Crizotinib: A piperidine and aminopyridine derivative that acts as an inhibitor of RECEPTOR PROTEIN-TYROSINE KINASES, including ANAPLASTIC LYMPHOMA KINASE (ALK) and HEPATOCYTE GROWTH FACTOR RECEPTOR (HGFR; c-Met). It is used in the treatment of NON-SMALL CELL LUNG CANCER. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
crizotinib : A 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine that has R configuration at the chiral centre. The active enantiomer, it acts as a kinase inhibitor and is used for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) [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]
| ID Source | ID |
|---|---|
| PubMed CID | 11626560 |
| CHEMBL ID | 601719 |
| CHEBI ID | 64310 |
| SCHEMBL ID | 93829 |
| MeSH ID | M0553416 |
| Synonym |
|---|
| HY-50878 |
| BB 0261738 |
| VGH , |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)pyridin-2-amine |
| 877399-52-5 |
| chebi:64310 , |
| pf-02341066 |
| CHEMBL601719 , |
| nsc-756645 |
| crizotinib |
| pf-2341066 |
| bdbm50306682 |
| 3-(2,6-dichloro-3-fluorobenzyloxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine |
| (r)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine |
| xalkori |
| (r)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)-pyridin-2-ylamine |
| nsc-749005 |
| nsc749005 |
| pf2341066 |
| crizotinib (jan/usan/inn) |
| D09731 |
| xalkori (tn) |
| pf 02341066 |
| nsc 756645 |
| 53ah36668s , |
| 2-pyridinamine, 3-((1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(4-piperidinyl)-1h-pyrazol-4-yl)- |
| crizotinib [usan:inn] |
| unii-53ah36668s |
| AKOS015995207 |
| (r)-crizotinib |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1h-pyrazol-4-yl]pyridin-2-amine |
| pf 2341066 |
| crizotinibum |
| BCPP000116 |
| pf-2341066,crizotinib |
| NCGC00250400-01 |
| crizotinib [mi] |
| crizotinib [who-dd] |
| crizotinib [jan] |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine |
| crizotinib [vandf] |
| crizotinib [orange book] |
| crizotinib [inn] |
| crizotinib [usan] |
| crizotinib [mart.] |
| AKOS015901233 |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1h-pyrazol-4-yl]-2-pyridinamine |
| gtpl4903 |
| BRD-K78431006-001-01-1 |
| SCHEMBL93829 |
| (r)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-am ine |
| KTEIFNKAUNYNJU-GFCCVEGCSA-N |
| 3-[(r)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1h-pyrazol-4-yl)-pyridin-2-ylamine |
| crizotinib (pf-02341066) |
| DB08865 |
| J-510370 |
| mfcd12407409 |
| EX-A096 |
| GS-6178 |
| crizotinib, >=98% (hplc) |
| crizotinib (pf-2341066) |
| NCGC00250400-12 |
| NCGC00250400-09 |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1h-pyra zol-4-yl]-2-pyridinamine |
| 3-[(1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1h-pyrazol-4-yl]pyridin-2-amine |
| SW202555-3 |
| Q5186964 |
| 877399-52-5 (free base) |
| 877399-52-5, 877399-53-6 (acetate) |
| AMY10313 |
| BRD-K78431006-001-03-7 |
| CCG-264803 |
| DTXSID701009329 , |
| nsc800080 |
| nsc-749769 |
| nsc749769 |
| nsc-800080 |
| NCGC00250400-02 |
| crizotinib- bio-x |
| BC164334 |
| l01xe16 |
| dtxcid601436157 |
| crizotinib (mart.) |
| 3-((1r)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1h-pyrazol-4-yl)pyridin-2-amine |
| met tyrosine kinase inhibitor pf-02341066 |
| Z2065417924 |
Crizotinib is a small molecule inhibitor that targets mesenchymal epithelial transition factor (c-MET) It has been successfully studied for its anti-cancer effects in non-small cell lung cancer, pancreatic, gastric, renal, prostate, and breast carcinomas.
Crizotinib (CRIZO) has been widely employed to treat non-small-cell lung cancer. It has been approved for patients with advanced lung adenocarcinoma harboring rearrangements of c-ROS-1 and anaplastic lymphoma kinase (ALK) genes.
Crizotinib could inhibit the proliferation of OS cells with an increase in the apoptosis levels and causing G0/G1 arrest by targeting MTH1 and activating ROS. It was found to increase the survival rate of mice infected with bacteria and decrease pulmonary inflammation activity in an animal model.
Crizotinib-treated DCs showed reduced activation markers, such as CD83, decreased chemokine-guided migration, lower antigen uptake and produced inferior levels of pro-inflammatory cytokines, especially Interleukin-12.
Crizotinib is generally well tolerated and the most frequent adverse events include gastrointestinal effects, visual disorders, edema, fatigue and liver enzyme abnormalities. The 3 drugs clinically associated with severe cardiac adverse events (crizotinIB, sunitinib, nilotinib) all proved to be cardiotoxic in our in vitro tests.
This case report describes a pharmacokinetic drug-drug interaction between crizotinib, a tyrosine kinase inhibitor, and sofosbuvir/velpatasvir, a dir.
The HSP90 inhibitor, onalespib, was combined with either crizotinib or erlotinib in ALK- or EGFR-activated xenograft models. The main objectives of the present study were to develop and refine a physiologically based pharmacokinetic (PBPK) model.
Crizotinib (PF-2341066) is a small, orally bioavailable molecule that inhibits growth of tumors with ALK activity as shown in a subgroup of non-small lung cancer patients with EML4-ALK expression. The oral absolute bioavailability of crizotinIB in rats was 68.
High-dose pulsatile therapy may be an effective dosing strategy for crizotinib in NSCLC showing progression to metastasis in the brain. Rabbits dosed intravenously (IV) with crizotineib or nilotinib showed QTc prolongation.
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| biomarker | A substance used as an indicator of a biological state. |
| EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | An EC 2.7.10.* (protein-tyrosine kinase) inhibitor that interferes with the action of receptor protein-tyrosine kinase (EC 2.7.10.1). |
| [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 |
|---|---|
| 3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine | A pyrazolylpiperidine that consists of 4-(pyrazol-1-yl)piperidine carrying a 2-amino-3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]pyridin-5-yl group at the 4-position of the pyrazole ring. |
| [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] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Fumarate hydratase | Homo sapiens (human) | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| PPM1D protein | Homo sapiens (human) | Potency | 14.7403 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 0.9776 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 11.5277 | 0.0013 | 10.1577 | 42.8575 | AID1259252; AID1259253; AID1259255; AID1259256 |
| G | Vesicular stomatitis virus | Potency | 4.6285 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 17.3839 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| polyprotein | Zika virus | Potency | 37.2212 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 0.6884 | 0.0000 | 5.0182 | 79.2586 | AID686947 |
| Interferon beta | Homo sapiens (human) | Potency | 10.6956 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 4.6285 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 4.6285 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 4.6285 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| AID384130 | Cytotoxicity against human SNU182 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383618 | Cytotoxicity against human Calu1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351350 | Antiproliferative activity against IL3-stimulated mouse BAF3 cells after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID1679436 | Inhibition of human SLK using Histone H3 as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1625294 | Inhibition of E13;A20 EML4-ALK variant (unknown origin) expressed in human NCI-H3122 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID383936 | Cytotoxicity against human SK-HEP-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556680 | Inhibition of ALK F1174L mutant (unknown origin) at 1 uM | |||
| AID383385 | Cytotoxicity against human 1205Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1580401 | Anti-neprotic activity in human Jurkat cells FADD defient assessed as reduction in TNFalpha-induced necroptosis preincubated for 30 mins followed by addition of TNFalpha-stimulation and further incubated for over night by Cell Titer Glo assay | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID1610128 | Inhibition of recombinant human N-terminal GST-tagged ALK G1202R mutant (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated with enzyme and substrate for 5 mins followed by ATP addition followed by furth | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID624960 | Binding constant for RSK2(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679447 | Inhibition of human LYN using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1190093 | Antiproliferative activity against human EBC1 cells after 72 hrs | 2015 | Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3 | Discovery and SAR study of c-Met kinase inhibitors bearing an 3-amino-benzo[d]isoxazole or 3-aminoindazole scaffold. |
| AID1137602 | Induction of apoptosis in human NCI-H1993 cells at 1 uM after 24 hrs using propidium iodide by flow cytometry | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1891328 | Inhibition of ALK L1196M mutant (unknown origin) using biotinylated substrate incubated for 1 hr in the presence of ATP at Km concentration by HTRF assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617232 | Inhibition of c-MET | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384888 | Cytotoxicity against human KYSE410 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1070242 | Cytotoxicity against mouse BAF3 cells assessed as growth inhibition after 72 hrs by [3H]-thymidine incorporation assay | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID384379 | Cytotoxicity against human OUMS23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383630 | Cytotoxicity against human CL40 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1544446 | Inhibition of JAK2 V617F mutant in HEL cells assessed as increase in JAK2 autophosphorylation at Y1007/Y1008 residues after 2.5 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID1610126 | Inhibition of recombinant human N-terminal GST-tagged ALK (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated with enzyme and substrate for 5 mins followed by ATP addition followed by further incubation | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID383931 | Cytotoxicity against human SISO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383917 | Cytotoxicity against human HeLaS3(sc) cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID384174 | Cytotoxicity against human UACC812 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624758 | Binding constant for RIPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425151 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1325439 | Antitumor activity against human KARPAS299 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po qd administered for 14 days measured twice per week during compound dosing relative to vehicle-treated control | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556683 | Inhibition of ALK R1275Q mutant (unknown origin) at 1 uM | |||
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178231 | Inhibition of ALK L1196M mutant (unknown origin) after 60 mins by ELISA | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID383910 | Cytotoxicity against human HCT116 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556663 | Antiproliferative activity against ROS1-addicted human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
| AID1678052 | Cytotoxicity against EGFR-positive human H1975 cells incubated for 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| 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. |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1070238 | Competitive inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate in presence of 100 uM ATP | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID383374 | Inhibition of PKCmu | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383371 | Inhibition of EphB2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384671 | Cytotoxicity against human HGC27 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID1544434 | Selectivity ratio of IC50 for human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells to IC50 for human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic d | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID1679448 | Inhibition of human MEKK2 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383367 | Inhibition of PDGFRbeta | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384892 | Cytotoxicity against human KYSE520 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425177 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1917912 | Anticancer activity against human SH-SY5Y cells assessed as cell viability at 25 uM incubated for 48 hrs in presence of pyronaridine by checkerboard assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Multiple approaches to repurposing drugs for neuroblastoma. |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1679478 | Inhibition of human c-MER using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383115 | Inhibition of Lck | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384691 | Cytotoxicity against human HT29 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384915 | Cytotoxicity against human SK-NEP1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1506794 | Inhibition of ROS1 in human HCC78 cells assessed as reduction in ERK phosphorylation at 2.5 uM incubated for 48 hrs by Western blot method | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID383905 | Cytotoxicity against human HCC56 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351343 | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID383370 | Inhibition of EphB4 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348165 | Antiproliferative activity against human NCI-H3122 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384165 | Cytotoxicity against human TASK1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679444 | Inhibition of human NEK9 using casein as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1419628 | Inhibition of wild type EML4/ALK G1269A mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID1544425 | Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells assessed as association rate constant by surface plasmon resonance assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| 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. |
| AID1074720 | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK G1269A mutant after 72 hrs by CellTiter Glo assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| 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. |
| AID1074725 | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells after 72 hrs by CellTiter Glo assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1074738 | Ratio of IC50 for human EML4-fused ALK L1152R mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384876 | Cytotoxicity against human KP2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384407 | Cytotoxicity against human RERF-LC-Ad1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1778600 | Inhibition of c-MET (unknown origin) by ELISA | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation. |
| AID383624 | Cytotoxicity against human CCK81 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1330629 | Cytotoxicity against human KARPAS299 cells harboring NPM-ALK assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| 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. |
| AID1186996 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| AID1070239 | Competitive inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate in presence of 10 uM ATP | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383392 | Cytotoxicity against human 42-MG-BA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID1395249 | Antiproliferative activity against human EBC1 cells after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID383576 | Cytotoxicity against human A375.S2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID758044 | Cytotoxicity against mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
| 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. |
| AID1314066 | Cytotoxicity against human MIAPaCa2 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors. |
| AID384365 | Cytotoxicity against human NCI-H838 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383078 | Inhibition of Abl | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1191203 | Inhibition of ROS1 in human HCC78 cells after 48 hrs by CellTitre-Glo assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1632333 | Inhibition of c-Met (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 26, Issue:18 | Design, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold. |
| AID384624 | Cytotoxicity against human MFE-296 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1610125 | Antiproliferative activity against human NCI-H2228 cells expressing EML4-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| 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. |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID384651 | Cytotoxicity against human NCI-H1693 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384167 | Cytotoxicity against human TE7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384399 | Cytotoxicity against human PC-3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384916 | Cytotoxicity against human SK-N-SH cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1074722 | Inhibition of ALK-fusion driven cell proliferation in human KARPAS299 cells after 72 hrs by CellTiter Glo assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID383585 | Cytotoxicity against human AU565 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384665 | Cytotoxicity against human NCI-H2029 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383586 | Cytotoxicity against human AZ521 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351311 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID1891338 | Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID383937 | Cytotoxicity against human SK-LU-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID614836 | Inhibition of human c-MET | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Combined SVM-based and docking-based virtual screening for retrieving novel inhibitors of c-Met. |
| AID383616 | Cytotoxicity against human CAL62 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384885 | Cytotoxicity against human KYSE220 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1598145 | Inhibition of recombinant human ALK expressed in HEK293 cells assessed as reduction in ALK autophosphorylation at Tyr1604 residue incubated for 60 mins by sandwich ELISA | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10 | Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors. |
| AID384157 | Cytotoxicity against human SW948 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383306 | Inhibition of FGR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267046 | Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383921 | Cytotoxicity against human SBC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544437 | Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679459 | Inhibition of human HPK1 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383377 | Inhibition of P70S6K | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1550984 | Cytotoxicity against human A549 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID384633 | Cytotoxicity against human MOG-G-UVW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1764400 | Unbound brain concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383604 | Cytotoxicity against human C33A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384368 | Cytotoxicity against human Nthyl-ori 3-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1070240 | Inhibition of NPM/ALK L1196M mutant (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID1425120 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1876068 | Inhibition of Alk (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID383622 | Cytotoxicity against human CaR1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1550988 | Inhibition of N-terminal GST-tagged human ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384692 | Cytotoxicity against human HT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267030 | Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384901 | Cytotoxicity against human VMRC-RCW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID608692 | Inhibition of 6xHis-tagged NPM-ALK using biotinylated-poly(GT) peptide as substrate after 60 mins | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
| 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. |
| AID1679490 | Inhibition of human ABL1 using EAIYAAPFAKKK as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1570570 | Resistance index, ratio of Kd for N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells to Kd for wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1191196 | Inhibition of ROS1 (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID1419624 | Inhibition of ROS1 G2032R mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679451 | Inhibition of human LCK using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID1425197 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1074740 | Inhibition of human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID383935 | Cytotoxicity against human SKG-IIIb cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383574 | Cytotoxicity against human A373-C6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1274917 | Inhibition of recombinant human PDGFR-beta using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID384426 | Cytotoxicity against human LS174T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1678051 | Cytotoxicity against EGFR-positive human A549 cells incubated for 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1267050 | Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384445 | Cytotoxicity against human MDA-MB-435S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556693 | Induction of apoptosis in ROS1-addicted human HCC78 cells at 2 times of IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 25.84%) | |||
| AID1679474 | Inhibition of human EPHA1 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383649 | Cytotoxicity against human COR-L 105 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074712 | Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID384372 | Cytotoxicity against human OAW28 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384444 | Cytotoxicity against human MDA-MB-415 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267033 | Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384143 | Cytotoxicity against human SW1417 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679433 | Inhibition of human TNK1 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384643 | Cytotoxicity against human NCI-H1563 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425076 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1556662 | Antiproliferative activity against ALK-addicted human NCI-H3122 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
| AID384145 | Cytotoxicity against human SW156 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679450 | Inhibition of human LIMK1 using cofilin as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617338 | Inhibition of ABL in mouse BaF3-BCL cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1678048 | Inhibition of ALK L1196M mutant (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID1421260 | Inhibition of human N-terminal GST-tagged ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | |||
| AID384845 | Cytotoxicity against human HUP-T4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1778602 | Antiproliferative activity against human MKN-45 cells incubated for 72 hrs | 2021 | European journal of medicinal chemistry, Aug-05, Volume: 220 | Discovery of pyrrolo[2,3-d]pyrimidine derivatives as potent Axl inhibitors: Design, synthesis and biological evaluation. |
