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 | The target landscape of clinical kinase drugs. |
AID1664417 | Cell cycle arrest in mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as accumulation at S phase at 1 uM measured after 24 hrs by flow cytometry analysis (Rvb = 52.43 %) | |||
AID1617466 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
AID1527526 | Hepatic clearance in human cryopreserved hepatocytes at 1 uM measured after 240 mins by LC-MS/MS analysis relative to hepatic blood flow | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1664399 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay | |||
AID1441914 | Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1616561 | Inhibition of GST-tagged human EGFR D770_N771insNPG mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
AID1484463 | MRT in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1481442 | Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1424986 | 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 | The target landscape of clinical kinase drugs. |
AID1772745 | Inhibition of wild type EGFR (unknown origin) measured after 60 mins by ADP-Glo kinase based luminescence assay | |||
AID1425108 | 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 | The target landscape of clinical kinase drugs. |
AID1585298 | Inhibition of recombinant human N-terminal GST-tagged EGFR (696-end residues) expressed in baculovirus expression system using Srctide as substrate by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1458989 | Metabolic stability in human plasma at 5 uM incubated for 1 hr by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1424988 | 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 | The target landscape of clinical kinase drugs. |
AID1884794 | Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1824047 | Selectivity index, ratio of IC50 for Antiproliferative activity against human A549 cells expressing wild type EGFR to IC50 for antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
AID1390636 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | |||
AID1658305 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay | 2020 | ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6 | Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines. |
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 | The target landscape of clinical kinase drugs. |
AID1580135 | Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
AID1481313 | Inhibition of Tel-fused EGFR C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1824045 | Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay | |||
AID1425061 | 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 | The target landscape of clinical kinase drugs. |
AID1425195 | 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 | The target landscape of clinical kinase drugs. |
AID1688938 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in G2 phase at 1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 8.25 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1412326 | Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as ERK1/2 phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis | |||
AID1585300 | Inhibition of EGFR T790M/L858R double mutant phosphorylation at Y1068 residue in human NCI-H1975 cells up to 10 uM after 4 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1424968 | 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 | The target landscape of clinical kinase drugs. |
AID1709322 | In vivo inhibition of EGFR T790M/L858R double mutant in nude mouse xenografted with human NCI-H1975 cells assessed as reduction in AKT phosphorylation at 5 mg, ig measured after 6 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1656712 | Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1423833 | Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay | |||
AID1583836 | Inhibition of wild type GST-tagged human EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1898664 | Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1585294 | Selectivity index, ratio of IC50 for human Calu3 cells harboring WT EGFR to IC50 for human PC9 cells harboring EGFR mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1390632 | Inhibition of recombinant human GST-tagged mTOR cytoplasmic domain (1360 to 2549 residues) expressed in baculovirus expression system at 1 uM by LanthaScreen assay relative to control | |||
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 | The target landscape of clinical kinase drugs. |
AID1445481 | Inhibition of human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin incubated for 2 to 90 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1458984 | Selectivity ratio of EC50 for human A431 cells expressing wild type EGFR to EC50 for human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1730457 | Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1730460 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells at 1 to 1000 nM incubated for 2 hrs followed by EGF stimulation and measured after 15 mins hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1389859 | Selectivity ratio of IC50 for recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system to IC50 for recombinant human GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (668 to 1210 re | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1527528 | Protein binding in mouse plasma assessed as free fraction after 3 hrs by HPLC-MS/MS-based equilibrium dialysis method | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1527541 | Antitumor activity against human PC9 cells harboring del19/T790M/C797S triple mutant xenografted in BomTac:NMRI-Foxn1nu mouse assessed as tumor growth inhibition at 25 mg/kg, po qd administered for 19 days relative to control | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1898669 | Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1425189 | 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 | The target landscape of clinical kinase drugs. |
AID1807711 | Inhibition of MAP3K9 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1884789 | Inhibition of wild type EGFR (unknown origin) by mobility shift assay | |||
AID1688932 | Induction of apoptosis in human HCC827 cells assessed as early apoptotic cells at 1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.72%) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
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 | The target landscape of clinical kinase drugs. |
AID1424899 | 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 | The target landscape of clinical kinase drugs. |
AID1824101 | Induction of apoptosis in human NCI-H1975 cells assessed as increase in viable cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 94.6%) | |||
AID1585322 | Toxicity in castrated nude mouse xenografted with human NCI-H1975 cells assessed as body weight loss at 20 mg/kg, po daily for 14 consecutive days relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1896803 | Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1709318 | Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1365584 | Inhibition of wild-type EGFR (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1583869 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR mediated ERK phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1807716 | Inhibition of PRKCA (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1807699 | Inhibition of EGF-induced phosphorylation of wild type EGFR in human A-431 cells preincubated for 2 hrs followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1772746 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
AID1676513 | Inhibition of human N-terminal GST-tagged EGFR L858R/T790M 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 20 mins by HTRF as | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1481308 | Inhibition of EGFR L858R mutant in human H3255 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1772780 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at 0.5 to 1 uM incubated for 48 hrs incubated by western blot analysis | |||
AID1412325 | Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as AKT phosphorylation up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis | |||
AID1424910 | 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 | The target landscape of clinical kinase drugs. |
AID1585928 | Antiproliferative activity against NHBE cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1861571 | Induction of apoptosis in human NCI-H1975 cells assessed as viable cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 96.2 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1481441 | Induction of apoptosis in human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1423827 | Selectivity ratio of IC50 for inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant to IC50 for inhibition of recombinant human EGFR T790M/L858R double mutant | |||
AID1497672 | Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
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 | The target landscape of clinical kinase drugs. |
AID1580125 | Inhibition of recombinant human GST-tagged EGFR T790M/L858R mutant expressed in baculovirus expression system using Tyr 04 as substrate incubated for 1 hr by Z'-LYTE assay | |||
AID1599835 | Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR |
AID1760297 | Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1484441 | Half life in dog liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1580148 | Inhibition of cell migration in human NCI-H1975 cells at 25 nM incubated for 24 hrs by phase contrast microscopy relative to control | |||
AID1656710 | Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1585932 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 1 uM after 24 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1688936 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in G2 phase at 0.1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 8.25 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1458987 | Apparent permeability across basolateral to apical side in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1708245 | Selectivity ratio of IC50 for human L02 cells to IC50 for antiproliferative activity against human NCI-H1975 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1708238 | Inhibition of recombinant human GST-tagged EGFR expressed in baculovirus expression system using tyr-04 peptide as substrate incubated for 60 mins in presence of ATP by Z'-LYTE assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1291345 | Drug metabolism in plasma of patient with EGFR TKI-resistant NSCLC assessed as AZ7550 formation at 20 to 240 mg, po qd | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1807706 | Inhibition of DYRK1A (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1708239 | Selectivity ratio of IC50 for inhibition of recombinant human GST-tagged EGFR expressed in baculovirus expression system to IC50 for inhibition of recombinant human GST-tagged EGFR T790M/L858R double mutant (668 to 1210 residues) expressed in baculovirus | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1167171 | Drug metabolism in rat plasma assessed as dealkylation of compound | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1359372 | Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1585933 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 1 uM after 48 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1519420 | Induction of apoptosis in human A549 cells assessed as late apoptotic cells at 0.462 uM after 24 hrs by AnnexinV-FITC/propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 1.74 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1445480 | Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin incubated for 2 to 90 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1391285 | Antiproliferative activity against human HCC827 cells at 1 uM after 72 hrs by MTT assay relative to control | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1909239 | Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
AID1717443 | Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay | |||
AID1412318 | Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay | |||
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 | 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 | The target landscape of clinical kinase drugs. |
AID1519442 | Inhibition of EFGR phosphorylation in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1519418 | Induction of apoptosis in human A549 cells assessed as viable cells at 0.462 uM after 24 hrs by AnnexinV-FITC/propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 94.42 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1425072 | 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 | The target landscape of clinical kinase drugs. |
AID1580139 | Selectivity index, ratio of IC50 for human HK2 cells to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
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 | The target landscape of clinical kinase drugs. |
AID1585283 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1730476 | Half life in human liver microsomes assessed as half life preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1853203 | Inhibition of EGFR L858R/T790M mutant (unknown origin) in human NCI-H1975 cells | 2022 | RSC medicinal chemistry, Dec-14, Volume: 13, Issue:12 | Advanced approaches of developing targeted covalent drugs. |
AID1425007 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1865403 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) expressed in mouse BaF3 cells assessed as down streaming of ERK phosphorylation at Thr202/Tyr204 residues | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1424979 | 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 | The target landscape of clinical kinase drugs. |
AID1583863 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM by Western blot analysis | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1167157 | Antitumor activity against human PC9 cells harboring EGFR exon 19 deletion activating 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 | 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. |
AID1896771 | Inhibition of EGFR (unknown origin) d747-752/P7535 mutant assessed as percent of control activity at 1 uM by radiometric protein kinase-reaction biology assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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 | The target landscape of clinical kinase drugs. |
AID1585929 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 0.1 uM after 24 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1298660 | Inhibition of wild-type EGFR (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1872387 | Inhibition of cell growth in human Lymphoma cell line bearing EZH2 T790M mutant | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
AID1709326 | Cmax in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
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 | The target landscape of clinical kinase drugs. |
AID1861554 | Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1865634 | Inhibition of recombinant human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) expressed in baculovirus infected Sf21 insect cells insect cells using AQT0734 as substrate measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1861582 | Induction of apoptosis in human NCI-H1299 cells assessed as early apoptotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.11 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1424894 | 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 | The target landscape of clinical kinase drugs. |
AID1896772 | Inhibition of wild type EGFR (unknown origin) preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1382539 | Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as early apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 1.34%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1445473 | Ratio of Kinact human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus to Ki for human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1848539 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1289545 | Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1658306 | Selectivity index, ratio of IC50 for human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by MTT assay to IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cel | 2020 | ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6 | Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines. |
AID1425038 | 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 | The target landscape of clinical kinase drugs. |
AID1915576 | Inhibition of EGFR T790M (unknown origin) incubated for 40 mins in presence of ATP | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1720096 | Inhibition of HDAC (unknown origin) | 2020 | Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17 | Dual-Target Inhibitors Based on HDACs: Novel Antitumor Agents for Cancer Therapy. |
AID1740138 | Inhibition of TEL-fused EGFR T790M/L858R mutant (unknown origin) transfected in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
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 | The target landscape of clinical kinase drugs. |
AID1497674 | Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1425142 | 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 | The target landscape of clinical kinase drugs. |
AID1527527 | Hepatic clearance in mouse cryopreserved hepatocytes at 1 uM measured after 240 mins by LC-MS/MS analysis relative to hepatic blood flow | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1167117 | Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1167162 | Ratio of free Cave in rat at 200 mg/kg, po as single dose at 24 hrs to IC50 for INSR (unknown origin) | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1664394 | Inhibition of wild type EGFR (unknown origin) by ELISA | |||
AID1167166 | Cardiotoxicity in anesthetized guinea pig assessed as QT prolongation at fCmax concentration | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1599557 | Inhibition of cathepsin C (unknown origin) | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12 | Identification and Optimization of Novel Cathepsin C Inhibitors Derived from EGFR Inhibitors. |
AID1865399 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant xenografted in Balb/c nude mouse assessed as in tumor growth inhibition at 20 mg/kg, po administered once daily measured after 14 days | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
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 | The target landscape of clinical kinase drugs. |
AID1412317 | Inhibition of recombinant human EGFR T790M/L858R double mutant (696 to end residues) using poly(Glu, Tyr) 4 : 1 as substrate after 1 hr by ELISA | |||
AID1519413 | Inhibition of wildtype EGFR (unknown origin) using biotin as substrate in presence of ATP by mobility shift assay based ELISA | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1861606 | Plasma protein binding in rat assessed as unbound fraction at 1 uM incubated for 4 hrs by rapid equilibrium dialysis method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1730451 | Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1730480 | Intrinsic clearance in cynomolgus monkey liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1688939 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in S phase at 1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 41.26 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1676531 | Inhibition of C-terminal His6-tagged HER2 (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 60 mins in presence of XL665-labeled streptavi | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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 | The target landscape of clinical kinase drugs. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1527520 | Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1461709 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1484437 | Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1167172 | Drug metabolism in mouse plasma assessed as dealkylation of compound | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1580132 | Selectivity index, ratio of IC50 for human NCI-H292 cells expressing EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
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 | The target landscape of clinical kinase drugs. |
AID1730450 | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system at 0.01 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1423831 | Inhibition of EGFR 19D/T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis | |||
AID1709335 | AUC (0 to infinity) in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1167108 | Thermodynamic solubility of the compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1896801 | Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1497691 | Inhibition of wild type EGFR (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
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 | The target landscape of clinical kinase drugs. |
AID1807704 | Inhibition of CHEK2 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1896773 | Inhibition of EGFR (unknown origin) Del19 mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1481311 | Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1425207 | 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 | The target landscape of clinical kinase drugs. |
AID1865643 | Selectivity ratio of Ki for human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) (unknown origin) to Ki for human N-terminal GST-tagged EGFR L858R/T790M mutant (669 to 1210 residues) (unknown origin) | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1583837 | Inhibition of GST-tagged human EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1389857 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using FAM-labelled peptide as substrate pretreated for 10 mins followed by substrate addition me | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1461706 | Solubility of the compound in PBS at pH 7.4 | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1730464 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as decrease in ERK activation at 10 nM incubated for 2 followed by compound washout and measured within 12 hrs by Western blot analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1274049 | Inhibition of EGFR T790M/deletion (746 to 750 residues) mutant (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. |
AID1861580 | Induction of apoptosis in human NCI-H1299 cells assessed as viable cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 98.05 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
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 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1425074 | 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 | The target landscape of clinical kinase drugs. |
AID1167147 | Antitumor activity against human A431 cells 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 | 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. |
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 | Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. |
AID1167161 | Inhibition of INSR (unknown origin) | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1708232 | Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1771703 | Inhibiton of wild type EGFR (unknown origin) assessed as residual enzyme activity using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme for 3 hrs at 10XIC50 followed by 100-fold dilution and measured after 30 mins by rapid dilu | |||
AID1664396 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA | |||
AID1167123 | Half life of the compound by GSH reduction assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1708243 | Cytotoxicity against HLF cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1865648 | Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1425082 | 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 | The target landscape of clinical kinase drugs. |
AID1730488 | Drug metabolism in Sprague-Dawley rat liver microsomes assessed as AZ5104 metabolite levels preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1425200 | 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 | The target landscape of clinical kinase drugs. |
AID1861579 | Induction of apoptosis in human NCI-H1299 cells assessed as viable cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 98.05 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1527532 | Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1585926 | Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1807705 | Inhibition of CSNK1G2 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1688934 | Induction of apoptosis in human HCC827 cells assessed as necrotic cells at 1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 7.12 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1861576 | Induction of apoptosis in human NCI-H1975 cells assessed as late apoptotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 1.35 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1519432 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 0.462 uM after 24 hrs by propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 3.45 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1458992 | Intrinsic clearance in mouse liver microsomes at 3 uM after 50 mins by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
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: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1497681 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
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 | The target landscape of clinical kinase drugs. |
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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1585935 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 10 uM after 24 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
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 | The Ascension of Targeted Covalent Inhibitors. |
AID1865636 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant expressed in baculovirus infected Sf21 insect cells assessed as Kinact using AQT0734 as substrate measured up to 240 mins by fluorescence | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1709331 | Oral bioavailability in rat at 5 mg/kg by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1390633 | Inhibition of EGFR L858R/T790M mutant phosphorylation in human NCI-H1975 cells after 1 hr by ELISA | |||
AID1424917 | 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 | The target landscape of clinical kinase drugs. |
AID1321092 | Inhibition of EGFR L858R/T790M mutant phosphorylation in human patient derived H1975 cells incubated for 3 hrs by ELISA method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 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 |
AID1580134 | Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
AID1813865 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Proteome-wide Identification of Off-Targets of a Potent EGFR |
AID1896798 | Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1865633 | Inhibition of recombinant human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) expressed in baculovirus infected Sf21 insect cells assessed as Kinact using AQT0734 as substrate measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1627104 | Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant phosphorylation in human NCI-H1975 cells at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | 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. |
AID1617470 | Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
AID1861577 | Induction of apoptosis in human NCI-H1975 cells assessed as necrotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 3.28 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1424966 | 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 | The target landscape of clinical kinase drugs. |
AID1585295 | Selectivity index, ratio of IC50 for human Calu3 cells harboring WT EGFR to IC50 for human HCC827 cells harboring EGFR mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1815789 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISA | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1616562 | Inhibition of GST-tagged human HER2 V777_G778insCG mutant mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
AID1412316 | Inhibition of Wild type human EGFR using poly(Glu, Tyr) 4 : 1 as substrate after 1 hr by ELISA | |||
AID1861581 | Induction of apoptosis in human NCI-H1299 cells assessed as early apoptotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.11 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1484461 | AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1519440 | Inhibition of EFGR protein expression in human HeLa cells at 0.1 to 5 uM after 24 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
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 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1709321 | In vivo inhibition of EGFR T790M/L858R double mutant in nude mouse xenografted with human NCI-H1975 cells assessed as reduction in EGFR phosphorylation at 5 mg, ig measured after 6 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1583840 | Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1730489 | Drug metabolism in Beagle dog liver microsomes assessed as AZ5104 metabolite levels preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1585284 | Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1424951 | 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 | The target landscape of clinical kinase drugs. |
AID1390648 | Inhibition of human GST-tagged TIE2 cytoplasmic domain expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1424944 | 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 | The target landscape of clinical kinase drugs. |
AID1909244 | Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | |||
AID1458976 | Inhibition of wild type N-terminal GST-fused human EGFR cytoplasmic domain expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 25 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1730455 | Selectivity ratio of IC50 for antiproliferative activity against human A-431 cells to IC50 for antiproliferative activity against human NCI-H1975 cells | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1807712 | Inhibition of MAP4K4 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1445475 | Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
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: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
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 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1291343 | Half life in mouse at 25 mg/kg, po | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1824042 | Selectivity index, ratio of IC50 Inhibition of wild type EGFR (unknown origin) to IC50 for Inhibition of EGFR T790M/C797S double mutant (unknown origin) | |||
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 | Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. |
AID1298662 | Selectivity index, ratio IC50 for wild-type EGFR (unknown origin) expressed in baculovirus expression system to IC50 for EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1458993 | Intrinsic clearance in human liver microsomes at 3 uM after 50 mins by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1390653 | Inhibition of PI3Kalpha (unknown origin) at 1 uM by fluorescent polarization assay relative to control | |||
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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
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 | The target landscape of clinical kinase drugs. |
AID1519421 | Induction of apoptosis in human A549 cells assessed as necrotic cells at 0.462 uM after 24 hrs by AnnexinV-FITC/propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 0.33 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1390657 | Inhibition of recombinant human CDK2 at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1458990 | Metabolic stability in mouse plasma at 5 uM incubated for 1 hr by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1867482 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
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 | The target landscape of clinical kinase drugs. |
AID1884795 | Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay | |||
AID1861585 | Induction of apoptosis in human NCI-H1299 cells assessed as necrotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.24 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1580133 | Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1390656 | Inhibition of recombinant human GST-tagged EPHA2 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1807710 | Inhibition of MAP2K1 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1519430 | Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 0.462 uM after 24 hrs by propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 74.31 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1424985 | 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 | The target landscape of clinical kinase drugs. |