| AID778821 | Antiproliferative activity against human SNU5 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384366 | Cytotoxicity against human NCI-N87 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384865 | Cytotoxicity against human KATO II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1580398 | Binding affinity to human RIPK3 by kinome scan based method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID1419638 | Intrinsic absorptive permeability from basolateral side to apical side of dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID1261791 | Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study. |
| 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. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617343 | Inhibition of IR | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384171 | Cytotoxicity against human U138 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1424938 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1678053 | Inhibition of ALK (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID1274913 | Inhibition of recombinant human Mer using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID384661 | Cytotoxicity against human NCI-H196 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384136 | Cytotoxicity against human SUIT2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384881 | Cytotoxicity against human KU-19-19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383914 | Cytotoxicity against human HeLa 229 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1544429 | Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID383388 | Cytotoxicity against human 1A6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1550987 | Inhibition of N-terminal GST-tagged human ALK L1196M mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1580399 | Binding affinity to MLKL (unknown origin) assessed as increase in thermal stabilization at 10 uM incubated for 30 mins by thermal shift dye based qPCR analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID1351317 | Inhibition of recombinant ALK L1152R mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383097 | Inhibition of Tie2 by cellular assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383865 | Cytotoxicity against human EFM19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384653 | Cytotoxicity against human NCI-H1734 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383634 | Cytotoxicity against human COLO 741 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1419632 | Inhibition of wild type EML4/ALK G1202R mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383892 | Cytotoxicity against human H69V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267028 | Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID1276909 | Inhibition of recombinant N-terminal GST-tagged human Met using FLPeptide 2 as substrate after 90 mins by mobility shift assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. |
| AID1274926 | Antitumor activity against human EBC1 cells xenografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po qd administered for 21 days relative to control | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID1348648 | Antiproliferative activity against human MCF7 cells after 72 hrs by Alamarblue assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383889 | Cytotoxicity against human GTL16 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1056223 | Inhibition of NPM-fused ALK phosphorylation (unknown origin) expressed in human karpas 299 cells after 90 mins by Sandwich-ELISA | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383933 | Cytotoxicity against human SK-CO1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383862 | Cytotoxicity against human DU145 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1350826 | Inhibition of TEL-fused ALK C1156Y mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| 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. |
| AID383626 | Cytotoxicity against human ChaGo-K-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID384196 | Cytotoxicity against human NCI-H358 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1579904 | Inhibition of ALK (unknown origin) by TR-FRET assay | |||
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679464 | Inhibition of human FES using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384179 | Cytotoxicity against human VMRC-LCD cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384168 | Cytotoxicity against human TGW cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1454437 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
| 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. |
| AID617248 | Inhibition of TRKB at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1074735 | Ratio of IC50 for human EML4-fused ALK S1206Y mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1579885 | Lipophilicity, log D of the compound | |||
| AID384847 | Cytotoxicity against human IGR37 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624810 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1395245 | Antiproliferative activity against human MKN45 cells at 5 uM after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID1556691 | Induction of apoptosis in ROS1-addicted human HCC78 cells at 0.5 times of IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 25.84%) | |||
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1153108 | Inhibition of human EML4-fused ALK G1202R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1769651 | Inhibition of ALK (unknown origin) preincubated for 10 mins followed by addition of substrate and ATP for 25 mins by caliper EZ reader method | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| 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. |
| AID383919 | Cytotoxicity against human HeLa TG Cap cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384683 | Cytotoxicity against human Hs 578T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1153148 | Ratio of drug level in CSF to unbound concentration in plasma in NSCLC patient at 250 mg, bid | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID1267032 | Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID1310835 | Inhibition of human Ron using KKSRGDYMTMQIG as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID1679476 | Inhibition of human DDR1 using KKSRGDYMTMQIG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1070245 | Inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate preincubated for 10 mins followed by ATP addition measured after 15 mins by ELISA | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID384872 | Cytotoxicity against human KMRC20 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID642897 | Cytotoxicity against human SU-DHL1 cells expressing ALK coexpressing NPM | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383894 | Cytotoxicity against human HBE135-E6E7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1186994 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| AID384180 | Cytotoxicity against human VMRC-LCP cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383102 | Inhibition of Aurora A | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1506793 | Inhibition of ROS1 in human HCC78 cells assessed as reduction in AKT phosphorylation at 2.5 uM incubated for 48 hrs by Western blot method | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID384867 | Cytotoxicity against human KG-1-C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1424936 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID384663 | Cytotoxicity against human NCI-H2009 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384672 | Cytotoxicity against human HPAF-II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID384648 | Cytotoxicity against human NCI-H1650 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384150 | Cytotoxicity against human SW780 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384646 | Cytotoxicity against human NCI-H1581 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383926 | Cytotoxicity against human SCLC21H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1153093 | Inhibition of wild type human recombinant ALK kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobility sh | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| 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. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384194 | Cytotoxicity against human NCI-H2452 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384890 | Cytotoxicity against human KYSE50 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1673958 | Inhibition of ROS1 L2026M mutant (unknown origin) in presence of ATP by microfluidic mobility shift assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| 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. |
| AID383578 | Cytotoxicity against human A431 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383924 | Cytotoxicity against human SCCH26 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617241 | Inhibition of TIE2 in mouse 3T3-E cells assessed growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID383395 | Cytotoxicity against human 769-P cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424913 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID658392 | Inhibition of AXL kinase | 2011 | ACS medicinal chemistry letters, Dec-08, Volume: 2, Issue:12 | Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. |
| 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. |
| AID1506775 | Induction of apoptosis in human HCC78 cells assessed as viable cells level at 2.5 uM incubated fro 48 hrs by Annexin-V FITC and propidium iodide staining based flow cytometry (Rvb = 80.8%) | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID1267029 | Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384629 | Cytotoxicity against human MKN45 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1700684 | Inhibition of human ALK F1197M mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351314 | Inhibition of recombinant ALK T1151M mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID384428 | Cytotoxicity against human Lu-134-A-H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384647 | Cytotoxicity against human NCI-H1623 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544426 | Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells assessed as dissociation rate constant by surface plasmon resonance assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID383638 | Cytotoxicity against human COLO 858 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384434 | Cytotoxicity against human M059J cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384675 | Cytotoxicity against human HMCB cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383898 | Cytotoxicity against human HCC15 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384190 | Cytotoxicity against human NCI-H2342 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1261806 | Toxicity in NPM-ALK-positive human KARPAS299 cells xenografted SCID mouse assessed as mortality at 50 mg/kg, po qd for 11 days | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study. |
| AID384650 | Cytotoxicity against human NCI-H1666 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624983 | Binding constant for ABL1(H396P)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1565033 | Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Novel derivatives of anaplastic lymphoma kinase inhibitors: Synthesis, radiolabeling, and preliminary biological studies of fluoroethyl analogues of crizotinib, alectinib, and ceritinib. |
| AID1774075 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
| AID1553338 | Selectivity ratio of EC50 for antiproliferative activity against patient-derived GBM cells to EC50 for antiproliferative activity against patient-derived GBM cells in presence of temozolomide | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID625081 | Binding constant for RSK4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556658 | Inhibition of recombinant human N-terminal GST-tagged ALK (catalytic domain 1058 - 1620 residues) expressed in baculovirus system assessed as decrease in substrate phosphorylation using TK peptide as substrate preincubated with enzyme for 30 mins followed | |||
| AID1274919 | Inhibition of recombinant human EGFR using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID384440 | Cytotoxicity against human MDA-H2774 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID778816 | Antiproliferative activity against human MCF7 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID383577 | Cytotoxicity against human A427 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1864494 | Inhibition of human OCT3 overexpressed in HEK293 cells assessed as intracellularly accumulation of ASP+ at 20 uM incubated for 5 mins by HPLC-MS/MS analysis relative to control | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1325424 | Antiproliferative activity against ALK constitutively activated human SU-DHL1 cells after 72 hrs by SRB or CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID383940 | Cytotoxicity against human SK-MES cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383345 | Inhibition of Syk | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383879 | Cytotoxicity against human TMK1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1274898 | Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID617246 | Inhibition of TRKA | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1769652 | Inhibition of ALK L1196M mutant (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID384158 | Cytotoxicity against human T.T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425147 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1153097 | Octanol-water distribution coefficient, Log D of the compound at pH 7.4 by HPLC-based shake-flask method | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| 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. |
| AID1419637 | Intrinsic clearance in human liver microsomes | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1312499 | Antitumor activity against mouse NIH/3T3 cells expressing wild type EML4-ALK xenografted in nude mouse assessed as tumor growth inhibition at 100 mg/kg, po qd administered for 10 days | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1679473 | Inhibition of human EPHA4 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID383875 | Cytotoxicity against human FTC133 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384384 | Cytotoxicity against human OVKATE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384412 | Cytotoxicity against human RKN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384177 | Cytotoxicity against human UO31 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425031 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178224 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID384418 | Cytotoxicity against human RT4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1504743 | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| 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. |
| AID384891 | Cytotoxicity against human KYSE510 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1416643 | Inhibition of recombinant ALK (unknown origin) after 1 hr by fluorescence assay | 2017 | MedChemComm, Oct-01, Volume: 8, Issue:10 | Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1074741 | Free plasma concentration in human at 250 mg, bid | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID384615 | Cytotoxicity against human MDA-MB-468 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679465 | Inhibition of human FER using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384149 | Cytotoxicity against human SW48 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384170 | Cytotoxicity against human U118 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383607 | Cytotoxicity against human Ca Ski cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1425180 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1504753 | Inhibition of recombinant human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383908 | Cytotoxicity against human HCC827cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1416646 | Induction of apoptosis in human NCI-H2228 cells at 2.5 uM after 48 hrs by annexin V-FITC/propidium iodide staining-based flow cytometric method (Rvb = 4.5%) | 2017 | MedChemComm, Oct-01, Volume: 8, Issue:10 | Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383883 | Cytotoxicity against human G402 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383099 | Inhibition of Bmx | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1579891 | Cytotoxicity against human NCI-H3122 cells harboring EML4-ALK E13;A20 mutant incubated for 72 hrs by Cell titer blue assay | |||
| AID383593 | Cytotoxicity against human BHT101 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383373 | Inhibition of CDK7/cyclin H/MAT1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1074737 | Ratio of IC50 for human EML4-fused ALK F1174L mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID383645 | Cytotoxicity against human COLO 699 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425026 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1330638 | Inhibition of ROS1 (unknown origin) using peptide as substrate after 60 mins by HTRF assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID1348646 | Antiproliferative activity against human A549 cells after 72 hrs by Alamarblue assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID384866 | Cytotoxicity against human KATO III cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1580385 | Binding affinity to human RIPK1 by kinome scan based method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID384411 | Cytotoxicity against human RERF-LC-Sq1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384857 | Cytotoxicity against human Ishikawa 02 ER cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1153096 | Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID625002 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID778812 | Antiproliferative activity against human HCT116 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383915 | Cytotoxicity against human HeLa AG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074719 | Octanol-water distribution coefficient, Log D of the compound at pH 7.4 by RP-HPLC analysis | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| 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. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID383610 | Cytotoxicity against human CAL120 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383922 | Cytotoxicity against human SBC5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544444 | Inhibition of JAK2 V617F mutant in HEL cells assessed as reduction in phosphorylation at STAT3 Y705 residue after 2.5 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384147 | Cytotoxicity against human SW1783 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383621 | Cytotoxicity against human Capan2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425102 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID384849 | Cytotoxicity against human IGROV1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624713 | Binding constant for ERK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383890 | Cytotoxicity against human H3255 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1495543 | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human HCC1937 cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform. |
| 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. |
| AID384883 | Cytotoxicity against human KYSE150 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1484909 | Inhibition of ALK (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| 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. |
| AID1679484 | Inhibition of human Aurora B using [H-LRRASLG] as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384163 | Cytotoxicity against human T98G cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1186995 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 24 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| AID1897147 | Inhibition of ALK (unknown origin) | 2022 | RSC medicinal chemistry, Nov-16, Volume: 13, Issue:11 | Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies. |
| AID384863 | Cytotoxicity against human JR 019 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383619 | Cytotoxicity against human Calu3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
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| 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. |
| AID1679480 | Inhibition of human BMX using poly[Glu:Tyr](4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
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| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1680103 | Inhibition of SLC34A2-ROS1 (unknown origin) expressed in human HCC78 cells assessed as reduction in cell viability | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
| AID1553327 | Antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID383648 | Cytotoxicity against human COLO 849 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1074721 | Inhibition of ALK-fusion driven cell proliferation in human NCI-H3122 cells harboring ALK L1196M mutant after 72 hrs by CellTiter Glo assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| 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. |
| AID1074724 | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID384443 | Cytotoxicity against human MDA-MB-361 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384631 | Cytotoxicity against human MKN74 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679437 | Inhibition of human SYK using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624986 | Binding constant for ABL1(Q252H)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1330632 | Cytotoxicity against human NCI-H460 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425019 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | 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. |
| 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. |
| 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. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383927 | Cytotoxicity against human SEG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1178253 | Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1/L1196M mutant after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID384682 | Cytotoxicity against human Hs 417.Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384367 | Cytotoxicity against human NH6 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383369 | Inhibition of Fms | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348166 | Antiproliferative activity against human HCC78 cells after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors. |
| AID384906 | Cytotoxicity against human WM 266-4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1419634 | Inhibition of ALK (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424977 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1267045 | Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384380 | Cytotoxicity against human OV1063 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1917908 | Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Multiple approaches to repurposing drugs for neuroblastoma. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617237 | Inhibition of RON at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1153109 | Inhibition of human EML4-fused ALK 1151Tins mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| 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. |
| AID384189 | Cytotoxicity against human NCI-H23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384645 | Cytotoxicity against human NCI-H1573 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383617 | Cytotoxicity against human CAL-85-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1137615 | Antiproliferative activity against ALK-dependent human KARPAS299 cells after 72 hrs | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
| AID383906 | Cytotoxicity against human HCC70 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421256 | Antiproliferative activity against human KARPAS299 cells harboring NPM-ALK after 72 hrs by MTT assay | |||
| 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. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID384904 | Cytotoxicity against human WI-38 VA13 sub 2 RA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384679 | Cytotoxicity against human HPAC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1070243 | Selectivity ratio of IC50 for crizotinib-resistant recombinant ALK catalytic domain (1064 to 1427) L1196M mutant (unknown origin) to IC50 for recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID384862 | Cytotoxicity against human JR 013 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1137582 | Inhibition of recombinant INSR (unknown origin) using fluorescent dye-labelled KKSRGDYMTMQIG peptide peptide as substrate after 1 hr by IMAP assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1769648 | Inhibition of recombinant human C-terminal His/FLAG-tagged HDAC1 (1 to 482 residues) expressed in Sf9 insect cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by addition of substrate and trypsin measured by flourescence assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID617242 | Inhibition of TIE2 at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID383881 | Cytotoxicity against human G361 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384392 | Cytotoxicity against human Panc08.13 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384415 | Cytotoxicity against human RPMI-7951 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383934 | Cytotoxicity against human SKG-IIIa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1395244 | Antiproliferative activity against human SNU5 cells at 5 uM after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1407755 | Inhibition of SHIP2 (unknown origin) assessed as remaining enzyme activity at 30 uM using PtdIns(3,4,5)P3 as substrate preincubated for 20 mins followed by substrate addition measured for 50 mins by malachite green staining based assay relative to control | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease. |
| AID383644 | Cytotoxicity against human COLO 680N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384141 | Cytotoxicity against human SW1271 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1864496 | Inhibition of OCT1 (unknown origin) overexpressed in HEK293 cells assessed as intracellular accumulation of ASP+ measured at 20 uM for 5 mins by Analyst AD plate reader method relative to control | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | Substrates and Inhibitors of the Organic Cation Transporter 3 and Comparison with OCT1 and OCT2. |
| AID1267049 | Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID383623 | Cytotoxicity against human CCF-STTG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383859 | Cytotoxicity against human DMS 273 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1421262 | Inhibition of human N-terminal GST-tagged ALK G1202R mutant cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | |||
| AID1544428 | Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells assessed as change in melting temperature at 100 uM by RT-PCR based fluorescence thermal shi | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID384176 | Cytotoxicity against human UM-UC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1314065 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors. |
| AID383065 | Inhibition of c-Met | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID1267053 | Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID617339 | Inhibition of ABL at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384419 | Cytotoxicity against human RVH-421 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1679477 | Inhibition of human c-SRC using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383350 | Inhibition of IRK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| 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. |
| AID384148 | Cytotoxicity against human SW1990 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1774076 | Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%) | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
| AID1679445 | Inhibition of human MEKK3 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384882 | Cytotoxicity against human KYSE140 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID384382 | Cytotoxicity against human OVCAR8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679487 | Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| 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. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1074723 | Inhibition of ALK-fusion driven cell proliferation in human NCI-H2228 cells after 72 hrs by CellTiter Glo assay | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID383907 | Cytotoxicity against human HCC78 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384373 | Cytotoxicity against human OAW42 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1070244 | Inhibition of crizotinib-resistant recombinant ALK catalytic domain (1064 to 1427) L1196M mutant (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate preincubated for 10 mins followed by ATP addition measure | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| 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. |
| AID1302002 | Binding affinity to human ALK (1084 to 1410 residues) expressed in baculovirus infected Sf21 insect cells assessed as dissociation rate constant by surface plasmon resonance assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Pyrazolylamine Derivatives Reveal the Conformational Switching between Type I and Type II Binding Modes of Anaplastic Lymphoma Kinase (ALK). |
| AID383611 | Cytotoxicity against human CAL12T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383637 | Cytotoxicity against human COLO 857 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1504751 | Inhibition of recombinant human N-terminal GST-tagged ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID1191197 | Inhibition of ALK (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID383872 | Cytotoxicity against human EPLC-272H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1504745 | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384388 | Cytotoxicity against human PA1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383375 | Inhibition of BTK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384654 | Cytotoxicity against human NCI-H1755 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383916 | Cytotoxicity against human HeLa S3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424969 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384664 | Cytotoxicity against human NCI-H2023 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383575 | Cytotoxicity against human A-375 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1395243 | Inhibition of GST-tagged human c-MET preincubated for 20 mins followed by [33P]-ATP addition and measured after 2 hrs by Hot-Spot kinase assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| 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. |
| AID1424906 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1419622 | Inhibition of wild type ROS1 (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| 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. |
| AID1407756 | Inhibition of SHIP2 (unknown origin) assessed as decrease in PIP2 production using PtdIns(3,4,5)P3 as substrate preincubated for 20 mins followed by substrate addition measured for 50 mins by malachite green staining based assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384636 | Cytotoxicity against human MSTO-211H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1764401 | Ratio of drug concentration in brain to plasma of P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
| 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. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617349 | Inhibition of VEGFR2 by cellular potency assay | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1137581 | Inhibition of recombinant c-MET (unknown origin) using poly-AEKY peptide as substrate after 60 mins by ADPGlo assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1056231 | Inhibition of c-Met phosphorylation in human MKN845 cells after 1 hr by western blotting | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors. |
| AID383608 | Cytotoxicity against human Caco-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384879 | Cytotoxicity against human KP4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679455 | Inhibition of human IRR using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1421257 | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by MTT assay | |||
| 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. |
| AID1662735 | Inhibition of c-Met (unknown origin) by ADP-Glo kinase assay | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors. |
| 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. |
| AID1679470 | Inhibition of human EPHA7 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID617235 | Inhibition of ALK | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| 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. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1891337 | Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID1191198 | Inhibition of c-Met kinase (unknown origin) | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID1679463 | Inhibition of human FGR using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384617 | Cytotoxicity against human ME180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617346 | Inhibition of LCK | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624736 | Binding constant for RPS6KA5(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID383912 | Cytotoxicity against human HDQ-P1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID383348 | Inhibition of TrkA | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384864 | Cytotoxicity against human JR 029 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384677 | Cytotoxicity against human HOP92 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384378 | Cytotoxicity against human ONCO-DG-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383867 | Cytotoxicity against human EFM-192B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1153099 | Efflux ratio of permeability from basolateral to apical side to apical to basolateral side of MDCK cells expressing MDR1 at pH 7.4 | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID1679439 | Inhibition of human ROS using KKKSPGEYVNIEFG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384142 | Cytotoxicity against human SW13 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1350836 | Antiproliferative activity against human NCI-H3122 cells harboring EML4-fused ALK varian1 after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID1074733 | Ratio of IC50 for human EML4-fused ALK L1196M mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1419629 | Inhibition of wild type EML4/ALK S1206Y mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1764398 | Substrate activity at P-gp (unknown origin) assessed as net efflux ratio | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1074718 | Apparent total intrinsic clearance in human liver microsomes | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1471775 | Inhibition of ALK in human H2228 cells assessed as effect on ERK phosphorylation at 0.5 uM after 3 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| 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. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351316 | Inhibition of recombinant ALK R1275Q mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384433 | Cytotoxicity against human LUDLU1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1500177 | Cytotoxicity against human MKN45 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID642888 | Cytotoxicity against mouse BAF3 cells expressing Tel-ALK after 48 hrs by CellTiter-Glo assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID1350827 | Inhibition of TEL-fused ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID1829585 | Inhibition of 2-FAM-InsP5 binding to human SHIP2 catalytic domain (419 to 832 residues) assessed as change in polarization by fluorescence polarization based displacement assay | 2021 | Journal of medicinal chemistry, 04-08, Volume: 64, Issue:7 | Allosteric Site on SHIP2 Identified Through Fluorescent Ligand Screening and Crystallography: A Potential New Target for Intervention. |
| AID383932 | Cytotoxicity against human SK-BR3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383601 | Cytotoxicity against human BxPC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384173 | Cytotoxicity against human U373 MG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384128 | Cytotoxicity against human SNG-M cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1312454 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID384858 | Cytotoxicity against human J82 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384895 | Cytotoxicity against human LCLC-103H cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384377 | Cytotoxicity against human OE33 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384160 | Cytotoxicity against human T24 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384852 | Cytotoxicity against human IM-95m cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1610127 | Inhibition of recombinant human N-terminal GST-tagged ALK L1196M mutant (1058 to 1620 residues) expressed in baculovirus expression system using Srctide as substrate incubated with enzyme and substrate for 5 mins followed by ATP addition followed by furth | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID778815 | Antiproliferative activity against human SKOV3 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1570563 | Inhibition of c-MET D1228V mutant phosphorylation at Tyr1234/Tyr1235 residues in CRISPR/Cas9 modified human NCI-H1993 cells incubated for 4 hrs by HTRF assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
| AID384423 | Cytotoxicity against human LNZTA3WT4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1506792 | Inhibition of ROS1 in human HCC78 cells assessed as reduction in STAT3 phosphorylation at 2.5 uM incubated for 48 hrs by Western blot method | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID1580400 | Binding affinity to RIPK1 (unknown origin) assessed as increase in thermal stabilization at 10 uM incubated for 30 mins by thermal shift dye based qPCR analysis | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID624901 | Binding constant for RSK1(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1419639 | Intrinsic absorptive permeability from apical side to basolateral side of dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1680099 | Inhibition of EML4/ALK L1196M mutant (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
| AID1679461 | Inhibition of human GCK using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1610129 | Inhibition of recombinant human N-terminal GST-tagged ROS (1883 to 2347 residues) expressed in baculovirus expression system using IRS1 as substrate incubated with enzyme and substrate for 5 mins followed by ATP addition followed by further incubation for | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID383592 | Cytotoxicity against human BFTC909 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383869 | Cytotoxicity against human EFO21 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348641 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by Alamarblue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID1471773 | Antiproliferative activity against human H2228/CR cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384193 | Cytotoxicity against human NCI-H2444 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1229121 | Antiproliferative activity against mouse BAF3/TPR-Met cells after 72 hrs | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
| AID383397 | Cytotoxicity against human 8305C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556688 | Induction of apoptosis in ALK-addicted human NCI-H3122 cells at 0.5 times of IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 9.82%) | |||
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| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383612 | Cytotoxicity against human CAL148 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679449 | Inhibition of human LOK using RLGRDKYKTLRQIRQ as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1056224 | Inhibition of c-Met phosphorylation in human MKN845 cells after 90 mins by Sandwich-ELISA | 2013 | ACS medicinal chemistry letters, Aug-08, Volume: 4, Issue:8 | Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors. |
| AID384394 | Cytotoxicity against human PANC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383639 | Cytotoxicity against human COLO 206F cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383584 | Cytotoxicity against human AsPC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384861 | Cytotoxicity against human JIMT1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1153149 | Selectivity ratio of IC50 for human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells to IC50 for wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| 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. |
| AID384205 | Cytotoxicity against human NCI-H727 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1656371 | Inhibition of MST1R (unknown origin) | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies. |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1700647 | Inhibition of N-terminal GST tagged wild-type human ALK cytoplasmic domain (1058-1620 amino acids) expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. |
| AID778817 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1351348 | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| 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. |
| AID1679472 | Inhibition of human EPHA5 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1350837 | Antiproliferative activity against human NCI-H2228 cells harboring EML4-fused ALK varian3 after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID384186 | Cytotoxicity against human NCI-H2196 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1229108 | Inhibition of C-Met (unknown origin) using polu (Glu,Tyr)4:1 substrate after 30 mins incubation by multi-well spectrophotometry | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
| AID384383 | Cytotoxicity against human OVISE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383614 | Cytotoxicity against human CAL51 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384397 | Cytotoxicity against human PA-TU-8988T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384870 | Cytotoxicity against human KMH2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384405 | Cytotoxicity against human RCM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617350 | Inhibition of PDGFRbeta by cellular potency assay | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1679430 | Inhibition of human TRKC using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID617236 | Inhibition of RON in mouse 3T3 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1312453 | Antiproliferative activity against human SUP-M2 cells after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1679438 | Inhibition of human SIK2 using AMARAASAAALARRR as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID384662 | Cytotoxicity against human NCI-H1975 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1312451 | Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1506776 | Induction of apoptosis in human HCC78 cells assessed as early apoptotic cells level at 2.5 uM incubated fro 48 hrs by Annexin-V FITC and propidium iodide staining based flow cytometry (Rvb = 6.33%) | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID1348640 | Antiproliferative activity against human MKN45 cells after 72 hrs by Alamarblue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID617344 | Inhibition of LCK in human Jurkat cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384206 | Cytotoxicity against human NCI-H810 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1153107 | Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
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| AID384859 | Cytotoxicity against human JHH1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1679434 | Inhibition of human TAOK2 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1544435 | Selectivity ratio of IC50 for human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells to IC50 for human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic d | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1876070 | Cytotoxicity against human RD cells | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1074713 | Inhibition of human EML4-fused ALK C1156Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1310805 | Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
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| AID1425103 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1424932 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID383347 | Inhibition of Axl | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID608694 | Inhibition of recombinant MET using biotinylated-poly(GT) peptide as substrate after 60 mins | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137585 | Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| 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. |
| AID384430 | Cytotoxicity against human LU99A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351344 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID1348639 | Antiproliferative activity against human EBC1 cells after 72 hrs by Alamarblue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID1697357 | Binding affinity to wild-type human partial length ERK3 (M1 to P413 residues) expressed in bacterial expression system by kinomescan method | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22 | Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors. |
| 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. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1506777 | Induction of apoptosis in human HCC78 cells assessed as late apoptotic cells level at 2.5 uM incubated fro 48 hrs by Annexin-V FITC and propidium iodide staining based flow cytometry (Rvb = 13.8%) | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| 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. |
| AID384425 | Cytotoxicity against human LoVo cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1550981 | Cytotoxicity against mouse BA/F3 cells harboring ALK G1202R mutation incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID384639 | Cytotoxicity against human NCI-H1048 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1276952 | Inhibition of c-Met (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs. |
| AID1267036 | Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID617347 | Selectivity ratio of IC50 for c-MET kinase in GTL-16 cells to IC50 for VEGFR2 by cellular potency assay | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID383861 | Cytotoxicity against human DoTc2 4510 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383100 | Inhibition of FGFR3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544436 | Selectivity ratio of IC50 for TYK2 (unknown origin) to IC50 for human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679462 | Inhibition of human FYN using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384907 | Cytotoxicity against human WM 1552C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556661 | Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay | |||