AID1740146 | Inhibition of wild type EGFR in human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
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 | The target landscape of clinical kinase drugs. |
AID1580127 | Inhibition of recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system using Tyr 04 as substrate incubated for 1 hr by Z'-LYTE assay | |||
AID1580136 | Cytotoxicity against human HLF cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
AID1425186 | 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 | The target landscape of clinical kinase drugs. |
AID1865645 | Inhibition of EGFR L858R/T790M mutant in human H1975 cells assessed as reduction in autophosphorylation at Y1068 residue at 5 to 50 nM after 2 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1424984 | 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 | The target landscape of clinical kinase drugs. |
AID1389853 | Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1291344 | Drug metabolism in mouse assessed as AUC of AZ5104 at 25 mg/kg, po relative to parent compound | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1167116 | Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1807702 | Inhibition of BRSK1 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1425095 | 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 | The target landscape of clinical kinase drugs. |
AID1756998 | Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1709313 | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant using biotinylated TK peptide as substrate measured after 30 mins by HTRF assay | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1423825 | Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) T790M/L858R/C797S mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | |||
AID1771695 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate up to 10 uM preincubated with enzyme for 3 hrs followed by substrate and ATP addition by TR-FRET assay | |||
AID1469777 | Inhibition of EGF-stimulated wild type EGFR phosphorylation in human LoVo cells incubated for 2 hrs followed by EGF stimulation for 10 mins by ELISA | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
AID1458978 | Inhibition of recombinant human GST-tagged EGFR L858R/T790M double mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 20 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1688931 | Induction of apoptosis in human HCC827 cells assessed as viable cells at 1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 72.15 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1756965 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1824040 | Inhibition of EGFR T790M/C797S double mutant (unknown origin) using flurogenic substrate in presence of ATP by HTRF assay | |||
AID1824086 | Induction of apoptosis in human NCI-H1299 cells assessed as increase in early apoptotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 0.79%) | |||
AID1484440 | Half life in rat liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1359371 | Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay | |||
AID1824041 | Inhibition of wild type EGFR (unknown origin) using flurogenic substrate in presence of ATP by HTRF assay | |||
AID1481443 | Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1469776 | Inhibition of N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (696-end residues) expressed in baculovirus infected Sf21 insect cells | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3 | Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions. |
AID1298661 | Inhibition of EGFR T790M/L858R mutant (unknown origin) expressed in baculovirus expression system after 1 hr by ELISA | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1425093 | 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 | The target landscape of clinical kinase drugs. |
AID1527521 | Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1771700 | Inhibition of EGFR del19/T790M/C797S triple mutant (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme for 3 hrs followed by substrate and ATP addition by TR-FRET assay | |||
AID1585304 | Antitumor activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant xenografted in castrated nude mouse assessed as tumor growth inhibition at 20 mg/kg, po daily for 14 consecutive days measured on day 15 relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1709329 | Half life in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1688909 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in G1 phase at 1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 50.48 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1424937 | 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 | The target landscape of clinical kinase drugs. |
AID1481316 | Inhibition of Tel-fused EGFR T790M/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1441907 | Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1702617 | Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1484475 | Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1359369 | Inhibition of recombinant human GST-tagged EGFR T790M/L858R double mutant expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | |||
AID1425154 | 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 | The target landscape of clinical kinase drugs. |
AID1412327 | Glutathione reactivity of the compound assessed as pseudo first order reaction rate constant for GSH adduct formation at 37 degC by LC analysis | |||
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 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1461711 | Inhibition of wild-type EGFR (unknown origin) using Tyr 4 peptide as substrate in presence of ATP by Z-LYTE kinase assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1688937 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in S phase at 0.1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 41.26 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
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 | The target landscape of clinical kinase drugs. |
AID1824043 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay | |||
AID1896799 | Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1885367 | Antitumor activity against human NCI-H1975 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 25 mg/kg po qd administered via oral gavage for 14 days | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. |
AID1904310 | Protac activity at VHL/EGFR L858R mutant (unknown origin) assessed as inhibition of EGFR incubated for 40 mins in presence of ATP by Kinase Glo luminescence assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
AID1498608 | Inhibition of EGFR L858R/T790M double mutant in EGF-stimulated human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Ser-473 residue at 100 nM by Western blot method | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation. |
AID1458986 | Apparent permeability across apical to basolateral side in human Caco2 cells at 5 uM incubated for 2 hrs | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1909237 | Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
AID1434568 | Inhibition of N-terminal 6His/TEV protease cleavage site-tagged wild type human EGFR using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1459011 | Kinetic solubility in Hepes buffer at 500 uM at pH 7.4 after 90 mins | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1484436 | Antiproliferative activity against human A431 cells harboring wild-type EGFR | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1441930 | Ratio of Kinact to Ki for human N-terminal GST-tagged EGFR L858R mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1425129 | 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 | The target landscape of clinical kinase drugs. |
AID1484430 | Selectivity ratio of IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant to IC50 for human A431 cells harboring wild-type EGFR | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1867496 | Induction of apoptosis in human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as dead cells at 0.25 uM incubated for 24 hrs by annexin-V/propidium iodide staining-based flow cytometry analysis (Rvb = 0.43 %) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1807694 | Inhibition of EGF-induced phosphorylation of wild type EGFR 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: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1673934 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
AID1565416 | Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
AID1904307 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1461708 | Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1580140 | Selectivity index, ratio of IC50 for human BJ cells to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
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 | The target landscape of clinical kinase drugs. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1425128 | 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 | The target landscape of clinical kinase drugs. |
AID1585296 | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant (696-end residues) by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1424922 | 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 | The target landscape of clinical kinase drugs. |
AID1425141 | 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 | The target landscape of clinical kinase drugs. |
AID1527534 | Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1481444 | Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as PARP cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1484458 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg administered via gavage after 24 hrs by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1709323 | In vivo inhibition of EGFR T790M/L858R double mutant in nude mouse xenografted with human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 5 mg, ig measured after 6 hrs by Western blot analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1289554 | Inhibition of EGFR deletion/T790M mutant autophosphorylation in human PC9-DRH cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
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 | The target landscape of clinical kinase drugs. |
AID1167175 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1898671 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1772779 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 0.5 to 1 uM incubated for 48 hrs incubated by western blot analysis | |||
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 | The target landscape of clinical kinase drugs. |
AID1481349 | Inhibition of Tel-fused IGF1R (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1708244 | Cytotoxicity against HEK293-A cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1481319 | Inhibition of full length EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1527525 | Aqueous solubility of compound in McIlvaine buffer at 1 mg/ml at pH 6.8 by HPLC-DAD/UV analysis | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1424950 | 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 | The target landscape of clinical kinase drugs. |
AID1730551 | Elimination half life in Sprague-Dawley rat at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1898668 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
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 | The target landscape of clinical kinase drugs. |
AID1484442 | Half life in monkey liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1580130 | Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1167115 | Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1239424 | Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16 | Development of Selective Covalent Janus Kinase 3 Inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1424972 | 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 | The target landscape of clinical kinase drugs. |
AID1709328 | AUC (0 to infinity) in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1481357 | Inhibition of wild-type EGFR in human H1355 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1481318 | Inhibition of full length EGFR T790M/L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1441941 | Reversible inhibition of human N-terminal GST-tagged EGFR L858R mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate assessed as inactivation constant preincubated for 2 to 9 | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1824072 | Induction of cell cycle arrest in human NCI-H1975 cells assessed as accumulation at S phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 32.7 %) | |||
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 | The target landscape of clinical kinase drugs. |
AID1289551 | Inhibition of EGFR deletion mutant autophosphorylation in human HCC827 cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1382531 | Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1390659 | Inhibition of recombinant human full length His-tagged AKT1 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1756968 | Inhibition of recombinant human N-terminal GST-tagged EGFR T790M mutant (669 to 1210 residues) expressed in baculovirus expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET a | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1708237 | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system using tyrosine 4 peptide as substrate after 60 mins in presence of ATP FRET based Z'-LYTE assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1585297 | Inhibition of recombinant human GST-tagged EGFR L858R mutant expressed in baculovirus expression system by fluorescence assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1424927 | 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 | 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 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1445477 | Inhibition of human EGFR T790M/C797S/L858R triple mutant preincubated for 20 mins followed by [33P]ATP addition measured after 2 hrs | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1585292 | Selectivity index, ratio of IC50 for human A431 cells harboring WT EGFR to IC50 for human PC9 cells harboring EGFR mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1390658 | Inhibition of recombinant human full length His-tagged PIM1 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1289550 | Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1484453 | Tmax in Sprague-Dawley rat at 10 mg/kg, po administered via gavage by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1656713 | Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1527529 | Protein binding in human plasma assessed as free fraction after 3 hrs by HPLC-MS/MS-based equilibrium dialysis method | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1445472 | Ratio of Kinact for human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus to Ki for human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1484439 | Half life in mouse liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1865641 | Inhibition of recombinant human N-terminal GST-tagged HER2 wild type (679 to 1255 residues) expressed in baculovirus infected Sf9 insect cells assessed as Kinact/Ki ratio using AQT0794 measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1481354 | Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1274037 | Inhibition of EGFR T790M/L858R mutant (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. |
AID1909245 | Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | |||
AID1884792 | Selectivity index, ratio of IC50 for wild-type EGFR (unknown origin) to IC50 for EGFR L858R/T790M/C797S mutant (unknown origin) | |||
AID1896800 | Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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 | The target landscape of clinical kinase drugs. |
AID1730487 | Drug metabolism in CD1 mouse liver microsomes assessed as AZ5104 metabolite levels preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1424210 | Antitumor activity against human NCI-H1975 cells xenografted in STOCK-Foxn1nu/Nju nude mouse assessed as inhibition of tumor growth at 20 mg/kg/day, po qd for 14 days relative to untreated control | 2017 | European journal of medicinal chemistry, Jun-16, Volume: 133 | Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). |