| AID384688 | Cytotoxicity against human Hs 894(E).Lu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1310834 | Inhibition of human c-Met using [KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556660 | Inhibition of recombinant human N-terminal GST-tagged ROS1 (catalytic domain 1883 - 2347 residues) expressed in baculovirus system assessed as decrease in substrate phosphorylation using TK peptide as substrate at 1 uM preincubated with enzyme for 30 mins | |||
| AID1673942 | Antiproliferative activity against human MGH021-4 cells harboring ALK G1269A mutant after 72 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| 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. |
| AID1137586 | Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| 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. |
| AID1700687 | Inhibition of human ALK S1206Y mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. |
| AID384613 | Cytotoxicity against human MDA-MB-436 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544445 | Inhibition of JAK2 V617F mutant in HEL cells assessed as reduction in phosphorylation at STAT5 Y694 residue after 2.5 hrs by Western blot analysis | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID384659 | Cytotoxicity against human NCI-H1915 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679446 | Inhibition of human MST1 using KKSRGDYMTMQIG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1292204 | Cytotoxicity against human EBC1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384637 | Cytotoxicity against human MT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1580406 | Ratio of binding affinity to human RIPK3 to human MLKL by kinome scan based method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384669 | Cytotoxicity against human NCI-H2087 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384868 | Cytotoxicity against human KHM3S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679486 | Inhibition of human ARK5 using KKKVSRSGLYRSPSMPENLNRPR as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383625 | Cytotoxicity against human CFPAC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1891329 | Inhibition of wild type ALK (unknown origin) using biotinylated substrate incubated for 1 hr in the presence of ATP at Km concentration by HTRF assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID384690 | Cytotoxicity against human HT115 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384889 | Cytotoxicity against human KYSE450 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1769656 | Antiproliferative activity against human NCI-H2228 cells harboring EML4/ALK L1196M mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1572907 | Inhibition of recombinant ALK (unknown origin) using peptide substrate measured after 1 hr by LanthaScreen assay | 2019 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7 | Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1553331 | Antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs by 5-Ethynyl-2'-deoxyuridine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID1471792 | Inhibition of human wild type EML4 fused ALK expressed in mouse Ba/F3 cells assessed as decrease in cell proliferation at 0.1 to 1 uM preincubated for 72 hrs followed by methyl-3H-thymidine incorporation measured after 8 hrs by filter scintillation counte | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID1917909 | Anticancer activity against human HT-1080 cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Multiple approaches to repurposing drugs for neuroblastoma. |
| AID1553333 | Synergistic antiproliferative activity against patient-derived GBM cells assessed as reduction in cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID1500164 | Inhibition of human GST-tagged c-MET preincubated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by Hot-SpotSM kinase assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
| 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. |
| AID384161 | Cytotoxicity against human T47D cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1544427 | Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells assessed as dissociation constant by surface plasmon resonance assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID384851 | Cytotoxicity against human IM95 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351313 | Inhibition of recombinant ALK G1202R mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID384909 | Cytotoxicity against human WM35 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617239 | Inhibition of AXL at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| 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. |
| AID1153095 | Inhibition of wild type human EML4-fused ALK expressed in mouse NIH-3T3 cells assessed as phosphorylated ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID384369 | Cytotoxicity against human NUGC2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348642 | Antiproliferative activity against human PC3 cells after 72 hrs by Alamarblue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID1700685 | Inhibition of human ALK G1269A mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. |
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| AID624927 | Binding constant for RPS6KA4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1337143 | Binding affinity to ALK (unknown origin) | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
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| AID383591 | Cytotoxicity against human BFTC905 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679858 | Apparent permeability across apical to basolateral side in human Caco2 cells | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1556657 | Inhibition of recombinant human N-terminal GST-tagged ROS1 (catalytic domain 1883 - 2347 residues) expressed in baculovirus system assessed as decrease in substrate phosphorylation using TK peptide as substrate preincubated with enzyme for 30 mins followe | |||
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID384169 | Cytotoxicity against human TYK-nu cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1764581 | Antitumor activity against human U-87MG cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, po administered once daily for 14 days by caliper method | |||
| 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. |
| AID384421 | Cytotoxicity against human Saos-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1348643 | Antiproliferative activity against human COLO205 cells after 72 hrs by Alamarblue assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID383929 | Cytotoxicity against human SHP77 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1506791 | Inhibition of ROS1 phosphorylation in human HCC78 cells at 2.5 uM incubated for 48 hrs by Western blot method | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID1454436 | Displacement of ALLO-1 from allosteric site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | |
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| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1419631 | Inhibition of wild type EML4/ALK L1152R mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID1421264 | Inhibition of human N-terminal GST-tagged EGFR cytoplasmic domain (669 to 1210 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | |||
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| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1186993 | Cytotoxicity against human HepG2 cells assessed as cell viability at 100 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| AID1550974 | Inhibition of N-terminal GST-tagged human ROS1 cytoplasmic domain (1883 to 2347 residues) expressed in Baculovirus expression system using IRS1 as substrate incubated for 1 hr by mobility shift assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID1351345 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK L1196M mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| 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. |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1774079 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
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| 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. |
| 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. |
| AID383876 | Cytotoxicity against human TT2609-C02 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID642898 | Inhibition of ALK | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| 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. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178255 | Antiproliferative activity against crizotinib-resistant human LAN5 cells harboring ALK R1275Q mutant after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID1500176 | Cytotoxicity against human EBC1 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
| AID1261789 | Inhibition of recombinant ALK (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISA | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study. |
| AID383887 | Cytotoxicity against human GOS3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383646 | Cytotoxicity against human COLO 818 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1610124 | Antiproliferative activity against human SK-N-BE(2) cells expressing wild type ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| 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. |
| AID383909 | Cytotoxicity against human HCE7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679441 | Inhibition of human RON using KKSRGDYMTMQIG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384656 | Cytotoxicity against human NCI-H1792 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1310830 | Antitumor activity against human NCI-H3122 cells xenografted in SCID/beige mouse assessed as tumor growth inhibition at 100 mg/kg, po administered once-daily for 19 days | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID383920 | Cytotoxicity against human HeLa.P3(s) cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384860 | Cytotoxicity against human JHH4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1550982 | Cytotoxicity against mouse BA/F3 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384873 | Cytotoxicity against human KMRM-M1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383864 | Cytotoxicity against human EBC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383597 | Cytotoxicity against human BT483 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679460 | Inhibition of human GLK using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624988 | Binding constant for ABL1(T315I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384431 | Cytotoxicity against human LU99B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1579877 | Inhibition of ALK in human KARPAS299 cells assessed as reduction in NPM-ALK phosphorylation after 1 hrs by ELISA | |||
| AID1504746 | Antiproliferative activity against human A549 cells harboring EGFR after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID384684 | Cytotoxicity against human Hs 633T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384439 | Cytotoxicity against human MC-IXC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1330630 | Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID384614 | Cytotoxicity against human MDA-MB-453 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383294 | Inhibition of c-Src | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384429 | Cytotoxicity against human Lu135 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383342 | Inhibition of Ret | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1680102 | Inhibition of ROS1 (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
| AID383573 | Cytotoxicity against human A2780 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383884 | Cytotoxicity against human GAMG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID702213 | Selectivity ratio of Ki for c-Met Y1230C mutant to Ki for wild type c-MET | 2012 | Journal of medicinal chemistry, Sep-27, Volume: 55, Issue:18 | Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-y |
| AID1769643 | Antiproliferative activity against human SH-SY5Y cells harboring ALK F1174L mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID1153098 | Apparent total intrinsic clearance in human liver microsomes | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID383629 | Cytotoxicity against human CL34 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID624900 | Binding constant for RSK1(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383900 | Cytotoxicity against human HCC1937 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679432 | Inhibition of human TRKA using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| 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. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID608693 | Inhibition of recombinant IRK using biotinylated-poly(GT) peptide as substrate after 60 mins | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
| 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. |
| AID617342 | Inhibition of IR at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID617231 | Inhibition of c-MET at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1556679 | Inhibition of ALK L1196M mutant (unknown origin) at 1 uM relative to control | |||
| AID1267034 | Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1550983 | Cytotoxicity against human HCC78 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID383390 | Cytotoxicity against human 23132/87 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID384134 | Cytotoxicity against human STC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383870 | Cytotoxicity against human EGI1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384187 | Cytotoxicity against human NCI-H2228 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID642893 | Cytotoxicity against mouse BAF3 cells expressing ALK L1196M mutant coexpressing EML4 after 48 hrs by MTS assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384903 | Cytotoxicity against human WI-26 VA4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384666 | Cytotoxicity against human NCI-H2030 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384181 | Cytotoxicity against human VMRC-MELG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617228 | Lipophilicity, log D of the compound at pH 7.4 | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384393 | Cytotoxicity against human Panc10.05 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679426 | Inhibition of human YES using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384437 | Cytotoxicity against human MCF7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1229119 | Antiproliferative activity against human MKN45 cells after 72 hrs | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
| AID1261802 | Antitumor activity against NPM-ALK-positive human KARPAS299 cells xenografted in SCID mouse assessed as decrease in tumor volume at 50 mg/kg, po qd administered for 11 days measured on day 11 post last dose | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study. |
| 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. |
| AID383873 | Cytotoxicity against human EVSA-T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID642895 | Cytotoxicity against human SH-SY5Y cells expressing ALK F1174L mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1419636 | Octanol-water distribution coefficient, log D of the compound at pH 7.4 by RP-HPLC analysis | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| 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. |
| AID1579883 | Inhibition of ALK in mouse NIH-3T3 cells | |||
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624806 | Binding constant for RPS6KA4(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384138 | Cytotoxicity against human SVts8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383874 | Cytotoxicity against human fR2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425112 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1500183 | Cytotoxicity against human HFL1 cells assessed as decrease in cell viability at 50 uM after 72 hrs by Cell Titer-Glo assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
| 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. |
| 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. |
| AID1350825 | Inhibition of full length ALK F1174L mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID383384 | Cytotoxicity against human 5637 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383866 | Cytotoxicity against human EFM192A cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1774078 | Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method | 2021 | Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19 | Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383654 | Cytotoxicity against human DLD1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1395246 | Antiproliferative activity against human EBC1 cells at 5 uM after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383635 | Cytotoxicity against human COLO 792 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384842 | Cytotoxicity against human HuCCT1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074739 | Ratio of IC50 for human EML4-fused ALK 1151Tins mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1579875 | Inhibition of c-Met (unknown origin) | |||
| AID1407766 | Cytotoxicity against mouse HT22 cells assessed as decrease in cell viability at 10 uM after 24 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease. |
| AID383653 | Cytotoxicity against human Daoy cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1875891 | Antiviral activity against EV-A71 infected in RD cells assessed as reduction in virus titre by crystal violet staining method relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1889931 | Inhibition of TRKA G595R mutant (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 63 | Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1769655 | Antiproliferative activity against human SKNBE2 cells harboring wild type ALK assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID1678046 | Inhibition of c-Met (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID384441 | Cytotoxicity against human MDA-MB-157 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679482 | Inhibition of human AXL using EAIYAAPFAKKK as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| 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. |
| AID1889930 | Inhibition of wild type TRKA (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 63 | Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation. |
| AID384627 | Cytotoxicity against human MKN1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384198 | Cytotoxicity against human NCI-H460 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1544431 | Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID1274918 | Inhibition of recombinant human KDR using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| 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. |
| AID1348647 | Antiproliferative activity against human HCT116 cells after 72 hrs by Alamarblue assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID1570562 | Inhibition of c-Met phosphorylation at Tyr 1234/Tyr1235 residues in human NCI-H1993 cells incubated for 4 hrs by HTRF assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
| AID1229109 | Antiproliferative activity against human EBC1 cells after 72 hrs | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
| AID1267054 | Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384673 | Cytotoxicity against human HLE cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679483 | Inhibition of human Aurora C using [H-LRRASLG] as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1330631 | Cytotoxicity against human A549 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624749 | Binding constant for CASK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384432 | Cytotoxicity against human LU99C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383891 | Cytotoxicity against human H4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1178223 | Antiproliferative activity against human SUP-M2 cells harboring NPM-ALK after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID617340 | Inhibition of ABL | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1302001 | Binding affinity to human ALK (1084 to 1410 residues) expressed in baculovirus infected Sf21 insect cells assessed as association rate constant by surface plasmon resonance assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Pyrazolylamine Derivatives Reveal the Conformational Switching between Type I and Type II Binding Modes of Anaplastic Lymphoma Kinase (ALK). |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556686 | Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
| 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. |
| AID1074711 | Inhibition of human EML4-fused ALK G1269A mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1274911 | Inhibition of recombinant human Axl using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617341 | Inhibition of IR in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384197 | Cytotoxicity against human NCI-H441 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384414 | Cytotoxicity against human RO82-W-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384131 | Cytotoxicity against human SNU398 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1416644 | Cytotoxicity against human NCI-H2228 cells harboring EML4-ALK fusion protein assessed as decrease in cell viability after 72 hrs by MTT assay | 2017 | MedChemComm, Oct-01, Volume: 8, Issue:10 | Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. |
| AID1891336 | Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID1137627 | Antitumor activity against mouse BAF3 cells expressing EML4-ALK fusion protein allografted in nude mouse assessed as tumor growth inhibition at 50 mg/kg, po qd for 2 weeks relative to vehicle-treated control | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383579 | Cytotoxicity against human A549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383885 | Cytotoxicity against human GCT cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383860 | Cytotoxicity against human DMS 53 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556682 | Inhibition of ALK C1156Y mutant (unknown origin) at 1 uM | |||
| AID1556685 | Antiproliferative activity against mouse BAF3 cells expressing wild type CD74/ROS1 assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
| AID383389 | Cytotoxicity against human 201T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383897 | Cytotoxicity against human HCC1395 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1186992 | Cytotoxicity against human HepG2 cells assessed as cell viability at 10 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| 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. |
| AID383620 | Cytotoxicity against human Capan1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384152 | Cytotoxicity against human SW1710 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384422 | Cytotoxicity against human LNZTA3WT11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384192 | Cytotoxicity against human NCI-H2405 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1267042 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID1274916 | Inhibition of recombinant human PDGFR-alpha using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID1579876 | Inhibition of ALK (unknown origin) | |||
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351315 | Inhibition of recombinant ALK S1206Y mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID383080 | Inhibition of VEGFR2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID778818 | Antiproliferative activity against human NCI-H441 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1662734 | Antiproliferative activity against human MKN45 cells overexpressing c-MET assessed as reduction in cell proliferation | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors. |
| AID1679467 | Inhibition of human EPHB4 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384153 | Cytotoxicity against human SW527 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383351 | Inhibition of IGF1R | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1572908 | Antiproliferative activity against human KARPAS299 cells after 3 days by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 29, Issue:7 | Discovery of 3,6-diaryl-1H-pyrazolo[3,4-b]pyridines as potent anaplastic lymphoma kinase (ALK) inhibitors. |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1312447 | Antitumor activity against mouse NIH/3T3 cells expressing EML4-ALK L1196M mutant xenografted in nude mouse assessed as tumor growth inhibition at 100 mg/kg, po qd administered for 10 days | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1679466 | Inhibition of human FAK using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384854 | Cytotoxicity against human IPC298 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1178220 | Inhibition of c-Met kinase (unknown origin) after 60 mins by ELISA | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1350824 | Inhibition of TEL-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID383631 | Cytotoxicity against human COLO 201 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1153106 | Inhibition of human EML4-fused ALK S1206Y mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383893 | Cytotoxicity against human HARA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617247 | Inhibition of TRKB in pig PAE cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID383636 | Cytotoxicity against human COLO 853 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383627 | Cytotoxicity against human CL11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384844 | Cytotoxicity against human HUP-T3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1656370 | Inhibition of c-MET (unknown origin) assessed as reduction in ADP production incubated for 10 mins by spectrophotometric method | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Promiscuity of in Vitro Secondary Pharmacology Assays and Implications for Lead Optimization Strategies. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384135 | Cytotoxicity against human SU.86.86 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351346 | Antiproliferative activity against mouse BAF3 cells harboring EML4-ALK G1202R mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| 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. |
| AID384620 | Cytotoxicity against human MES-SA cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1312491 | Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383393 | Cytotoxicity against human 639-V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383895 | Cytotoxicity against human HBE4-E6E7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1274912 | Inhibition of recombinant human TyrO3 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| 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. |
| AID384632 | Cytotoxicity against human ML1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383589 | Cytotoxicity against human BEAS-2B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384652 | Cytotoxicity against human NCI-H1703 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384626 | Cytotoxicity against human MIA PaCa-2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679435 | Inhibition of human TIE2 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID384424 | Cytotoxicity against human LOU-NH91 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1416651 | Inhibition of EML4-fused ALK autophosphorylation at Tyr1282/1283 in human NCI-H2228 cells at 2.5 uM after 48 hrs by Western blot method | 2017 | MedChemComm, Oct-01, Volume: 8, Issue:10 | Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer. |
| AID1137579 | Inhibition of recombinant EGFR (unknown origin) using poly-GT peptide as substrate by Transcreener assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| 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. |
| AID384416 | Cytotoxicity against human RT-112 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384403 | Cytotoxicity against human PLC/PRF/5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384162 | Cytotoxicity against human T84 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137583 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID384896 | Cytotoxicity against human LCLC-97TM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1350838 | Antiproliferative activity against CHO cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| 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. |
| AID642896 | Cytotoxicity against human SMS-KCN cells expressing ALK R1275Q mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID384634 | Cytotoxicity against human MRC9 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425005 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| 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. |
| AID1330643 | Antitumor activity against non-small cell lung cancer cells harboring ROS1 rearrangement in patient assessed as response rate after 8 weeks | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID617233 | Inhibition of ALK in human KARPAS299 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384188 | Cytotoxicity against human NCI-H2286 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625050 | Binding constant for PKN2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384140 | Cytotoxicity against human SW1116 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1678049 | Cytotoxicity against human KARPAS299 cells harboring NMP-ALK incubated for 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID383349 | Inhibition of TrkB | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384191 | Cytotoxicity against human NCI-H2347 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351312 | Inhibition of recombinant ALK L1196M mutant (unknown origin) using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID778814 | Antiproliferative activity against human SK-MEL-28 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1330633 | Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID1769642 | Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID384146 | Cytotoxicity against human SW1573 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384436 | Cytotoxicity against human MCAS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383868 | Cytotoxicity against human EFM-192C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383580 | Cytotoxicity against human ABC-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1471793 | Inhibition of human wild type EML4 fused ALK L1196M mutant expressed in mouse Ba/F3 cells assessed as decrease in cell proliferation at 0.1 to 1 uM preincubated for 72 hrs followed by methyl-3H-thymidine incorporation measured after 8 hrs by filter scinti | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID384183 | Cytotoxicity against human NCI-H2135 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383387 | Cytotoxicity against human 143B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1191202 | Inhibition of c-Met (unknown origin) incubated for 20 mins followed by [33P]ATP addition measured after 120 mins by HotSpot assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID1182155 | Inhibition of ROS1 (unknown origin) assessed as remaining activity | 2014 | Bioorganic & medicinal chemistry, Aug-01, Volume: 22, Issue:15 | Structure-based optimization and biological evaluation of trisubstituted pyrazole as a core structure of potent ROS1 kinase inhibitors. |
| AID384871 | Cytotoxicity against human KMRC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383596 | Cytotoxicity against human BT474 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1310801 | Inhibition of human ALK using poly[Glu:Tyr] (4:1) as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID383896 | Cytotoxicity against human HBE4-E6E7-C1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384848 | Cytotoxicity against human IGR39 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384674 | Cytotoxicity against human HLF cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID758045 | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
| AID1274924 | Inhibition of recombinant human ErbB2 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1274920 | Inhibition of recombinant human Flt-1 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679442 | Inhibition of human PKCnu using KKLNRTLSVA as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383067 | Inhibition of Ron | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1267037 | Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID1310803 | Inhibition of human InsR using myelin basic protein as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| 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. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679458 | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384132 | Cytotoxicity against human SNU449 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383903 | Cytotoxicity against human HCC38 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID778823 | Antiproliferative activity against human MKN45 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| 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. |
| AID384856 | Cytotoxicity against human Ishikawa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1769653 | Inhibition of ALK G1202R mutant (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1579878 | Inhibition of ALK in human SUDHL1 cells assessed as reduction in NPM-ALK phosphorylation after 1 hrs by ELISA | |||
| AID384182 | Cytotoxicity against human NCI-H2122 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1137614 | Antiproliferative activity against cMET-amplified human EBC1 cells after 72 hrs | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
| 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. |
| AID1337142 | Binding affinity to MET (unknown origin) | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6 | Non-kinase targets of protein kinase inhibitors. |
| AID384874 | Cytotoxicity against human KP-1N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1419640 | Efflux ratio in dog RRCK cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID1556692 | Induction of apoptosis in ROS1-addicted human HCC78 cells at IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 25.84%) | |||
| AID383878 | Cytotoxicity against human FU97 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1330637 | Inhibition of ALK L1196M mutant (unknown origin) using peptide as substrate after 60 mins by HTRF assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384410 | Cytotoxicity against human RERF-LC-MS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1550976 | Inhibition of N-terminal GST-tagged human EGFR cytoplasmic domain (669 to 1210 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID625001 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1350828 | Inhibition of TEL-fused ALK G1202R mutant (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID1679469 | Inhibition of human EPHA8 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384630 | Cytotoxicity against human MKN7 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383581 | Cytotoxicity against human ACHN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1274925 | Inhibition of recombinant human ABL using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID1550979 | Cytotoxicity against human KARPAS299 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1579874 | Inhibition of ALK (unknown origin) by kinome scan-based assay | |||
| AID1504750 | Inhibition of recombinant human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384914 | Cytotoxicity against human ZR-75-30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384413 | Cytotoxicity against human RMG-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679471 | Inhibition of human EPHA6 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1917907 | Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay | 2022 | Bioorganic & medicinal chemistry, 11-01, Volume: 73 | Multiple approaches to repurposing drugs for neuroblastoma. |
| AID1891327 | Inhibition of ALK C1156Y mutant (unknown origin) using biotinylated substrate incubated for 1 hr in the presence of ATP at Km concentration by HTRF assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID384126 | Cytotoxicity against human SK-N-AS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679456 | Inhibition of human IRAK1 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384638 | Cytotoxicity against human NB69 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| 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. |
| AID1292203 | Inhibition of recombinant c-MET (unknown origin) using poly (Glu,Tyr) 4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jun-10, Volume: 115 | Design and synthesis of novel benzo[d]oxazol-2(3H)-one derivatives bearing 7-substituted-4-enthoxyquinoline moieties as c-Met kinase inhibitors. |
| AID384175 | Cytotoxicity against human UMC11 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1325425 | Antiproliferative activity against ALK constitutively activated human KARPAS299 cells after 72 hrs by SRB or CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1274921 | Inhibition of recombinant human Flt-3 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID384894 | Cytotoxicity against human LC-1 sq cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624981 | Binding constant for ABL1(F317L)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1419623 | Inhibition of ROS1 L2026M mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
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| AID1495542 | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot m | 2018 | Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10 | Design, Synthesis, and Testing of Potent, Selective Hepsin Inhibitors via Application of an Automated Closed-Loop Optimization Platform. |
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| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID758043 | Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
| AID1769649 | Inhibition of HDAC2 (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
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| AID1556690 | Induction of apoptosis in ALK-addicted human NCI-H3122 cells at 2 times of IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 9.82%) | |||
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1553339 | Selectivity ratio of IC50 for antiproliferative activity against patient-derived GBM cells to IC50 for antiproliferative activity against patient-derived GBM cells in presence of temozolomide | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID624716 | Binding constant for CSNK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID1679454 | Inhibition of human JAK1 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
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| AID384125 | Cytotoxicity against human SK-MES1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383376 | Inhibition of Cdk1/cyclin B | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID383606 | Cytotoxicity against human C-4 II cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383641 | Cytotoxicity against human COLO 678 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384887 | Cytotoxicity against human KYSE30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID642891 | Cytotoxicity against mouse BAF3 cells expressing EML4-ALK after 48 hrs by MTS assay | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
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| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617240 | Inhibition of AXL | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1314067 | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Synthesis and biological evaluation of Oblongifolin C derivatives as c-Met inhibitors. |
| AID617245 | Inhibition of TRKA at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
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| AID383583 | Cytotoxicity against human ASH3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384649 | Cytotoxicity against human NCI-H1651 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384893 | Cytotoxicity against human KYSE70 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1764399 | Unbound plasma concentration in P-gp knock out Sprague-Dawley rat at 5 mg/ml/kg, po measured upto 4 hrs by LC-MS analysis | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
| AID1544433 | Inhibition of TYK2 (unknown origin) using peptide as substrate preincubated for 10 mins followed by substrate addition by mobility shift assay | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| 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. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384693 | Cytotoxicity against human HTC-C3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383603 | Cytotoxicity against human C32 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178221 | Inhibition of ALK (unknown origin) after 60 mins by ELISA | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID1330639 | Inhibition of c-Met (unknown origin) using peptide as substrate after 60 mins by HTRF assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1504752 | Inhibition of recombinant human N-terminal GST-tagged c-MET cytoplasmic domain (956 to 1390 residues) expressed in baculovirus expression system using peptide substrate after 1 hr by mobility shift assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID1662738 | Antitumor activity against human MKN45 cells xenografted in nude mouse assessed as tumor growth inhibition at 20 mg/kg, po administered once daily for 14 days relative to control | 2020 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 30, Issue:13 | Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors. |
| AID1312456 | Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617243 | Inhibition of TIE2 | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID617238 | Inhibition of AXL in human HEK293 cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID767456 | Inhibition of ALK (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Selectivity data: assessment, predictions, concordance, and implications. |
| AID384875 | Cytotoxicity against human KP-1NL cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384667 | Cytotoxicity against human NCI-H2073 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384409 | Cytotoxicity against human RERF-LC-KJ cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384897 | Cytotoxicity against human LK2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383899 | Cytotoxicity against human HCC1806 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
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| AID1610123 | Antiproliferative activity against human SH-SY5Y cells expressing ALK F1174L mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424901 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1579873 | Inhibition of c-MET (unknown origin) by kinome scan-based assay | |||
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383632 | Cytotoxicity against human COLO 205 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679862 | Inhibition of GLK (unknown origin) by alphascreen assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383600 | Cytotoxicity against human thymidine kinase deficient Bu25 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267043 | Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625091 | Binding constant for MAST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1267035 | Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID383378 | Inhibition of PRK2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1500178 | Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by Cell Titer-Glo assay | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Structure-based design, synthesis, and evaluation of 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine derivatives as novel c-Met inhibitors. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383595 | Cytotoxicity against human BICR 78 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384404 | Cytotoxicity against human QGP1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624970 | Binding constant for CDK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1506771 | Inhibition of ROS1 (unknown origin) using poly (Glu,Tyr)4:1 substrate and ATP incubated for 60 mins by ELISA | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384127 | Cytotoxicity against human SK-OV3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1153094 | Inhibition of human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus system using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to ATP addition measured after 1 hr by microfluidic mobilit | 2014 | Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11 | Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros o |
| AID384911 | Cytotoxicity against human YAPC cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383928 | Cytotoxicity against human SF295 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384658 | Cytotoxicity against human NCI-H1869 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384908 | Cytotoxicity against human WM278 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384905 | Cytotoxicity against human WiDr cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383871 | Cytotoxicity against human EJ138 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137608 | Inhibition of purified recombinant c-MET (unknown origin) after 60 mins by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities. |
| 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. |
| AID1579884 | Inhibition of ALK L1196M mutant in mouse NIH-3T3 cells | |||
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617234 | Inhibition of ALK at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1350839 | Antiproliferative activity against CHL cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID1679431 | Inhibition of human TRKB using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| 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. |
| AID1679481 | Inhibition of human BLK using poly[Glu:Tyr](4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383642 | Cytotoxicity against human COLO 679 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383598 | Cytotoxicity against human BT549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1350823 | Inhibition of EML4-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID384400 | Cytotoxicity against human PC-3[JPC-3] cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624967 | Binding constant for RPS6KA5(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679427 | Inhibition of human TYK2 using KKSRGDYMTMQIG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1764402 | Unbound brain-to-plasma concentration ratio in P-gp knock out Sprague-Dawley rat | 2021 | Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5 | Development of an |
| AID383877 | Cytotoxicity against human FTC238 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074716 | Inhibition of human EML4-fused ALK L1152R mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID384642 | Cytotoxicity against human NCI-H1437 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617348 | Selectivity ratio of IC50 for c-MET kinase in GTL-16 cells to IC50 for PDGFRbeta by cellular potency assay | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID778852 | Inhibition of c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 60 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| 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. |
| 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. |
| AID384670 | Cytotoxicity against human NCI-H2110 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1556681 | Inhibition of ALK L1196M mutant (unknown origin) at 1 uM | |||