AID1390638 | Inhibition of wild-type EGFR phosphorylation in human A431 cells preincubated for 1 hr followed by EGF stimulation measured after 45 mins by ELISA | |||
AID1730473 | Half life in Sprague-Dawley rat liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 20 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1585293 | Selectivity index, ratio of IC50 for human A431 cells harboring WT EGFR to IC50 for human HCC827 cells harboring EGFR mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1359368 | Inhibition of recombinant human GST-tagged wild type EGFR expressed in baculovirus expression system using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | |||
AID1425084 | 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 | The target landscape of clinical kinase drugs. |
AID1484452 | Half life in Sprague-Dawley rat at 10 mg/kg, po administered via gavage by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1824104 | Induction of apoptosis in human NCI-H1975 cells assessed as increase in necrotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 0.35%) | |||
AID1425156 | 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 | The target landscape of clinical kinase drugs. |
AID1458977 | Inhibition of human recombinant GST-tagged EGFR L858R mutant expressed in baculovirus expression system preincubated for 30 mins followed by ATP and TK-substrate addition measured after 15 mins by HTRF assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1915575 | Inhibition of EGFR wildtype (unknown origin) incubated for 40 mins in presence of ATP | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
AID1167146 | Antitumor activity against human PC9 cells harboring EGFR exon 19 deletion activating 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 | 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. |
AID1857186 | Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
AID1390662 | Inhibition of recombinant human GST-tagged JAK1 cytoplasmic domain expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1425029 | 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 | The target landscape of clinical kinase drugs. |
AID1289546 | Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
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 | The target landscape of clinical kinase drugs. |
AID1815788 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) measured by ELISA | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1688913 | Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1704924 | Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of potent small molecule PROTACs targeting mutant EGFR. |
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 | The target landscape of clinical kinase drugs. |
AID1289547 | Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR L858R/T790M double mutant in human NCI-H1975 cells | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1857185 | Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay | |||
AID1289555 | Inhibition of EGFR L858R mutant autophosphorylation in human H3255 cells after 2 hrs by sandwich ELISA | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1760296 | Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Recent progress on HDAC inhibitors with dual targeting capabilities for cancer treatment. |
AID1656709 | Antiproliferative activity against human H1975-1 harboring EGFR L858R/T790M mutant measured after 72 hrs by sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
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 | The target landscape of clinical kinase drugs. |
AID1424948 | 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 | The target landscape of clinical kinase drugs. |
AID1484431 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1709314 | Inhibition of wild-type EGFR (unknown origin) using biotinylated TK peptide as substrate measured after 30 mins by HTRF assay | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1390660 | Inhibition of recombinant human full length GST-tagged SYK expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1896775 | Inhibition of EGFR (unknown origin) L858R/T790M mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1497693 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1389854 | Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
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: 199 | Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR |
AID1824060 | Induction of cell cycle arrest in human NCI-H1299 cells assessed as accumulation at S phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 24.8%) | |||
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 | The target landscape of clinical kinase drugs. |
AID1807713 | Inhibition of MAPK3 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1484450 | Intrinsic clearance in human hepatocytes assessed per million cells | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1824044 | Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1585288 | Selectivity index, ratio of IC50 for human A431 cells harboring WT EGFR to IC50 for human NCI-H1975 cells harboring EGFR T790M/L858R double mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1885396 | Antitumor activity against mouse Ba/F3 EGFR-Del19/T790M/C797S cells implanted in NOD SCID mouse assessed as reduction in tumor volume at 25 mg/kg, po qd administered via oral gavage for 14 days | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. |
AID1423824 | Inhibition of recombinant human EGFR T790M/L858R double mutant using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | |||
AID1815816 | Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1583842 | Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
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 | The target landscape of clinical kinase drugs. |
AID1481370 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1580129 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1424975 | 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 | The target landscape of clinical kinase drugs. |
AID1481372 | Inhibition of EGFR exon 19 deletion mutant in human HCC827 cells assessed as reduction in P70S6K phosphorylation at Thr389 site at 1 uM measured after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1709341 | Drug metabolism in rat assessed as N-(4-methoxy-2-(methyl(2-(methylamino)ethyl)amino)-5-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)acrylamide formation at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1382529 | Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1481317 | Inhibition of full length EGFR exon 19 deletion mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1848537 | Inhibition of N-terminal GST-tagged human recombinant wild type EGFR (695 to end residues) expressed in baculovirus-infected Sf9 cells using poly (4:1 Glu,Tyr) peptide as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1807697 | Inhibition of EGF-induced phosphorylation of EGFR T790M/L858R double mutant in human NCI-H1975 cells preincubated for 2 hrs followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1909871 | Antiproliferative activity against mouse Ba/F3 EGFR-H773-V774ins_NPH cells measured after 72 hrs by CellTiter-Glo assay | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | Insight into Targeting Exon20 Insertion Mutations of the Epidermal Growth Factor Receptor with Wild Type-Sparing Inhibitors. |
AID1390651 | Inhibition of recombinant human GST-tagged EPHB2 cytoplasmic domain (616 to 884 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1585299 | Selectivity index, ratio of IC50 for recombinant human N-terminal GST-tagged EGFR (696-end residues) expressed in baculovirus expression system to IC50 for recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant (696-end residues) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1807709 | Inhibition of IGF1R (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1425131 | 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 | The target landscape of clinical kinase drugs. |
AID1703395 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1704926 | Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of potent small molecule PROTACs targeting mutant EGFR. |
AID1461707 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1898673 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1730452 | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1896797 | Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1481353 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1167176 | Antitumor activity against human A431 cells xenografted in SCID mouse assessed as tumor growth inhibition at 2.5 mg/kg/day, po qd for 7 days relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1730477 | Intrinsic clearance in CD1 mouse liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1390645 | Inhibition of recombinant human His-tagged KIT cytoplasmic domain (544 to 976 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1441938 | Reversible inhibition of human N-terminal GST-tagged EGFR L858R mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated for 2 to 90 mins followed by 6-fold dilution | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1580141 | Selectivity index, ratio of IC50 for human HLF cells to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
AID1717440 | Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay | |||
AID1298671 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1424983 | 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 | The target landscape of clinical kinase drugs. |
AID1167169 | Drug metabolism in rat plasma assessed as loss of indole N-methyl group | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1425133 | 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 | The target landscape of clinical kinase drugs. |
AID1815231 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) measured by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1865364 | Inhibition of EGFR L858R/T790M/C797S mutant (unkown origin) expressed in mouse BaF3 cells assessed as phosphorylation at Tyr1068 residue | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1425134 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1424959 | 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 | The target landscape of clinical kinase drugs. |
AID1730472 | Half life in CD1 mouse liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1815232 | Inhibition of wild type EGFR (unknown origin) measured by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1389856 | Inhibition of recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using FAM-labelled peptide as substrate pretreated for 10 mins followed by substrate addition measured after 1 hr by mobil | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1688910 | Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1359373 | Selectivity index, ratio of IC50 for EGFR T790M/L858R double mutant expressing human NCI-H1975 cells to IC50 for wild type EGFR expressing human A431 cells | |||
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 | The target landscape of clinical kinase drugs. |
AID1607091 | In vivo inhibition of EFGR T790M mutant in human NCI-H1975 cells xenografted in NCr nude mouse assessed as reduction of EGFR phosphorylation at Y1173 residue 2.5 mg/kg measured up to 24 hrs relative to control | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Discovery of (2 |
AID1365586 | Inhibition of EGFR L858R/T790M mutant (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1425204 | 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 | The target landscape of clinical kinase drugs. |
AID1880130 | Inhibition of EGFR phosphorylation (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 | The Ascension of Targeted Covalent Inhibitors. |
AID1585920 | Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1861583 | Induction of apoptosis in human NCI-H1299 cells assessed as late apoptotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 1.53 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1872409 | Inhibition of KDM1A (unknown origin) | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present). |
AID1815233 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1709315 | Selectivity ratio of IC50 for inhibition of wild-type EGFR (unknown origin) to IC50 for inhibition of recombinant human N-terminal GST-tagged EGFR T790M/L858R double mutant | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1688935 | Induction of cell cycle arrest in human HCC827 cells assessed as accumulation in G1 phase at 0.1 uM incubated for 32 hrs by PI staining based flow cytometry analysis (Rvb = 50.48 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1730475 | Half life in cynomolgus monkey liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1389858 | Inhibition of recombinant human GST-tagged EGFR T790M mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using FAM-labelled peptide as substrate pretreated for 10 mins followed by substrate addition measured after | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1815819 | Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1424908 | 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 | The target landscape of clinical kinase drugs. |
AID1772747 | Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
AID1425096 | 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 | The target landscape of clinical kinase drugs. |
AID1391281 | Inhibition of wild type EGFR (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1321094 | Inhibition of EGFR E746 to A750 deletion mutant phosphorylation in human patient derived HCC827 cells incubated for 3 hrs by ELISA method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 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 |
AID1896770 | Inhibition of EGFR (unknown origin) Del19 mutant assessed as percent of control activity at 1 uM by radiometric protein kinase-reaction biology assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1824070 | Induction of cell cycle arrest in human NCI-H1975 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 24.2%) | |||
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 | The target landscape of clinical kinase drugs. |
AID1519415 | Selectivity ratio of IC50 for wildtype EGFR (unknown origin) to IC50 for EGFR T790M/L858R double mutant (unknown origin) by mobility shift assay based ELISA | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1880133 | Inhibition of wild-type HER2 phosphorylation in human BT-474 cells | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 | The Ascension of Targeted Covalent Inhibitors. |
AID1167103 | Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1425183 | 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 | The target landscape of clinical kinase drugs. |
AID1865640 | Inhibition of recombinant human N-terminal GST-tagged HER2 wild type (679 to 1255 residues) expressed in baculovirus infected Sf9 insect cells using AQT0794 measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
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 | The target landscape of clinical kinase drugs. |
AID1664395 | Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISA | |||
AID1425053 | 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 | The target landscape of clinical kinase drugs. |
AID1664400 | Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay | |||
AID1390640 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay | |||
AID1441911 | Inhibition of human N-terminal GST-tagged EGFR L858R mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated with enzyme for 30 mins followed by substrate addition | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1708234 | Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1425050 | 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 | The target landscape of clinical kinase drugs. |
AID1391282 | Inhibition of EGFR L858R mutant (unknown origin) using poly (Glu, Tyr) as substrate after 40 mins by kinase-glo plus luminescence assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1441912 | Inhibition of human N-terminal GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated with enzyme for 30 mins followed by substr | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1756967 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) expressed in baculovirus expression system using peptide as substrate incubated for 2 hrs followed by substrate addition and measured after 30 mins by TR-FRET assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1481351 | Inhibition of EGFR T790M/L858R mutant (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1688927 | Induction of apoptosis in human HCC827 cells assessed as viable cells at 0.1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 76.79 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1497692 | Inhibition of EGFR L858R mutant (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1382540 | Induction of apoptosis in human HCC827 cells harboring EGFR E746-A750 deletion mutant assessed as late apoptotic cells at 3 uM after 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 27.14%) | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1390647 | Inhibition of recombinant human His-tagged PDGFRbeta cytoplasmic domain (558 to 1106 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1909243 | Inhibition of wild type EGFR (unknown origin) by ELISA | |||
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 | The target landscape of clinical kinase drugs. |
AID1824046 | Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay | |||
AID1896796 | Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1425162 | 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 | The target landscape of clinical kinase drugs. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1702616 | Inhibition of human EGFR cytoplasmic domain L858R/T790M mutant (669 to 1210 residues) expressed in baculovirus infected Sf21 cells using biotin-labeled TK substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentration and fu | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1423832 | Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay | |||
AID1585301 | Inhibition of EGFR T790M/L858R double mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1167165 | Toxicity in rat assessed as hyperglycemia at 200 mg/kg, po as single dose measured over 24 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1824039 | Inhibition of EGFR del19 (unknown origin) using flurogenic substrate in presence of ATP by HTRF assay | |||
AID1580144 | Cytotoxicity against human HK2 cells assessed as change in cell morphology at 5 and 10 uM incubated for 48 hrs by microscopic analysis | |||
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 | The target landscape of clinical kinase drugs. |
AID1872386 | Inhibition of cell growth in human multiple BC cells bearing wildtype EZH2 | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
AID1291352 | Apparent half life in patient with EGFR TKI-resistant NSCLC at 20 to 240 mg, po qd | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1441910 | Inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated with enzyme for 30 mins followed by substrate addition mea | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
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 | The target landscape of clinical kinase drugs. |
AID1861553 | Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1861575 | Induction of apoptosis in human NCI-H1975 cells assessed as late apoptotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 1.35 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
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 | The target landscape of clinical kinase drugs. |
AID1627105 | Inhibition of EGF-induced EGFR kinase domain L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in ERK phosphorylation at 1 to 1000 nM pre-incubated for 2 hrs followed by stimulation with EGF for 15 mins by Western blot method | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | 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. |
AID1882660 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7 | Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy. |
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 | The target landscape of clinical kinase drugs. |
AID1390661 | Inhibition of recombinant human full length His-tagged MEK1 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1445468 | Inhibition of human N-terminal GST-fused EGFR L858R mutant (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 15 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1730448 | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system at 1 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1815787 | Inhibition of wild type EGFR (unknown origin) measured by ELISA | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1617469 | Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
AID1167148 | Clearance in iv dosed Han Wistar rat | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1583844 | Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1481314 | Inhibition of Tel-fused EGFR L858R mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1658307 | Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay | 2020 | ACS medicinal chemistry letters, Jun-11, Volume: 11, Issue:6 | Selective Covalent Targeting of Mutated EGFR(T790M) with Chlorofluoroacetamide-Pyrimidines. |
AID1423834 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay | |||
AID1585936 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 10 uM after 48 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1425097 | 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 | The target landscape of clinical kinase drugs. |
AID1904337 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
AID1884793 | Inhibition of c-Met (unknown origin) by mobility shift assay | |||
AID1884788 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) at 300 nM by mobility shift assay | |||
AID1898667 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1412319 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay | |||
AID1441913 | Inhibition of wild-type EGFR in human A431 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1656711 | Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1484462 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv after 24 hrs by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1887652 | Antiproliferative against in mouse Ba/F3 EGFR-T790M/C797S/L858R cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Emerging Approaches to Overcome Acquired Drug Resistance Obstacles to Osimertinib in Non-Small-Cell Lung Cancer. |
AID1424987 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1441929 | Ratio of Kinact to Ki for reversible inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1425081 | 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 | The target landscape of clinical kinase drugs. |
AID1861584 | Induction of apoptosis in human NCI-H1299 cells assessed as late apoptotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 1.53 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1423830 | Inhibition of EGFR T790M/L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as reduction in EGF-induced receptor phosphorylation at 1 to 3 uM preincubated for 2 hrs followed by EGF stimulation for 15 mins by Western blot analysis | |||
AID1424981 | 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 | The target landscape of clinical kinase drugs. |
AID1865637 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant expressed in baculovirus infected Sf21 insect cells using AQT0734 as substrate measured up to 240 mins by fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1884791 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by mobility shift assay | |||
AID1298672 | Selectivity ratio, ratio IC50 for human A431 cells overexpressing wild-type EGFR to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1580138 | Selectivity index, ratio of IC50 for human LO2 cells to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
AID1709319 | Selectivity ratio of IC50 for human A-431 cells harboring wild-type EGFR to IC50 for human NCI-H1975 cells harboring EGFR L858R/T790M double mutant | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1481312 | Inhibition of Tel-fused EGFR (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1484444 | Intrinsic clearance in mouse liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1481356 | Inhibition of wild-type EGFR in human NCI-H2122 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1702620 | Antiproliferative activity against human U87MG Human EGFR vIII cells overexpressing EGFRvIII mutant assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1904339 | Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
AID1664418 | Cell cycle arrest in mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as accumulation at G2 phase at 1 uM measured after 24 hrs by flow cytometry analysis (Rvb = 7.94 %) | |||
AID1815229 | Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1390652 | Inhibition of recombinant truncated human His-tagged MET expressed in mammalian expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1412324 | Inhibition of EGFR T790M/L858R double mutant phosphorylation in human NCI-H1975 cells up to 1000 nM preincubated for 16 hrs followed by EGF stimulation measured after 30 mins by Western blot analysis | |||
AID1730478 | Intrinsic clearance in Sprague-Dawley rat liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1730453 | Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1612546 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) using substrate-biotin by ELISA-based mobility shift assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
AID1885395 | Antitumor activity against mouse Ba/F3 EGFR-T790M/C797S/L858R cells implanted in NOD SCID mouse assessed as reduction in tumor volume at 25 mg/kg, po qd administered via oral gavage for 14 days | 2022 | Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14 | Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. |
AID1321093 | Inhibition of EGFR L858R mutant phosphorylation in human patient derived H3255 cells incubated for 3 hrs by ELISA method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 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 |
AID1382534 | Inhibition of wild type EGFR L858R/T790M double mutant (unknown origin) using Poly (Glu, Tyr) as substrate after 40 mins by kinase-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1815815 | Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1390635 | Inhibition of recombinant human GST-tagged wild-type EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay | |||
AID1484460 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1740145 | Inhibition of wild type EGFR in human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
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 | 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 | 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. |
AID1691144 | Induction of EGFR degradation in human A431 cells by Western blot analysis | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design and synthesis of selective degraders of EGFR |
AID1434571 | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR |
AID1585922 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1762240 | Inhibition of EGFR (unknown origin) | 2021 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 41 | Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1167119 | Unbound fraction in human plasma | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1424918 | 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 | The target landscape of clinical kinase drugs. |
AID1425091 | 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 | The target landscape of clinical kinase drugs. |
AID1815818 | Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1730470 | Toxicity in Balb/c nude mouse xenografted with human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as change in body weight at 1.5 to 2.5 mg/kg, po QD administered via gavage for 24 days and measured twice weekly | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1717442 | Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay | |||
AID1425092 | 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 | The target landscape of clinical kinase drugs. |
AID1291335 | Inhibition of EGFR T790M/L858R double mutant phosphorylation in human H1975 cells preincubated for 2 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1580137 | Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
AID1583841 | Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1580128 | Selectivity index, ratio of IC50 for recombinant human GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus expression system to IC50 for recombinant human GST-tagged EGFR T790M/L858R expressed in baculovirus expression system | |||
AID1390646 | Inhibition of recombinant human His-tagged FGFR1 cytoplasmic domain (308 to 731 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1756964 | Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. |
AID1425169 | 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 | The target landscape of clinical kinase drugs. |
AID1390650 | Inhibition of recombinant human full length His-tagged aurora A expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
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 | Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors. |
AID1771702 | Ratio of IC50 for inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr to IC50 for inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate | |||
AID1861552 | Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1730449 | Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in baculovirus expression system at 0.1 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1412328 | Stability in fetal bovine serum assessed as pseudo first order reaction rate constant | |||
AID1425080 | 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 | The target landscape of clinical kinase drugs. |
AID1481358 | Inhibition of wild-type EGFR in human H1703 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1709337 | MRT (0 to infinity) in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1497673 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1585308 | Antitumor activity against human PC9 cells harboring EGFR exon-19 del mutant xenografted in castrated nude mouse assessed as tumor growth inhibition at 10 mg/kg, po daily for 14 consecutive days measured on day 15 relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1424934 | 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 | 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 | The target landscape of clinical kinase drugs. |
AID1527530 | Apparent permeability of compound at pH 7.4 by LC-MS based PAMPA method | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1425035 | 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 | The target landscape of clinical kinase drugs. |
AID1612548 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
AID1887631 | Antiproliferative against in mouse Ba/F3 EGFR-Del19/T790M/C797S cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Emerging Approaches to Overcome Acquired Drug Resistance Obstacles to Osimertinib in Non-Small-Cell Lung Cancer. |
AID1424947 | 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 | The target landscape of clinical kinase drugs. |
AID1585924 | Selectivity index, ratio of IC50 for human A431 cells harboring wild-type EGFR to IC50 for human NCI-H1975 cells harboring EGFR T790M/L858R double mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1425198 | 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 | The target landscape of clinical kinase drugs. |
AID1289556 | Selectivity ratio of IC50 for EGF-stimulated wild type EGFR in human A549 cells to IC50 for EGFR deletion mutant in human PC9 cells | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5 | Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants. |
AID1481359 | Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1583870 | Inhibition of EGFR in human DFCI076 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1896804 | Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1824087 | Induction of apoptosis in human NCI-H1299 cells assessed as increase in late apoptotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 4.39%) | |||
AID1807708 | Inhibition of GSK3B (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1481355 | Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1691145 | Induction of EGFR L858R/T790M mutant degradation in human NCI-H1975 cells by Western blot analysis | 2020 | European journal of medicinal chemistry, Apr-15, Volume: 192 | Design and synthesis of selective degraders of EGFR |
AID1424994 | 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 | The target landscape of clinical kinase drugs. |