| AID1678045 | Inhibition of ROS1 (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1550986 | Inhibition of N-terminal GST-tagged human ALK cytoplasmic domain (1058 to 1620 residues) expressed in Baculovirus expression system using srctide as substrate incubated for 1 hr by mobility shift assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID384178 | Cytotoxicity against human VM-CUB1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384154 | Cytotoxicity against human SW620 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384621 | Cytotoxicity against human MEL-SA/Dx-5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1419626 | Inhibition of wild type EML4/ALK F1174L mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1506778 | Induction of apoptosis in human HCC78 cells assessed as necrotic cells level at 2.5 uM incubated fro 48 hrs by Annexin-V FITC and propidium iodide staining based flow cytometry (Rvb = 0.06%) | 2017 | MedChemComm, Mar-01, Volume: 8, Issue:3 | Identification of mitoxantrone as a new inhibitor of ROS1 fusion protein in non-small cell lung cancer cells. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383911 | Cytotoxicity against human HCT8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1484907 | Inhibition of c-Met (unknown origin) using poly (Glu, Tyr) 4:1 as substrate after 1 hr by ELISA | 2017 | European journal of medicinal chemistry, Jul-28, Volume: 135 | The discovery of novel benzothiazinones as highly selective non-ATP competitive glycogen synthase kinase 3β inhibitors for the treatment of ovarian cancer. |
| AID384204 | Cytotoxicity against human NCI-H661 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1891326 | Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay | 2022 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 66 | Discovery and preclinical evaluations of WX-0593, a novel ALK inhibitor targeting crizotinib-resistant mutations. |
| AID383633 | Cytotoxicity against human COLO 320DM cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID778820 | Antiproliferative activity against human EBC1 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID383394 | Cytotoxicity against human 647-V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID384618 | Cytotoxicity against human MEL-HO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383888 | Cytotoxicity against human GP5d cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384201 | Cytotoxicity against human NCI-H596 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617244 | Inhibition of TRKA in pig PAE cells assessed as growth factor-induced autophosphorylation by sandwich ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1471737 | Antiproliferative activity against human NCI-H2228 cells after 72 hrs by MTT assay | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID384386 | Cytotoxicity against human OVSAYO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384843 | Cytotoxicity against human huH-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1267052 | Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| 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. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383939 | Cytotoxicity against human SK-MEL-30 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384619 | Cytotoxicity against human MEL-JUSO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID384616 | Cytotoxicity against human MDST8 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1678050 | Cytotoxicity against human HCC78 cells harboring SLC34A2-ROS1 incubated for 72 hrs by MTT assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID384200 | Cytotoxicity against human NCI-H522 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383588 | Cytotoxicity against human BE(2)-C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383111 | Inhibition of ALK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348150 | Inhibition of recombinant human GST-tagged ALK expressed in baculovirus expression system by Z'LYTE assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors. |
| AID383396 | Cytotoxicity against human 786-O cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384689 | Cytotoxicity against human HT 1080 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384628 | Cytotoxicity against human MKN28 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384886 | Cytotoxicity against human KYSE270 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1769650 | Inhibition of HDAC6 (unknown origin) | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID384401 | Cytotoxicity against human PC-9 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1274914 | Inhibition of recombinant human FGFR1 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383599 | Cytotoxicity against human BT-B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679489 | Inhibition of human ABL2 using EAIYAAPFAKKK as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID383650 | Cytotoxicity against human COR-L 23/CPR cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384184 | Cytotoxicity against human NCI-H2170 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383372 | Inhibition of Fyn | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1178252 | Antiproliferative activity against crizotinib-resistant mouse NIH/3T3 cells harboring EML4-ALK variant 1 after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1678047 | Inhibition of ALK G1202R mutant (unknown origin) using peptide substrate incubated for 60 mins in presence of ATP by HTRF assay | 2020 | Bioorganic & medicinal chemistry, 10-15, Volume: 28, Issue:20 | Fragment-based modification of 2,4-diarylaminopyrimidine derivatives as ALK and ROS1 dual inhibitors to overcome secondary mutants. |
| AID1267048 | Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID384396 | Cytotoxicity against human PA-TU-8988S cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384640 | Cytotoxicity against human NCI-H1299 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556687 | Antiproliferative activity against mouse BAF3 cells expressing CD74/ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay | |||
| AID384172 | Cytotoxicity against human U2 OS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424967 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | 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. |
| 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. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1395248 | Antiproliferative activity against human EBC1 cells at 1 uM after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID1419633 | Inhibition of wild type EML4/ALK 1151Tins mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| 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. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1570565 | Inhibition of N-terminal NH-tagged and avi-tagged dephosphorylated c-MET D1228V mutant (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
| AID1889932 | Inhibition of ALK (unknown origin) | 2022 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 63 | Pyrizolo[1,5-a]pyrimidine derivatives of the second-generation TRK inhibitor: Design, synthesis and biological evaluation. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1680101 | Inhibition of CD74-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell viability | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
| AID384657 | Cytotoxicity against human NCI-H1793 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1679440 | Inhibition of human PYK2 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1769657 | Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424990 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID383938 | Cytotoxicity against human SK-MEL-3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1074708 | Efflux ratio of permeability from basolateral to apical side to apical to basolateral side of dog RRCK cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| 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. |
| AID1238088 | Inhibition of c-Met (unknown origin) at 100 uM | 2015 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 25, Issue:16 | Design and synthesis of novel substituted naphthyridines as potential c-Met kinase inhibitors based on MK-2461. |
| 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. |
| AID1201860 | Inhibition of recombinant c-Met (unknown origin) using poly (Glu,Tyr)4:1 substrate incubated for 60 mins by ELISA method | 2015 | European journal of medicinal chemistry, May-05, Volume: 95 | Enhancing the cellular anti-proliferation activity of pyridazinones as c-met inhibitors using docking analysis. |
| AID1419630 | Inhibition of wild type EML4/ALK L1196M mutant (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID384913 | Cytotoxicity against human ZR-75-1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1274910 | Inhibition of recombinant human RON at 100 nM using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624808 | Binding constant for TRKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384846 | Cytotoxicity against human IGR1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID617337 | Inhibition of TRKB | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID384164 | Cytotoxicity against human Takigawa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384370 | Cytotoxicity against human NUGC3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383925 | Cytotoxicity against human SCH cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1267031 | Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| 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. |
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384635 | Cytotoxicity against human MS751 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679453 | Inhibition of human JAK2 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1229120 | Antiproliferative activity against human SNU5 cells after 72 hrs | 2015 | ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5 | Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors. |
| AID384395 | Cytotoxicity against human PA-TU-8902 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1421259 | Antiproliferative activity against human A549 cells after 72 hrs by MTT assay | |||
| AID1267044 | Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID1679457 | Inhibition of human IR using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383923 | Cytotoxicity against human SCaBER cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384623 | Cytotoxicity against human MFE280 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383930 | Cytotoxicity against human SiHa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351342 | Antiproliferative activity against human SU-DHL1 cells harboring NPM-ALK after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID384408 | Cytotoxicity against human RERF-LC-Ad2 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1421255 | Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay | |||
| AID384644 | Cytotoxicity against human NCI-H1568 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383594 | Cytotoxicity against human BIC1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384438 | Cytotoxicity against human MCF-7/ADR cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1425132 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1274897 | Inhibition of recombinant c-Met (unknown origin) using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| 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. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384376 | Cytotoxicity against human OE21 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383886 | Cytotoxicity against human GMS10 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384398 | Cytotoxicity against human PC14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384420 | Cytotoxicity against human S-117 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384159 | Cytotoxicity against human T.Tn cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384144 | Cytotoxicity against human SW1463 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384195 | Cytotoxicity against human NCI-H322 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1186991 | Cytotoxicity against human HepG2 cells assessed as cell viability at 1 uM after 4 hrs by Cell-Titer Glo assay | 2014 | Journal of medicinal chemistry, Oct-09, Volume: 57, Issue:19 | Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants. |
| AID383904 | Cytotoxicity against human HCC44 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383379 | Inhibition of PKBeta | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624937 | Binding constant for FLT3(ITD) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384390 | Cytotoxicity against human Panc03.27 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1580397 | Binding affinity to human MLKL by kinome scan based method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID383590 | Cytotoxicity against human BEN cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1274915 | Inhibition of recombinant human IGF1R using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID384676 | Cytotoxicity against human HMVII cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1348633 | Inhibition of human GST-tagged c-MET using KKKSPGEYVNIEFG as substrate preincubated for 20 mins followed by [gamma-33P]ATP addition and measured after 2 hrs by filter-binding assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID1556689 | Induction of apoptosis in ALK-addicted human NCI-H3122 cells at IC50 incubated for 48 hrs by Annexin V-FITC/propidium iodide staining-based flow cytometric analysis (Rvb = 9.82%) | |||
| AID759249 | Ratio of IC50 for cMET Y1230C mutant (unknown origin) to IC50 for wild type cMET (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
| AID384435 | Cytotoxicity against human M14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1070236 | Inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate in presence of 700 uM ATP | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID1074736 | Ratio of IC50 for human EML4-fused ALK C1156Y mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1348151 | Inhibition of recombinant human GST-tagged ROS1 expressed in baculovirus expression system by Z'LYTE assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis, biological evaluation and molecular modeling of novel 2-amino-4-(1-phenylethoxy) pyridine derivatives as potential ROS1 inhibitors. |
| AID384877 | Cytotoxicity against human KP3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1070237 | Competitive inhibition of recombinant wild type ALK catalytic domain (1064 to 1427) (unknown origin) expressed in baculovirus expression system using ARDIYRASFFRKGGCAMLPVK as substrate in presence of 1000 uM ATP | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1330644 | Antitumor activity against non-small cell lung cancer cells harboring ROS1 rearrangement in patient assessed as disease control rate after 8 weeks | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID1302005 | Induction of conformational changes in human ALK (1084 to 1410 residues) expressed in baculovirus infected Sf21 insect cells | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8 | Pyrazolylamine Derivatives Reveal the Conformational Switching between Type I and Type II Binding Modes of Anaplastic Lymphoma Kinase (ALK). |
| 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. |
| 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. |
| AID383652 | Cytotoxicity against human DAN-G cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383613 | Cytotoxicity against human CAL29 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384381 | Cytotoxicity against human OVCAR5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384678 | Cytotoxicity against human HOS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID460491 | Inhibition of recombinant c-Met by TR-FRET assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4 | Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors. |
| AID383651 | Cytotoxicity against human COR-L23 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383368 | Inhibition of Sky | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID617225 | Inhibition of human recombinant c-MET kinase expressed in A549 cells assessed as inhibition of HGF-induced autophosphorylation by ELISA method | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID759242 | Antitumor activity against human KARPAS299 xenograft model assessed as tumor growth inhibition at 50 mg/kg qd | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
| 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. |
| AID1191200 | Inhibition of ROS1 (unknown origin) incubated for 20 mins followed by [33P]ATP addition measured after 120 mins by HotSpot assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1312455 | Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1679475 | Inhibition of human EPHA2 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID460492 | Inhibition of recombinant KDR by TR-FRET assay | 2010 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4 | Discovery of 6-benzyloxyquinolines as c-Met selective 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. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624805 | Binding constant for RSK3(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679488 | Inhibition of human ACK1 using EAIYAAPFAKKK as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384166 | Cytotoxicity against human TCO1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1610122 | Antiproliferative activity against human KARPAS299 cells expressing NMP-ALK assessed as reduction in cell viability incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1074745 | Inhibition of human recombinant ALK L1196M mutant kinase domain (amino acids 1093 to 1141) expressed in baculovirus using 5'FAM-KKSRGDYMTMQIG-CONH2 as substrate incubated for 15 mins prior to Km levels of ATP addition measured after 1 hr by microfluidic m | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID384899 | Cytotoxicity against human LN229 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID778855 | Antitumor activity against mouse NIH/3T3 cells expressing TPR/Met allografted in mouse assessed as tumor growth inhibition at 50 mg/kg, po qd administered for 2 weeks measured twice per week relative to vehicle-treated control | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1137580 | Inhibition of recombinant EGFR L858R mutant (unknown origin) using poly-GT peptide as substrate after 1 hr by Transcreener assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID384655 | Cytotoxicity against human NCI-H1781 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID759248 | Ratio of IC50 for cMET Y1230H mutant (unknown origin) to IC50 for wild type cMET (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1673943 | Antiproliferative activity against human NCI-H3122-CR1 cells harboring ALK L1196M mutant after 72 hrs by CellTiter-Glo assay | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19 | Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| AID384442 | Cytotoxicity against human MDA-MB-231 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1580405 | Ratio of binding affinity to human RIPK1 to human MLKL by kinome scan based method | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. |
| AID1419635 | Inhibition of L1196M mutant (unknown origin) | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID678094 | Antiproliferative activity against human EBC1 cells expressing elevated levels of constitutively active c-Met after 72 hrs by SRB assay | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
| AID384371 | Cytotoxicity against human NUGC4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384402 | Cytotoxicity against human PL45 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384900 | Cytotoxicity against human LN405 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074709 | Inhibition of human EML4-fused ALK L1196M mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384374 | Cytotoxicity against human OCUM1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679429 | Inhibition of human TYK1 using EAIYAAPFAKKK as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1274923 | Inhibition of recombinant human EPH-A2 using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID383863 | Cytotoxicity against human DV 90 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1395247 | Antiproliferative activity against human MKN45 cells at 1 uM after 72 hrs by Cell Titer-Glo assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1553337 | Cytotoxicity against patient-derived GBM cells assessed as LDH release after 96 hrs by spectrophotometric method | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID778819 | Antiproliferative activity against human NCI-H661 cells after 72 hrs | 2013 | Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21 | Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors. |
| AID1350813 | Antiproliferative activity against mouse BAF3 cells after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679428 | Inhibition of human TYRO3 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421261 | Inhibition of human N-terminal GST-tagged ALK cytoplasmic domain (1058 to 1620 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | |||
| AID384878 | Cytotoxicity against human KP-3L cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1267051 | Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1679479 | Inhibition of human c-MET using KKKSPGEYVNIEFG as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| 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. |
| AID384385 | Cytotoxicity against human OVMIU cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384641 | Cytotoxicity against human NCI-H1435 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625058 | Binding constant for VRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384151 | Cytotoxicity against human SW900 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383391 | Cytotoxicity against human 273T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384681 | Cytotoxicity against human Hs 257.T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1261790 | Inhibition of gatekeeper ALK L1196M mutant (unknown origin) using poly (Glu, Tyr)4:1 substrate incubated for 60 mins by ELISA | 2015 | European journal of medicinal chemistry, Nov-13, Volume: 105 | Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study. |
| AID1679443 | Inhibition of human PEAK1 using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID384880 | Cytotoxicity against human KPL1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384687 | Cytotoxicity against human Hs 746T cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384137 | Cytotoxicity against human SVG p12 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1421258 | Antiproliferative activity against mouse BAF3 cells harboring G1202R mutation after 72 hrs by MTT assay | |||
| 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. |
| AID384427 | Cytotoxicity against human LS180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383647 | Cytotoxicity against human COLO 824 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1556659 | Inhibition of recombinant human N-terminal GST-tagged ALK (catalytic domain 1058 - 1620 residues) expressed in baculovirus system assessed as decrease in substrate phosphorylation using TK peptide as substrate at 1 uM preincubated with enzyme for 30 mins | |||
| AID383582 | Cytotoxicity against human AGS cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1419625 | Inhibition of wild type EML4/ALK (unknown origin) expressed in NIH/3T3 cells | 2017 | European journal of medicinal chemistry, Jul-07, Volume: 134 | First macrocyclic 3 |
| AID1550985 | Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID1425032 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1471774 | Inhibition of ALK in human H2228 cells assessed as decrease in AKT phosphorylation at 0.5 uM after 3 hrs by Western blot method | 2017 | Journal of medicinal chemistry, 11-22, Volume: 60, Issue:22 | Identification of 4-Phenoxyquinoline Based Inhibitors for L1196M Mutant of Anaplastic Lymphoma Kinase by Structure-Based Design. |
| AID1074734 | Ratio of IC50 for human EML4-fused ALK G1269A mutant to IC50 for human wild type EML4-fused ALK expressed in mouse NIH-3T3 cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1697359 | Binding affinity to recombinant wild-type ERK3 (9 to 327 residues) (unknown origin) expressed in Escherichia coli by microscale thermophoresis assay | 2020 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 30, Issue:22 | Biochemical, cellular and structural characterization of novel and selective ERK3 inhibitors. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1679452 | Inhibition of human KHS using MBP as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1876069 | Antiviral activity against EV-A71 at 10 uM relative to control | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2 | Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1679423 | Inhibition of GLK (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625000 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624722 | Binding constant for MKK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384202 | Cytotoxicity against human NCI-H630 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1626852 | Binding affinity to MET (unknown origin) by isothermal titration calorimetry | 2016 | Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15 | Discovery and Pharmacokinetic and Pharmacological Properties of the Potent and Selective MET Kinase Inhibitor 1-{6-[6-(4-Fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylsulfanyl]benzothiazol-2-yl}-3-(2-morpholin-4-ylethyl)urea (SAR125844). |
| 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. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1137587 | Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| AID1769654 | Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | Discovery of 2,4-pyrimidinediamine derivatives as potent dual inhibitors of ALK and HDAC. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1691166 | Protac activity at VHL/EML4-ALK G1202R mutant fusion protein (unknown origin) expressed in HEK293T cells assessed as inhibition of cell growth | 2020 | European journal of medicinal chemistry, May-01, Volume: 193 | Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance. |
| AID617229 | Binding affinity to human recombinant c-MET assessed as inhibition of autophosphorylation by continuous fluorometric assay | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1137584 | Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors. |
| 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. |
| AID383640 | Cytotoxicity against human COLO 320 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384850 | Cytotoxicity against human IHH4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID642894 | Cytotoxicity against human Kelly cells expressing ALK F1174L mutant | 2011 | ACS medicinal chemistry letters, May-12, Volume: 2, Issue:5 | Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors. |
| AID384199 | Cytotoxicity against human NCI-H520 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1625292 | Inhibition of E6a/b;A20 EML4-ALK (unknown origin) expressed in human NCI-H2228 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1178254 | Antiproliferative activity against crizotinib-resistant human Kelly cells harboring ALK F1174L mutant after 72 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1 | Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases. |
| AID1191201 | Inhibition of ALK (unknown origin) incubated for 20 mins followed by [33P]ATP addition measured after 120 mins by HotSpot assay | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Synthesis and biological evaluation of new pyrazol-4-ylpyrimidine derivatives as potential ROS1 kinase inhibitors. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID383901 | Cytotoxicity against human HCC1954 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383602 | Cytotoxicity against human C170 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383913 | Cytotoxicity against human HeLa cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383386 | Cytotoxicity against human 1321N cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1274922 | Inhibition of recombinant human c-Src using poly (Glu,Tyr)4:1 as substrate after 60 mins by ELISA | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Pyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase. |
| AID384406 | Cytotoxicity against human RERF-GC-1B cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1348649 | Antiproliferative activity against human SGC7901 cells after 72 hrs by Alamarblue assay relative to control | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1310804 | Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID384417 | Cytotoxicity against human RT112/84 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1325416 | Antiproliferative activity against ALK constitutively activated human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 11-15, Volume: 26, Issue:22 | Metabolism-based structure optimization: Discovery of a potent and orally available tyrosine kinase ALK inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| AID1312452 | Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | An orally available tyrosine kinase ALK and RET dual inhibitor bearing the tetracyclic benzo[b]carbazolone core. |
| 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. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID678093 | Inhibition of c-Met incubated for 60 mins at spectrophotometry | 2012 | Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17 | Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors. |
| AID383628 | Cytotoxicity against human CL14 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384902 | Cytotoxicity against human VMRC-RCZ cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384884 | Cytotoxicity against human KYSE180 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1310802 | Inhibition of human IGF1R using KKKSPGEYVNIEFG as substrate and [gamma-33P]ATP measured after 1 hr | 2016 | Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10 | Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. |
| AID1550980 | Cytotoxicity against human NCI-H2228 cells incubated for 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jun-01, Volume: 171 | Discovery of novel mutant-combating ALK and ROS1 dual inhibitors bearing imidazolidin-2-one moiety with reasonable PK properties. |
| AID383605 | Cytotoxicity against human C-4 I cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384155 | Cytotoxicity against human SW756 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1330640 | Inhibition of EGFR (unknown origin) using peptide as substrate after 60 mins by HTRF assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID383902 | Cytotoxicity against human HCC366 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383615 | Cytotoxicity against human CAL54 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384387 | Cytotoxicity against human OVTOKO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID383400 | Cytotoxicity against human A2058 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1074717 | Intrinsic absorptive permeability from apical to basolateral side of dog RRCK cells | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| AID1679468 | Inhibition of human EPHB1 using poly[Glu:Tyr] (4:1) as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID1070241 | Inhibition of NPM/ALK (unknown origin) transfected in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by [3H]-thymidine incorporation assay | 2014 | Bioorganic & medicinal chemistry, Feb-15, Volume: 22, Issue:4 | Synthesis and biological evaluation of benzo[4,5]imidazo[1,2-c]pyrimidine and benzo[4,5]imidazo[1,2-a]pyrazine derivatives as anaplastic lymphoma kinase inhibitors. |
| AID384389 | Cytotoxicity against human Panc02.03 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1570564 | Inhibition of wild type N-terminal NH-tagged and avi-tagged dephosphorylated c-MET (956 to 1390 residues) (unknown origin) expressed in sf21 cells using poly (Glu,Tyr) as substrate measured after 60 mins by ADP-Glo kinase assay | 2019 | ACS medicinal chemistry letters, Sep-12, Volume: 10, Issue:9 | Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors. |
| AID1425139 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID1553329 | Synergistic antiproliferative activity against patient-derived GBM cells assessed as cell viability after 48 hrs in presence of temozolomide by 5-Ethynyl-2'-deoxyuridine incorporation assay | 2019 | Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18 | The synthesis of a novel Crizotinib heptamethine cyanine dye conjugate that potentiates the cytostatic and cytotoxic effects of Crizotinib in patient-derived glioblastoma cell lines. |
| AID1267047 | Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23 | Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1700686 | Inhibition of human ALK L1196M mutant expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay | 2020 | Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22 | Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384898 | Cytotoxicity against human LN18 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679485 | Inhibition of human Aurora A using [H-LRRASLG] as substrate at 0.5 uM by [gamma-33P]-ATP assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1544432 | Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr | 2019 | Bioorganic & medicinal chemistry letters, 06-15, Volume: 29, Issue:12 | Design, synthesis and structure-activity relationship study of aminopyridine derivatives as novel inhibitors of Janus kinase 2. |
| AID384375 | Cytotoxicity against human OE19 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384668 | Cytotoxicity against human NCI-H2085 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1625286 | Cytotoxicity against human NB39 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12 | Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID1350818 | Inhibition of NPM-fused ALK (unknown origin) expressed in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by CellTiter-Glo assay | 2017 | European journal of medicinal chemistry, Oct-20, Volume: 139 | Discovery of N-(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425150 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367 | The target landscape of clinical kinase drugs. |
| AID383398 | Cytotoxicity against human 8505C cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1679861 | Inhibition of GLK (unknown origin) transfected in human 293T cells co-transfected with GFP-fused PKCtheta assessed as reduction in PKCtheta phosphorylation by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10 | Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity. |
| AID758042 | Cytotoxicity against human KARPAS299 cells after 2 to 3 days by luciferase reporter gene assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14 | Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam |
| AID1074715 | Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA | 2014 | Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4 | Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib. |
| 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. |
| AID384185 | Cytotoxicity against human NCI-H2172 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1504744 | Antiproliferative activity against human NCI-H2228 cells harboring EML4-ALK after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R. |
| AID1330636 | Inhibition of ALK (unknown origin) using peptide as substrate after 60 mins by HTRF assay | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Design, synthesis and biological evaluation of novel 4-arylaminopyrimidine derivatives possessing a hydrazone moiety as dual inhibitors of L1196M ALK and ROS1. |
| AID1421263 | Inhibition of human N-terminal GST-tagged ROS cytoplasmic domain (1883 to 2347 residues) expressed in baculovirus expression system after 1 hr by mobility shift assay | |||
| 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. |
| AID617345 | Inhibition of LCK at 1 uM | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID383609 | Cytotoxicity against human Caki1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1680100 | Inhibition of ALK L1196M mutant (unknown origin) | 2018 | ACS medicinal chemistry letters, Sep-13, Volume: 9, Issue:9 | Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib. |
| AID383918 | Cytotoxicity against human HeLa TG cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383643 | Cytotoxicity against human SNU16 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384680 | Cytotoxicity against human HRT18 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384139 | Cytotoxicity against human SW1088 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1351349 | Antiproliferative activity against mouse BAF3 cells harboring CD74-ROS1 G2032R mutant after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| AID384912 | Cytotoxicity against human YKG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384910 | Cytotoxicity against human WM793b cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID384203 | Cytotoxicity against human NCI-H647 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383882 | Cytotoxicity against human G401 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384156 | Cytotoxicity against human SW837 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID384685 | Cytotoxicity against human Hs 683 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50 | Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID624979 | Binding constant for ABL1(F317I)-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| AID1351347 | Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 after 72 hrs by SRB or CCK8 assay | 2018 | European journal of medicinal chemistry, Jan-20, Volume: 144 | Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID625082 | Binding constant for RSK4(Kin.Dom.2-C-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11 | Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC 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. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID686947 | qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen | 2013 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15 | Identification of potent Yes1 kinase inhibitors using a library screening approach. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1797738 | AR Transcriptional Activation Assay and MDA Whole-Cell Binding Assay from Article 10.1021/jm070231h: \\Substituted 6-(1-Pyrrolidine)quinolin-2(1H)-ones as Novel Selective Androgen Receptor Modulators.\\ | 2007 | Journal of medicinal chemistry, Oct-18, Volume: 50, Issue:21 | Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators. |
| AID1802323 | Kinobeads Competition Assay from Article 10.1021/acschembio.6b00709: \\Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.\\ | 2016 | ACS chemical biology, 12-16, Volume: 11, Issue:12 | Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs. |
| AID1801605 | c-Met Z-LYTE Assay from Article 10.1016/j.bioorg.2016.02.009: \\Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.\\ | 2016 | Bioorganic chemistry, Apr, Volume: 65 | Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors. |
| AID1801606 | ALK HTRF Assays from Article 10.1016/j.bioorg.2016.02.009: \\Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors.\\ | 2016 | Bioorganic chemistry, Apr, Volume: 65 | Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine derivatives as c-Met inhibitors. |
| 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. |
| 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. |
| AID1345550 | Human ALK receptor tyrosine kinase (Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family) | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1345540 | Human MET proto-oncogene, receptor tyrosine kinase (Type X RTKs: HGF (hepatocyte growth factor) receptor family) | 2011 | Journal of medicinal chemistry, Sep-22, Volume: 54, Issue:18 | Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). |
| AID1345540 | Human MET proto-oncogene, receptor tyrosine kinase (Type X RTKs: HGF (hepatocyte growth factor) receptor family) | 2011 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15 | Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition. |
| [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 | 5 (0.29) | 29.6817 |
| 2010's | 1244 (71.37) | 24.3611 |
| 2020's | 494 (28.34) | 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 (68.38) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 112 (6.29%) | 5.53% |
| Reviews | 226 (12.70%) | 6.00% |
| Case Studies | 450 (25.28%) | 4.05% |
| Observational | 12 (0.67%) | 0.25% |
| Other | 980 (55.06%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| Molecular Analysis for Therapy Choice (MATCH) [NCT02465060] | Phase 2 | 6,452 participants (Anticipated) | Interventional | 2015-08-17 | Active, not recruiting | ||
| Phase II Trial of Adjuvant Crizotinib in High-Risk Uveal Melanoma Following Definitive Therapy [NCT02223819] | Phase 2 | 34 participants (Actual) | Interventional | 2015-03-31 | Completed | ||
| Randomized Multicenter Phase III Open-Label Study to Evaluate and Compare the Efficacy and Safety of XZP-3621 Versus Crizotinib in Chinese Patients With Treatment-Naive Anaplastic Lymphoma Kinase-Positive Advanced Non-Small Cell Lung Cancer [NCT05204628] | Phase 3 | 238 participants (Anticipated) | Interventional | 2022-02-07 | Not yet recruiting | ||
| MATCH Treatment Subprotocol G: Phase II Study of Crizotinib in Patients With ROS1 Translocations (Other Than Patients With Non-Small Cell Lung Cancer) [NCT04439253] | Phase 2 | 4 participants (Actual) | Interventional | 2015-08-12 | Active, not recruiting | ||
| A PHASE 1, OPEN-LABEL, CROSSOVER STUDY TO ESTABLISH BIOEQUIVALENCE OF AN ENCAPSULATED MICROSPHERE FORMULATION (eMS) TO THE FORMULATED CAPSULE (FC) OF CRIZOTINIB IN HEALTHY ADULT PARTICIPANTS [NCT04856293] | Phase 1 | 25 participants (Actual) | Interventional | 2021-04-16 | Completed | ||
| A Phase 1, Open-label, Single Dose Study To Evaluate The Effects Of Food And The Proton Pump Inhibitor, Esomeprazole, On The Pharmacokinetics Of Crizotinib In A Coated Microsphere Formulation In Adult Healthy Volunteers [NCT03137134] | Phase 1 | 18 participants (Actual) | Interventional | 2017-06-20 | Completed | ||
| Phase Ib, Open-label, Multicenter, Dose-escalation Study Followed by an Extension Phase to Evaluate the Safety and Activity of the Combination of Crizotinib With Temozolomide and Radiotherapy in Patients With Newly Diagnosed Glioblastoma [NCT02270034] | Phase 1 | 38 participants (Actual) | Interventional | 2014-08-13 | Completed | ||
| MATCH Treatment Subprotocol F: Crizotinib in Patients With Tumors (Other Than Adenocarcinoma of Lung or ALCL) With ALK Rearrangements [NCT04439266] | Phase 2 | 5 participants (Actual) | Interventional | 2015-08-12 | Active, not recruiting | ||
| Crizotinib in Pretreated Metastatic Non-small-cell Lung Cancer With MET Amplification or MET Exon 14 Mutation or ROS1 Translocation (METROS) [NCT02499614] | Phase 2 | 80 participants (Anticipated) | Interventional | 2014-12-31 | Recruiting | ||
| A Pilot Study of Crizotinib in Patients With c-MET Positive Gastric Adenocarcinoma as a Third-line Chemotherapy [NCT02435108] | Phase 2 | 2 participants (Actual) | Interventional | 2014-05-15 | Completed | ||
| A PHASE 1B STUDY OF CRIZOTINIB IN COMBINATION WITH PEMBROLIZUMAB (MK-3475) IN PATIENTS WITH UNTREATED ADVANCED ALK-TRANSLOCATED NON SMALL CELL LUNG CANCER [NCT02511184] | Phase 1 | 9 participants (Actual) | Interventional | 2015-10-31 | Terminated(stopped due to Decision based on the low enrollment mainly due to high efficacy drugs available in 1st line ALK-positive NSCLC (eg alectinib), not due to any safety concerns) | ||
| A Phase IB Study of Crizotinib (XALKORI) and Sunitinib (SUTENT) in Metastatic Breast Cancer [NCT02074878] | Phase 1 | 3 participants (Actual) | Interventional | 2014-06-30 | Terminated(stopped due to Poor accrual so the study was halted on May 16, 2017.) | ||
| AN OPEN-LABEL, SINGLE-ARM STUDY OF THE LONG-TERM SAFETY OF XALKORI (REGISTERED) IN PATIENTS FROM CHINA WITH ADVANCED NON-SMALL CELL LUNG CANCER (NSCLC) HARBORING A TRANSLOCATION OR INVERSION EVENT INVOLVING THE ANAPLASTIC LYMPHOMA KINASE (ALK) OR ROS1 LOC [NCT03672643] | Phase 4 | 41 participants (Actual) | Interventional | 2019-01-28 | Terminated(stopped due to The trial is terminated based on business decision, not due to safety concerns or regulatory requirements.) | ||
| SPECIAL INVESTIGATION OF XALKORI FOR NSCLC (REGULATORY POST MARKETING COMMITMENT PLAN) [NCT01597258] | 2,029 participants (Actual) | Observational | 2012-05-29 | Completed | |||
| N-of-1 Trial of Actionable Target Identification in Metastatic Cancer for Palliative Systemic Therapy [NCT02142036] | Phase 2 | 50 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| AcSé CRIZOTINIB : Secured Access to Crizotinib for Patients With Tumors Harboring a Genomic Alteration on One of the Biological Targets of the Drug. [NCT02034981] | Phase 2 | 246 participants (Actual) | Interventional | 2013-08-31 | Active, not recruiting | ||
| A Randomized Phase III Trial for Surgically Resected Early Stage Non-small Cell Lung Cancer: Crizotinib Versus Observation for Patients With Tumors Harboring the Anaplastic Lymphoma Kinase (ALK) Fusion Protein [NCT02201992] | Phase 3 | 168 participants (Anticipated) | Interventional | 2015-03-23 | Recruiting | ||
| LCI-GU-URO-CRI-001: A Phase II Study of Crizotinib in Patients With c-MET or RON-Positive Metastatic Urothelial Cancer [NCT02612194] | Phase 2 | 8 participants (Actual) | Interventional | 2016-09-27 | Terminated(stopped due to Study closed to accrual due to low accrual numbers.) | ||
| A Randomized Phase 2 Trial of Brentuximab Vedotin (SGN35, NSC# 749710), or Crizotinib (NSC#749005, Commercially Labeled) in Combination With Chemotherapy for Newly Diagnosed Patients With Anaplastic Large Cell Lymphoma (ALCL) [NCT01979536] | Phase 2 | 137 participants (Actual) | Interventional | 2013-11-13 | Active, not recruiting | ||
| A Dutch National Study on Behalf of the CPCT to Facilitate Patient Access to Commercially Available, Targeted Anti-cancer Drugs to Determine the Potential Efficacy in Treatment of Advanced Cancers With a Known Molecular Profile [NCT02925234] | Phase 2 | 1,550 participants (Anticipated) | Interventional | 2016-08-31 | Recruiting | ||
| A Study In Trained Taste Panel Healthy Adult Volunteers To Investigate The Palatability Of Select Formulations Of Crizotinib Oral Liquid [NCT01125904] | Phase 1 | 5 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
| A Phase 1 Study of Crizotinib in Combination With Enzalutamide in Metastatic Castration-resistant Prostate Cancer Before or After Progression on Docetaxel. [NCT02207504] | Phase 1 | 24 participants (Actual) | Interventional | 2014-08-31 | Completed | ||
| A Biomarker-Driven Protocol for Previously Treated ALK-Positive Non-Squamous NSCLC Patients: The NCI-NRG ALK Protocol [NCT03737994] | Phase 2 | 10 participants (Actual) | Interventional | 2019-07-25 | Active, not recruiting | ||
| Targeted Therapy in Children and Adolescents With Recurrent, Progressive and Unresectable Inflammatory Myofibroblastic Tumor With the Inhibitor of Tyrosine Kinase -Crizotinib [NCT03874273] | Phase 2/Phase 3 | 25 participants (Anticipated) | Interventional | 2019-02-01 | Recruiting | ||
| Single-arm, Multi-center Clinical Study of Crizotinib Combined With Etoposide Capsule Followed by Auto-HSCT for Relapsed and Refractory Anaplastic Lymphoma Kinase (ALK)-Positive Anaplastic Large Cell Lymphoma (ALCL) [NCT03707847] | Phase 4 | 20 participants (Anticipated) | Interventional | 2018-10-01 | Recruiting | ||
| EUCROSS: A Phase II Trial to Evaluate Efficacy and Safety of Crizotinib Treatment in Advanced Adenocarcinoma of the Lung Harbouring ROS1 Translocations [NCT02183870] | Phase 2 | 34 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
| A Multicenter Prospective Study of Treatment ALK(+) Systemic Anaplastic Large Cell Lymphoma With Crizotinib [NCT02487316] | Phase 4 | 0 participants (Actual) | Interventional | 2015-07-31 | Withdrawn | ||
| A Phase IB/II Study of Lorlatinib Combinations in Anaplastic Lymphoma Kinase-Rearranged Lung Cancer [NCT04292119] | Phase 1/Phase 2 | 96 participants (Anticipated) | Interventional | 2020-05-01 | Recruiting | ||