AID1484451 | Intrinsic clearance in rat hepatocytes assessed per million cells | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1708242 | Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1703386 | Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1583867 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in EGFR phosphorylation at 0.1 to 1 uM in presence of ceritinib by Western blot analysis | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
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 | 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 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1664402 | Selectivity index, ratio of IC50 for human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay to IC50 for mouse BAF3 cells harboring EGFR 19D/T790M/C797S assessed as reduction in cell viability by CCK8 assay | |||
AID1291336 | Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1291346 | Drug metabolism in plasma of patient with EGFR TKI-resistant NSCLC assessed as AZ5104 formation at 20 to 240 mg, po qd | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1865404 | Inhibition of EGFR L858R/C797S mutant (unknown origin) expressed in mouse BaF3 cells assessed as down streaming of ERK phosphorylation at Thr202/Tyr204 residues | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1497679 | Inhibition of EGFR L858R mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1702613 | Inhibition of wild type N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus infected Sf21 cells at 1 uM using biotin-labeled TK substrate preincubated for 30 mins followed by substrate and ATP addition at Km | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1425034 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1484449 | Half life in rat hepatocytes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1898662 | Inhibition of human EGFR L858R/T790M/C797S mutant expressed in Sf9 insect cells in presence of ATP measured by HTRF assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1909238 | Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
AID1867481 | Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1865638 | Inhibition of recombinant human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant expressed in baculovirus infected Sf21 insect cells assessed as Kinact/Ki ratio using AQT0734 as substrate measured up to 240 mins by flu | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1390634 | Inhibition of recombinant truncated human His-tagged IGF1R expressed in mammalian expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1481440 | Induction of apoptosis in human H3255 cells harboring EGFR L858R mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1730552 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1865647 | Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1740147 | Inhibition of wild type EGFR in human A-431 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1424941 | 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 | The target landscape of clinical kinase drugs. |
AID1585286 | Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1583843 | Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1382530 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1730445 | Inhibition of wild type EGFR (unknown origin) expressed in baculovirus expression system at 1 uM using poly (Glu-Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA relative to control | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1730528 | Tmax in Sprague-Dawley rat assessed as AZ5104 at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1390654 | Inhibition of recombinant human His-tagged KDR cytoplasmic domain (789 to 1356 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1824059 | Induction of cell cycle arrest in human NCI-H1299 cells assessed as accumulation at G2/M phase at 2.5 uM after 36 hrs by PI staining based flow cytometry analysis (Rvb = 5.6%) | |||
AID1565420 | Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
AID1425079 | 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 | The target landscape of clinical kinase drugs. |
AID1771675 | Inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate incubated for 1 hr by TR-FRET assay | |||
AID1809473 | Inhibition of EGFR Exon19Del/C797S double mutant (unknown origin) by biochemical assay | 2021 | Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 | Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance. |
AID1580143 | Cytotoxicity against human LO2 cells assessed as change in cell morphology at 5 and 10 uM incubated for 48 hrs by microscopic analysis | |||
AID1688912 | Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1391278 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1580145 | Cytotoxicity against human HEK293A cells assessed as change in cell morphology at 5 and 10 uM incubated for 48 hrs by microscopic analysis | |||
AID1484434 | Inhibition of human recombinant cytoplasmic GST-tagged EGFR T790M/L858R double mutant (668 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 15 mins followed by substrate addition measured after 60 mins by FRET-based Z' | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1481438 | Induction of apoptosis in human PC9 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1896802 | Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1865365 | Inhibition of EGFR L858R/C797S mutant (unkown origin) expressed in mouse BaF3 cells assessed as phosphorylation at Tyr1068 residue | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1484438 | Half life in human liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1583845 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1167130 | Cmax in mouse at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1425187 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1167110 | Inhibition of IGF1R (unknown origin) | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1815248 | Selectivity ratio of IC50 for EGFR L858R/T790M double mutant (unknown origin) to IC50 for wildtype EGFR (unknown origin) measured by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1423835 | Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay | |||
AID1365587 | Inhibition of EGFR exon 19 deletion mutant (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21 | Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
AID1909241 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) by ELISA | |||
AID1599837 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) transfected in mouse BAF3 cells assessed as inhibition of EGF-induced EGFR phosphorylation at 1 uM by Western blot analysis relative to control | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR |
AID1617467 | Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k | 2019 | Journal of natural products, 11-22, Volume: 82, Issue:11 | Discovery of an Oleanolic Acid/Hederagenin-Nitric Oxide Donor Hybrid as an EGFR Tyrosine Kinase Inhibitor for Non-Small-Cell Lung Cancer. |
AID1481350 | Inhibition of wild-type EGFR (unknown origin) autophosphorylation at Y1068 expressed in mouse BAF3 cells after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1583851 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs in presence of ceritinib by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
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 | The target landscape of clinical kinase drugs. |
AID1484433 | Inhibition of human recombinant cytoplasmic GST-tagged EGFR L858R mutant expressed in baculovirus using TK-substrate-biotin preincubated for 15 mins followed by substrate addition measured after 60 mins by FRET-based Z'-Lyte assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1861572 | Induction of apoptosis in human NCI-H1975 cells assessed as viable cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 96.2 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1861573 | Induction of apoptosis in human NCI-H1975 cells assessed as early apoptotic cells at 0.1 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 0.11 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1497680 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1867480 | Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1709325 | Tmax in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1390649 | Inhibition of recombinant human full length untagged PKCalpha expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1824103 | Induction of apoptosis in human NCI-H1975 cells assessed as increase in late apoptotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 3.85%) | |||
AID1321095 | Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | 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 |
AID1708247 | Selectivity ratio of IC50 for HEK293-A cells to IC50 for antiproliferative activity against human NCI-H1975 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1527533 | Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1389855 | Selectivity ratio of IC50 for human A549 cells expressing wild-type EGFR/K-Ras mutant to IC50 for human NCI-H1975 cells expressing EGFR L858R/T790M double mutant | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
AID1580142 | Selectivity index, ratio of IC50 for human HEK293A cells to IC50 for human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
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 | 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. |
AID1676515 | Inhibition of human N-terminal GST-tagged EGFR (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 25 mins by HTRF assay | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. |
AID1167155 | AUC in mouse at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1481315 | Inhibition of Tel-fused EGFR L858R/C797S mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1589887 | Inhibition of probe binding to EGFR L858R mutant (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors. |
AID1688911 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1585921 | Selectivity index, ratio of IC50 for wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells to IC50 for human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1848540 | Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1730474 | Half life in Beagle dog liver microsomes preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1664416 | Cell cycle arrest in mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as accumulation at G1 phase at 1 uM measured after 24 hrs by flow cytometry analysis (Rvb = 39.62 %) | |||
AID1585937 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as cell viability at 10 uM after 72 hrs by MTT assay (Rvb = 98.3%) | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1867479 | Inhibition of EGFR L858R/T790M/C797S mutant (unknown origin) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1425042 | 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 | 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 | The target landscape of clinical kinase drugs. |
AID1708298 | Antitumor activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant xenografted in nude mouse assessed as tumor volume at 15 mg/kg, po administered once daily for 7 days (Rvb = 843 mm3) | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1703389 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1815226 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) measured at 0.1 uM by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1896774 | Inhibition of EGFR (unknown origin) L858R mutant preincubated with compound 30 mins followed ATP addition incubated for 30 mins by HTRF KinEASE TK assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
AID1484443 | Intrinsic clearance in human liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1607086 | Antitumor activity against human NCI-H1975 cells harboring EGFR T790M mutant xenografted in NCr nude mouse assessed as tumor growth inhibition at 2.5 mg/kg, po qd administered for 18 days post 10 days of implantation | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Discovery of (2 |
AID1730530 | AUC (0 to 24 hrs) in Sprague-Dawley rat assessed as AZ5104 at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1730529 | Elimination half life in Sprague-Dawley rat assessed as AZ5104 at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1484432 | Inhibition of human recombinant cytoplasmic GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 15 mins followed by substrate addition measured after 60 mins by FRET-based Z'-Lyte assay | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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 | The target landscape of clinical kinase drugs. |
AID1167120 | Unbound fraction in nude mouse plasma | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1867494 | Induction of apoptosis in human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as early apoptotic cells at 0.25 uM incubated for 24 hrs by annexin-V/propidium iodide staining-based flow cytometry analysis (Rvb = 0.3 %) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1807696 | Oral bioavailability in mouse | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1865646 | Inhibition of HER2 in human BT474 cells assessed as reduction in autophosphorylation at Y1221/1222 residue at 5 to 100 nM after 6 hrs by Western blot analysis | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1740136 | Inhibition of TEL-fused EGFR (unknown origin) transfected in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1484445 | Intrinsic clearance in rat liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
AID1709330 | MRT (0 to infinity) in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1898660 | Inhibition of human EGFR L858R/T790M double mutant expressed in Sf9 insect cells in presence of ATP measured by HTRF assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1807707 | Inhibition of FLT3 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1424995 | 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 | The target landscape of clinical kinase drugs. |
AID1708235 | Selectivity ratio of IC50 for antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR to IC50 for antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1708241 | Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1709333 | Cmax in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1772744 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) measured after 60 mins by ADP-Glo kinase based luminescence assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1688930 | Induction of apoptosis in human HCC827 cells assessed as necrotic cells at 0.1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 6.68 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1519419 | Induction of apoptosis in human A549 cells assessed as early apoptotic cells at 0.462 uM after 24 hrs by AnnexinV-FITC/propidium iodide staining based FACSCalibur flow cytometry analysis (Rvb = 3.51 %) | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
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 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
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: 182 | 1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC. |
AID1724046 | Inhibition of EGFR (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18 | Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors. |
AID1824048 | Selectivity index, ratio of IC50 for Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR to IC50 for antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant | |||
AID1425212 | 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 | The target landscape of clinical kinase drugs. |
AID1167149 | Oral bioavailability in Han Wistar rat at 5 mg/kg | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
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 | The target landscape of clinical kinase drugs. |
AID1807714 | Inhibition of MAPK8 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1688928 | Induction of apoptosis in human HCC827 cells assessed as early apoptotic cells at 0.1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 2.31 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1612550 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
AID1425157 | 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 | The target landscape of clinical kinase drugs. |