| A Phase 1/2 Study of Crizotinib, an Oral Small Molecule Inhibitor of Anaplastic Lymphoma Kinase (ALK) and C-Met, in Children With Relapsed/Refractory Solid Tumors and Anaplastic Large Cell Lymphoma [NCT00939770] | Phase 1/Phase 2 | 122 participants (Actual) | Interventional | 2009-09-21 | Completed | ||
| Canadian Profiling and Targeted Agent Utilization Trial (CAPTUR): A Phase II Basket Trial [NCT03297606] | Phase 2 | 720 participants (Anticipated) | Interventional | 2018-03-23 | Recruiting | ||
| Phase II Trial of Crizotinib in c-MET Mutation Metastatic/Recurrent/Persistent Endometrial Cancer [NCT04030429] | Phase 2 | 40 participants (Anticipated) | Interventional | 2019-09-01 | Recruiting | ||
| Modular Phase 1B Hypothesis-Testing, Biomarker-Driven, Talazoparib Combination Trial (TalaCom) [NCT04693468] | Phase 1 | 111 participants (Anticipated) | Interventional | 2020-12-01 | Recruiting | ||
| A PHASE 1B/2, OPEN-LABEL, DOSE-FINDING STUDY TO EVALUATE SAFETY, EFFICACY, PHARMACOKINETICS AND PHARMACODYNAMICS OF AVELUMAB (MSB0010718C) IN COMBINATION WITH EITHER CRIZOTINIB OR PF-06463922 IN PATIENTS WITH ADVANCED OR METASTATIC NON-SMALL CELL LUNG CAN [NCT02584634] | Phase 1/Phase 2 | 43 participants (Actual) | Interventional | 2015-12-18 | Terminated(stopped due to The study was terminated since there was no need for further safety or efficacy data to be collected. The participants having benefit from the Investigational treatments have been moved to a continuation study (NCT05059522)) | ||
| A Randomized, Phase II Efficacy Assessment of Multiple MET Kinase Inhibitors (Cabozantinib [NSC #761968], Crizotinib [NSC #749005], Savolitinib [NSC #785348], and Sunitinib [NSC #736511]) in Metastatic Papillary Renal Carcinoma (PAPMET) [NCT02761057] | Phase 2 | 152 participants (Actual) | Interventional | 2016-04-05 | Active, not recruiting | ||
| Crizotinib (Xalkori (Registered)) Expanded Access Protocol For The Treatment Of Japanese Patients With Advanced Non-small Cell Lung Cancer (Nsclc) Harboring A Translocation Or Inversion Involving The Ros1 Oncogene [NCT02824094] | 0 participants | Expanded Access | No longer available | ||||
| A Multicentre, Open-label, Randomised, Controlled Study of Molecularly Precision Target Therapy Based on Tumor Molecular Profiling With GEMOX in Advanced or Recurrent Extrahepatic Cholangiocarcinoma and Gallbladder Carcinoma [NCT02836847] | Phase 2 | 152 participants (Anticipated) | Interventional | 2016-07-31 | Recruiting | ||
| Genomics-Based Target Therapy for Children With Relapsed or Refractory Malignancy [NCT02638428] | Phase 2 | 90 participants (Anticipated) | Interventional | 2015-12-31 | Recruiting | ||
| Randomized, Open Label, Multicenter, Phase III Study of Entrectinib Versus Crizotinib in Patients With Locally-Advanced or Metastatic Non-Small Cell Lung Cancer Harboring ROS1 Gene Rearrangements With and Without Central Nervous System Metastases [NCT04603807] | Phase 3 | 220 participants (Anticipated) | Interventional | 2021-09-30 | Recruiting | ||
| A Multi-centered, Randomized, Open-label Phase III Study to Evaluate the Efficacy and Safety of TGRX-326 Comparing With Crizotinib in Patients of Advanced ALK-positive or Metastatic Non-Small Cell Lung Cancer [NCT06082635] | Phase 3 | 297 participants (Anticipated) | Interventional | 2023-11-30 | Not yet recruiting | ||
| CRIZOTINIB (XALKORI(REGISTERED)) EXPANDED ACCESS PROTOCOL FOR THE TREATMENT OF ADULT OR PEDIATRIC PATIENTS WITH SOLID OR HEMATOLOGIC MALIGNANCIES THAT HARBOR A CRIZOTINIB-SENSITIVE MOLECULAR ALTERATION BUT WHO ARE UNABLE TO SWALLOW CRIZOTINIB CAPSULES [NCT02473497] | 0 participants | Expanded Access | Available | ||||
| Personalized Adaptive Radiation Therapy With Individualized Systemic Targeted Therapy (PARTIST) for Locally Advanced, Non-small Cell Lung Cancer With Genomic Driver Mutations [NCT02277457] | Early Phase 1 | 0 participants (Actual) | Interventional | 2015-09-30 | Withdrawn | ||
| Pilot Study of Crizotinib in Relapsed ALK+ Lymphomas [NCT02419287] | Phase 2 | 12 participants (Actual) | Interventional | 2015-04-30 | Completed | ||
| A Multicenter, International, Rollover Study of Alectinib in Patients With Anaplastic Lymphoma Kinase (ALK)-Positive or Rearranged During Transfection (RET)-Positive Cancer [NCT03194893] | Phase 3 | 200 participants (Anticipated) | Interventional | 2017-07-05 | Recruiting | ||
| An Open-label, Randomized, Multicenter Phase 3 Study Comparing WX-0593 to Crizotinib in Anaplastic Lymphoma Kinase (ALK) Positive Non-Small Cell Lung Cancer (NSCLC) Patients [NCT04632758] | Phase 3 | 292 participants (Actual) | Interventional | 2019-06-01 | Active, not recruiting | ||
| A Phase 1, Fixed Sequence, Cross-Over Study To Estimate The Effect Of Multiple Dose Rifampin On The Single Dose Pharmacokinetics Of Crizotinib (PF-02341066) In Healthy Volunteers [NCT01147055] | Phase 1 | 15 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| Phase 2, Open-label Single Arm Study Of The Efficacy And Safety Of Pf-02341066 In Patients With Advanced Non-small Cell Lung Cancer (Nsclc) Harboring A Translocation Or Inversion Involving The Anaplastic Lymphoma Kinase (Alk) Gene Locus [NCT00932451] | Phase 2 | 1,069 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Phase II Study of ROS1 Targeting With Crizotinib in Advanced E-cadherin Negative, ER Positive Lobular Breast Cancer, Diffuse Gastric Cancer, Triple Negative Lobular Breast Cancer or CDH1-mutated Solid Tumours [NCT03620643] | Phase 2 | 58 participants (Anticipated) | Interventional | 2019-05-09 | Active, not recruiting | ||
| A Phase I Study of Crizotinib and Ganetespib (STA-9090) in ALK Positive Lung Cancers [NCT01579994] | Phase 1 | 13 participants (Actual) | Interventional | 2012-04-16 | Completed | ||
| PD-1 Immune Checkpoint Inhibitors and Immune-Related Adverse Events: a Cohort Study [NCT04115410] | 4,724 participants (Anticipated) | Observational | 2020-07-01 | Not yet recruiting | |||
| A Multicenter, Randomized, Open-label Study to Evaluate the Efficacy and Safety of TQ-B3139 Versus Crizotinib in the First Line Treatment of Subjects With Anaplastic Lymphoma Kinase (ALK) Positive Non-Small Cell Lung Cancer (NSCLC) [NCT04009317] | Phase 3 | 260 participants (Anticipated) | Interventional | 2019-08-13 | Recruiting | ||
| An Open-label, Multi-center, Phase II Umbrella Study to Assess Efficacy of Targeted Therapy or Immunotherapy Directed by Next Generation Sequencing (NGS) in Chinese Patients With Advanced NSCLC (TRUMP) [NCT03574402] | Phase 2 | 400 participants (Anticipated) | Interventional | 2018-07-09 | Recruiting | ||
| National Lung Matrix Trial: Multi-drug, Genetic Marker-directed, Non-comparative, Multi-centre, Multi-arm Phase II Trial in Non-small Cell Lung Cancer [NCT02664935] | Phase 2 | 423 participants (Actual) | Interventional | 2015-05-31 | Active, not recruiting | ||
| Phase II, Open Label, Single Arm Study of the Efficacy and Safety of Crizotinib in East Asian Patients With Advanced ALK-Negative NSCLC Harboring a Translocation or Inversion Involving the c-ROS Oncogene (ROS1) Locus [NCT01945021] | Phase 2 | 129 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
| Observational Study to IDEntify Patients With Advanced/Metastatic NSCLC and ALK and ROS1 Translocation and to Establish Their Therapeutic Management (IDEALK&ROS) [NCT02679170] | 141 participants (Actual) | Observational | 2016-06-29 | Completed | |||
| Explore the Relationship Between Single Nucleotide Polymorphisms and Crizotinib Response and Toxicity in Patients With Non-Small Cell Lung Cancer [NCT06062810] | Phase 2/Phase 3 | 600 participants (Anticipated) | Interventional | 2024-03-28 | Not yet recruiting | ||
| IDE196 (Darovasertib) in Combination With Crizotinib Versus Investigator's Choice of Treatment as First-line Therapy in HLA-A2 Negative Metastatic Uveal Melanoma (DAR-UM-2) [NCT05987332] | Phase 2/Phase 3 | 380 participants (Anticipated) | Interventional | 2023-10-31 | Recruiting | ||
| Evaluation of Combination Checkpoint Inhibitor Plus Targeted Inhibitor (Erlotinib or Crizotinib) for EGFR or ALK Mutated Stage IV Non-small Cell Lung Cancer: Phase Ib With Expansion Cohorts [NCT01998126] | Phase 1 | 14 participants (Actual) | Interventional | 2013-12-02 | Completed | ||
| A Phase 1, Open-label, Crossover Taste And Pharmacokinetic Study In Healthy Adult Volunteers To Evaluate The Palatability And Estimate The Bioavailability Of Three Prototype Formulations Of Crizotinib [NCT02006277] | Phase 1 | 21 participants (Actual) | Interventional | 2013-12-31 | Completed | ||
| A Real World Study to Evaluate the Efficacy and Safety of First Line Crizotinib in ALK Rearranged Advanced Non Squamous Non-small Cell Lung Cancer [NCT03647111] | 120 participants (Anticipated) | Observational | 2018-01-01 | Recruiting | |||
| Phase 1/2, Open Label, Randomized Study Of The Safety, Efficacy, And Pharmacokinetics Of Erlotinib With Or Without Pf 02341066 In Patients With Advanced Non Small Cell Adenocarcinoma Of The Lung. [NCT00965731] | Phase 1 | 27 participants (Actual) | Interventional | 2010-01-31 | Completed | ||
| Phase 3, Randomized, Open-label Study Of The Efficacy And Safety Of Pf-02341066 Versus Standard Of Care Chemotherapy (Pemetrexed Or Docetaxel) In Patients With Advanced Non-small Cell Lung Cancer (Nsclc) Harboring A Translocation Or Inversion Event Involv [NCT00932893] | Phase 3 | 347 participants (Actual) | Interventional | 2009-09-30 | Completed | ||
| Adjuvant Lung Cancer Enrichment Marker Identification and Sequencing Trial (ALCHEMIST) [NCT02194738] | 8,300 participants (Anticipated) | Interventional | 2014-09-26 | Recruiting | |||
| A Phase 1, Single Dose Bioequivalence And Food Effect Study In Healthy Volunteers Comparing The Commercial Image Capsules To The Immediate Release Tablets And Powder In Capsule Formulations Of Crizotinib (PF-02341066), And The Commercial Image Capsule In [NCT01154218] | Phase 1 | 36 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| A Phase 1, Open-label, Dose Escalation Study To Evaluate Safety, Pharmacokinetics And Pharmacodynamics Of Combined Oral C-met/Alk Inhibitor (Pf-02341066) And Pan-her Inhibitor (Pf-00299804) In Patients With Advanced Non-small Cell Lung Cancer [NCT01121575] | Phase 1 | 70 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| XALKORI ROS1+NSCLC DRUG USE INVESTIGATION [NCT03375242] | 100 participants (Anticipated) | Observational | 2017-10-25 | Recruiting | |||
| Open-label, Phase 2 Clinical Trial of Crizotinib for Children and Adults With Neurofibromatosis Type 2 and Progressive Vestibular Schwannomas [NCT04283669] | Phase 2 | 19 participants (Anticipated) | Interventional | 2020-02-18 | Active, not recruiting | ||
| Phase I Study of the Combination of Crizotinib and Dasatinib in Pediatric Research Participants With Diffuse Pontine Glioma (DIPG) and High-Grade Glioma (HGG) [NCT01644773] | Phase 1 | 36 participants (Actual) | Interventional | 2012-11-27 | Completed | ||
| A Phase 1 Study of Crizotinib in Combination With Conventional Chemotherapy for Relapsed or Refractory Solid Tumors or Anaplastic Large Cell Lymphoma [NCT01606878] | Phase 1 | 46 participants (Actual) | Interventional | 2013-04-29 | Completed | ||
| An International Phase 4 Field Study for Analyzing the Psychometric Properties of the Updated Module on Assessing Quality of Life of Patients With Lung Cancer (EORTC QLQ-LC29) [NCT02745691] | 523 participants (Actual) | Observational | 2016-04-01 | Completed | |||
| Phase II Study of Crizotinib for ROS1 and MET Activated Lung Cancer (CROME) [NCT04084717] | Phase 2 | 50 participants (Anticipated) | Interventional | 2019-12-03 | Recruiting | ||
| A Study of HSP90 Inhibitor AT13387 Alone and in Combination With Crizotinib in the Treatment of Non-small Cell Lung Cancer (NSCLC) [NCT01712217] | Phase 1/Phase 2 | 220 participants (Actual) | Interventional | 2012-10-31 | Completed | ||
| A Phase I, Single Dose, Parallel-Group Study To Evaluate The Pharmacokinetics Of Crizotinib (PF-02341066) In Subjects With Impaired Renal Function [NCT01419041] | Phase 1 | 16 participants (Actual) | Interventional | 2011-11-30 | Completed | ||
| Randomized, Multicenter, Phase III, Open-Label Study of Alectinib Versus Crizotinib in Asian Patients With Treatment-Naive Anaplastic Lymphoma Kinase-Positive Advanced Non-Small Cell Lung Cancer [NCT02838420] | Phase 3 | 187 participants (Actual) | Interventional | 2016-08-03 | Active, not recruiting | ||
| Molecular Characterization and Clinical Outcomes of ALK Tyrosine Kinase Inhibitors in ALK-rearranged Advanced Pure Squamous Cell Carcinoma [NCT05014464] | 5,927 participants (Actual) | Observational | 2013-10-03 | Completed | |||
| CONTINUING ACCESS TO THE TYROSINE KINASE INHIBITOR OF VEGFR-2, AG-013736 (A406) FOR PATIENTS PREVIOUSLY RECEIVING AG-013736 IN CLINICAL TRIALS [NCT00828919] | 52 participants (Actual) | Interventional | 2003-03-07 | Completed | |||
| Crizotinib Combined With Bevacizumab as First-line Therapy in Metastatic Lung Adenocarcinoma Cancer With ALK Translocation or MET Amplification or ROS1 Translocation (CAMAR) [NCT02946359] | Phase 2 | 60 participants (Anticipated) | Interventional | 2016-07-31 | Recruiting | ||
| "Cross-tumoral Phase 2 Clinical Trial Exploring Crizotinib (PF-02341066) in Patients With Advanced Tumors Induced by Causal Alterations of ALK and/or MET (CREATE)" [NCT01524926] | Phase 2 | 582 participants (Anticipated) | Interventional | 2012-09-30 | Completed | ||
| Randomized, Open-label, Multicenter, Phase 3 Trial of Repotrectinib Versus Crizotinib in Participants With Locally Advanced or Metastatic Tyrosine Kinase Inhibitor (TKI)-naïve ROS1-positive Non-Small Cell Lung Cancer (NSCLC) (TRIDENT-3) [NCT06140836] | Phase 3 | 230 participants (Anticipated) | Interventional | 2024-01-15 | Recruiting | ||
| A Real World Study to Evaluate the Efficacy and Safety of First Line Crizotinib in ROS1-rearranged Non-squamous Non-small Cell Lung Cancer [NCT03646994] | 40 participants (Anticipated) | Observational | 2018-08-01 | Recruiting | |||
| A Phase 1, Open Label, Dose Escalation, Single Oral Dose Study In Japanese Healthy Male Volunteers To Investigate The Safety, Tolerability And Pharmacokinetics Of PF-02341066 [NCT01250730] | Phase 1 | 18 participants (Actual) | Interventional | 2010-12-31 | Completed | ||
| Population Pharmacokinetics, Effectiveness and Safety of Antineoplastic Drugs in Elderly Patients [NCT05467189] | 500 participants (Anticipated) | Observational [Patient Registry] | 2021-01-01 | Recruiting | |||
| A Phase I Trial of Sorafenib (CRAF, BRAF, KIT, RET, VEGFR, PDGFR Inhibitor) or Crizotinib (MET, ALK, ROS1 Inhibitor) in Combination With Vemurafenib (BRAF Inhibitor) in Patients With Advanced Malignancies [NCT01531361] | Phase 1 | 46 participants (Actual) | Interventional | 2012-02-06 | Completed | ||
| A Two Steps Phase I Trial of Pazopanib or Pemetrexed in Combination With Crizotinib Followed by the Triplet, Crizotinib Plus Pazopanib Plus Pemetrexed in Patients With Advanced Malignancies [NCT01548144] | Phase 1 | 178 participants (Actual) | Interventional | 2012-04-30 | Terminated(stopped due to PI request) | ||
| A Phase 1, Open Label, Single Dose, Randomized, Cross-Over Study To Estimate The Effect Of Esomeprazole On The Pharmacokinetics Of Crizotinib In Healthy Volunteers [NCT01549574] | Phase 1 | 16 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
| Real-world Study of Non-small Cell Lung Cancer Treatment With ALK-tyrosine Kinase Inhibitors (ALK TKI) in Sweden: Drug Sequencing, Treatment Duration and Overall Survival - A Retrospective Study Using Swedish Register Data [NCT04647110] | 549 participants (Actual) | Observational | 2020-12-14 | Completed | |||
| Study to Investigate Outcome of Individualized Treatment Based on Pharmacogenomic Profiling & Ex Vivo Drug Sensitivity Testing of Patient-derived Organoids in Patients With Metastatic Colorectal Cancer [NCT05725200] | Phase 2 | 40 participants (Anticipated) | Interventional | 2022-09-27 | Recruiting | ||
| A Phase 1/2 Study of IDE196 in Patients With Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions [NCT03947385] | Phase 1/Phase 2 | 278 participants (Anticipated) | Interventional | 2019-06-28 | Recruiting | ||
| Randomized, Multicenter, Phase III, Open-Label Study of Alectinib Versus Crizotinib in Treatment-Naive Anaplastic Lymphoma Kinase-Positive Advanced Non-Small Cell Lung Cancer [NCT02075840] | Phase 3 | 303 participants (Actual) | Interventional | 2014-08-19 | Active, not recruiting | ||
| Phase 2 Open-label Single Arm Study Of The Efficacy And Safety Of Crizotinib In East Asian Patients With Advanced Non-Small Cell Lung Cancer (NSCLC) Harboring A Translocation Or Inversion Involving The Anaplastic Lymphoma Kinase (ALK) Gene Locus [NCT01500824] | Phase 2 | 0 participants (Actual) | Interventional | 2014-05-31 | Withdrawn | ||
| A Phase 1, Fixed Sequence, Cross-Over Study To Estimate The Effect Of Multiple Doses Of Ketoconazole On The Single Dose Pharmacokinetics Of Crizotinib (PF-02341066) In Healthy Volunteers [NCT01149785] | Phase 1 | 15 participants (Actual) | Interventional | 2010-07-31 | Completed | ||
| A Phase I Trial of Dasatinib in Combination With Crizotinib in Patients With Advanced Malignancies [NCT01744652] | Phase 1 | 62 participants (Actual) | Interventional | 2013-03-31 | Completed | ||
| A Phase 1, Single Dose, Randomized, Cross-Over Absolute Bioavailability Study In Healthy Volunteers Comparing Oral To Intravenous Administration Of Crizotinib (PF-02341066) [NCT01168934] | Phase 1 | 14 participants (Actual) | Interventional | 2010-08-31 | Completed | ||
| A Phase 1, Open-Label, Dose Escalation Study to Evaluate Safety, Pharmacokinetics and Pharmacodynamics of Combined Oral C-Met/ALK Inhibitor (PF-02341066) and Pan-Her Inhibitor (PF-0299804) in Patients With Advanced Non-Small Cell Lung Cancer [NCT01441128] | Phase 1 | 20 participants (Actual) | Interventional | 2011-09-01 | Terminated | ||
| A Phase 1B, Open-Label, Dose Escalation Study To Evaluate Safety, Pharmacokinetics And Pharmacodynamics Of Crizotinib (PF-02341066) Plus VEGF Inhibitor Combinations In Patients With Advanced Solid Tumors. [NCT01441388] | Phase 1 | 0 participants (Actual) | Interventional | 2011-12-31 | Withdrawn(stopped due to Business/Operational issues) | ||
| A Phase I Relative Bioavailability Study To Compare The Powder-In-Capsule And Immediate Release Tablet Of PF-02341066 In Healthy Volunteers [NCT00939731] | Phase 1 | 24 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
| A Master Protocol of Phase 1/2 Studies of Nivolumab in Advanced NSCLC Using Nivolumab as Maintenance After Induction Chemotherapy or as First-line Treatment Alone or in Combination With Standard of Care Therapies (CheckMate 370: CHECKpoint Pathway and niv [NCT02574078] | Phase 1/Phase 2 | 341 participants (Actual) | Interventional | 2015-11-23 | Completed | ||
| S1300: A Randomized, Phase II Trial of Crizotinib Plus Pemetrexed Versus Pemetrexed Monotherapy in ALK-Positive Non-squamous NSCLC Patients Who Have Progressed Systemically After Previous Clinical Benefit From Crizotinib Monotherapy [NCT02134912] | Phase 2 | 1 participants (Actual) | Interventional | 2014-08-31 | Terminated(stopped due to science has moved forward and there is no intent to complete the study) | ||
| Treatment With Crizotinib Single Patient Expanded Access IND 134375 [NCT03085186] | 0 participants | Expanded Access | No longer available | ||||
| The Therapeutic Effect of Crizotinib in Patients With ALK-rearrangement-negative But High Expression of ALK Phosphorylation [NCT05792644] | 15 participants (Actual) | Interventional | 2018-01-01 | Completed | |||
| A Sequential Phase I Study of MEK1/2 Inhibitors PD-0325901 or Binimetinib Combined With cMET Inhibitor PF-02341066 in Patients With RAS Mutant and RAS Wild Type (With Aberrant c-MET) Colorectal Cancer [NCT02510001] | Phase 1 | 82 participants (Actual) | Interventional | 2014-11-30 | Completed | ||
| A Phase 1, Open-Label, Single Dose, Randomized, Cross-Over Relative Bioavailability Study Comparing An Oral Liquid Formulation To A Formulated Capsule Of Crizotinib (PF 02341066) In Healthy Volunteers [NCT01297595] | Phase 1 | 22 participants (Actual) | Interventional | 2011-03-31 | Completed | ||
| Phase 3 Randomized Study Comparing X-396 (Ensartinib) to Crizotinib in Anaplastic Lymphoma Kinase (ALK) Positive Non-Small Cell Lung Cancer (NSCLC) Patients [NCT02767804] | Phase 3 | 290 participants (Actual) | Interventional | 2016-06-30 | Active, not recruiting | ||
| A Phase One Open-Label Single-Radiolabeled Dose Study To Investigate The Absorption, Metabolism And Excretion Of [14C]PF-02341066 In Healthy Male Volunteers [NCT01082380] | Phase 1 | 6 participants (Actual) | Interventional | 2010-03-31 | Completed | ||
| A Phase I Study To Evaluate The Effect Of Hepatic Impairment On The Pharmacokinetics And Safety Of Crizotinib In Advanced Cancer Patients [NCT01576406] | Phase 1 | 88 participants (Actual) | Interventional | 2012-07-31 | Completed | ||
| A PHASE 1B, OPEN LABEL, DOSE ESCALATION STUDY TO EVALUATE SAFETY, PHARMACOKINETICS AND PHARMACODYNAMICS OF AXITINIB (AG-013736) IN COMBINATION WITH CRIZOTINIB (PF-02341066) IN PATIENTS WITH ADVANCED SOLID TUMORS [NCT01999972] | Phase 1 | 50 participants (Actual) | Interventional | 2014-02-26 | Completed | ||
| PHASE 1 SAFETY, PHARMACOKINETIC AND PHARMACODYNAMIC STUDY OF PF-02341066, A MET/HGFR SELECTIVE TYROSINE KINASE INHIBITOR, ADMINISTERED ORALLY TO PATIENTS WITH ADVANCED CANCER [NCT00585195] | Phase 1 | 596 participants (Actual) | Interventional | 2006-04-19 | Completed | ||
| A PHASE 3, RANDOMIZED, OPEN-LABEL STUDY OF LORLATINIB (PF-06463922) MONOTHERAPY VERSUS CRIZOTINIB MONOTHERAPY IN THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED ALK-POSITIVE NON-SMALL CELL LUNG CANCER [NCT03052608] | Phase 3 | 296 participants (Actual) | Interventional | 2017-04-27 | Active, not recruiting | ||
| PHASE 1/2 STUDY OF PF-06463922 (AN ALK/ROS1 TYROSINE KINASE INHIBITOR) IN PATIENTS WITH ADVANCED NON-SMALL CELL LUNG CANCER HARBORING SPECIFIC MOLECULAR ALTERATIONS [NCT01970865] | Phase 1/Phase 2 | 334 participants (Actual) | Interventional | 2014-01-08 | Completed | ||
| A Randomized Phase II Study of Individualized Combined Modality Therapy for Stage III Non-small Cell Lung Cancer (NSCLC) [NCT01822496] | Phase 2 | 59 participants (Actual) | Interventional | 2013-11-04 | Terminated | ||
| A Phase II Trial to Evaluate Crizotinib in the Neoadjuvant Setting in Patients With Surgically Resectable, ALK, ROS1, or MET-oncogene Positive Non-small Cell Lung Cancer [NCT03088930] | Phase 2 | 3 participants (Actual) | Interventional | 2017-12-13 | Completed | ||
| CRIZOTINIB MASTER PROTOCOL: AN OPEN-LABEL CONTINUATION STUDY FOR PARTICIPANTS CONTINUING FROM PFIZER-SPONSORED CRIZOTINIB CLINICAL STUDIES [NCT05160922] | Phase 4 | 80 participants (Anticipated) | Interventional | 2021-12-27 | Recruiting | ||
| PHASE 1B OPEN-LABEL STUDY OF THE SAFETY AND CLINICAL ACTIVITY OF CRIZOTINIB (PF-02341066) IN TUMORS WITH GENETIC EVENTS INVOLVING THE ANAPLASTIC LYMPHOMA KINASE (ALK ) GENE LOCUS [NCT01121588] | Phase 1 | 44 participants (Actual) | Interventional | 2011-03-22 | Terminated(stopped due to Termination of further treatment on the study due to the availability of commercial supply or a rollover study (NCT05160922) that will allow active subjects to continue receiving treatment.) | ||
| Platform Study of Genotyping Guided Precision Medicine for Rare Tumors in China [NCT04423185] | Phase 2 | 770 participants (Anticipated) | Interventional | 2020-08-15 | Not yet recruiting | ||
| A Phase 3 Multicenter Open-label Study of Brigatinib (AP26113) Versus Crizotinib in Patients With ALK-positive Advanced Lung Cancer [NCT02737501] | Phase 3 | 275 participants (Actual) | Interventional | 2016-05-26 | Completed | ||
| Drug Treatment Patterns and Effects for Metastatic Non-small Cell Lung Cancer Patients In NORway (DELINOR) [NCT05834348] | 20,605 participants (Anticipated) | Observational | 2023-06-26 | Recruiting | |||
| PHASE 3, RANDOMIZED, OPEN-LABEL STUDY OF THE EFFICACY AND SAFETY OF CRIZOTINIB VERSUS PEMETREXED/CISPLATIN OR PEMETREXED/CARBOPLATIN IN PREVIOUSLY UNTREATED EAST ASIAN PATIENTS WITH NON-SQUAMOUS CARCINOMA OF THE LUNG HARBORING A TRANSLOCATION OR INVERSION [NCT01639001] | Phase 3 | 207 participants (Actual) | Interventional | 2012-09-29 | Completed | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||