AID1481369 | Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as reduction in Akt phosphorylation at Thr308/Ser473 site at 1 uM measured after 4 hrs by Western blot analysis | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1167159 | Average free plasma concentration in rat at 200 mg/kg, po as single dose at 24 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1167167 | Toxicity in rat assessed as increase insulin level at 200 mg/kg, po as single dose measured over 24 hrs relative to control | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1730550 | Tmax in Sprague-Dawley rat at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1527519 | Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1425058 | 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 | The target landscape of clinical kinase drugs. |
AID1390641 | Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay | |||
AID1867493 | Induction of apoptosis in human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as viable cells at 0.25 uM incubated for 24 hrs by annexin-V/propidium iodide staining-based flow cytometry analysis (Rvb = 99.1 %) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1291342 | Drug metabolism in mouse assessed as AUC of AZ7550 at 25 mg/kg, po relative to parent compound | 2016 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8 | Recent progress on third generation covalent EGFR inhibitors. |
AID1688929 | Induction of apoptosis in human HCC827 cells assessed as late apoptotic cells at 0.1 uM incubated for 32 hrs by annexin V-FITC and PI staining based flow cytometry analysis (Rvb = 14.23 %) | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1519412 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1382532 | Inhibition of wild type EGFR (unknown origin) using Poly (Glu, Tyr) as substrate after 40 mins by kinase-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1461710 | Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
AID1815790 | Selectivity ratio of IC50 for wild type EGFR (unknown origin) to IC50 for EGFR L858R/T790M/C797S triple mutant (unknown origin) measured by ELISA | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1865382 | Inhibition of EGFR L858R/T790M mutant expressed in human NCI-H1975 cells | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1425020 | 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 | The target landscape of clinical kinase drugs. |
AID1664398 | Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay | |||
AID1424892 | 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 | The target landscape of clinical kinase drugs. |
AID1390664 | Inhibition of recombinant human full length His-tagged CHK1 expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1807698 | Inhibition of EGF-induced phosphorylation of wild type EGFR in human LoVo cells preincubated for 2 hrs followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1815227 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) measured at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1390655 | Inhibition of recombinant full-length human His-tagged GSK3beta expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
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 | The target landscape of clinical kinase drugs. |
AID1441942 | Reversible inhibition of human N-terminal GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate assessed as inactivation constant preincubat | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
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 | The target landscape of clinical kinase drugs. |
AID1425057 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1909242 | Inhibition of EGFR L858R/T790M mutant (unknown origin) by ELISA | |||
AID1730454 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1498610 | Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells preincubated for 2 hrs followed by compound washout measured up to 24 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation. |
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 | The target landscape of clinical kinase drugs. |
AID1425001 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1865632 | Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1498611 | Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as reduction in ERK1/2 phosphorylation preincubated for 2 hrs followed by compound washout measured after 12 hrs by Western blot method | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation. |
AID1519417 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1359370 | Selectivity ratio of IC50 for recombinant human GST-tagged wild type EGFR to IC50 for recombinant human GST-tagged EGFR T790M/L858R double mutant | |||
AID1872385 | Inhibition of cell growth in human multiple BC cells bearing EZH2 T790M mutant | 2022 | European journal of medicinal chemistry, Mar-05, Volume: 231 | Recent strategies targeting Embryonic Ectoderm Development (EED) for cancer therapy: Allosteric inhibitors, PPI inhibitors, and PROTACs. |
AID1616560 | Inhibition of GST-tagged human EGFR D770GY mutant using poly(Glu, Tyr) 4:1 substrate incubated for 120 mins by kinase-Glo plus luminescent kinase assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
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 | The target landscape of clinical kinase drugs. |
AID1771721 | Inhibition of EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of EGF-stimulated receptor phosphorylation at 1 uM incubated for 4 hrs followed by EGF stimulation for 10 mins by western blot analys | |||
AID1391277 | Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1664401 | Selectivity index, ratio of IC50 for human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay to IC50 for human NCI-H1975 cells harboring EGFR 19D/T790M assessed as reduction in cell viability by CCK8 assay | |||
AID1167109 | Inhibition of human ERG | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1484454 | Cmax in Sprague-Dawley rat at 10 mg/kg, po administered via gavage after 24 hrs by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1424925 | 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 | The target landscape of clinical kinase drugs. |
AID1848536 | Inhibition of N-terminal GST-tagged human recombinant EGFR T790M/L858R mutant (695 to end residues) expressed in baculovirus-infected Sf9 cells using poly (4:1 Glu,Tyr) peptide as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay | |||
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 | The target landscape of clinical kinase drugs. |
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: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1441931 | Ratio of Kinact to Ki for human N-terminal GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1484446 | Intrinsic clearance in dog liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
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 | The target landscape of clinical kinase drugs. |
AID1167164 | Toxicity in rat at 200 mg/kg, po as single dose measured over 24 hrs | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1583838 | Inhibition of GST-tagged human EGFR T790M/L858R double mutant cytoplasmic domain (668 to 1210 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1167102 | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1167170 | Drug metabolism in mouse plasma assessed as loss of indole N-methyl group | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1274046 | Inhibition of wild type EGFR (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2 | 4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase. |
AID1585289 | Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
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 | The target landscape of clinical kinase drugs. |
AID1425089 | 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 | The target landscape of clinical kinase drugs. |
AID1896794 | Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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: 199 | Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR |
AID1382535 | Inhibition of wild type EGFR L858R/T790M/C797S mutant (unknown origin) using Poly (Glu, Tyr) as substrate after 40 mins by kinase-Glo luminescence assay | 2018 | European journal of medicinal chemistry, Mar-25, Volume: 148 | Discovery of 2,4,6-trisubstitued pyrido[3,4-d]pyrimidine derivatives as new EGFR-TKIs. |
AID1425137 | 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 | The target landscape of clinical kinase drugs. |
AID1484459 | Half life in Sprague-Dawley rat at 1 mg/kg, iv by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1481310 | Inhibition of Tel-fused EGFR T790M mutant (unknown origin) expressed in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1585979 | Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR. |
AID1704925 | Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of potent small molecule PROTACs targeting mutant EGFR. |
AID1612547 | Selectivity ratio of IC50 for wild-type EGFR (unknown origin) to IC50 for EGFR T790M/L858R double mutant (unknown origin) | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
AID1424952 | 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 | The target landscape of clinical kinase drugs. |
AID1583862 | Inhibition of EGFR in human DFCI032 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1656715 | Inhibition of wild type EGFR (unknown origin) | 2020 | Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3 | Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones. |
AID1730456 | Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1585291 | Selectivity index, ratio of IC50 for human Calu3 cells harboring WT EGFR to IC50 for human NCI-H1975 cells harboring EGFR T790M/L858R double mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1583835 | Inhibition of GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using Poly G:T (4:1) as substrate after 30 mins by Z-LYTE assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
AID1585303 | Inhibition of WT EGFR in human A431 cells assessed as reduction in ERK phosphorylation at T202/Y204 residues up to 10 uM after 4 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1497678 | Inhibition of wild type EGFR (unknown origin) using Poly(Glu,Tyr) as substrate after 40 mins by Kinase-Glo luminescence assay | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
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 | The target landscape of clinical kinase drugs. |
AID1458991 | Fraction unbound in mouse 100% plasma at 5 uM incubated for 6 hrs by LC-MS method | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1424920 | 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 | The target landscape of clinical kinase drugs. |
AID1703387 | Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Oct-01, Volume: 203 | Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. |
AID1771720 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of EGF-stimulated receptor phosphorylation at 1 uM incubated for 4 hrs followed by EGF stimulation for 10 mins by western blot analys | |||
AID1708236 | Inhibition of recombinant human GST-tagged EGFR T790M/L858R double mutant (668 to 1210 residues) expressed in baculovirus expression system using Tyr 4 as substrate incubated for 60 mins by Z'-Lyte assay | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1425100 | 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 | The target landscape of clinical kinase drugs. |
AID1898661 | Inhibition of human EGFR L858R mutant expressed in Sf9 insect cells in presence of ATP measured by HTRF assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1807703 | Inhibition of cdk1/Cyclin B (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1730557 | Apparent oral clearance in Sprague-Dawley rat at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1815817 | Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2022 | ACS medicinal chemistry letters, Feb-10, Volume: 13, Issue:2 | Optimization of Brigatinib as New Wild-Type Sparing Inhibitors of EGFR |
AID1425173 | 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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1807695 | Selectivity ratio of EC50 for inhibition of EGF-induced phosphorylation of wild type EGFR in human NCI-H1975 cells to EC50 for inhibition of EGF-induced phosphorylation of EGFR T790M/L858R double mutant in human NCI-H1975 cells preincubated for 120 mins f | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1519411 | Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1390644 | Inhibition of recombinant human His-tagged FLT3 cytoplasmic domain (564 to 958 residues) expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1484447 | Intrinsic clearance in monkey liver microsomes | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1461712 | Inhibition of EGFR L858R/T790M mutant (unknown origin) using Tyr 4 peptide as substrate in presence of ATP by Z-LYTE kinase assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17 | Synthesis and evaluation of osimertinib derivatives as potent EGFR inhibitors. |
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 | The target landscape of clinical kinase drugs. |
AID1861555 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1607089 | Toxicity in NCr nude mouse xenografted with human NCI-H1975 cells harboring EGFR T790M mutant assessed as effect on body weight at 2.5 mg/kg, po qd administered for 18 days post 10 days of implantation | 2020 | Journal of medicinal chemistry, 05-14, Volume: 63, Issue:9 | Discovery of (2 |
AID1599832 | Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay | 2019 | ACS medicinal chemistry letters, Jun-13, Volume: 10, Issue:6 | Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFR |
AID1771725 | Cytotoxicity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay | |||
AID1688919 | Inhibition of EGFR in human HCC827 cells assessed as reduction in Akt phosphorylation incubated for 36 hrs by Western blot analysis | 2020 | European journal of medicinal chemistry, Mar-01, Volume: 189 | Discovery of potent epidermal growth factor receptor (EGFR) degraders by proteolysis targeting chimera (PROTAC). |
AID1424942 | 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 | The target landscape of clinical kinase drugs. |
AID1583839 | Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Discovery of a potent dual ALK and EGFR T790M inhibitor. |
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 | The target landscape of clinical kinase drugs. |
AID1425065 | 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 | The target landscape of clinical kinase drugs. |
AID1425136 | 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 | The target landscape of clinical kinase drugs. |
AID1483369 | Inhibition of EGFR L858R/T790M double mutant (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
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 | The target landscape of clinical kinase drugs. |
AID1884790 | Inhibition of EGFR L858R/T790M mutant (unknown origin) by mobility shift assay | |||
AID1709332 | Tmax in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1815228 | Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay | 2021 | European journal of medicinal chemistry, Dec-15, Volume: 226 | Design, synthesis and biological evaluation of aminopyrimidine derivatives bearing a 4,5,6,7-tetrahydrothieno [3,2-c]pyridine as potent EGFR inhibitors. |
AID1612549 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
AID1612545 | Inhibition of wild-type EGFR (unknown origin) using substrate-biotin by ELISA-based mobility shift assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFR |
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 | The target landscape of clinical kinase drugs. |
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 | The target landscape of clinical kinase drugs. |
AID1425115 | 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 | The target landscape of clinical kinase drugs. |
AID1585302 | Inhibition of WT EGFR phosphorylation at Y1068 residue in human A431 cells up to 10 uM after 4 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1708240 | Selectivity ratio of IC50 for HK-2 cells to IC50 for antiproliferative activity against human NCI-H1975 cells | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1904354 | Antiproliferative activity against human PC-9 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
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 | The target landscape of clinical kinase drugs. |
AID1458981 | Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
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 | The target landscape of clinical kinase drugs. |
AID1730858 | Inhibition of EGFR L858R/T790M (unknown origin) by mobility shift assay | 2021 | European journal of medicinal chemistry, Mar-05, Volume: 213 | Design, synthesis and evaluation of novel ErbB/HDAC multitargeted inhibitors with selectivity in EGFR |
AID1702619 | Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1441937 | Reversible inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated for 2 to 90 mins followed by 6-fold dilution | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1730491 | Drug metabolism in human liver microsomes assessed as AZ5104 metabolite levels preincubated for 10 mins under shaking condition followed by NADPH generating system addition and measured up to 60 mins by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1807700 | Inhibition of EGF-induced phosphorylation of wild type EGFR in human NCI-H2073 cells preincubated for 2 hrs followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1425018 | 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 | The target landscape of clinical kinase drugs. |
AID1519414 | Inhibition of EGFR T790M/L858R double mutant (unknown origin) using biotin as substrate in presence of ATP by mobility shift assay based ELISA | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design, synthesis and 3D-QSAR analysis of novel thiopyranopyrimidine derivatives as potential antitumor agents inhibiting A549 and Hela cancer cells. |
AID1861578 | Induction of apoptosis in human NCI-H1975 cells assessed as necrotic cells at 1.0 uM incubated for 48 hrs by AnnexinV-FITC/propidium iodide staining based flow cytometry analysis (Rvb = 3.28 % ) | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Discovery of highly potent and selective CRBN-recruiting EGFR |
AID1481309 | Inhibition of EGFR exon 19 deletion mutant in human PC9 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1441940 | Reversible inhibition of wild-type human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate assessed as inactivation constant preincubated for 2 to 90 m | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1898674 | Displacement of sapitinib-BODIPY tracer from C-terminal NanoLuc-fused full length wild type EGFR (unknown origin) transfected in HEK293T cells incubated for 2 hrs by NanoBRET assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
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 | The target landscape of clinical kinase drugs. |
AID1896795 | Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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 | The target landscape of clinical kinase drugs. |
AID1481360 | Growth inhibition of CHL cells after 72 hrs by CellTiter-Glo assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
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 | The target landscape of clinical kinase drugs. |
AID1585287 | Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1702614 | Inhibition of human EGFR cytoplasmic domain L858R/T790M mutant (669 to 1210 residues) expressed in baculovirus infected Sf21 cells at 1 uM using biotin-labeled TK substrate preincubated for 30 mins followed by substrate and ATP addition at Km concentratio | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1585285 | Selectivity index, ratio of GI50 for human A431 cells harboring WT EGFR to GI50 for human NCI-H1975 cells harboring EGFR T790M/L858R double mutant | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1704923 | Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Discovery of potent small molecule PROTACs targeting mutant EGFR. |
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 | The target landscape of clinical kinase drugs. |
AID1434569 | Inhibition of N-terminal 6His/TEV protease cleavage site-tagged human EGFR L858R/T790M double mutant (696 to 1022 residues) using poly (Glu,Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR |
AID1412315 | Selectivity ratio of IC50 for Wild type human EGFR to IC50 for recombinant human EGFR T790M/L858R double mutant (696 to end residues) | |||
AID1391276 | Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. |
AID1359379 | Antitumor activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells xenografted in BALB/c athymic nude mouse assessed as tumor growth inhibition at 10 mg/kg, po bid for 21 days | |||
AID1807701 | Inhibition of BRAF (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1898672 | Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1740141 | Inhibition of EGFR L858R mutant in human NCI-H3255 cells assessed as cell growth inhibition measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1458985 | Permeability of the compound at 500 uM incubated for 20 hrs by PAMPA | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1730549 | Cmax in Sprague-Dawley rat at 6 mg/kg/day, IG administered as single dose and measured up to 24 hrs by LC-MS/MS analysis | 2021 | Journal of medicinal chemistry, 01-28, Volume: 64, Issue:2 | Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer. |
AID1585324 | Toxicity in castrated nude mouse xenografted with human HCC827 cells assessed as body weight loss at 10 mg/kg, po daily for 14 consecutive days relative to control | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1824085 | Induction of apoptosis in human NCI-H1299 cells assessed as increase in viable cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 94.1%) | |||
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 | The target landscape of clinical kinase drugs. |
AID1585325 | Half life in po dosed mouse | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | Design, synthesis and evaluation of the osimertinib analogue (C-005) as potent EGFR inhibitor against NSCLC. |
AID1702618 | Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
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 | The target landscape of clinical kinase drugs. |
AID1865379 | Inhibition of wild type EGFR expressed in human NCI-H2073 cells | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1481439 | Induction of apoptosis in human HCC827 cells harboring EGFR exon 19 deletion mutant assessed as caspase-3 cleavage at 1 uM after 48 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7 | Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode. |
AID1740148 | Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2020 | European journal of medicinal chemistry, Sep-15, Volume: 202 | Design, synthesis and biological evaluation of 4-aniline quinazoline derivatives conjugated with hydrogen sulfide (H |
AID1865381 | Inhibition of EGFR L858R mutant expressed in human NCI-H3255 cells | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19 | Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib. |
AID1389852 | Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8 | Discovery of selective EGFR modulator to inhibit L858R/T790M double mutants bearing a N-9-Diphenyl-9H-purin-2-amine scaffold. |
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 | The target landscape of clinical kinase drugs. |
AID1425008 | 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 | The target landscape of clinical kinase drugs. |
AID1298670 | Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay | 2016 | Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12 | Discovery of 5-(methylthio)pyrimidine derivatives as L858R/T790M mutant selective epidermal growth factor receptor (EGFR) inhibitors. |
AID1425068 | 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 | The target landscape of clinical kinase drugs. |
AID1484456 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po administered via gavage by LC-MS/MS analysis | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. |
AID1424991 | 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 | The target landscape of clinical kinase drugs. |
AID1445474 | Ratio of Kinact N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus to Ki for human N-terminal GST-fused EGFR T790M/L858R double mutant (669 to 1210 residues) expressed in baculovirus | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1425086 | 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 | The target landscape of clinical kinase drugs. |
AID1390643 | Inhibition of human full length Src expressed in baculovirus expression system at 1 uM using tyrosine04 peptide as substrate after 60 mins in presence of ATP by Z-LYTE assay relative to control | |||
AID1425119 | 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 | The target landscape of clinical kinase drugs. |
AID1709312 | Antitumor activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 5 mg/kg, po administered once daily for 11 days relative to control | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1616563 | Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. |
AID1904311 | Protac activity at VHL/EGFR L858R/T790M mutant (unknown origin) assessed as inhibition of EGFR incubated for 40 mins in presence of ATP by Kinase Glo luminescence assay | 2022 | Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6 | Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. |
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 | The target landscape of clinical kinase drugs. |
AID1709336 | Half life in rat assessed as N-(5-(4-(1H-indol-3-yl)pyrimidin-2-ylamino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide level at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1709327 | AUC (0 to 8 hrs) in rat at 5 mg/kg, po by LC-MS analysis | 2021 | Bioorganic & medicinal chemistry, 04-15, Volume: 36 | Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity. |
AID1445469 | Inhibition of human N-terminal GST-fused EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus using TK-substrate-biotin preincubated for 30 mins followed by substrate addition measured after 25 mins by HTFR assay | 2017 | Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13 | Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site. |
AID1807715 | Inhibition of PLK2 (unknown origin) at 1 uM measured after 1 hr relative to control | 2021 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 52 | Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors. |
AID1824102 | Induction of apoptosis in human NCI-H1975 cells assessed as increase in early apoptotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 1.24%) | |||
AID1483367 | Inhibition of wild-type EGFR (unknown origin) | 2017 | Journal of medicinal chemistry, 06-08, Volume: 60, Issue:11 | Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping. |
AID1424973 | 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 | The target landscape of clinical kinase drugs. |
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 | 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 | The target landscape of clinical kinase drugs. |
AID1717446 | Inhibition of EGFR L858R/T790M/C797S (unknown origin) using Poly (Glu, Tyr) as substrate measured after 40 mins by kinase-glo assay | |||
AID1824088 | Induction of apoptosis in human NCI-H1299 cells assessed as increase in necrotic cells at 2.5 uM after 36 hrs by annexin-V-FITC/PI staining based flow cytometric analysis (Rvb = 0.75%) | |||
AID1708299 | Antitumor activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant xenografted in nude mouse assessed as tumor growth inhibition at 15 mg/kg, po administered once daily for 7 days relative to control | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR |
AID1898670 | Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1896769 | Inhibition of wild type EGFR (unknown origin) assessed as percent of control activity at 1 uM by radiometric protein kinase-reaction biology assay | 2022 | Journal of medicinal chemistry, 12-08, Volume: 65, Issue:23 | Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. |
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 | The target landscape of clinical kinase drugs. |
AID1585925 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry, 12-15, Volume: 26, Issue:23-24 | The synthesis of 4-arylamido-2-arylaminoprimidines as potent EGFR T790M/L858R inhibitors for NSCLC. |
AID1771676 | Inhibition of wild type EGFR (unknown origin) using fluoresceine-labelled poly-GT peptide as substrate preincubated with enzyme for 3 hrs followed by substrate and ATP addition by TR-FRET assay | |||
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 | The target landscape of clinical kinase drugs. |
AID1167154 | Fraction unbound in Han Wistar rat plasma | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1425069 | 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 | The target landscape of clinical kinase drugs. |
AID1880129 | Inhibition of EGFR L858R/T790M mutant phosphorylation (unknown origin) | 2022 | Journal of medicinal chemistry, 04-28, Volume: 65, Issue:8 | The Ascension of Targeted Covalent Inhibitors. |
AID1898665 | Inhibition of wild type human EGFR expressed in Sf9 insect cells in presence of ATP measured by HTRF assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. |
AID1867495 | Induction of apoptosis in human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as late apoptotic cells at 0.25 uM incubated for 24 hrs by annexin-V/propidium iodide staining-based flow cytometry analysis (Rvb = 0.14 %) | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Discovery and structural optimization of potent epidermal growth factor receptor (EGFR) inhibitors against L858R/T790M/C797S resistance mutation for lung cancer treatment. |
AID1527522 | Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay | 2019 | Journal of medicinal chemistry, 11-27, Volume: 62, Issue:22 | Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors. |
AID1167121 | Intrinsic clearance in rat hepatocytes measured per 10'6 cells | 2014 | Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20 | 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. |
AID1458983 | Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 09-28, Volume: 60, Issue:18 | Structure-Guided Development of Covalent and Mutant-Selective Pyrazolopyrimidines to Target T790M Drug Resistance in Epidermal Growth Factor Receptor. |
AID1702615 | Inhibition of wild type N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus infected Sf21 cells using biotin-labeled TK substrate preincubated for 30 mins followed by substrate and ATP addition at Km concent | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance. |
AID1441939 | Reversible inhibition of human N-terminal GST-tagged EGFR L858R/T790M double mutant cytoplasmic domain (669 to 1210 end amino acid residues) expressed in baculovirus expression system using TK peptide substrate preincubated for 2 to 90 mins followed by 6- | 2017 | Journal of medicinal chemistry, 03-23, Volume: 60, Issue:6 | Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor. |
AID1498607 | Inhibition of EGFR L858R/T790M double mutant phosphorylation in EGF-stimulated human NCI-H1975 cells at 1 to 100 nM by Western blot method | 2018 | Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13 | Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation. |
AID1865644 | Selectivity ratio of Kinact for human N-terminal GST-tagged EGFR (669 to 1210 residues) (unknown origin) L858R/T790M mutant to Kinact for human N-terminal GST-tagged EGFR wild type (669 to 1210 residues) (unknown origin) | 2022 | ACS medicinal chemistry letters, Dec-08, Volume: 13, Issue:12 | Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). |
AID1497694 | Inhibition of EGFR L858R/T790M/C797S triple mutant (unknown origin) | 2018 | Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12 | Synthesis and biological evaluation of irreversible EGFR tyrosine kinase inhibitors containing pyrido[3,4-d]pyrimidine scaffold. |
AID1804171 | DRC analysis by immunofluorescence from Article 10.1128/AAC.00819-20: \\Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs.\\ | 2020 | Antimicrobial agents and chemotherapy, 06-23, Volume: 64, Issue:7 | Identification of Antiviral Drug Candidates against SARS-CoV-2 from FDA-Approved Drugs. |
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 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
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 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1345502 | Human epidermal growth factor receptor (Type I RTKs: ErbB (epidermal growth factor) receptor family) | 2016 | Journal of hematology & oncology, Apr-12, Volume: 9 | Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 465 (35.88) | 24.3611 |
2020's | 831 (64.12) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (88.27) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 134 (10.19%) | 5.53% |
Reviews | 140 (10.65%) | 6.00% |
Case Studies | 273 (20.76%) | 4.05% |
Observational | 22 (1.67%) | 0.25% |
Other | 746 (56.73%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |