| Assay ID | Title | Year | Journal | Article |
|---|
| AID1345503 | Human fms related tyrosine kinase 3 (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1345520 | Human fms related tyrosine kinase 4 (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1345914 | Human ret proto-oncogene (Type XIV RTKs: RET) | 2013 | Genes to cells : devoted to molecular & cellular mechanisms, Feb, Volume: 18, Issue:2
| Activity-based kinase profiling of approved tyrosine kinase inhibitors. |
| AID1345555 | Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1345555 | Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1345514 | Human fibroblast growth factor receptor 1 (Type V RTKs: FGF (fibroblast growth factor) receptor family) | 2003 | Clinical cancer research : an official journal of the American Association for Cancer Research, Jan, Volume: 9, Issue:1
| In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. |
| AID1345506 | Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family) | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1345590 | Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2003 | Clinical cancer research : an official journal of the American Association for Cancer Research, Jan, Volume: 9, Issue:1
| In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. |
| AID1345590 | Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family) | 2013 | Genes to cells : devoted to molecular & cellular mechanisms, Feb, Volume: 18, Issue:2
| Activity-based kinase profiling of approved tyrosine kinase inhibitors. |
| AID479522 | Inhibition of C-Raf | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID1173970 | Reversible inhibition of FLT3 (unknown origin) assessed as dissociation constant | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core. |
| AID479527 | Inhibition of FGFR1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID256615 | Average Binding Constant for p38-gamma; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764726 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 0.58%) | | | |
| AID507846 | Binding affinity to BRAF | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1808762 | Antivascular activity against HUVEC assessed as inhibition of tube formation incubated for 6 hrs by inverted microscopy | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Novel Small-Molecule Antiangiogenesis Agents to Treat Diabetic Retinopathy. |
| 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. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256600 | Average Binding Constant for EPHA8; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID710260 | Cytotoxicity against HUVECs assessed as growth inhibition at 0.5 to 2 uM after 48 hrs by SRB assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. |
| 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. |
| 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. |
| 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 |
| AID1185748 | Antiproliferative activity against human L02 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. |
| AID507565 | Binding affinity to IKK-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508139 | Cmax in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507870 | Binding affinity to CDK9 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507861 | Binding affinity to CAMKK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID491725 | Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1550003 | Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID507911 | Binding affinity to EGFR G719S mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507880 | Binding affinity to CLK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID479517 | Inhibition of CAMK4 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| 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. |
| AID491723 | Antiproliferative activity against human MOLM13 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155202 | Antitumor activity against human HT-29 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 80 mg/kg/day administered qd measured up to day 21 relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID507668 | Binding affinity to PFTAIRE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218110 | Cmax in human plasma at 50 mg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1876081 | Cytotoxicity against human Huh7.5 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. |
| AID435285 | Binding constant for DMPK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507887 | Binding affinity to CSNK1G2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID383114 | Inhibition of Gak | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID507642 | Binding affinity to NDR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1217867 | Drug excretion in feces of human at 5 mg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID1425062 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1875912 | Inhibition of AAK1 kinase in HEK-293 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. |
| AID1158442 | Cytotoxicity against HUVEC | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| 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. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563409 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID435933 | Binding constant for PKN2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425184 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID738216 | Growth inhibition of human PC3 cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1424488 | Antitumor activity in patient with metastatic renal cell carcinoma assessed as progression free survival during phase 3 trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID463624 | Inhibition of KIT | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507661 | Binding affinity to PAK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435829 | Binding constant for RPS6KA1(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507863 | Binding affinity to CDC2L2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507588 | Binding affinity to LIMK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507632 | Binding affinity to MST1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1581233 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1629520 | Cytotoxicity mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| 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. |
| AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507910 | Binding affinity to EGFR G719C mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID458665 | Inhibition of mouse GM-CSF-stimulated cell proliferation of growth factor dependent mouse FDC-P1 cells expressing human FMS after 48 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID649458 | Inhibition of PDGFR | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID256618 | Average Binding Constant for PHkg2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID216911 | Inhibition of Vascular endothelial growth factor receptor 2 | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| 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. |
| AID1764713 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 69.08%) | | | |
| AID1440348 | Inhibition of human KIT | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1563375 | Inhibition of c-KIT K642E mutant in human GIST882 cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1517775 | Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID1602306 | Half life of the compound in potassium phosphate buffer at 10 uM in presence of 100 fold excess reduced glutathione by HPLC analysis | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507904 | Binding affinity to DRAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435910 | Binding constant for MAP4K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1876072 | Antiviral activity against DENV 1 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID684153 | Inhibition of N-terminal GST-tagged Flt1 using poly(Glu,Tyr) as substrate after 60 mins by alphascreen assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
| AID1764689 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 12 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID479494 | Inhibition of gamma secretase mediated amyloid beta 40 generation in human H4 cells at 10 uM by LPECL assay | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID463636 | Inhibition of Flt3 | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID1586425 | Antiangiogenic activity against HMEC1 cells after 20 hrs by tube formation assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID1387030 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID507843 | Binding affinity to BMPR1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1218121 | AUC (0 to infinity) in female cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1290542 | Cytotoxicity against mouse SVEC4-10 cells assessed as cell viability after 24 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Synthesis and preliminary evaluation of 5,7-dimethyl-2-aryl-3H-pyrrolizin-3-ones as angiogenesis inhibitors. |
| AID507618 | Binding affinity to MERTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID508098 | Binding affinity to STK39 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID384660 | Cytotoxicity against human NCI-H1944 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| AID507616 | Binding affinity to MEK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1629523 | Inhibition of TEL-fused cKIT T670I/V559D double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| 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. |
| AID638915 | Inhibition of RET at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507638 | Binding affinity to MYLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID256587 | Average Binding Constant for ACK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256624 | Average Binding Constant for FGFR3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID384391 | Cytotoxicity against human Panc04.03 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. |
| 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. |
| AID1563517 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at S473 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID507679 | Binding affinity to PIK3CA H1047L mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435677 | Binding constant for LOK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1587952 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507073 | Inhibition of recombinant PI3Kbeta by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1587965 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507826 | Binding affinity to AKT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507663 | Binding affinity to PCTK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1488414 | Inhibition of Axl (unknown origin) | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
| AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256601 | Average Binding Constant for EPHA3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1173971 | Binding affinity to FLT3 (unknown origin) assessed as dissociation half life | 2014 | Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
| Design, synthesis and biological evaluation of FLT3 covalent inhibitors with a resorcylic acid core. |
| AID383295 | Inhibition of BIKE | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID638912 | Inhibition of c-Kit at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| 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. |
| 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. |
| AID1630240 | Cell cycle arrest in human HCT116 cells assessed as accumulation at S phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 46.36 %) | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID624832 | Binding constant for IKK-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID508111 | Binding affinity to TLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764704 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at sub-G1 phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 4.24%) | | | |
| AID624845 | Binding constant for CDK7 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. |
| 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. |
| 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. |
| AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1387032 | Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID508086 | Binding affinity to SIK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1764649 | Inhibition of PDGFRalpha (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| 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. |
| AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID759168 | Inhibition of human wild-type ABL (Ser229 to Gln513)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507845 | Binding affinity to BMX | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507954 | Binding affinity to FLT3 D835Y mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424895 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID161263 | Inhibition of Platelet-derived growth factor receptor beta (PDGF-Rbeta) | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| 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. |
| AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438509 | Ratio of IC50 for human MV4-11 cells to Kd for FLT3 catalytic domain expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1587944 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| AID1563507 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y703 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID256625 | Average Binding Constant for PAK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424970 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508082 | Binding affinity to SBK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1478166 | Inhibition of human EPHA7 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| 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. |
| AID507634 | Binding affinity to MST3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID671885 | Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID619791 | Cytotoxicity against human MV4-11 cells assessed as cell viability at 10 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| AID1224769 | Delta TM value showing the stabilisation of GSK3B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID608769 | Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent. |
| AID718826 | Inhibition of KDR at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
| AID1478165 | Inhibition of human EPHA5 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID507624 | Binding affinity to MKNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507639 | Binding affinity to MYO3A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256658 | Average Binding Constant for p38-beta; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID383314 | Inhibition of NTRK1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID507658 | Binding affinity to PAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID508028 | Binding affinity to PIK4CB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224802 | Delta TM value showing the stabilisation of TNIK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1395593 | Effect on VEGFR2 protein expression in human HT-29 cells assessed as secreted VEGFR2 level in culture media at 25 uM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1602358 | Ratio of inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system in presence of 1 mM ATP to inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus express | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507866 | Binding affinity to CDK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435937 | Binding constant for TESK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1600268 | Antiangiogenic activity against HUVEC assessed as inhibition of cell proliferation measured after 30 mins by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID508092 | Binding affinity to SRPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507857 | Binding affinity to CAMK2D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1158448 | Toxicity in BALBc/J mouse assessed as maximal tolerated dose | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID1587979 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID649621 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID624726 | Binding constant for HIPK1 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. |
| AID1387027 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| 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. |
| AID747274 | Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and antiproliferative evaluation of piperazine-1-carbothiohydrazide derivatives of indolin-2-one. |
| 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. |
| 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. |
| AID1224799 | Delta TM value showing the stabilisation of NDR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID507082 | Inhibition of recombinant c-Src T338I mutant by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1465752 | Inhibition of KIT V559D/V654A double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID1310407 | Cytotoxicity against human PC3 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and apoptosis inducing effect of novel (Z)-3-(3'-methoxy-4'-(2-amino-2-oxoethoxy)-benzylidene)indolin-2-ones as potential antitumour agents. |
| AID435652 | Binding constant for EGFR(L747-E749del, A750P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507655 | Binding affinity to p38-gamma | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424490 | Antitumor activity in patient with metastatic renal cell carcinoma assessed as overall survival during phase 3 trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID1218251 | Drug excretion in urine of female Sprague-Dawley rat at 5 mg/kg, iv administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1224748 | Delta TM value showing the stabilisation of AMPKA2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435275 | Binding constant for BIKE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1764762 | Antitumor activity against human MV4-11 cells xenografted in mouse assessed as tumor growth inhibition at 5 mg/kg, po administered for 20 days measured once every 2 days relative to control | | | |
| AID1602340 | Binding affinity to human FLT3 ITD mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| 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. |
| AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1395592 | Effect on VEGFR2 protein expression in human HT-29 cells assessed as VEGFR2 level at 25 uM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1155276 | Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563485 | Antitumor activity against mouse BAF3(transformed) cells harboring c-KIT T670I mutant implanted in BALB/c nu mouse assessed as tumor weight at 40 mg/kg/day, po administered via gavage for 11 days (Rvb = 1.83 g) | | | |
| AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256673 | Average Binding Constant for PAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID458673 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 500 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID383328 | Inhibition of STK18 | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| AID1387033 | Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID629474 | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID1224776 | Delta TM value showing the stabilisation of ERK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID469538 | Antitumor activity against human MV411 cells in xenografted athymic nude mouse model assessed as decrease in tumor size at 30 mg/kg, po qd for 28 days | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors. |
| AID507864 | Binding affinity to CDK11 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID384622 | Cytotoxicity against human MEWO cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1478162 | Inhibition of human EPHA2 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID418604 | Inhibition of VEGFR2 | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
| N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
| 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. |
| AID459250 | Inhibition of FLT3 by ELISA-based kinase assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| AID624887 | Binding constant for ERK3 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. |
| AID1175321 | Inhibition of PDGFRalpha (unknown origin) at 100 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake. |
| 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. |
| 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. |
| 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. |
| AID1764766 | Antitumor activity against human MOLM-13 cells xenografted in mouse assessed as tumor regression at 40 mg/kg, po administered for 16 days measured on day 9 relative to control | | | |
| AID256614 | Average Binding Constant for YES; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737719 | Inhibition of wild-type human partial length AMPK alpha1 (M1 to E306 residues) expressed in bacterial expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624895 | Binding constant for MEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424916 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1629517 | Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624970 | Binding constant for CDK5 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. |
| AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507850 | Binding affinity to BRSK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID665079 | Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| 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. |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155228 | Toxicity in BALB/c nude mouse xenografted with human NCI-H460 cells assessed as change in body weight at 40 mg/kg/day administered qd relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624899 | Binding constant for ROS1 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. |
| AID508128 | Binding affinity to ULK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID645866 | Antitumor activity against human Calu6 cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 80 mg/kg, po qd for 11 days | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
| 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. |
| AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1781306 | Intrinsic clearance in mouse liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/SM analysis | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID507422 | Inhibition of recombinant Ret by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID383093 | Inhibition of PDGFRbeta 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. |
| AID1424991 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1764647 | Inhibition of c-KIT (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID1478172 | Inhibition of human KHS at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID507610 | Binding affinity to MARK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1431172 | Displacement of [3H]colchicine from bovine brain tubulin at 1 uM measured after 10 mins by liquid scintillation counting method relative to control | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| 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. |
| 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. |
| AID1304251 | Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis and biological evaluation of oxindole linked indolyl-pyrimidine derivatives as potential cytotoxic agents. |
| 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. |
| 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. |
| AID350249 | Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID1737718 | Cytotoxicity against human K562 cells assessed as reduction in cell viability at 50 uM incubated for 24 hrs by celltox-green assay relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1154765 | Antitumor activity against human U251 cells xenografted into athymic NCr mouse assessed as decrease in tumor growth at 30 mg/kg twice weekly measured up to 34 days | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| AID256607 | Average Binding Constant for STK18; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID1155240 | Binding affinity to CHK1 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID383329 | Inhibition of STK4 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1433927 | Inhibition of vitronectin binding to alphaVbeta3 in human EPC at 1 to 10000 nM measured after 30 mins in presence of MnCl2 by crystal violet staining based cell adhesion assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID710532 | Inhibition of KDR at 10 uM incubated for 60 mins using poly(Glu,Tyr)4:1 substrate and 10 uM ATP by ELISA | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID458685 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 31 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID734224 | Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents. |
| AID1550006 | Effect on VEGFR2 in human A549 cells assessed as membrane VEGFR2 level at 100 uM incubated for 24 hrs by flow cytometric analysis relative to control | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID517659 | Inhibition of FLT3 by time resolved fluorescence method | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| AID1563341 | Inhibition of c-KIT N822K mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507589 | Binding affinity to LIMK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID669867 | Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. |
| AID1563533 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in ERK phosphorylation at T204 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID773014 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507605 | Binding affinity to MAPKAPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1542973 | Antiproliferative activity against human BT474 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| AID1155245 | Binding affinity to PYK2 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1204921 | Inhibition of RET (unknown origin) assessed as decrease in autophoshorylation | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. |
| AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764727 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 0.25%) | | | |
| 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. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764709 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G1 phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 69.08%) | | | |
| AID256675 | Average Binding Constant for PTK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624903 | Binding constant for SRPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508049 | Binding affinity to PRKD3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1760968 | Inhibition of recombinant human His-tagged VEGFR2 expressed in Baculovirus expression system using ADP-Glo as substrate measured after 30 mins in presence of ATP by ADP-Glo kinase assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID481815 | Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. |
| AID1384629 | Inhibition of DLK (unknown origin) | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. |
| AID479518 | Inhibition of CDK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID256649 | Average Binding Constant for CSK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID479514 | Inhibition of Aurora A | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID773011 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| AID508072 | Binding affinity to RPS6KA1(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1169707 | Half life in mouse liver microsomes by LC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
| AID507662 | Binding affinity to PCTK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID1310411 | Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and apoptosis inducing effect of novel (Z)-3-(3'-methoxy-4'-(2-amino-2-oxoethoxy)-benzylidene)indolin-2-ones as potential antitumour agents. |
| AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507594 | Binding affinity to LZK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID383298 | Inhibition of CLK1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1764699 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 7.29%) | | | |
| AID627289 | Inhibition of RSK1 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID1517769 | Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| 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. |
| AID625098 | Binding constant for IRAK4 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. |
| AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507869 | Binding affinity to CDK8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID665085 | Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1563339 | Inhibition of c-KIT D820G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID438533 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 30 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1563338 | Inhibition of c-KIT D820E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1155249 | Binding affinity to FYN (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1395078 | Antiproliferative activity against HUVEC after 48 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity. |
| AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1599895 | Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as reduction in cell growth incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID507976 | Binding affinity to IGF1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256560 | Average Binding Constant for FGR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624723 | Binding constant for CSNK1A1L kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1550013 | Antiangiogenic activity against HMEC1 cells assessed as inhibition of tube formation incubated for 20 hrs by matrigel based tube formation assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| 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. |
| AID1517767 | Cytotoxicity against human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID1764703 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 7.29%) | | | |
| 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. |
| 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. |
| AID1224757 | Delta TM value showing the stabilisation of CDK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID508032 | Binding affinity to PIP5K1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507816 | Binding affinity to ABL1 T315I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563331 | Inhibition of c-KIT V654A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1563342 | Inhibition of c-KIT Y823D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1373033 | Half life in rat liver microsomes at 1 uM by LC/MS analysis | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer. |
| AID491720 | Antiproliferative activity against human U937 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID719247 | Inhibition of gamma secretase in human H4 cells expressing APP695 assessed as inhibition of Abeta42 production after 20 to 24 hrs by liquid phase electrochemiluminescence assay | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
| Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3. |
| 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. |
| AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1302369 | Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425006 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624795 | Binding constant for MET(M1250T) 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. |
| AID1764735 | Induction of apoptosis in human MOLM-13 cells assessed as necrotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 0.45%) | | | |
| 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. |
| 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. |
| AID536889 | Antitumor activity against human HT-29 cells xenografted in po dosed BALB/cA nude mouse assessed as inhibition of tumor growth administered 11 days after tumor implantation qd for 14 days | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID627290 | Inhibition of RSK2 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID1176835 | Inhibition of FLT1 (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID1630231 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase after 24 hrs by propidium iodide staining based flow cytometry | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705893 | Cytotoxicity against human A498 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity. |
| 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. |
| 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. |
| AID1363086 | Half life in mouse liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | | | |
| 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. |
| AID599568 | Antitumor activity against human MDA-MB-231 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1602302 | Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system at 0.1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition measured after 120 mins in presence of ATP by A | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID773015 | Inhibition of c-KIT (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID507890 | Binding affinity to CSNK2A2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID66610 | Inhibition of epidermal growth factor receptor (EGF-R) | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID256633 | Average Binding Constant for PRKACA; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID508119 | Binding affinity to TRKC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1586463 | Inhibition of VEGFR2 phosphorylation in human A549 cells assessed as phosphorylated VEGFR2 level at 10 uM after 30 mins by Western blot assay relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID1602301 | Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system at 1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition and measured after 120 mins in presence of ATP by | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| 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. |
| 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. |
| AID638922 | Inhibition of RON at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| 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. |
| AID599566 | Antitumor activity against human A549 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1302362 | Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID1312691 | Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated ERK1/2 at 1 uM incubated for 24 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
| AID1563411 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in STAT3 phosphorylation at Y705 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1563374 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479742 | Inhibition of PRAK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID684154 | Inhibition of N-terminal GST-tagged FGFR1 using poly(Glu,Tyr) as substrate after 30 mins by alphascreen assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
| AID479732 | Inhibition of MST2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID758914 | Inhibition of human LRRK2 (1885 to 2132) using 5-Fluo-Ahx-RLGRDKYKTLRQIRQGNTK-OH as substrate after 60 mins by fluorescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 23, Issue:14
| Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2. |
| AID1290591 | Cytotoxicity against human PC3 cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry. |
| AID1764728 | Induction of apoptosis in human MOLM-13 cells assessed as viable cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 92.83%) | | | |
| 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. |
| AID1563329 | Inhibition of c-KIT L576P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID479743 | Inhibition of RSK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID507671 | Binding affinity to PHKG2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID479734 | Inhibition of p70S6K | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID1395077 | Inhibition of VEGFR2 (unknown origin) using TK substrate after 1 hr by HTRF assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity. |
| 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. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563322 | Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay | | | |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1764707 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G2/M phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 8.25%) | | | |
| 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. |
| 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. |
| AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1503806 | Antiangiogenic activity in HUVEC assessed as inhibition of tube like structures formation at < 100 nM after 14 hrs by matrigel based inverted microscopy | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors. |
| AID1224756 | Delta TM value showing the stabilisation of CAMKK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1224797 | Delta TM value showing the stabilisation of MPSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID753547 | Antitumor activity against human MDA-MB-435 cells xenografted in chicken embryo chorioallantoic membrane assessed as inhibition of tumor volume at 20 mg/kg measured after 2 days | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
| Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor. |
| 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. |
| AID1478066 | Inhibition of human VEGFR2 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer 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. |
| AID665087 | Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID350248 | Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624980 | Binding constant for ABL1(F317I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507848 | Binding affinity to BRK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424408 | Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent advances (2015-2016) in anticancer hybrids. |
| AID1207481 | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform | | | |
| AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425044 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764694 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 16.31%) | | | |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563525 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S236 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1424507 | Antitumor activity in patient with renal cell carcinoma assessed as progression free survival during phase 2 trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID507620 | Binding affinity to MET M1250T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1302370 | Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID508065 | Binding affinity to RIPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625033 | Binding constant for PCTK1 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. |
| 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. |
| AID507813 | Binding affinity to ABL1 H396P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1586364 | Antiproliferative activity against HEK293 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508107 | Binding affinity to TGFBR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764725 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 0.31%) | | | |
| AID1876074 | Antiviral activity against DENV 3 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID479736 | Inhibition of PIM2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507964 | Binding affinity to GRK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID384686 | Cytotoxicity against human Hs 707(A).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. |
| 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. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1302352 | Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435661 | Binding constant for full-length MKNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435906 | Binding constant for EGFR(L747-T751del,Sins) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507970 | Binding affinity to HIPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1175322 | Inhibition of PDGFRbeta (unknown origin) at 100 uM | 2014 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 24, Issue:24
| Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3β (GSK-3β) with cellular activity of promoting glucose uptake. |
| AID1218130 | Terminal half life in male cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| 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. |
| AID383325 | Inhibition of STK16 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1207387 | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform | | | |
| AID693403 | Competitive inhibition of recombinant GST-tagged VEGFR2 cytoplasmic domain in presence of ATP | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, in silico, in vitro, and in vivo investigation of 5-[¹¹C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2. |
| 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. |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID649616 | Plasma concentration at steady state in BALB/c mouse xenografted with BA/F3 cells expressing FLT3-ITD mutant at 20 mg/kg, po qd | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563520 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T202 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1581259 | Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID507593 | Binding affinity to LYN | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1236881 | Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID459247 | Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| AID479727 | Inhibition of LYN | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507619 | Binding affinity to MET | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1895649 | Inhibition of VEGFR2 (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| AID507599 | Binding affinity to MAP3K3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1387037 | Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID507573 | Binding affinity to JAK1 JH2 domain | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID684191 | Inhibition of FGFR1 phosphorylation in human MDA-MB-231 cells xenografted mouse at 100 mg/kg | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
| AID507584 | Binding affinity to KIT V559D,V654A mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508105 | Binding affinity to TEC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624908 | Binding constant for TEC 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. |
| AID1587987 | Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID508110 | Binding affinity to TIE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507927 | Binding affinity to EPHB1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256586 | Average Binding Constant for STK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435193 | Binding constant for RPS6KA6(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479730 | Inhibition of MET | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1224763 | Delta TM value showing the stabilisation of CLK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID1764653 | Selectivity ratio of IC50 for c-KIT (unknown orign) to IC50 for FLT3 (unknown origin) | | | |
| AID383082 | Inhibition of Kit | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID738480 | Binding affinity to phosphorylated ABL1 (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| 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. |
| AID507952 | Binding affinity to FLT3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435527 | Binding constant for FGFR3(G697C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1381314 | Lipophilicity, chromatographic hydrophobicity index of the compound at pH 5.5 by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID1381312 | Lipophilicity, chromatographic hydrophobicity index of the compound at pH 10.5 by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1895653 | Inhibition of FLT3 (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| 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. |
| AID665077 | Inhibition of recombinant PLK1 using RBERCHKtide as substrate assessed as inhibition of [33P]Phosphate incorporation into substrate after 80 mins by scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508050 | Binding affinity to PRKG1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1387028 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1421411 | Inhibition of recombinant human Erbb2 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID1503805 | Antiangiogenic activity in HUVEC assessed as inhibition of tube like structures formation at 100 nM to 1 uM after 14 hrs by matrigel based inverted microscopy | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors. |
| 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. |
| 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. |
| AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1155272 | Antiproliferative activity against human TT cells pretreated for 72 hrs followed by compound-washout measured after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID1517776 | Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| 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. |
| AID507645 | Binding affinity to NEK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1440376 | Toxicity in Harlan nude mouse xenografted with human MV4-11 cells administered ig qd for 20 days | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1517771 | Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624863 | Binding constant for MARK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507966 | Binding affinity to GSK3A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID734139 | Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastati |
| AID624937 | Binding constant for FLT3(ITD) 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. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1549998 | Antiproliferative activity against human HT-29 cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID1764687 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 111 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| 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. |
| AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID479524 | Inhibition of DYRK1A | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1302372 | Antiproliferative activity against CHL cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID507875 | Binding affinity to CHEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID1424496 | Antitumor activity in patient with renal cell carcinoma assessed as progression free survival during phase 3 non-inferiority trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| 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. |
| AID1764717 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 0.31%) | | | |
| AID256664 | Average Binding Constant for EGFR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID384869 | Cytotoxicity against human KHOS/NP cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1218254 | Drug excretion in feces of female cynomolgus monkey at 6 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID491750 | Inhibition of KDR | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID383316 | Inhibition of PHKG1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID508099 | Binding affinity to SYK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID729550 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
| AID256569 | Average Binding Constant for PAK7/PAK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID1373031 | Half life in human liver microsomes at 1 uM by LC/MS analysis | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer. |
| 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. |
| 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. |
| AID1599892 | Inhibition of VEGFR2 (unknown origin) using Poly (Glu, Tyr) 4:1 as substrate preincubated with substrate followed by enzyme challenge for 1 hr by ELISA | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID1563521 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T204 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1186615 | Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
| AID1705891 | Inhibition of VEGFR2 (unknown origin) by Kinase-Glo max reagent-based assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity. |
| 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. |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224768 | Delta TM value showing the stabilisation of DMPK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID1484885 | Inhibition of PDGFRbeta (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at 1 uM after 1 hr by ELISA relative to control | 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. |
| AID507908 | Binding affinity to EGFR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID507585 | Binding affinity to LATS1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507646 | Binding affinity to NEK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID383305 | Inhibition of FGFR2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1301409 | Inhibition of human recombinant AXL expressed in Escherichia coli BL21 infected with T7 phage by qPCR method | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. |
| 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. |
| 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. |
| AID1737703 | Inhibition of recombinant human His6-tagged AMPK alpha1 using ULight CRBtide as substrate incubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1764719 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 0.25%) | | | |
| 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. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508132 | Binding affinity to YANK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID508080 | Binding affinity to RPS6KA6(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID438342 | Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1737727 | Inhibition of wild-type human partial length autoinhibited KIT (Y545 to D952 residues) expressed in mammalian expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1424997 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1587997 | Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as tumor regression at 40 mg/kg, po administe | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256653 | Average Binding Constant for FGFR1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID256603 | Average Binding Constant for FER; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical 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. |
| AID1301837 | Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID508114 | Binding affinity to TNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224758 | Delta TM value showing the stabilisation of CDK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| 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. |
| AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224753 | Delta TM value showing the stabilisation of CAMK2D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID157326 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.5% bovine serum albumin | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1433900 | Drug uptake in human EPC assessed as alphavbeta3-mediated drug uptake by measuring intracellular content per mg protein at 1 uM measured after 8 hr by HPLC-ESI-MS/MS analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID513987 | Inhibition of VEGFR2 expressed in human A431 cells | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents. |
| 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. |
| AID507602 | Binding affinity to MAP4K3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1433897 | Drug internalization in human EPC assessed as alphavbeta3-mediated drug uptake by measuring intracellular content per mg protein at 1 uM measured after 1 hr by HPLC-ESI-MS/MS analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1224761 | Delta TM value showing the stabilisation of CLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID626121 | Inhibition of ERK phosphorylation at Thr202/Tyr204 in VEGF-stimulated HUVEC at 1 uM preincubated for 1 hr before VEGF induction measured after 5 mins by Western blot analysis | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| 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. |
| AID1737722 | Inhibition of wild-type human full length BTK (M1 to S659 residues) expressed in mammalian expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) 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. |
| AID507920 | Binding affinity to EPHA2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID1550018 | Induction of apoptosis in human A549 cells assessed as apoptotic cells at 100 uM incubated for 24 hrs by FITC-Annexin V staining based flow cytometric analysis (Rvb = 20%) | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID507607 | Binding affinity to MARK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID649465 | Inhibition of FLT3 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID1737726 | Inhibition of wild-type human partial length JAK1 JH2 pseudokinase domain (R537 to D855 residues) expressed in mammalian expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| 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. |
| AID1302371 | Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435168 | Binding constant for LTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479726 | Inhibition of LCK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507664 | Binding affinity to PCTK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508044 | Binding affinity to PRKCE | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764712 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at sub-G1 phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 4.24%) | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID508059 | Binding affinity to RET M918T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1530782 | Antimigratory activity in human MCF7 cells assessed as inhibition of wound healing at 1.25 uM after 8 to 48 hrs by phase contrast microscopic analysis | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
| AID1764734 | Induction of apoptosis in human MOLM-13 cells assessed as late apoptotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 4.54%) | | | |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID508029 | Binding affinity to PIM1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563510 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y703 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507874 | Binding affinity to CHEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563515 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R cells assessed as reduction in c-KIT autophosphorylation at Y823 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764640 | Induction of tumor recurrence mouse xenografted with human MOLM-13 cells at 20 to 40 mg/kg, po | | | |
| AID446377 | Inhibition of human recombinant N-terminally 6X-His-tagged SIRT3 at 50 uM after 4 hrs in presence of NAD+ by fluorescent deacetylase assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins). |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581230 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID507879 | Binding affinity to CLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507587 | Binding affinity to LCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764681 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 37 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID759166 | Inhibition of ABL T315I mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| AID1195285 | Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. |
| AID507916 | Binding affinity to EGFR L858R,T790M mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764688 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 37 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID508116 | Binding affinity to TNNI3K | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224786 | Delta TM value showing the stabilisation of PIM1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1876076 | Antiviral activity against EBOV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1155243 | Binding affinity to c-KIT (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID383587 | Cytotoxicity against human B-CPAP cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508109 | Binding affinity to TIE1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID481818 | Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. |
| 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. |
| AID1764701 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 64.73%) | | | |
| AID1764729 | Induction of apoptosis in human MOLM-13 cells assessed as early apoptotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 2.18%) | | | |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508088 | Binding affinity to SNARK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1488411 | Inhibition of fibroblast growth factor-induced neovascularization in mouse corneal micropocket at 80 mg/kg, qd relative to control | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
| AID508061 | Binding affinity to RET V804M mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764780 | Toxicity in mouse xenografted with human MOLM-13 cells assessed as induction of cytoplasmic condensation at 40 mg/kg, po administered for 20 days by hematoxylin and eosin staining assay | | | |
| AID256645 | Average Binding Constant for JAK2 (Kin.Dom. 2); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1602343 | Binding affinity to non-auto-inhibited form of wild type human N-terminal GST-tagged FLT3 expressed in baculovirus expression | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507630 | Binding affinity to MRCKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1327311 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G0/G1 phase at 4 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 50.4 %) | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| 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. |
| AID1581224 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1602316 | Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system preincubated for 5 to 30 mins followed by myelobasic protein addition and measured after 120 mins in presence of 100 uM ATP by | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID256634 | Average Binding Constant for CSNK1G2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID507886 | Binding affinity to CSNK1G1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1587950 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1433923 | Antiangiogenic activity in human EPC assessed as inhibition of VEGF-A induced tubule formation at 10 nM measured after 6 hrs by matrigel based phase contrast microscopic analysis relative to control | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID759165 | Inhibition of cKIT V559D/T670I double mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| AID438534 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 30 mg/kg, po QD for 28 days measured after dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID1186614 | Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
| 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. |
| AID507424 | Inhibition of recombinant PDGFR by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID479519 | Inhibition of CHK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID157327 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 1% bovine serum albumin | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| 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. |
| AID1335670 | Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| 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. |
| 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. |
| AID624848 | Binding constant for CSNK2A1 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. |
| AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764697 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 64.73%) | | | |
| AID1373032 | Half life in mouse liver microsomes at 1 uM by LC/MS analysis | 2018 | Bioorganic & medicinal chemistry, 02-01, Volume: 26, Issue:3
| Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer. |
| AID1424956 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID657320 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents. |
| AID1542977 | Antiproliferative activity against human NHFB cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1572261 | Inhibition of wild type EGFR (unknown origin) by bioluminescent ADP-glo kinase assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
| Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1207541 | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | | | |
| AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507606 | Binding affinity to MAPKAPK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507574 | Binding affinity to JH1 catalytic domain JAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1218177 | AUC (0 to infinity) in female Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID256667 | Average Binding Constant for ABL1(E255K); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID383077 | Inhibition of AAK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1563320 | Antitumor activity against mouse BAF3(transformed) cells harboring c-KIT Y823D mutant implanted in BALB/c nu mouse assessed as tumor weight at 40 mg/kg/day, po administered via gavage for 9 days (Rvb = 0.96 g) | | | |
| AID383330 | Inhibition of TNIK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID507827 | Binding affinity to AKT2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256661 | Average Binding Constant for PDGFRB; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507617 | Binding affinity to MELK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507907 | Binding affinity to DYRK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507948 | Binding affinity to FGFR3 G697C mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507567 | Binding affinity to INSR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508126 | Binding affinity to ULK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1586362 | Antiproliferative activity against human HL60 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256657 | Average Binding Constant for LCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID508141 | AUC (0 to 24 hrs) in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID619793 | Cytotoxicity against human A549 cells assessed as cell viability at 10 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| 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. |
| 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. |
| AID1587947 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507833 | Binding affinity to ARK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479530 | Inhibition of GSK3-beta | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1587973 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507825 | Binding affinity to ADCK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507934 | Binding affinity to ERBB4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1302367 | Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| 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. |
| AID625070 | Binding constant for PFTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587964 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1224807 | Delta TM value showing the stabilisation of YSK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID383308 | Inhibition of InsR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1453241 | Inhibition of PAK6 (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
| Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study. |
| AID507898 | Binding affinity to DDR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1399366 | Inhibition of PDGF-BB-induced PDGFRbeta activation in human SH-SY5Y cells pretreated for 60 mins followed by PDGF-BB addition and measured after 10 mins by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
| Design, synthesis and preclinical evaluation of 5-methyl-N |
| AID508095 | Binding affinity to STK33 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1744429 | Inhibition of human GRK5 using porcine brain tubulin as substrate incubated for 3 to 5 mins by [gamma32P]ATP based radiometric assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. |
| 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. |
| AID624813 | Binding constant for MINK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID491752 | Inhibition of cKIT | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1224806 | Delta TM value showing the stabilisation of VRK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID73459 | Inhibition of Fibroblast growth factor receptor 1 | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1737720 | Inhibition of wild-type human partial length AMPK alpha2 (M1 to E306 residues) expressed in bacterial expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1600267 | Antiangiogenic activity against VEGF-induced HUVEC assessed as inhibition of cell proliferation preincubated for 30 mins followed by VEGF addition measured after 24 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID1310410 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and apoptosis inducing effect of novel (Z)-3-(3'-methoxy-4'-(2-amino-2-oxoethoxy)-benzylidene)indolin-2-ones as potential antitumour agents. |
| 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. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1387025 | Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1895667 | Inhibition of FLT3-ITD (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| AID1563522 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at T308 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508115 | Binding affinity to TNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625019 | Binding constant for AKT3 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. |
| AID256602 | Average Binding Constant for EPHA2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1425166 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1744445 | Inhibition of PKA (unknown origin) incubated for 30 mins using REBtide substrate by ADP-Glo assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. |
| AID256674 | Average Binding Constant for PKMYT1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID491719 | Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1433896 | n-Octanol-buffer distribution coefficient, log D of the compound at pH 7.4 incubated for 4 hrs by HPLC-UV-vis based shake flask method | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID256643 | Average Binding Constant for CAMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1478175 | Inhibition of human TAK1 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID491727 | Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID479510 | Inhibition of ABL | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507915 | Binding affinity to EGFR L858R mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563415 | Inhibition of AKT autophosphorylation at T308 residue in human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID479740 | Inhibition of PKD2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1267244 | Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Structure-activity relationship study of anticancer thymidine-quinoxaline conjugates under the low radiance of long wavelength ultraviolet light for photodynamic therapy. |
| AID1764720 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 98.86%) | | | |
| AID507844 | Binding affinity to BMPR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256670 | Average Binding Constant for ABL1(T315I); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563376 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID256642 | Average Binding Constant for VEGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID759169 | Inhibition of cSRC T338M mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| 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. |
| AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1302353 | Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID508120 | Binding affinity to TSSK1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224760 | Delta TM value showing the stabilisation of CHEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID157324 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells without bovine serum albumin | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| 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. |
| 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. |
| AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1764690 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 4 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1155248 | Binding affinity to PHKgamma2 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID508113 | Binding affinity to TNIK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID507836 | Binding affinity to AURKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424953 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1440367 | Antitumor activity against human MV4-11 cells xenografted in Harlan nude mouse assessed as tumor growth inhibition at 10 mg/kg, ig qd for 20 days relative to control | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID507867 | Binding affinity to CDK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID599959 | Binding affinity to human KIT D816V mutant incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| 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. |
| 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. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID739334 | Cytotoxicity against human ACHN cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| Cytotoxic scalarane sesterterpenes from a Korean marine sponge Psammocinia sp. |
| AID1465758 | Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID1563524 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S235 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID507882 | Binding affinity to CSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID745346 | Inhibition of VEGFR1 phosphorylation in growth factor-stimulated HUVEC | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). |
| AID1460373 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents. |
| AID508136 | Binding affinity to YSK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507935 | Binding affinity to ERK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508089 | Binding affinity to SRC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1611386 | Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent. |
| AID629475 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID719380 | Inhibition of human recombinant FLT3 expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate at 10 uM after 90 mins by LANCE method relative to staurosporine | 2012 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
| Modification of a promiscuous inhibitor shifts the inhibition from γ-secretase to FLT-3. |
| 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. |
| AID1381305 | Inhibition of FLT3 ITD mutant (unknown origin) using TAMRA-Src- tide as substrate at 12.5 uM after 1 hr by fluorescence polarization assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID1587945 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| AID1581223 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID507673 | Binding affinity to PIK3C2G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1381303 | Aqueous solubility in pH 7.4 phosphate buffer at 120 uM after 24 hrs by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID507918 | Binding affinity to EGFR S752-I759del mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256589 | Average Binding Constant for EPHA4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764723 | Induction of apoptosis in human MV4-11 cells assessed as necrotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 0.25%) | | | |
| 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. |
| AID1764700 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 10.46%) | | | |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID507900 | Binding affinity to DLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1217864 | Drug excretion in urine of male cynomolgus monkey at 6 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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. |
| AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID290408 | Inhibition of KDR | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8
| Pharmacophore modeling and in silico screening for new KDR kinase inhibitors. |
| AID508023 | Binding affinity to PIK3CA M1043I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID1224775 | Delta TM value showing the stabilisation of ERK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID626035 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation at 1 uM by BrdU incorporation assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| AID665075 | Inhibition of recombinant FAK using poly(Glu,Tyr)4 as substrate assessed as inhibition of [33P]Phosphate incorporation into substrate after 80 mins by scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
| Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
| AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507652 | Binding affinity to p38-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID625037 | Binding constant for PIK3CA(C420R) 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. |
| AID383302 | Inhibition of DAPK3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1334912 | Growth inhibition of human HuH7 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Design, synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybrids. |
| AID1581229 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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. |
| AID216912 | Inhibition of Vascular endothelial growth factor receptor in 3T3 cells | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1387036 | Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| 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. |
| AID508134 | Binding affinity to YES | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID636126 | Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors. |
| 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. |
| AID256592 | Average Binding Constant for LIMK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1630234 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID383311 | Inhibition of MAP4K5 | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1586359 | Antiproliferative activity against human MCF7 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID1599932 | Inhibition of EGFR (unknown origin) using Poly (Glu, Tyr) 4:1 as substrate preincubated with substrate followed by enzyme challenge for 1 hr by ELISA | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1236880 | Cytotoxicity against human HeLa cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID638924 | Inhibition of FGFR1 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID619785 | Cytotoxicity against human A549 cells assessed as cell viability at 1 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424897 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1876075 | Antiviral activity against DENV 4 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID508108 | Binding affinity to TGFBR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1563377 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID507939 | Binding affinity to ERK5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID599570 | Inhibition of VEGF-induced cell proliferation in HUVEC by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID507623 | Binding affinity to MKNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1517773 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID383079 | Inhibition of PDGFR | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| AID1737725 | Inhibition of wild-type human partial length FLT1 (R781 to F1239 residues) expressed in bacterial expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| 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. |
| AID491724 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| 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. |
| AID507808 | Binding affinity to AAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1224762 | Delta TM value showing the stabilisation of CLK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID507595 | Binding affinity to MAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID255700 | In vivo effective dose required to inhibit uterine edema induced by 17 beta-estradiol (20-25 ug/mouse) in BALB/c female mouse | 2005 | Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
| Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. |
| AID1381311 | Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| 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. |
| AID435165 | Binding constant for JAK1(Kin.Dom.1/JH2 - pseudokinase) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID507641 | Binding affinity to NDR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587942 | Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID256573 | Average Binding Constant for PAK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID479745 | Inhibition of SRC | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507821 | Binding affinity to ACVR2A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507913 | Binding affinity to EGFR L747-S752del, P753S mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435443 | Binding constant for TXK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID1549999 | Antiproliferative activity against human MCF7 cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID435558 | Binding constant for RPS6KA3(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224779 | Delta TM value showing the stabilisation of NEK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435830 | Binding constant for RPS6KA2(Kin.Dom.2 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID256576 | Average Binding Constant for MKNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1705892 | Cytotoxicity against human CAKI-1 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity. |
| AID1764685 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 1000 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID507921 | Binding affinity to EPHA3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1611385 | Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent. |
| 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. |
| 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. |
| AID507577 | Binding affinity to JNK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID479744 | Inhibition of SGK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1195284 | Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. |
| AID1581258 | Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1409080 | Inhibition of human PDGFRbeta at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID1465755 | Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID671090 | Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. |
| 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. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764710 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at S phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 16.28%) | | | |
| AID1154762 | Toxicity in athymic BALBc/J mouse xenografted with human MDA-MB-435 cells assessed as body weight at 30 mg/kg twice weekly | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| AID1302361 | Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1431176 | Cytotoxicity against human A431 cells | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID508034 | Binding affinity to PKAC-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507919 | Binding affinity to EPHA1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1431173 | Inhibition of VEGFR-2 in human U251 cells assessed as reduction in VEGF induced phosphorylation preincubated for 60 mins followed by VEGF addition measured after 10 mins by ELISA method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| AID1335668 | Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| 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. |
| 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. |
| AID508035 | Binding affinity to PKAC-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1207414 | Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform | | | |
| AID458684 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 1 nM relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID1218185 | AUC (0 to infinity) in male Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID1737730 | Cytotoxicity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by MTS assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421409 | Inhibition of recombinant human EGFR at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID1600368 | Antiangiogenic activity in Leghorn chicken fertilized egg chorioallantoic membrane measured after 48 hrs by CAM assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| 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. |
| AID1425179 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1224773 | Delta TM value showing the stabilisation of ASK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1204917 | Inhibition of RET (unknown origin) | 2015 | Journal of medicinal chemistry, May-14, Volume: 58, Issue:9
| Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. |
| 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. |
| AID1600260 | Cytotoxicity against human HCT116 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID619792 | Cytotoxicity against human DLD1 cells assessed as cell viability at 10 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625085 | Binding constant for ULK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1431174 | Inhibition of EGFR in human A431 cells assessed as reduction in EGF induced phosphorylation preincubated for 60 mins followed by EGF addition measured after 10 mins by ELISA method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224787 | Delta TM value showing the stabilisation of PIM2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID507622 | Binding affinity to MINK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507902 | Binding affinity to DMPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218120 | Tmax in female cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1304253 | Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis and biological evaluation of oxindole linked indolyl-pyrimidine derivatives as potential cytotoxic agents. |
| AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID638914 | Inhibition of PDGFRbeta at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID756127 | Inhibition of human recombinant soluble epoxide hydrolase assessed as cyano(6-methoxy-naphthalen-2-yl)methyl trans-[(3-phenyloxyran-2-yl)methyl] carbonate conversion to 6-methoxy-2-naphthaldehyde preincubated for 5 mins prior to substrate addition by fluo | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
| Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. |
| 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. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID479496 | Inhibition of gamma secretase mediated amyloid beta 42 generation in human H4 cells at 10 uM by LPECL assay | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1176839 | Inhibition of PDGFRbeta (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| 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. |
| AID1395537 | Induction of apoptosis in human HT-29 cells assessed as viable cells at 25000 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 82 +/- 1%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| 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. |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID738481 | Binding affinity to non phosphorylated ABL1 (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1424891 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| 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. |
| 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. |
| 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. |
| AID626036 | Inhibition of VEGFR2 phosphorylation at tyr-1175 in VEGF-stimulated HUVEC at 1 uM preincubated for 1 hr before VEGF induction measured after 5 mins by Western blot analysis | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| AID1386991 | Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1764731 | Induction of apoptosis in human MOLM-13 cells assessed as necrotic apoptotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 0.45%) | | | |
| 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. |
| AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1218119 | Cmax in female cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID1224752 | Delta TM value showing the stabilisation of CAMK2B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1764651 | Inhibition of VEGFR1 (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID434172 | Antitumor activity against human SK-RC-52 cells xenografted BALB/c nu/nu mouse assessed as inhibition of tumor growth at 20 mg/kg, ip | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
| In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives. |
| AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563325 | Inhibition of c-KIT V559A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID507805 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508078 | Binding affinity to RPS6KA5(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625051 | Binding constant for PRKCQ 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. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1757408 | Inhibition of PDGFRbeta (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway 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. |
| AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1207447 | Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform | | | |
| 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. |
| AID1600270 | Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID1876097 | Antiviral activity against WNV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| 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. |
| 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. |
| 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. |
| AID747273 | Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and antiproliferative evaluation of piperazine-1-carbothiohydrazide derivatives of indolin-2-one. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764684 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 1 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1509578 | Cytotoxicity against human HuH7 cells infected with DENV2 New Guinea C by microplate alamar blue assay | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. |
| AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1409090 | Inhibition of human Flt1 at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| 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. |
| AID256561 | Average Binding Constant for BTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID738226 | Binding affinity to MET (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1563532 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in ERK phosphorylation at T202 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1453239 | Inhibition of PAK4 (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
| Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study. |
| AID1764692 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 10.46%) | | | |
| AID507852 | Binding affinity to CAMK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1433898 | Drug internalization in human EPC assessed as alphavbeta3-mediated drug uptake per mg protein at 1 uM measured after 1 hr by HPLC-ESI-MS/MS analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| 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. |
| AID624995 | Binding constant for CSF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256631 | Average Binding Constant for FLT4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224796 | Delta TM value showing the stabilisation of LOK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1302364 | Antiproliferative activity against human GIST48B cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID331981 | Inhibition of c-Met dependent HGF-induced human DU145 cell scattering | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
| 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. |
| AID1155246 | Binding affinity to FGFR1 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1764736 | Induction of apoptosis in human MOLM-13 cells assessed as viable cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 92.83%) | | | |
| AID693405 | Cytotoxicity against VEGFR expressing human HT-29 cells after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, in silico, in vitro, and in vivo investigation of 5-[¹¹C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2. |
| AID1387035 | Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625039 | Binding constant for PIK3CA(E545A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1509570 | Binding affinity to wild type DNA-tagged human AAK1 (G25 to L333 residues) expressed in bacterial expression system by quantitative PCR based KINOMEscan assay | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. |
| AID256574 | Average Binding Constant for STK3_m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1586453 | Inhibition of VEGFR2 internalization in HMEC1 cells at 14 uM after 24 hrs by immunofluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID1587974 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1866826 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation incubated for 6 hrs by capillary tube formation assay | 2022 | Journal of natural products, 04-22, Volume: 85, Issue:4
| Nyuzenamide C, an Antiangiogenic Epoxy Cinnamic Acid-Containing Bicyclic Peptide from a Riverine |
| AID479498 | Toxicity in human H4 cells at 10 uM | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID256567 | Average Binding Constant for EPHA6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID1781303 | Half life in human liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/SM analysis | | | |
| AID507811 | Binding affinity to ABL1 F317I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID508077 | Binding affinity to RPS6KA4(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1217835 | Tmax in female Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507675 | Binding affinity to PIK3CA C420R mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507929 | Binding affinity to EPHB3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1478171 | Inhibition of human PDGFR at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID614648 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 after 60 mins by activity based 100 fold dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1231619 | Antiangiogenic activity in Sprague-Dawley rat thoracic aorta ring assessed as inhibition of microvessel outgrowth at 0.33 uM measured on day 6 by inverse microscopic analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents. |
| AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507651 | Binding affinity to OSR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507932 | Binding affinity to ERBB2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764686 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 333 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID507627 | Binding affinity to MLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507677 | Binding affinity to PIK3CA E545A mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507903 | Binding affinity to DRAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507855 | Binding affinity to CAMK2A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563316 | Toxicity in BALB/c nu mouse xenografted with human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I mutant assessed as death at 20 mg/kg/day, po administered via gavage for 3 days | | | |
| AID256632 | Average Binding Constant for CDK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID1301838 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID1433914 | Cytotoxicity against human EPC assessed as cell viability at 1 uM measured after 24 to 72 hrs by trypan blue exclusion assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1744431 | Selectivity index, ratio of IC50 for bovine GRK2 to IC50 for human GRK5 using porcine brain tubulin as substrate by [gamma-32P]-ATP assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224774 | Delta TM value showing the stabilisation of p38beta produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID256562 | Average Binding Constant for PAK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID508046 | Binding affinity to PRKCQ | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1478064 | Inhibition of human ABL at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID481817 | Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA | 2010 | Bioorganic & medicinal chemistry, May-15, Volume: 18, Issue:10
| Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256616 | Average Binding Constant for CDK5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID508027 | Binding affinity to PIK3CG | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218231 | Volume of distribution at steady state in female Sprague-Dawley rat plasma at 5 mg/kg, iv administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256668 | Average Binding Constant for ABL1(H396P); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase 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. |
| AID507949 | Binding affinity to FGFR4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1276910 | Inhibition of recombinant N-terminal 6His-tagged VEGFR-2 (unknown origin) using FL-Peptide 22 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. |
| AID507649 | Binding affinity to NIM1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID479525 | Inhibition of ERK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507656 | Binding affinity to PAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581218 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1302363 | Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1896571 | Antiproliferative activity against human A498 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 78 | Sunitinib-based Proteolysis Targeting Chimeras (PROTACs) reduced the protein levels of FLT-3 and c-KIT in leukemia cell lines. |
| AID1337498 | Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Design, synthesis, and biological evaluation of (2E)-(2-oxo-1, 2-dihydro-3H-indol-3-ylidene)acetate derivatives as anti-proliferative agents through ROS-induced cell apoptosis. |
| AID1218122 | Terminal half life in female cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1327319 | Cytotoxicity against HGC cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435190 | Binding constant for full-length PIP5K1A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1387049 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and V654 mutant (unknown origin) allografted in CB17 SCID mouse assessed as inhibition of tumor growth at 80 mg/kg, po qd measured on last day of dosing | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| 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. |
| AID507576 | Binding affinity to JNK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID614652 | Inhibition of human N-terminal His-tagged phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by activity based 100 fold dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1406762 | Antiproliferative activity against human HCT116 cells by MTT assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Diterpenoid lead stevioside and its hydrolysis products steviol and isosteviol: Biological activity and structural modification. |
| AID1550001 | Antiproliferative activity against human A549 cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507961 | Binding affinity to GAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1517768 | Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID1395587 | Effect on VEGF gene expression in human HT-29 cells assessed as VEGF level at 25 uM after 48 hrs by RT-qPCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1169706 | Half life in human liver microsomes by LC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
| 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. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507590 | Binding affinity to LKB1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587956 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1424497 | Antitumor activity in patient with renal cell carcinoma assessed as overall survival during phase 3 non-inferiority trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID1563336 | Inhibition of c-KIT D816H mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1195283 | Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. |
| 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. |
| AID1581225 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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. |
| AID1425022 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID507956 | Binding affinity to FLT3 K663Q mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1301836 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| 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. |
| 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. |
| AID1739053 | Binding affinity to human DDR1 | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
| AID665081 | Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID1218178 | Apparent terminal half life in female Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1587953 | Inhibition of human c-KIT ATP binding domain exon 14 T670I single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1878086 | Inhibition of FLT3-ITD autophosphorylation in human MV4-11 cells measured after 2 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID508053 | Binding affinity to PRKX | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1442001 | Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay | 2017 | Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
| Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1). |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435399 | Binding constant for DCAMKL3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1409079 | Inhibition of human PDGFRalpha at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID738217 | Growth inhibition of human HT-29 cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1304252 | Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis and biological evaluation of oxindole linked indolyl-pyrimidine derivatives as potential cytotoxic agents. |
| 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. |
| AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479733 | Inhibition of P38alpha | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1587971 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507583 | Binding affinity to KIT V559D,T670I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1744440 | Thermodynamic solubility of compound in phosphate buffer at 6 pH by shake flask method | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. |
| AID256672 | Average Binding Constant for CAMK2G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID256571 | Average Binding Constant for BIKE; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507830 | Binding affinity to AMPK-alpha1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1217868 | Drug excretion in urine of human at 5 mg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1478173 | Inhibition of human TNIK at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID256652 | Average Binding Constant for CAMK2B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1399364 | Inhibition of EGF-induced EGFR activation in human A431 cells pretreated for 60 mins followed by EGF addition and measured after 10 mins by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
| Design, synthesis and preclinical evaluation of 5-methyl-N |
| AID1395082 | Inhibition of VEGFR2 phosphorylation in HUVEC at 1 uM after 24 hrs by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity. |
| AID1301839 | Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| 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. |
| AID256648 | Average Binding Constant for RPS6KA5 (Kin.Dom 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical 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. |
| 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. |
| AID1764698 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 16.31%) | | | |
| 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. |
| AID1563334 | Inhibition of c-KIT S709F mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID507938 | Binding affinity to ERK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587962 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| AID479512 | Inhibition of AKT2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507841 | Binding affinity to BLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1581239 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID384129 | Cytotoxicity against human SNU1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1563323 | Inhibition of c-KIT in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID738218 | Growth inhibition of human KB cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| 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. |
| 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. |
| 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. |
| AID1453240 | Inhibition of PAK5 (unknown origin) | 2017 | Bioorganic & medicinal chemistry, 07-01, Volume: 25, Issue:13
| Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study. |
| 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. |
| AID1433894 | Stability in rat plasma assessed as compound remaining at 1 uM measured up to 8 hrs by HPLC-UV-Vis analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1312685 | Antiangiogenic activity in HUVEC assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
| AID1581226 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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. |
| 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. |
| AID1563531 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in pS6 phosphorylation at S236 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1587955 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1440375 | Antitumor activity against human MV4-11 cells xenografted in Harlan nude mouse assessed as tumor growth inhibition administered ig qd for 20 days | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1587998 | Antitumor activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant xenografted in NOD-SCID mouse assessed as tumor growth inhibition at 40 mg/kg, po ad | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1876073 | Antiviral activity against DENV 2 | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| 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. |
| AID1586430 | Inhibition of VEGFR2 internalization in HMEC1 cells assessed as membrane VEGFR2 level at 14 uM after 24 hrs by flow cytometry (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID1517772 | Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID619787 | Cytotoxicity against human DLD1 cells assessed as cell viability at 1 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256572 | Average Binding Constant for STK36; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1760969 | Antiproliferative activity against human HT-29 cells assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold. |
| AID1764652 | Inhibition of VEGFR2 (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID1395081 | In vivo antiangiogenic activity in chicken egg chorioallantoic membrane at 1 uM after 72 hrs | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity. |
| AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507809 | Binding affinity to ABL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224801 | Delta TM value showing the stabilisation of MST1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID256563 | Average Binding Constant for ULK3 m; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507937 | Binding affinity to ERK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1335666 | Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| 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. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625108 | Binding constant for MKNK2 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. |
| AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425185 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224789 | Delta TM value showing the stabilisation of PLK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1334913 | Growth inhibition of human SW620 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Design, synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybrids. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624716 | Binding constant for CSNK1D 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. |
| AID507615 | Binding affinity to MEK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1586375 | Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 22 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 28 +/- 0.6%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID718827 | Inhibition of Flt1 at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
| AID774152 | Half life in human liver microsomes at 1 uM by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID629513 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID608768 | Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1586424 | Induction of apoptosis in human A549 cells at 50 uM after 20 to 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 16%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID256617 | Average Binding Constant for TEK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID508039 | Binding affinity to PLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID636123 | Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors. |
| AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507612 | Binding affinity to MEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID256593 | Average Binding Constant for NEK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID435658 | Binding constant for JAK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1424949 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| 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. |
| AID1236878 | Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435441 | Binding constant for RPS6KA4(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID507831 | Binding affinity to AMPK-alpha2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID479735 | Inhibition of PAK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID1563519 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S236 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383315 | Inhibition of PCTK1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1739052 | Binding affinity to human NTRK1 | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
| AID1207774 | Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits | 2013 | Scientific reports, , Volume: 3 | MICE models: superior to the HERG model in predicting Torsade de Pointes. |
| AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737721 | Inhibition of wild-type human partial length VEGFR2 (R787 to P1253 residues) expressed in mammalian expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| 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. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425126 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507085 | Inhibition of recombinant EphB4R by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID256606 | Average Binding Constant for STK16; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764680 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 111 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508062 | Binding affinity to RIOK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1586360 | Antiproliferative activity against human HeLa cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID1764695 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G2/M phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 7.29%) | | | |
| AID608771 | Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507923 | Binding affinity to EPHA5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507924 | Binding affinity to EPHA6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256638 | Average Binding Constant for PRKAA1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507074 | Inhibition of recombinant PI3Kdelta by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID256630 | Average Binding Constant for FYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1424976 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1629524 | Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID507810 | Binding affinity to ABL1 E255K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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 |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID436050 | Binding constant for RPS6KA2(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1301840 | Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID638916 | Inhibition of EGFR at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID459248 | Inhibition of ALK by ELISA-based kinase assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| AID1155236 | Binding affinity to RET (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID491753 | Inhibition of VEGFR3 at 0.1 uM | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1224759 | Delta TM value showing the stabilisation of CDKL1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1440344 | Inhibition of human FLT3 | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID479746 | Inhibition of SYK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1421403 | Inhibition of recombinant human VEGFR1 at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| 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. |
| AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563508 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y719 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID599571 | Inhibition of bFGF-induced cell proliferation in HUVEC by MTT assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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. |
| 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. |
| AID507876 | Binding affinity to CIT | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID508135 | Binding affinity to YSK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425011 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507820 | Binding affinity to ACVR1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1440304 | Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1484889 | Inhibition of c-kit (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at 1 uM after 1 hr by ELISA relative to control | 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. |
| AID507678 | Binding affinity to PIK3CA E545K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1381315 | Lipophilicity, chromatographic hydrophobicity index of the compound at pH 1.2 by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID507807 | Toxicity against human A375 cells after 72 hrs by cell titer-blue assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID479529 | Inhibition of FYN | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID657322 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents. |
| AID1433893 | Inhibition of VEGF-A-induced cell proliferation in human EPC at 1 uM measured after 24 hrs by trypan blue exclusion assay relative to control | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1218127 | Cmax in male cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16
| FDA-approved drug labeling for the study of drug-induced liver injury. |
| AID1586428 | Binding affinity to recombinant human VEGFR2 assessed as free VEGFR2 level at 30 uM after 30 mins by ELISA relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| 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. |
| AID507840 | Binding affinity to BIKE | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224794 | Delta TM value showing the stabilisation of RSK2b produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1236877 | Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1224767 | Delta TM value showing the stabilisation of DAPK3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1587934 | Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507832 | Binding affinity to ANKK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1195286 | Antiproliferative activity against human A431 cells after 48 hrs by sulforhodamine B assay | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. |
| AID507580 | Binding affinity to KIT D816V mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1602315 | Toxicity in zebrafish embryo assessed as mortality at 10 uM measured 120 hpf by fluorescence microscopy | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID624702 | Binding constant for BRSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1158436 | Cytotoxicity against human MDA-MB-435 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID1186613 | Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
| AID1563340 | Inhibition of c-KIT D820Y mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID256585 | Average Binding Constant for EPHA7; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1631798 | Cytotoxicity against human MCF10A cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Design and synthesis of 4'-O-alkylamino-tethered-benzylideneindolin-2-ones as potent cytotoxic and apoptosis inducing agents. |
| AID624789 | Binding constant for KIT(D816V) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID614650 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by activity based 100 fold dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1155233 | Binding affinity to VEGFR2 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508055 | Binding affinity to PYK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508106 | Binding affinity to TESK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID255111 | Cellular inhibition of VEGF induced human KDR phosphorylation in 3T3 murine fibroblasts | 2005 | Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
| Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. |
| 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. |
| AID606557 | Binding affinity to human Cdk2 | 2011 | Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
| Irreversible Nek2 kinase inhibitors with cellular activity. |
| AID624749 | Binding constant for CASK 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. |
| 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. |
| AID507891 | Binding affinity to CTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507947 | Binding affinity to FGFR3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508025 | Binding affinity to PIK3CB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224755 | Delta TM value showing the stabilisation of CAMK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624843 | Binding constant for CAMK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1517770 | Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Synthesis, anticancer activity, and molecular modeling of 1,4-naphthoquinones that inhibit MKK7 and Cdc25. |
| AID507657 | Binding affinity to PAK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1399367 | Cytotoxicity against human A431 cells over-expressing EGFR | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
| Design, synthesis and preclinical evaluation of 5-methyl-N |
| AID508075 | Binding affinity to RPS6KA3(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1518669 | Inhibition of wildtype FLT3 (unknown origin) phosphorylation measured after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID1878078 | Inhibition of FLT3-D835Y autophosphorylation in human MV4-11 cells measured after 2 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507631 | Binding affinity to MST1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737707 | Inhibition of tracer 236 binding to recombinant human N-terminal GST-tagged full length KDR (790 to 1356 residues) expressed in baculovirus expression system incubated for 1 hr by Lanthascreen assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1587959 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| 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. |
| AID1224754 | Delta TM value showing the stabilisation of CAMK2G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1224783 | Delta TM value showing the stabilisation of PAK6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID383312 | Inhibition of MYLK2 | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| AID1155247 | Binding affinity to FAK (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1158439 | Cytotoxicity against human ER-positive MCF7 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| 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. |
| AID1581260 | Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID463633 | Inhibition of VEGFR2 | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| 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. |
| AID1845556 | Inhibition of NUAK1 (unknown origin) | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Development and Therapeutic Potential of NUAKs Inhibitors. |
| 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. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID665076 | Inhibition of recombinant VEGFR2 using poly(Glu,Tyr)4 as substrate assessed as inhibition of [33P]Phosphate incorporation into substrate after 80 mins by scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625029 | Binding constant for BRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1587967 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID256598 | Average Binding Constant for FRK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764724 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 98.86%) | | | |
| AID256666 | Average Binding Constant for ABL1(Q252H); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID479738 | Inhibition of PKCbeta2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID745345 | Inhibition of VEGFR2 phosphorylation in growth factor-stimulated HUVEC | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). |
| 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. |
| AID1737724 | Inhibition of wild-type human partial length autoinhibited CSF1R (Y538 to S939 residues) expressed in mammalian expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1381313 | Lipophilicity, chromatographic hydrophobicity index of the compound at pH 7.4 by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID1563378 | Growth inhibition of human GIST48B cells after 72 hrs by CCK8 assay | | | |
| AID1563516 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at T308 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| 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. |
| AID734225 | Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents. |
| AID479520 | Inhibition of CHK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID508129 | Binding affinity to VEGFR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507894 | Binding affinity to DAPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1395076 | Inhibition of VEGFR2 (unknown origin) at 10 uM using TK substrate after 1 hr by HTRF assay relative to control | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity. |
| AID1814372 | Inhibition of Flt-1 (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
| Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| 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. |
| AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID361268 | Inhibition of human recombinant Nek2 T175A mutant by coupled pyruvate kinase/lactate dehydrogenase assay | 2007 | The Journal of biological chemistry, Mar-02, Volume: 282, Issue:9
| Structure and regulation of the human Nek2 centrosomal kinase. |
| 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. |
| AID614641 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 preincubated for 120 mins in presence of ATP by AlphaScreen analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1587980 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID517655 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| 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. |
| 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. |
| AID508087 | Binding affinity to SLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425048 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1207267 | Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform | | | |
| AID507572 | Binding affinity to JH1 catalytic domain JAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1363084 | Half life in human liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | | | |
| AID1563326 | Inhibition of c-KIT V559D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508122 | Binding affinity to TXK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID508096 | Binding affinity to STK35 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID536891 | Antitumor activity against human HT-29 cells xenografted in BALB/cA nude mouse assessed as inhibition of tumor growth at 30 mg/kg, po administered 11 days after tumor implantation qd for 14 days | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID508103 | Binding affinity to TAOK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1830546 | Inhibition of FLT3 D835Y mutant (unknown origin) using Poly (Glu,Tyr) 4:1 as substrate incubated for 1 hr in presence of ATP by ELISA | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Discovery and structure - activity relationship exploration of pyrazolo[1,5-a]pyrimidine derivatives as potent FLT3-ITD 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. |
| 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. |
| 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. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID645868 | Toxicity in human Calu6 cells xenografted po dosed BALB/c mouse assessed as body weight change administered qd for 11 days | 2012 | Bioorganic & medicinal chemistry, Feb-15, Volume: 20, Issue:4
| Angiogenesis inhibitors identified by cell-based high-throughput screening: synthesis, structure-activity relationships and biological evaluation of 3-[(E)-styryl]benzamides that specifically inhibit endothelial cell proliferation. |
| 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. |
| 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. |
| 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. |
| AID671088 | Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. |
| AID507963 | Binding affinity to GRK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID157328 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 5% bovine serum albumin | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1581221 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1895651 | Inhibition of PDGFRbeta (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| AID256605 | Average Binding Constant for STK17B; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1633238 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. |
| 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. |
| AID491751 | Inhibition of FLT3 | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| AID1433899 | Drug internalization in human EPC assessed as alphavbeta3-mediated drug uptake at 1 uM measured after 1 hr by HPLC-ESI-MS/MS analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1224771 | Delta TM value showing the stabilisation of MEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID665080 | Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID507674 | Binding affinity to PIK3CA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID649620 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507926 | Binding affinity to EPHA8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1154758 | Antitumor activity against human MDA-MB-435 cells xenografted into flank of athymic BALBc/J mouse assessed as decrease in tumor growth at 30 mg/kg twice weekly measured up to 34 days | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| AID1224780 | Delta TM value showing the stabilisation of OSR1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1433904 | Inhibition of VEGFR2 (unknown origin) phosphorylation | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| 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. |
| AID507895 | Binding affinity to DCAMKL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID614649 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| 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. |
| 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. |
| AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID434174 | Toxicity in human SK-RC-52 cells xenografted BALB/c nu/nu mouse assessed as effect on body weight at 20 mg/kg, ip | 2009 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 19, Issue:16
| In vivo targeting of tumor-associated carbonic anhydrases using acetazolamide derivatives. |
| AID1764705 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G1 phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 69.08%) | | | |
| 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. |
| AID1224790 | Delta TM value showing the stabilisation of PLK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1424902 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563498 | Antitumor activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I mutant xenografted in BALB/c mouse assessed as tumor weight at 20 mg/kg/day, po administered via gavage for 28 days (Rvb = 1.87 g) | | | |
| AID1158441 | Cytotoxicity against mouse triple negative 4T1 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID734138 | Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastati |
| 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. |
| AID1587976 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1431171 | Displacement of [3H]colchicine from bovine brain tubulin at 5 uM measured after 10 mins by liquid scintillation counting method relative to control | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| AID1737427 | Inhibition of FLT3 (unknown origin) | | | |
| AID1550020 | Effect on VEGFR2 in human A549 cells assessed as total VEGFR2 level at 10 uM incubated for 24 hrs by flow cytometric analysis relative to control | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| 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. |
| AID1563511 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y719 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID256611 | Average Binding Constant for RIPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1363085 | Half life in rat liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis | | | |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID458664 | Inhibition of human FMS expressed in growth factor dependent mouse FDC-P1 cells assessed as inhibition of FMS-mediated cell proliferation in presence human CSF1 after 48 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID1431170 | Inhibition of bovine brain tubulin assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID507596 | Binding affinity to MAP3K1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1195287 | Antiangiogenic activity in VEGF-165 and bFGF-stimulated chicken embryo chorioallantoic membrane assessed as inhibition of blood vessel formation after 40 hrs by microscopy | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10
| The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents. |
| AID459249 | Inhibition of ABL by ELISA-based kinase assay | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| AID508127 | Binding affinity to ULK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507812 | Binding affinity to ABL1 F317L mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1631795 | Cytotoxicity against human DU145 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Design and synthesis of 4'-O-alkylamino-tethered-benzylideneindolin-2-ones as potent cytotoxic and apoptosis inducing agents. |
| 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. |
| 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. |
| AID1587984 | Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1586358 | Antiproliferative activity against human HT-29 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1629522 | Inhibition of TEL-fused cKIT D816V mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID508085 | Binding affinity to SIK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID710259 | Antimigratory activity against human HCT116 cells assessed as inhibition of cell migration after 24 hrs by wound healing assay | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. |
| AID1876071 | Antiviral activity against HCV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1327313 | Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1484884 | Inhibition of PDGFRalpha (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at 1 uM after 1 hr by ELISA relative to control | 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. |
| AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1399365 | Inhibition of VEGF-induced VEGFR2 activation in human U251 cells pretreated for 60 mins followed by VEGF addition and measured after 10 mins by ELISA | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
| Design, synthesis and preclinical evaluation of 5-methyl-N |
| AID624755 | Binding constant for ZAK 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. |
| AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID629511 | Cytotoxicity against human HL60 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID729980 | Inhibition of KDR (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| 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. |
| AID1465751 | Inhibition of KIT V559D/T670I double mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| 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. |
| 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. |
| AID1327317 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479533 | Inhibition of INSR | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1581216 | Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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. |
| AID491722 | Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID649467 | Antitumor activity against mouse BA/F3 cells expressing FLT3-ITD mutant xenografted in BALB/c mouse myeloproliferative model assessed as increase in host survival days at 120 mg/kg, po bid relative to control (Rvb = 20 days) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1815596 | Anti-angiogenesis activity against HUVEC cells assessed as reduction in tubule formation at 50 nM incubated for 6 hrs by inverted fluorescence microscopic analysis relative to control | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| 2,3-Difunctionalized Benzo[ |
| AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1158437 | Cytotoxicity against human triple negative MDA-MB-231 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| 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. |
| AID1478163 | Inhibition of human EPHA3 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| 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. |
| AID1224791 | Delta TM value showing the stabilisation of PRKACA produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID1550000 | Antiproliferative activity against human HeLa cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1218247 | Drug excretion in urine of male Sprague-Dawley rat at 15 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID1218228 | AUC (0 to infinity) in female Sprague-Dawley rat plasma at 5 mg/kg, iv administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1334911 | Growth inhibition of human HCT116 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
| Design, synthesis and cytotoxic activities of scopoletin-isoxazole and scopoletin-pyrazole hybrids. |
| 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. |
| AID1290540 | Antiangiogenic activity in human HUVEC cells assessed as angiogenesis rate at 10 uM after 5 hrs by endothelial tube formation assay relative to control | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Synthesis and preliminary evaluation of 5,7-dimethyl-2-aryl-3H-pyrrolizin-3-ones as angiogenesis inhibitors. |
| 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. |
| AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508066 | Binding affinity to RIPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID739335 | Cytotoxicity against human A498 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| Cytotoxic scalarane sesterterpenes from a Korean marine sponge Psammocinia sp. |
| AID435653 | Binding constant for EGFR(L747-S752del, P753S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507943 | Binding affinity to FER | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1224751 | Delta TM value showing the stabilisation of CAMK2A produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| 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. |
| AID1481733 | Anticancer activity against human RCC4 cells after 48 hrs by XTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
| Synthesis and anti-cancer activities of new sulfonamides 4-substituted-triazolyl nucleosides. |
| AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435942 | Selectivity for KIT as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507601 | Binding affinity to MAP4K2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID657323 | Cytotoxicity against human PC9 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents. |
| 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. |
| 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. |
| AID507823 | Binding affinity to ACVRL1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID256581 | Average Binding Constant for CAMK1G; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1224777 | Delta TM value showing the stabilisation of MST4(1) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155244 | Binding affinity to FMS (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID491721 | Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| 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. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1599894 | Antiproliferative activity against human HUVEC cells expressing VEGFR2 assessed as reduction in cell growth incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563528 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in AKT phosphorylation at T308 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID479532 | Inhibition of IGF1R | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1587949 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| 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. |
| AID1873225 | Inhibition of ABCG2 (unknown origin) expressed in human SAOS-2 cells mediated Hoechst 33342 efflux preincubated with compound for 15 mins followed by substrate addition and measured after 45 mins using Hoechst 33342 as substrate by flow cytometry | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
| AID458676 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells relative to control by Western blot | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID1630236 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G0/G1 phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 34.93 %) | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID256609 | Average Binding Constant for AAK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1581241 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507621 | Binding affinity to MET Y1235D mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1815605 | Antiangiogenic activity in BALB/c mouse assessed as reduction in neovascularization by measuring reduction in hemoglobin concentration at 2 uM by matrigel plug assay | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| 2,3-Difunctionalized Benzo[ |
| AID331983 | Inhibition of human VEGFR2-dependent HUVEC proliferation | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
| AID625017 | Binding constant for TIE1 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. |
| AID710262 | Antiangiogenic activity in HUVECs under hypoxic condition assessed as inhibition of tube formation at 2 uM after 18 hrs | 2012 | Journal of medicinal chemistry, Dec-13, Volume: 55, Issue:23
| Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. |
| AID1310408 | Cytotoxicity against human DU145 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and apoptosis inducing effect of novel (Z)-3-(3'-methoxy-4'-(2-amino-2-oxoethoxy)-benzylidene)indolin-2-ones as potential antitumour agents. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1563417 | Inhibition of AKT autophosphorylation at T308 residue in human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I mutant at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1218114 | Apparent oral clearance in human plasma at 50 mg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507858 | Binding affinity to CAMK2G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1440345 | Inhibition of human FLT3 ITD mutant | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID508052 | Binding affinity to PRKR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID491756 | Inhibition of cKIT at 0.1 uM | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| AID1602305 | Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID599565 | Antitumor activity against human IM9 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID507925 | Binding affinity to EPHA7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507878 | Binding affinity to CLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID773016 | Inhibition of PDGFR-beta (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID157329 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1631796 | Cytotoxicity against human BT549 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Design and synthesis of 4'-O-alkylamino-tethered-benzylideneindolin-2-ones as potent cytotoxic and apoptosis inducing agents. |
| AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507909 | Binding affinity to EGFR E746-A750del mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID738214 | Growth inhibition of African green monkey Vero cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507613 | Binding affinity to MEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507604 | Binding affinity to MAP4K5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID759167 | Inhibition of wild-type cKIT (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764732 | Induction of apoptosis in human MOLM-13 cells assessed as viable cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 92.83%) | | | |
| AID507578 | Binding affinity to JNK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1155239 | Binding affinity to ALK (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624715 | Binding constant for ERK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1154747 | Antiangiogenic activity in chicken chorioallantoic membrane assessed as inhibition of VEGF/bFGF-induced angiogenesis treated 8 hrs after VEGF/bFGF addition measured after 40 hrs by microscopy | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| 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. |
| AID331982 | Inhibition of human VEGFR2-dependent ERK phosphorylation in HUVEC | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
| 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. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1381306 | Inhibition of FLT3 ITD mutant (unknown origin) using TAMRA-Src- tide as substrate at 1.25 uM after 1 hr by fluorescence polarization assay relative to control | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| 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. |
| AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1140200 | Inhibition of VEGFR-2 (unknown origin) at 0.1 mg/ml after 1 hr by HTRF assay | 2014 | Bioorganic & medicinal chemistry letters, May-01, Volume: 24, Issue:9
| Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
| AID1395538 | Induction of apoptosis in human HT-29 cells assessed as apoptotic cells at 25000 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 13 +/- 3%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID625142 | Binding constant for TSSK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID638913 | Inhibition of PDGFRalpha at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| 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. |
| 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. |
| 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. |
| AID1155274 | Antiproliferative activity against human NCI-H526 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1600261 | Cytotoxicity against human SW480 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID1440347 | Inhibition of human PDGFRalpha | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1312690 | Inhibition of VEGFR2 phosphorylation in human MCF7 cells assessed as reduction in expression of phosphorylated Raf1 at 1 uM incubated for 24 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1218112 | AUC (0 to infinity) in human plasma at 50 mg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID508030 | Binding affinity to PIM2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1478169 | Inhibition of human Flt3 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID1436040 | Binding affinity to recombinant human CLK2 (D144 to R498 residues) expressed in bacterial expression system by KinomeScan assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID508043 | Binding affinity to PRKCD | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID619789 | Cytotoxicity against human MV4-11 cells assessed as cell viability at 1 uM after 3 days by colorimetric MTT assay | 2011 | European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
| Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents. |
| AID1158440 | Cytotoxicity against human taxoid-resistant MCF7 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID256584 | Average Binding Constant for CAMK1D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID729551 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 10 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
| AID1424965 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID508045 | Binding affinity to PRKCH | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507860 | Binding affinity to CAMKK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID738478 | Binding affinity to phosphorylated ABL1 (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1207294 | Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform | | | |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507859 | Binding affinity to CAMK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508058 | Binding affinity to RET | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID665074 | Inhibition of recombinant Aurora B using tetra(LRRWSLG) as substrate assessed as inhibition of [33P]Phosphate incorporation into substrate after 80 mins by scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507083 | Inhibition of recombinant VEGFR2 by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1409094 | Inhibition of human RET at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155211 | Toxicity in BALB/c nude mouse xenografted with human HT-29 cells assessed as mortality at 80 mg/kg/day administered qd measured on day 21 | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1302355 | Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID256669 | Average Binding Constant for ABL1(M351T); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507672 | Binding affinity to PIK3C2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID463634 | Inhibition of PDGFRbeta | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID718825 | Inhibition of PDGFRbeta at 100 uM | 2012 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
| Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3β inhibitors through virtual screening. |
| 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. |
| AID1207508 | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | | | |
| AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID1581227 | Inhibition of human c-KIT A loop exon 17 D816H single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID738224 | Binding affinity to TYRO3 (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID638920 | Inhibition of EPH-B2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1488407 | Antitumor activity against human MDA-MB-231 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 80 mg/kg, qd after 21 days relative to control | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
| 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. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID491749 | Inhibition of VEGFR3 | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID507670 | Binding affinity to PHKG1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID507571 | Binding affinity to ITK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1757407 | Inhibition of VEGFR1 (unknown origin) at 1 uM by ELISA | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Rational drug design of benzothiazole-based derivatives as potent signal transducer and activator of transcription 3 (STAT3) signaling pathway inhibitors. |
| AID435404 | Binding constant for EPHB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1218128 | Tmax in male cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1586373 | Cell cycle arrest in human A549 cells assessed as accumulation at subG0 phase at 22 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 2 +/- 0.8%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID1587985 | Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1510860 | Inhibition of VEGFR2 (unknown origin) | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma. |
| AID507080 | Inhibition of recombinant HCK by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1587946 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581222 | Inhibition of human c-KIT ATP binding domain exon 13 K642E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1478177 | Inhibition of human Src at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID508083 | Binding affinity to SgK085 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256640 | Average Binding Constant for PTK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID773012 | Antiproliferative activity against human BGC cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1186612 | Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Oct-06, Volume: 85 | Novel acylureidoindolin-2-one derivatives as dual Aurora B/FLT3 inhibitors for the treatment of acute myeloid leukemia. |
| AID626037 | Inhibition of AKT phosphorylation at Ser-473 in VEGF-stimulated HUVEC at 1 uM preincubated for 1 hr before VEGF induction measured after 30 mins by Western blot analysis | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| AID1155271 | Antiproliferative activity against human MV411 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1563512 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y823 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| AID507854 | Binding affinity to CAMK1G | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID479724 | Inhibition of IRAK4 at 5 uM | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID1312687 | Inhibition of VEGFR2 in HUVEC assessed as reduction in expression of phosphorylated VEGFR2 at 1 uM incubated for 24 hrs by Western blot analysis | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
| 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. |
| AID479492 | Inhibition of gamma secretase mediated amyloid beta 38 generation in human H4 cells at 10 uM by LPECL assay | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID671887 | Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. |
| AID1155230 | Inhibition of human ERG | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID1158371 | Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508037 | Binding affinity to PKN1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507936 | Binding affinity to ERK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1709289 | Inhibition of EGFR in human A431 cells preincubated for 60 mins followed by EGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1154759 | Antitumor activity against human MDA-MB-435 cells xenografted into flank of athymic BALBc/J mouse assessed as decrease in tumor vascular density at 30 mg/kg twice weekly by CD31/PECAM-1 immunohistochemical staining | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| AID614653 | Inhibition of human N-terminal His-tagged phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID1581242 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID383105 | Inhibition of FLT3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID479531 | Inhibition of HGK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| 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. |
| AID1217834 | Cmax in female Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1876003 | Antiviral activity against ZIKV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764645 | Inhibition of FLT3 ITD mutant (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID1478069 | Inhibition of human VEGFR2 | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| 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. |
| AID1424950 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1815607 | Antiangiogenic activity in BALB/c mouse assessed as assessed as reduction in CD31-positive microvessel density in ear tissue at 2 uM measured after 6 days by fluorescence microscopic analysis | 2022 | Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
| 2,3-Difunctionalized Benzo[ |
| AID507957 | Binding affinity to FLT3 N841I mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1781304 | Half life in mouse liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/SM analysis | | | |
| 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. |
| AID629476 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| 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. |
| 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. |
| AID665073 | Inhibition of recombinant AKT1 using GSK3 as substrate assessed as inhibition of [33P]Phosphate incorporation into substrate after 80 mins by scintillation counting | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID383323 | Inhibition of SLK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1876267 | Binding affinity to AAK1 (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinase Inhibitors as Underexplored Antiviral Agents. |
| 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. |
| AID1155273 | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID256637 | Average Binding Constant for JNK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507912 | Binding affinity to EGFR L747-E749del, A750P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1478176 | Inhibition of human SLK at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID1169708 | Half life in rat liver microsomes by LC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro. |
| AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID507899 | Binding affinity to DDR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1581238 | Inhibition of human c-KIT A loop exon 11/13 V559D/V654A double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1302354 | Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID1224798 | Delta TM value showing the stabilisation of DRAK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1563337 | Inhibition of c-KIT D816V mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155277 | Antiproliferative activity against human HK2 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507842 | Binding affinity to BMPR1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1155234 | Binding affinity to PDGFR-beta (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256588 | Average Binding Constant for PCTK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1154742 | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| 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. |
| AID383081 | Inhibition of FGFR1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID638919 | Inhibition of EPH-A2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1602341 | Binding affinity to human FLT3 ITD/D835V double mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507654 | Binding affinity to p38-delta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256677 | Average Binding Constant for STK38L; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID773017 | Inhibition of VEGFR2 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764683 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 4 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID753548 | Antiangiogenic activity in human MDA-MB-435 cells xenografted in chicken embryo chorioallantoic membrane assessed as inhibition of blood vessel formation at 20 mg/kg measured after 2 days | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
| Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor. |
| AID383321 | Inhibition of RPSKA3 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID256620 | Average Binding Constant for FLT3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID256565 | Average Binding Constant for MAP4K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383296 | Inhibition of CAMK2a | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID745356 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced tube formation after 24 hrs by phalloidin-sulforhodamine staining method | 2013 | European journal of medicinal chemistry, May, Volume: 63 | Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). |
| 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. |
| AID1312684 | Inhibition of recombinant human His-tagged cytoplasmic VEGFR2 (789 to 1356 residues) expressed in baculovirus expression system incubated for 1 hr by HTRF assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents. |
| AID1764711 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G2/M phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 8.25%) | | | |
| 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. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID479526 | Inhibition of ERK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| 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. |
| AID507862 | Binding affinity to CDC2L1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507940 | Binding affinity to ERK8 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507637 | Binding affinity to MYLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507962 | Binding affinity to GCN2 Kin.Dom.2, S808G mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID674078 | Inhibition of PDGF receptor | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. |
| 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. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508100 | Binding affinity to TAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624809 | Binding constant for MYLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1833477 | Inhibition of CSF1R (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | 2021 | Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
| Discovery of ( |
| AID1433895 | Stability in human plasma assessed as compound remaining at 1 uM measured up to 8 hrs by HPLC-UV-Vis analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1876266 | Binding affinity to GAK (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinase Inhibitors as Underexplored Antiviral Agents. |
| AID1433925 | In vivo antiangiogenic activity in EHS derived matrigel plug implanted FVB mouse assessed as inhibition of VEGF-A-induced angiogenesis at 10 mg/kg, ip administered daily for 4 days by microscopic method | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1611384 | Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent. |
| 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. |
| 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. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383318 | Inhibition of PRKAA1 | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| 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. |
| AID1764721 | Induction of apoptosis in human MV4-11 cells assessed as early apoptotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 0.31%) | | | |
| AID1764738 | Induction of apoptosis in human MOLM-13 cells assessed as late apoptotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 4.54%) | | | |
| AID508042 | Binding affinity to PLK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1737702 | Inhibition of recombinant human His6-tagged AMPK alpha1/beta1/gamma1 expressed in Escherichia coli cells using ULight Acetyl-CoA Carboxylase [Ser79] Peptide as substrate incubated for 30 mins by TR-FRET assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| 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. |
| AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435931 | Binding constant for PIM1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID671888 | Toxicity in human HeLa cells assessed as cell cycle arrest at G2M phase by flow cytometry based phenotypic drug discovery based assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. |
| AID671886 | Toxicity in endothelial precursor cells co-cultured with stromal precursor ADSC cells by total nuclei count detection based phenotypic drug discovery based assay | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. |
| AID1737715 | Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 24 hrs by cell-titer glo assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID256636 | Average Binding Constant for JNK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507076 | Inhibition of recombinant mTOR by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1304250 | Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis and biological evaluation of oxindole linked indolyl-pyrimidine derivatives as potential cytotoxic agents. |
| AID1720634 | Antiviral activity against DENV2 New Guinea C strain infected in Huh7 cells after 48 hrs by renilla luciferase assay | 2020 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
| Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines. |
| AID649611 | Antitumor activity against mouse BA/F3 cells expressing FLT3-ITD mutant xenografted in BALB/c mouse myeloproliferative model assessed as disease related death at 0.05 to 5 mg/kg, po measured after 100 days | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507896 | Binding affinity to DCAMKL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1465756 | Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID507586 | Binding affinity to LATS2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID774153 | Half life in mouse liver microsomes at 1 uM by LC-MS/MS analysis | 2013 | Journal of medicinal chemistry, Oct-10, Volume: 56, Issue:19
| Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. |
| AID1629526 | Inhibition of wild type cKIT T670I mutant in human GIST-5R cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383299 | Inhibition of CLK2 | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| AID507072 | Inhibition of recombinant PI3Kalpha by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1563500 | Antitumor activity against human GIST5R cells harboring c-KIT 560 to 578 deletion/T670I mutant xenografted in BALB/c mouse assessed as tumor growth inhibition at 20 mg/kg/day, po administered via gavage for 28 days relative to control | | | |
| AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID479725 | Inhibition of KDR | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1737728 | Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by celltox-green assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID638917 | Inhibition of ErbB2 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1224792 | Delta TM value showing the stabilisation of RIOK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID1424896 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1158438 | Cytotoxicity against human triple negative MDA-MB-468 cells | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID1176836 | Inhibition of KDR (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508093 | Binding affinity to SRPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID608772 | Cytotoxicity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent. |
| AID508056 | Binding affinity to QSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1599897 | Antiproliferative activity against human MDA-MB-231 cells expressing EGFR assessed as reduction in cell growth incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID627338 | Inhibition of LCK using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID1581219 | Inhibition of human c-KIT JM domain exon 11 V560G single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256570 | Average Binding Constant for PIM2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256619 | Average Binding Constant for RPS6KA3 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1527154 | Inhibition of VEGFR2 in HUVEC assessed as inhibition of VEGF-induced tube formation at 1 uM incubated for 8 hrs by inverted microscopic method | | | |
| AID1155226 | Antitumor activity against human NCI-H460 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 40 mg/kg/day administered qd measured up to day 21 relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1764722 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 0.58%) | | | |
| AID507955 | Binding affinity to FLT3 ITD mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508104 | Binding affinity to TBK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1465750 | Inhibition of wild type KIT (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| 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. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383309 | Inhibition of Jak1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID627131 | Inhibition of Aurora A using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| 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. |
| AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1518671 | Inhibition of FLT3 D835Y mutant (unknown origin) | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID507883 | Binding affinity to CSNK1A1L | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID614643 | Inhibition of human N-terminal His-tagged phosphorylated VEGFR2 preincubated for 120 mins in presence of ATP by AlphaScreen analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| 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. |
| AID1424961 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507824 | Binding affinity to ADCK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1381304 | Aqueous solubility in pH 5.5 phosphate buffer at 120 uM after 24 hrs by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 28, Issue:14
| Synthesis and characterization of amino acid substituted sunitinib analogues for the treatment of AML. |
| AID1327320 | Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1581232 | Inhibition of human c-KIT A loop exon 17 D820Y single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID256671 | Average Binding Constant for ABL1(Y253F); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425135 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID625115 | Binding constant for PAK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID608770 | Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
| Design, synthesis and biological evaluation of novel 4-thiazolidinones containing indolin-2-one moiety as potential antitumor agent. |
| AID1436042 | Binding affinity to recombinant human CLK4 (R135 to K481 residues) expressed in bacterial expression system by KinomeScan assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands. |
| AID1581231 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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. |
| AID1814376 | Inhibition of PDGFRbeta (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
| Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| 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. |
| 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. |
| AID479511 | Inhibition of AKT1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID383327 | Inhibition of STK17b | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1224766 | Delta TM value showing the stabilisation of CK1G3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507971 | Binding affinity to HIPK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID614651 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 assessed as dissociation half life after 60 mins by ligand displacement based enzyme-inhibitor dilution assay | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1599896 | Antiproliferative activity against human A549 cells expressing EGFR assessed as reduction in cell growth incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID1587958 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID624849 | Binding constant for CSNK2A2 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. |
| AID256608 | Average Binding Constant for MARK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1406763 | Antiproliferative activity against human HuH7 cells by MTT assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Diterpenoid lead stevioside and its hydrolysis products steviol and isosteviol: Biological activity and structural modification. |
| AID625058 | Binding constant for VRK2 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. |
| 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. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1910805 | Binding affinity to RIOK2 (unknown origin) assessed as dissociation constant | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Discovery of 8-(6-Methoxypyridin-3-yl)-1-(4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)-1,5-dihydro- |
| AID507640 | Binding affinity to MYO3B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435279 | Binding constant for full-length CDK9 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1581243 | Inhibition of human c-KIT A loop exon 11/17 V560G/N822K double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507628 | Binding affinity to MLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507570 | Binding affinity to IRAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID418602 | Inhibition of c-Met | 2009 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
| N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
| AID1155237 | Binding affinity to AXL (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID479521 | Inhibition of CK1delta | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1563496 | Antitumor activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I mutant xenografted in BALB/c mouse assessed as tumor growth inhibition at 20 mg/kg/day, po administered via gavage for 28 days relative to control | | | |
| AID1581240 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID256663 | Average Binding Constant for INSR; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1896569 | Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 78 | Sunitinib-based Proteolysis Targeting Chimeras (PROTACs) reduced the protein levels of FLT-3 and c-KIT in leukemia cell lines. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID513988 | Inhibition of PDGFRbeta expressed in human A431 cells | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents. |
| AID738474 | Binding affinity to MER (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1563327 | Inhibition of c-KIT V559G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID507644 | Binding affinity to NEK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507660 | Binding affinity to PAK6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID469537 | Antitumor activity against human MV411 cells in xenografted athymic nude mouse model assessed as decrease in tumor size at 10 mg/kg, po qd for 28 days measured after 29 to 36 days | 2009 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17
| Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors. |
| AID625046 | Binding constant for PIK3CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507837 | Binding affinity to AURKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID517654 | Inhibition of KDR autophosphorylation in HUVEC by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| 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. |
| AID1217921 | Drug excretion in feces of female Sprague-Dawley rat at 15 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID507600 | Binding affinity to MAP3K4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1586461 | Inhibition of VEGF165-induced VEGFR2 phosphorylation in HMEC1 cells assessed as phosphorylated VEGFR2 level at 10 uM preincubated for 24 hrs followed by VEGF stimulation for 30 mins by Western blot assay relative to control | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| 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. |
| AID1737723 | Inhibition of wild-type human partial length CSF1R (I564 to S939 residues) expressed in bacterial expression system at 100 nM by Kinomescan method relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1563530 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in pS6 phosphorylation at S235 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID507653 | Binding affinity to p38-beta | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1581215 | Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID479516 | Inhibition of CAMK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID507933 | Binding affinity to ERBB3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563523 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in AKT phosphorylation at S473 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| 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. |
| AID508071 | Binding affinity to RPS6KA1(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508076 | Binding affinity to RPS6KA4(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256582 | Average Binding Constant for NEK9; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID507853 | Binding affinity to CAMK1D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507951 | Binding affinity to FLT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID1737712 | Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1224788 | Delta TM value showing the stabilisation of PIM3 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID674079 | Competitive inhibition of VEGFR2 by qPCR method | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. |
| 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. |
| AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1327318 | Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| 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. |
| AID1581214 | Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID256646 | Average Binding Constant for JAK1 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1611387 | Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent. |
| AID1431175 | Inhibition of PDGFR-beta in human SF539 cells assessed as reduction in PDGF-BB induced phosphorylation preincubated for 60 mins followed by PDGF-BB addition measured after 10 mins by ELISA method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| 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. |
| AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435934 | Binding constant for PLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1440386 | Inhibition of human ERG expressed in CHO cells by Qpatch assay | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1764714 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 16.28%) | | | |
| AID508112 | Binding affinity to TLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218230 | Clearance in female Sprague-Dawley rat plasma at 5 mg/kg, iv administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID256613 | Average Binding Constant for Aurora2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID256583 | Average Binding Constant for CAMKK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID738476 | Binding affinity to AXL (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581236 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624836 | Binding constant for IKK-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID753550 | Antiangiogenic activity in chicken embryo chorioallantoic membrane assessed as inhibition of VEGF-induced blood vessel formation at 25 uM applied topically to filter paper surface after 48 hrs by stereo microscopic analysis | 2013 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 23, Issue:12
| Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor. |
| 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. |
| AID1406765 | Antiproliferative activity against human SW620 cells by MTT assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Diterpenoid lead stevioside and its hydrolysis products steviol and isosteviol: Biological activity and structural modification. |
| AID1218186 | Apparent terminal half life in male Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624815 | Binding constant for ERBB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507829 | Binding affinity to ALK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1630232 | Antiproliferative activity against human A549 cells after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID599957 | Binding affinity to human KIT incubated for 1 hr by kinase binding assay | 2011 | European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. |
| AID507575 | Binding affinity to JH1 catalytic domain of JAK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1433912 | Inhibition of VEGF-A-induced cell proliferation in human EPC at 1 uM measured after 48 hrs by trypan blue exclusion assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID1386989 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| 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. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224765 | Delta TM value showing the stabilisation of CK1G2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1424489 | Antitumor activity in patient with metastatic renal cell carcinoma assessed as objective response during phase 3 trial | 2017 | European journal of medicinal chemistry, Dec-15, Volume: 142 | Recent developments in small molecule therapies for renal cell carcinoma. |
| AID626025 | Cytotoxicity against human HUVEC | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| 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. |
| AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624791 | Binding constant for KIT(V559D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764718 | Induction of apoptosis in human MV4-11 cells assessed as late apoptotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 0.58%) | | | |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID756116 | Inhibition of full length recombinant c-RAF (unknown origin) using MEK1 as substrate after 1 hr by luminescence assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
| Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. |
| 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. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1876077 | Antiviral activity against CHIK virus | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections. |
| AID1764781 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 333 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1224803 | Delta TM value showing the stabilisation of PBK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256578 | Average Binding Constant for SLK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507914 | Binding affinity to EGFR L747-T751del, Sins mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID28843 | Solubility in 20 mM buffered solution after shaking for 24 hr at 22 degree celsius at pH 2 | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1876117 | Cytotoxicity against african green monkey Vero 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. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507892 | Binding affinity to DAPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507592 | Binding affinity to LTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID331980 | Inhibition of c-Met dependent HGF-induced human A549 cell migration | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
| Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. |
| AID435194 | Binding constant for RPS6KA6(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1629519 | Inhibition of TEL-fused cKIT T670I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID435674 | Binding constant for JAK3(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID383331 | Inhibition of TTK | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID508047 | Binding affinity to PRKD1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507974 | Binding affinity to HUNK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1602298 | Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID507942 | Binding affinity to FAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624875 | Binding constant for PDGFRB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1389795 | Antiangiogenic activity in chicken fertilized egg chorioallantoic membrane at 1 to 20 uM measured after 72 hrs | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
| Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents. |
| 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. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1327316 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1387023 | Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1503979 | Selectivity index, ratio of IC50 for VEGF-induced capillary tube formation in HUVEC to IC50 for growth inhibition of HUVEC | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| New Scaffold for Angiogenesis Inhibitors Discovered by Targeted Chemical Transformations of Wondonin Natural Products. |
| 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. |
| AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563526 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T202 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID517653 | Inhibition of PDGFRbeta autophosphorylation by cell based Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| AID507611 | Binding affinity to MAST1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1155278 | Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID256590 | Average Binding Constant for EPHB1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507801 | Antitumor activity against human MV4-11 cells xenografted mouse model assessed as inhibition of tumor growth at at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID614642 | Inhibition of human N-terminal His-tagged phosphorylated VEGFR2 in presence of ATP measured without preincubation by AlphaScreen analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507084 | Inhibition of recombinant EGFR by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID508033 | Binding affinity to PIP5K2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1542974 | Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| 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. |
| AID508081 | Binding affinity to RPS6KA6(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1509566 | Displacement of tracer 222 from GST-tagged recombinant human AAK1 catalytic domain (1 to 510 amino acids) expressed in insect cells shaken for 30 secs and incubated for 1 hr by LanthaScreen Eu kinase binding assay | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. |
| AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1586374 | Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 22 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 60 +/- 1%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508060 | Binding affinity to RET(V804L) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1155232 | Binding affinity to FLT3 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID671089 | Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14
| Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents. |
| AID458666 | Selectivity index, ratio of IC50 for mouse GM-CSF-stimulated proliferation of mouse FDC-P1 cells expressing human FMS to IC50 for human FMS-mediated mouse FDC-P1 cells proliferation in presence of human CSF1 | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Colony stimulating factor-1 receptor as a target for small molecule inhibitors. |
| AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507079 | Inhibition of recombinant c-Abl by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1503978 | Growth inhibition of HUVEC after 24 hrs in presence of VEGF by MTT assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| New Scaffold for Angiogenesis Inhibitors Discovered by Targeted Chemical Transformations of Wondonin Natural Products. |
| AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID327007 | Inhibition of KDR kinase at 10 uM by ELISA | 2008 | Journal of natural products, Jan, Volume: 71, Issue:1
| Gentisyl alcohol derivatives from the marine-derived fungus Penicillium terrestre. |
| AID1781305 | Intrinsic clearance in human liver microsomes at 1 uM measured up to 60 mins in presence of NADPH by LC-MS/SM analysis | | | |
| 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. |
| AID256647 | Average Binding Constant for SYK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID747275 | Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
| Synthesis and antiproliferative evaluation of piperazine-1-carbothiohydrazide derivatives of indolin-2-one. |
| AID256627 | Average Binding Constant for RPS6KA2 (Kin.Dom. 1); NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507650 | Binding affinity to NLK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1302365 | Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID1478168 | Inhibition of human Flt1 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1542975 | Antiproliferative activity against human SKOV3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| 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. |
| AID1587982 | Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1587961 | Inhibition of human c-KIT A loop exon 17 D820E single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1158370 | Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| 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. |
| AID256660 | Average Binding Constant for KIT; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID649466 | Inhibition of VEGFR2 | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| 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. |
| AID1218250 | Drug excretion in feces of female Sprague-Dawley rat at 5 mg/kg, iv administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1155275 | Antiproliferative activity against human NCI-H3122 cells after 72 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID636124 | Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA | 2012 | Bioorganic & medicinal chemistry, Jan-15, Volume: 20, Issue:2
| N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors. |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507818 | Binding affinity to ABL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563332 | Inhibition of c-KIT T670E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1587983 | Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1563502 | Antitumor activity against human GIST5R cells harboring c-KIT 560 to 578 deletion/T670I mutant xenografted in BALB/c mouse assessed as tumor weight at 20 mg/kg/day, po administered via gavage for 28 days (Rvb = 2.62 g) | | | |
| AID1224795 | Delta TM value showing the stabilisation of SLK produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1895639 | Inhibition of RET (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383320 | Inhibition of RPSKA2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1630244 | Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 0.1 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 16.91 %) | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625026 | Binding constant for MAP3K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421402 | Inhibition of recombinant human N-terminal His6-tagged KDR (790 to end residues) expressed in baculovirus infected Sf21 insect cells after 60 mins by ELISA | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID1602317 | Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system preincubated for 5 to 30 mins followed by myelobasic protein addition and measured after 120 mins in presence of 1 mM ATP by AD | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID508067 | Binding affinity to RIPK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218113 | Terminal half life in human plasma at 50 mg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507633 | Binding affinity to MST2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218184 | Tmax in male Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID1563527 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in ERK phosphorylation at T204 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1764648 | Inhibition of CSF1R (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID507950 | Binding affinity to FGR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID614644 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 after 10 mins by Global fit analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764682 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 12 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID1894638 | Inhibition of PAK4 (unknown origin) | 2021 | European journal of medicinal chemistry, Apr-15, Volume: 216 | Structural insights of oxindole based kinase inhibitors as anticancer agents: Recent advances. |
| AID1509569 | Antiviral activity against Dengue virus 2 New Guinea C infected in human HuH7 cells assessed as reduction in viral infection measured at 48 hrs post infection by renilla-luciferase substrate based assay | 2019 | Journal of medicinal chemistry, 06-27, Volume: 62, Issue:12
| Synthesis and Structure-Activity Relationships of 3,5-Disubstituted-pyrrolo[2,3- b]pyridines as Inhibitors of Adaptor-Associated Kinase 1 with Antiviral Activity. |
| AID1764650 | Inhibition of PDGFRbeta (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| 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. |
| AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID256655 | Average Binding Constant for CSNK1G1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID256591 | Average Binding Constant for EPHA5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID507667 | Binding affinity to PDPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508102 | Binding affinity to TAOK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256594 | Average Binding Constant for BMX; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID1327314 | Cytotoxicity against human 4TI cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1236879 | Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1478174 | Inhibition of human HCK at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID1440346 | Inhibition of human FLT3 D835Y mutant | 2017 | European journal of medicinal chemistry, Feb-15, Volume: 127 | Design, synthesis and biological evaluation of indolin-2-one-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase3 (FLT3). |
| AID1302356 | Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| 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. |
| AID1177368 | Binding affinity to VEGFR2 (unknown origin) assessed as residence time | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1
| Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization. |
| AID1155210 | Toxicity in BALB/c nude mouse xenografted with human HT-29 cells assessed as severe weight loss at 80 mg/kg/day administered qd measured after 12 to 15 days | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID256651 | Average Binding Constant for DAPK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID438538 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 30 mg/kg, po QD for 28 days measured after first 14 days of dosing period | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID674081 | Antiproliferative activity against human HT-29 cells expressing VEGFR after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. |
| AID1224804 | Delta TM value showing the stabilisation of VRK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1302359 | Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID517658 | Cytotoxicity against human MV4-11 cells by MTT assay | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| 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. |
| AID438002 | Inhibition of GST-tagged VEGFR expressed in Sf9 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
| AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1218135 | Retention time of compound by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581220 | Inhibition of human c-KIT ATP binding domain exon 13 V654A single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435902 | Binding constant for BRAF(V600E) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425104 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID626024 | Antiangiogenic activity in HUVEC assessed as decrease in VEGF-induced cell migration at 1 uM after 24 hrs by transwell migration assay | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1176838 | Inhibition of PDGFRalpha (unknown origin) at 1 uM by ELISA method | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of potent 1H-imidazo[4,5-b]pyridine-based c-Met kinase inhibitors via mechanism-directed structural optimization. |
| 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. |
| AID507598 | Binding affinity to MAP3K2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID729981 | Inhibition of FLT1 (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| 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. |
| AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1433905 | Inhibition of PDGFRbeta (unknown origin) phosphorylation | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| 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. |
| AID479515 | Inhibition of BTK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID638918 | Inhibition of c-Src at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| 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. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1236876 | Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1158372 | Cytotoxicity against human A431 cells by SRB assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID508022 | Binding affinity to PIK3CA H1047Y mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID383326 | Inhibition of STK17a | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| 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. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID384855 | Cytotoxicity against human IPTP/98 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1424900 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508124 | Binding affinity to TYK2(JH2domain-pseudokinase) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507847 | Binding affinity to BRAF V600E mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508054 | Binding affinity to PRP4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764644 | Inhibition of FLT3 (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424994 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID627129 | Inhibition of CHK1 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| 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. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID479528 | Inhibition of FLT3 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID508084 | Binding affinity to SgK110 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID383104 | Inhibition of Aurora C | 2007 | Proceedings of the National Academy of Sciences of the United States of 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. |
| 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. |
| AID665084 | Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| 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. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1207354 | Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | | | |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1218183 | Cmax in male Sprague-Dawley rat plasma at 15 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID507931 | Binding affinity to EPHB6 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1185747 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1581237 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID256596 | Average Binding Constant for CLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435648 | Binding constant for CAMKK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508063 | Binding affinity to RIOK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256595 | Average Binding Constant for CLK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID383307 | Inhibition of FLT4 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1302366 | Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID1224805 | Delta TM value showing the stabilisation of VRK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1431240 | Antiangiogenic activity in Leghorn chicken egg chorioallantoic membrane assessed as inhibition of human VEGF-165/bFGF-induced blood vessels formation measured after 40 hrs by microscopic method | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
| Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents. |
| AID507941 | Binding affinity to ERN1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID446374 | Inhibition of human recombinant N-terminally 6X-His-tagged SIRT2 after 4 hrs in presence of NAD+ by fluorescent deacetylase assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins). |
| 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. |
| AID507865 | Binding affinity to CDK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID256568 | Average Binding Constant for STK17A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1550002 | Antiproliferative activity against HMEC1 cells incubated for 2 days by MTT assay | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| 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. |
| 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. |
| AID256597 | Average Binding Constant for CLK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1217860 | Drug excretion in urine of female cynomolgus monkey at 6 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1563333 | Inhibition of c-KIT T670I/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507851 | Binding affinity to BTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1425081 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1290592 | Cytotoxicity against human MDA-MB-435 cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry. |
| 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. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507564 | Binding affinity to IKK-alpha | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1709291 | Inhibition of PDGFRbeta in human SH-SY5Y cells preincubated for 60 mins followed by PDGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1586361 | Antiproliferative activity against human A549 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID256604 | Average Binding Constant for STK10; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1489048 | Cytotoxicity against human K562 cells after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives. |
| AID1327332 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at G2/M phase at 4 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 26 %) | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1290593 | Cytotoxicity against human HT-29 cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry. |
| AID1764708 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at sub-G1 phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 4.24%) | | | |
| 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. |
| 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. |
| 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. |
| AID479523 | Inhibition of C-TAK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID256626 | Average Binding Constant for NTRK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID256610 | Average Binding Constant for Aurora3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435325 | Binding constant for RPS6KA4(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1600269 | Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID1875913 | Binding affinity to AAK1 in HEK-293 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. |
| AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563513 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R cells assessed as reduction in c-KIT autophosphorylation at Y703 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1387022 | Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID536879 | Inhibition of c-Kit after 30 mins by ELISA | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID1224770 | Delta TM value showing the stabilisation of JAK1~B produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID507897 | Binding affinity to DCAMKL3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID649407 | Inhibition of human recombinant c-Kit by radiometric assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1155242 | Binding affinity to ARG (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID256566 | Average Binding Constant for TNIK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1335671 | Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| AID256564 | Average Binding Constant for MAP3K4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID507828 | Binding affinity to AKT3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1465753 | Inhibition of KIT D816H mutant (unknown origin) using biotinylated poly-Glu-Tyr as substrate preincubated for 30 mins followed by substrate addition in presence of ATP by TR-FRET assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID508069 | Binding affinity to ROCK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764696 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 10.46%) | | | |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1586423 | Induction of apoptosis in human A549 cells at 100 uM after 20 to 24 hrs by Annexin V-FITC/propidium iodide staining based flow cytometry (Rvb = 16%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID1489046 | Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1421406 | Inhibition of recombinant human RET at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507849 | Binding affinity to BRSK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1503977 | Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation after 8 hrs by matrigel based inverted microscopic analysis | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| New Scaffold for Angiogenesis Inhibitors Discovered by Targeted Chemical Transformations of Wondonin Natural Products. |
| 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. |
| AID508068 | Binding affinity to ROCK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID614657 | Inhibition of VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells at 100 nM after 1 hr by ELISA | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| 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. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID738227 | Binding affinity to MET (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| 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. |
| AID507834 | Binding affinity to ASK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1424951 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1224764 | Delta TM value showing the stabilisation of CK1G1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1587941 | Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3 | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507881 | Binding affinity to CSF1R | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435690 | Binding constant for RPS6KA1(Kin.Dom.1 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1218129 | AUC (0 to infinity) in male cynomolgus monkey plasma at 6 mg/kg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1764643 | Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell Counting Kit-8 assay | | | |
| AID1764733 | Induction of apoptosis in human MOLM-13 cells assessed as early apoptotic cells at 10 nM incubated for 24 hrs by flow cytometry (Rvb = 2.18%) | | | |
| AID729741 | Cytotoxicity against human ACHN cells assessed as inhibition of cell viability after 6 days by MTT assay | 2013 | Journal of natural products, Feb-22, Volume: 76, Issue:2
| Bioactive sesterterpenoids from a Korean sponge Monanchora sp. |
| AID657324 | Cytotoxicity against human A375 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1387031 | Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1737708 | Inhibition of AMPK in human K562 cells assessed as p-ACC (Ser79) level in glucose free medium and in presence of 2-Deoxy-D-glucose measured after 3 hrs by ELISA | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1236875 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| 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. |
| 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. |
| AID1224782 | Delta TM value showing the stabilisation of PAK5 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| AID1302351 | Antiproliferative activity against mouse BAF3 cells | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507958 | Binding affinity to FLT4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1587981 | Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID507815 | Binding affinity to ABL1 Q252H mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID684383 | Inhibition of N-terminal GST-tagged KDR after 4 hrs by luciferase-luciferin coupled chemiluminescence assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
| The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. |
| AID508140 | Tmax in nu/nu mouse at 10 mg/kg, po | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1155241 | Binding affinity to ABL (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID507967 | Binding affinity to GSK3B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508051 | Binding affinity to PRKG2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764691 | Antiproliferative activity against human quizartinib-resistant MOLM-13 cells at 1 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507614 | Binding affinity to MEK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383399 | Cytotoxicity against human A172 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID507835 | Binding affinity to ASK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1896570 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay | 2022 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 78 | Sunitinib-based Proteolysis Targeting Chimeras (PROTACs) reduced the protein levels of FLT-3 and c-KIT in leukemia cell lines. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383303 | Inhibition of EphA7 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1436039 | Binding affinity to full length recombinant human CLK1 (M1 to I484 residues) expressed in bacterial expression system by KinomeScan assay | 2017 | European journal of medicinal chemistry, Jan-27, Volume: 126 | Novel CLK1 inhibitors based on N-aryloxazol-2-amine skeleton - A possible way to dual VEGFR2 TK/CLK ligands. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256644 | Average Binding Constant for CSNK1E; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1387057 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and V654 mutant (unknown origin) allografted in CB17 SCID mouse assessed as tumor regression at 80 mg/kg, po qd measured on last day of dosing | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1399368 | Antiangiogenic activity in Leghorn chicken embryo chorioallantoic membrane after 40 hrs by microscopic analysis | 2018 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
| Design, synthesis and preclinical evaluation of 5-methyl-N |
| AID383301 | Inhibition of DAPK2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1177367 | Binding affinity to VEGFR2 (unknown origin) by proteros reporter displacement assay | 2015 | ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1
| Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization. |
| AID507884 | Binding affinity to CSNK1D | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID157325 | Inhibition of PDGF-induced BrdU incorporation in 3T3 cells with 0.1% bovine serum albumin | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID508026 | Binding affinity to PIK3CD | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1503816 | Antiproliferative activity against human A498 cells after 48 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors. |
| AID255141 | Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr | 2005 | Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
| Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. |
| AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507817 | Binding affinity to ABL1 Y253F mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID738479 | Binding affinity to non phosphorylated ABL1 (unknown origin) at 75 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| 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. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508117 | Binding affinity to TRKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1518670 | Inhibition of FLT3 ITD mutant (unknown origin) phosphorylation measured after 2 hrs by Western blot analysis | 2019 | European journal of medicinal chemistry, Dec-15, Volume: 184 | Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. |
| 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. |
| AID508057 | Binding affinity to RAF1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764730 | Induction of apoptosis in human MOLM-13 cells assessed as late apoptotic cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 4.54%) | | | |
| AID256622 | Average Binding Constant for JNK1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507873 | Binding affinity to CDKL5 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507930 | Binding affinity to EPHB4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1433913 | Inhibition of VEGF-A-induced cell proliferation in human EPC at 1 uM measured after 72 hrs by trypan blue exclusion assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID479728 | Inhibition of MAPKAPK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507906 | Binding affinity to DYRK1B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1587968 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1335669 | Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| AID1878085 | Inhibition of FLT3 autophosphorylation in human RS4-11 cells measured after 2 hrs by Western blot analysis | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia. |
| AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508138 | Binding affinity to ZAP70 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563335 | Inhibition of c-KIT D816E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1563410 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as reduction in STAT3 phosphorylation at Y705 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID438507 | Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1563514 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R cells assessed as reduction in c-KIT autophosphorylation at Y719 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID507608 | Binding affinity to MARK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563479 | Antitumor activity against mouse BAF3(transformed) cells harboring c-KIT T670I mutant implanted in BALB/c nu mouse assessed as tumor growth inhibition at 40 mg/kg/day, po administered via gavage for 11 days relative to control | | | |
| 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. |
| AID435691 | Binding constant for SgK085 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1424943 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1705894 | Cytotoxicity against human RPTEC/TERT1 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity. |
| AID1764642 | Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Cell Counting Kit-8 assay | | | |
| 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. |
| AID507856 | Binding affinity to CAMK2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507597 | Binding affinity to MAP3K15 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507803 | Binding affinity to FLT3 catalytic domain by KinomeScan kinase binding assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508094 | Binding affinity to STK16 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1386988 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1335667 | Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| AID1224800 | Delta TM value showing the stabilisation of MST4 (2) produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID614658 | Inhibition of VEGF-induced autophosphorylation of tyrosine 1175 residue on VEGFR2 expressed in HEK293 cells at 100 nM measured 96 hrs post inhibitor washout by ELISA | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID674080 | Antiproliferative activity against human HAEC cells expressing VEGFR after 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. |
| AID1581217 | Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1185746 | Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. |
| AID1764737 | Induction of apoptosis in human MOLM-13 cells assessed as early apoptotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 2.18%) | | | |
| AID624930 | Binding constant for TNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1764702 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at S phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 16.31%) | | | |
| 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. |
| AID1301834 | Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID1387034 | Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1602339 | Binding affinity to human FLT3 D835H mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| 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. |
| AID738215 | Growth inhibition of human MCF7 cells at 10 uM after 72 hrs by MTT assay relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID256639 | Average Binding Constant for PHkg1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1602342 | Binding affinity to human FLT3 ITD/F691L double mutant expressed in baculovirus expression system | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| 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. |
| AID438001 | Inhibition of GST-tagged c-Met expressed in Sf9 cells | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors. |
| AID1764715 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at G2/M phase at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 8.25%) | | | |
| 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. |
| 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. |
| AID1744430 | Inhibition of bovine GRK2 using porcine brain tubulin as substrate incubated for 3 to 5 mins by [gamma32P]ATP based radiometric assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors. |
| AID256659 | Average Binding Constant for DAPK3; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1387026 | Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625066 | Binding constant for IRAK3 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. |
| AID256580 | Average Binding Constant for CAMKK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507659 | Binding affinity to PAK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1310409 | Cytotoxicity against human BT549 cells after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Aug-08, Volume: 118 | Design, synthesis and apoptosis inducing effect of novel (Z)-3-(3'-methoxy-4'-(2-amino-2-oxoethoxy)-benzylidene)indolin-2-ones as potential antitumour agents. |
| 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. |
| AID1599891 | Inhibition of VEGFR2 (unknown origin) using Poly (Glu, Tyr) 4:1 as substrate at 1 uM preincubated with substrate followed by enzyme challenge for 1 hr by ELISA relative to control | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase. |
| AID738475 | Binding affinity to MER (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID383304 | Inhibition of EphB1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1586376 | Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 22 uM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 10 +/- 0.8%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| 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. |
| AID350247 | Selectivity ratio of IC50 for human P-gp-negative KB-3-1 cells to human P-glycoprotein-expressing KBV1 cells | 2009 | Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
| Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells. |
| AID624717 | Binding constant for JNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID674077 | Inhibition of VEGF receptor | 2012 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
| Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis-radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib. |
| AID1236874 | Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability at 30 uM after 48 hrs by SRB assay | 2015 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 25, Issue:14
| Synthesis and antitumor activity of 5-(5-halogenated-2-oxo-1H-pyrrolo[2,3-b]pyridin-(3Z)-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| 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. |
| AID256559 | Average Binding Constant for EPHB4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507629 | Binding affinity to MRCKA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1370588 | Stability in mouse liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors. |
| AID507081 | Inhibition of recombinant c-Src by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1302373 | Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID1563518 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in pS6 phosphorylation at S235 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID507893 | Binding affinity to DAPK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1563324 | Inhibition of c-KIT T670I mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID383319 | Inhibition of PTK2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID508036 | Binding affinity to PKMYT1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID517657 | Inhibition of FLT3-ITD autophosphorylation in human MV4-11 cells by Western blot analysis | 2010 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 20, Issue:20
| Novel azulene-based derivatives as potent multi-receptor tyrosine kinase inhibitors. |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID627293 | Inhibition of c-Src using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425068 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID508137 | Binding affinity to ZAK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID693404 | Cytotoxicity against VEGFR expressing HAEC after 72 hrs by MTT assay | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Synthesis, in silico, in vitro, and in vivo investigation of 5-[¹¹C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2. |
| 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. |
| AID508079 | Binding affinity to RPS6KA5(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1737705 | Inhibition of recombinant human His6-tagged AMPK alpha2 using ULight CRBtide as substrate incubated for 1 hr followed by substrate addition and measured after 1 hr by TR-FRET assay | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID626038 | Inhibition of eNOS phosphorylation at Ser-1172 in VEGF-stimulated HUVEC at 1 uM preincubated for 1 hr before VEGF induction measured after 1 hr by Western blot analysis | 2011 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 21, Issue:21
| BRN-103, a novel nicotinamide derivative, inhibits VEGF-induced angiogenesis and proliferation in human umbilical vein endothelial cells. |
| 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. |
| AID1425088 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1327333 | Cell cycle arrest in human MDA-MB-231 cells assessed as accumulation at S phase at 4 uM after 24 hrs by propidium iodide staining based FACS analysis (Rvb = 24.6 %) | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1488408 | Antitumor activity against human Caki1 cells xenografted model assessed as tumor growth inhibition at 80 mg/kg, po qd relative to control | 2017 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 27, Issue:16
| Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy. |
| AID383880 | Cytotoxicity against human G-292 Clone A141B1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1764646 | Inhibition of FLT3 D835Y mutant (unknown origin) incubated for 30 mins in presence of ATP by mobility shift assay | | | |
| 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. |
| AID625121 | Binding constant for RET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563330 | Inhibition of c-KIT V654A/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID383313 | Inhibition of Nek2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1327315 | Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1563487 | Antitumor activity against mouse BAF3(transformed) cells harboring c-KIT D820G mutant implanted in BALB/c nu mouse assessed as tumor weight at 40 mg/kg/day, po administered via gavage for 9 days (Rvb = 1.67 g) | | | |
| AID1586454 | Inhibition of VEGFR2 internalization in human A549 cells at 22 uM after 24 hrs by immunofluorescence assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID1370589 | Stability in rat liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors. |
| 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. |
| AID1386987 | Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID1424985 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1231617 | Antiangiogenic activity in HUVEC assessed as inhibition of tubular structure formation at 0.033 to 0.33 uM after 8 hrs by microscopic analysis | 2015 | Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
| Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents. |
| AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507973 | Binding affinity to HPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508091 | Binding affinity to SRPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID614640 | Inhibition of human N-terminal His-tagged non-phosphorylated VEGFR2 in presence of ATP measured without preincubation by AlphaScreen analysis | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508101 | Binding affinity to TAO1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256676 | Average Binding Constant for SRC; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1561120 | Binding affinity to BRD7 (unknown origin) assessed as dissociation constant by qPCR analysis | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
| Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains. |
| AID536882 | Inhibition of VEGFR2-induced cell proliferation in HUVEC after 72 hrs by sulforhodamine B method | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID1630233 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay | 2016 | Bioorganic & medicinal chemistry letters, 10-01, Volume: 26, Issue:19
| Synthesis and antitumor activity evaluation of quinazoline derivatives bearing piperazine-1-carbodithioate moiety at C4-position. |
| AID1875911 | Antiviral activity against HCV infected in human Huh7.5 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. |
| AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1158373 | Antiangiogenic activity in fertile leghorn chicken egg Chorioallantoic membrane assessed as inhibition of human VEGF-165/bFGF-induced angiogenesis after 48 hrs by CAM assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID1709290 | Inhibition of VEGFR2 in human U251 cells preincubated for 60 mins followed by VEGF stimulation and measured after 10 mins by ELISA | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer. |
| AID1478065 | Inhibition of human DDR at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID1764693 | Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 64.73%) | | | |
| AID1486141 | Antiangiogenic activity in matrigel injected Swiss albino mouse assessed as reduction in hemoglobin content in matrigel plug at 2.5 mg/kg, ip every other day for 20 days by matrigel assay | | | |
| AID384133 | Cytotoxicity against human SNU5 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435444 | Binding constant for TYK2(Kin.Dom.2/JH1 - catalytic) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1478164 | Inhibition of human EPHA4 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID463635 | Inhibition of CSF1R | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| 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. |
| AID536880 | Inhibition of human VEGFR2 after 30 mins by ELISA | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID1478167 | Inhibition of human EPHA8 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID638911 | Inhibition of KDR at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID1424930 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID614647 | Ratio of IC50 for human N-terminal His-tagged phosphorylated VEGFR2 to IC50 for human N-terminal His-tagged non-phosphorylated VEGFR2 | 2011 | Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
| Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1460372 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
| Design, synthesis and biological activities of tetrandrine and fangchinoline derivatives as antitumer agents. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507965 | Binding affinity to GRK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507888 | Binding affinity to CSNK1G3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID507885 | Binding affinity to CSNK1E | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256641 | Average Binding Constant for ABL2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID1581235 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1764739 | Induction of apoptosis in human MOLM-13 cells assessed as necrotic cells at 100 nM incubated for 24 hrs by flow cytometry (Rvb = 0.45%) | | | |
| AID1217925 | Drug excretion in feces of male Sprague-Dawley rat at 15 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID1563328 | Inhibition of c-KIT V560D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID507643 | Binding affinity to NEK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID1586363 | Antiproliferative activity against HMEC1 cells by MTT assay | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID256628 | Average Binding Constant for LYN; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1155235 | Binding affinity to VEGFR1 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383310 | Inhibition of Lyn | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508070 | Binding affinity to ROS1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID756067 | Inhibition of human N-terminal GST-tagged LRRK2 after 1 hr by TR-FRET assay | 2013 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
| The development of CNS-active LRRK2 inhibitors using property-directed optimisation. |
| AID507647 | Binding affinity to NEK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587986 | Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1814375 | Inhibition of PDGFRalpha (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
| Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1290590 | Cytotoxicity against human A549 cells by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
| Identification of inhibitors for vascular endothelial growth factor receptor by using dynamic combinatorial chemistry. |
| AID1425124 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1563529 | Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GIST5R assessed as reduction in AKT phosphorylation at S473 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID665078 | Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| 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. |
| 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. |
| 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. |
| AID508064 | Binding affinity to RIOK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256654 | Average Binding Constant for FGFR2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507838 | Binding affinity to AURKC | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507421 | Inhibition of recombinant CK1 by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1587977 | Inhibition of human c-KIT A loop exon 11/17 V560G/D816V double mutant at 10 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| 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. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1629521 | Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID507636 | Binding affinity to MUSK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508125 | Binding affinity to TYRO3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID256599 | Average Binding Constant for TTK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID665086 | Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| 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. |
| AID256635 | Average Binding Constant for CAMK2D; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507877 | Binding affinity to CLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1302358 | Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID1155227 | Toxicity in BALB/c nude mouse xenografted with human HT-29 cells assessed as change in body weight at 80 mg/kg/day administered qd relative to control | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID491726 | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID507953 | Binding affinity to FLT3 D835H mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID256623 | Average Binding Constant for MYLK2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507872 | Binding affinity to CDKL3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435198 | Binding constant for TIE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID508048 | Binding affinity to PRKD2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507626 | Binding affinity to MLK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| 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. |
| AID1307963 | Inhibition of AChE (unknown origin) | 2016 | Journal of medicinal chemistry, 05-12, Volume: 59, Issue:9
| Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design. |
| AID507944 | Binding affinity to FES | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID508130 | Binding affinity to WEE1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507922 | Binding affinity to EPHA4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507077 | Inhibition of DNA-PK by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID1155231 | Binding affinity to VEGFR3 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| 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. |
| AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1301835 | Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID625072 | Binding constant for TBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID286534 | Inhibition of tumor growth in human 1080 cells xenografted in orally dosed SCID mouse | 2007 | Journal of medicinal chemistry, May-03, Volume: 50, Issue:9
| 1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel. |
| AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID491755 | Inhibition of FLT3 at 0.1 uM | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| AID1389794 | Inhibition of VEGFR2 phosphorylation in HUVEC at 1 uM after 24 hrs by Western blot analysis | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
| Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents. |
| AID1302360 | Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID649610 | Antitumor activity against mouse BA/F3 cells expressing FLT3-ITD mutant xenografted in BALB/c mouse myeloproliferative model assessed as increase in host survival days at 20 mg/kg, po qd relative to control (Rvb = 20 days) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| 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 |
| AID657321 | Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
| Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents. |
| AID508073 | Binding affinity to RPS6KA2(Kin.Dom.1-N-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID459253 | Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| AID507901 | Binding affinity to DMPK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4
| DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
| AID1224750 | Delta TM value showing the stabilisation of CAMK1G produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| 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. |
| AID507566 | Binding affinity to IKK-epsilon | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1502325 | Inhibition of VEGFR2 phosphorylation in human MCF7 cells at 4 uM incubated for 24 hrs by Western blot method | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507075 | Inhibition of recombinant PI3Kgamma by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| 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. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624940 | Binding constant for FLT3(R834Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224778 | Delta TM value showing the stabilisation of NEK2 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1395585 | Effect on c-MYC gene expression in human HT-29 cells assessed as c-MYC level at 25 uM after 48 hrs by RT-qPCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| 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. |
| AID1484887 | Inhibition of VEGFR-1 (unknown origin) using poly (Glu, Tyr) 4:1 as substrate at 1 uM after 1 hr by ELISA relative to control | 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. |
| 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. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507972 | Binding affinity to HIPK4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507806 | Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID383317 | Inhibition of PHKG2 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID383324 | Inhibition of STK10 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1304254 | Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Synthesis and biological evaluation of oxindole linked indolyl-pyrimidine derivatives as potential cytotoxic agents. |
| 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. |
| AID1629518 | Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID507625 | Binding affinity to MLCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1395586 | Effect on hTERT gene expression in human HT-29 cells assessed as hTERT level at 25 uM after 48 hrs by RT-qPCR analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID729979 | Inhibition of PDGFRbeta (unknown origin) at 100 uM after 60 mins by ELISA relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Design, synthesis and biological evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID161264 | Inhibition of Platelet-derived growth factor induced 3T3 cell proliferation | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1185745 | Inhibition of VEGFR2 (unknown origin) using ATP/substrate peptide after 1 hr by colorimetric ELISA | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Discovery of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinolin-4-amine derivatives as novel VEGFR-2 kinase inhibitors. |
| AID383322 | Inhibition of RPSKA5 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1387024 | Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| 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. |
| AID507819 | Binding affinity to ACVR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID384625 | Cytotoxicity against human MG63 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID507928 | Binding affinity to EPHB2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID507423 | Inhibition of recombinant INSR by radioactive phosphotransfer assay in presence of 10 uM ATP | 2008 | Nature chemical biology, Nov, Volume: 4, Issue:11
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. |
| AID507946 | Binding affinity to FGFR2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507960 | Binding affinity to FYN | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1631797 | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Design and synthesis of 4'-O-alkylamino-tethered-benzylideneindolin-2-ones as potent cytotoxic and apoptosis inducing agents. |
| 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. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507968 | Binding affinity to HCK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1218229 | Apparent terminal half life in female Sprague-Dawley rat plasma at 5 mg/kg, iv administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID508024 | Binding affinity to PIK3CA Q546K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1503817 | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors. |
| 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. |
| 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. |
| AID507822 | Binding affinity to ACVR2B | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508121 | Binding affinity to TTK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID638923 | Inhibition of IGF1R at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID507609 | Binding affinity to MARK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1581234 | Inhibition of human c-KIT A loop exon 17 Y823D single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| 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 |
| AID507889 | Binding affinity to CSNK2A1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1602304 | Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID508090 | Binding affinity to SRMS | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1465757 | Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| 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. |
| AID507814 | Binding affinity to ABL1 M351T mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1764706 | Induction of cell cycle arrest in human MOLM-13 cells assessed as accumulation at S phase at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 16.28%) | | | |
| 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. |
| AID1581312 | Antitumor activity against human GIST430 cells xenografted in NOD/SCID mouse assessed as decrease in tumor regrowth at 80 mg/kg, po qd administered on day 1,2,5 to 9 and 12 to 16 measured after 30 days by digital caliper method | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1814380 | Inhibition of RET (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
| Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| 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. |
| AID28844 | Solubility in 20 mM buffered solution after shaking for 24 hr at 22 degree celsius at pH 6 | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| 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. |
| AID1530769 | Antiproliferative activity against HUVEC after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
| AID256650 | Average Binding Constant for PIM1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| AID1530768 | Inhibition of recombinant human His-tagged VEGFR2 cytoplasmic domain (789 to 1356 residues) expressed in baculovirus expression system measured after 1 hr by HTRF assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224772 | Delta TM value showing the stabilisation of MAP2K6 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| 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. |
| 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. |
| AID507591 | Binding affinity to LOK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID479739 | Inhibition of PKCzeta | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID1154768 | Toxicity in athymic NCr mouse xenografted with human U251 cells at 30 mg/kg twice weekly measured up to 34 days | 2014 | ACS medicinal chemistry letters, May-08, Volume: 5, Issue:5
| Discovery of antitubulin agents with antiangiogenic activity as single entities with multitarget chemotherapy potential. |
| AID1530772 | Antiproliferative activity against human Ishikawa cells after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. |
| AID1814377 | Inhibition of c-Kit (unknown origin) at 100 uM incubated for 60 mins by ELISA relative to control | 2021 | Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11
| Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia. |
| 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. |
| AID1267229 | Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Structure-activity relationship study of anticancer thymidine-quinoxaline conjugates under the low radiance of long wavelength ultraviolet light for photodynamic therapy. |
| 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. |
| 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 |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1550007 | Effect on VEGFR2 in human A549 cells assessed as total VEGFR2 level at 100 uM incubated for 24 hrs by flow cytometric analysis relative to control | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID479731 | Inhibition of MSK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID627291 | Inhibition of ALK using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID256629 | Average Binding Constant for HCK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID1327312 | Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Oct-21, Volume: 122 | New (E)-1-alkyl-1H-benzo[d]imidazol-2-yl)methylene)indolin-2-ones: Synthesis, in vitro cytotoxicity evaluation and apoptosis inducing studies. |
| AID1155250 | Binding affinity to LCK (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1676129 | Anti-angiogenesis activity in HUVEC assessed as inhibition of VEGF-induced tube formation incubated for 6 hrs by capillary tube formation assay | 2020 | Journal of natural products, 09-25, Volume: 83, Issue:9
| Formicolides A and B, Antioxidative and Antiangiogenic 20-Membered Macrolides from a Wood Ant Gut Bacterium. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624953 | Binding constant for EPHA7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID507975 | Binding affinity to ICK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID508118 | Binding affinity to TRKB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1478170 | Inhibition of human Flt4 at 0.5 uM relative to control | 2018 | Journal of medicinal chemistry, 01-11, Volume: 61, Issue:1
| Discovery of Novel Potent VEGFR-2 Inhibitors Exerting Significant Antiproliferative Activity against Cancer Cell Lines. |
| AID624866 | Binding constant for MLK3 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. |
| AID627292 | Inhibition of c-Met using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| 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. |
| AID508131 | Binding affinity to WEE2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID436052 | Binding constant for full-length SNF1LK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID438537 | Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 30 mg/kg, po QD for 28 days measured during first 14 days of dosing | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23
| Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. |
| AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID256612 | Average Binding Constant for GAK; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID507917 | Binding affinity to EGFR L861Q mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID738225 | Binding affinity to TYRO3 (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| AID1218111 | Tmax in human plasma at 50 mg, po administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID383300 | Inhibition of CLK4 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID256656 | Average Binding Constant for p38-alpha; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| 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. |
| 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. |
| 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. |
| AID507582 | Binding affinity to KIT V559D mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1271026 | Inhibition of VGFR-2 (unknown origin) | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | 1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation. |
| 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. |
| AID507581 | Binding affinity to KIT L576P mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| 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. |
| AID1335672 | Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Synthesis and apoptosis inducing studies of triazole linked 3-benzylidene isatin derivatives. |
| AID507648 | Binding affinity to NEK9 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508031 | Binding affinity to PIM3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384853 | Cytotoxicity against human IMR90 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1489047 | Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
| Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives. |
| 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. |
| 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. |
| AID507676 | Binding affinity to PIK3CA E542K mutant | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1155238 | Binding affinity to FGFR3 (unknown origin) | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents. |
| AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624985 | Binding constant for ABL1(M351T)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID508074 | Binding affinity to RPS6KA2(Kin.Dom.2-C-terminal) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256662 | Average Binding Constant for ERBB2; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1465754 | Cytotoxicity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| 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. |
| 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. |
| AID1409085 | Inhibition of human c-KIT at 100 uM | 2018 | Bioorganic & medicinal chemistry, 11-01, Volume: 26, Issue:20
| Discovery and anti-inflammatory evaluation of benzothiazepinones (BTZs) as novel non-ATP competitive inhibitors of glycogen synthase kinase-3β (GSK-3β). |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID508097 | Binding affinity to STK36 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID734223 | Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA | 2013 | Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7
| Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents. |
| AID1370587 | Stability in human liver microsomes | 2018 | Bioorganic & medicinal chemistry letters, 02-01, Volume: 28, Issue:3
| Discovery of 2-arylquinazoline derivatives as a new class of ASK1 inhibitors. |
| AID507871 | Binding affinity to CDKL2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID773010 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| 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. |
| AID513990 | Antiangiogenic activity in fertilized chicken egg by CAM assay | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID671892 | In-vivo inhibition of angiogenesis in human U87MG cells xenografted in athymic nude Harlan mouse at 10 mg/kg oral gavage dosed twice daily for 3 days measured 3 days post dose by fluorescence microscopy | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
| Modern phenotypic drug discovery is a viable, neoclassic pharma strategy. |
| 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. |
| 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. |
| AID507666 | Binding affinity to PDGFRB | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507569 | Binding affinity to IRAK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435531 | Binding constant for MKNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1602303 | Irreversible inhibition of recombinant human FLT3 ITD mutant (571 to 993 residues) expressed in baculovirus expression system at 0.1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition measured after 120 mins in presence of ATP by ADP | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID479729 | Inhibition of MARK1 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID435779 | Binding constant for ALK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625073 | Binding constant for SGK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435787 | Binding constant for CLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID627128 | Inhibition of CHK2 using biotinylated substrate preincubated for 15 mins before substrate addition measured after 30 mins by fluorescence microplate analysis | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
| Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. |
| AID599569 | Antitumor activity against human K562 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID508040 | Binding affinity to PLK2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1503818 | Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay | 2017 | ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
| Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors. |
| AID1629516 | Inhibition of TEL-fused cKIT L567P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID1207327 | Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform | | | |
| AID1425082 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1433918 | Inhibition of VEGF-A-induced VEGFR2 phosphorylation in human EPC at 1 uM pretreated for 1 hr followed by VEGF-induction measured after 5 mins by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the α |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1481734 | Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay | 2017 | Bioorganic & medicinal chemistry letters, 05-01, Volume: 27, Issue:9
| Synthesis and anti-cancer activities of new sulfonamides 4-substituted-triazolyl nucleosides. |
| AID738477 | Binding affinity to AXL (unknown origin) at 1 uM after 1 hr relative to control | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation. |
| 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. |
| AID599567 | Antitumor activity against human HL60 cells | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5-halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamides. |
| AID1764679 | Antiproliferative activity against human sunitinib-resistant MOLM-13 cells at 1000 nM incubated for 72 hrs by CCK8 assay relative to control | | | |
| 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. |
| AID508123 | Binding affinity to TYK2(JH1domain-catalytic) | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12
| Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
| 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. |
| AID624735 | Binding constant for ANKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563509 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in c-KIT autophosphorylation at Y823 residue at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID1561121 | Binding affinity to BRD9 (unknown origin) assessed as dissociation constant by qPCR analysis | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
| Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains. |
| AID507905 | Binding affinity to DYRK1A | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID629512 | Cytotoxicity against human PC3 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID1764716 | Induction of apoptosis in human MV4-11 cells assessed as viable cells at 1 nM incubated for 24 hrs by flow cytometry (Rvb = 98.26%) | | | |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1224749 | Delta TM value showing the stabilisation of CAMK1D produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID479737 | Inhibition of PKA | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1760971 | Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation in presence of VEGF measured after 24 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold. |
| AID383089 | Inhibition of KDR 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. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID638921 | Inhibition of c-Met at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID479513 | Inhibition of AMPK | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507839 | Binding affinity to AXL | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID773013 | Antiproliferative activity against human T24 cells after 72 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
| Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1563343 | Inhibition of c-KIT A829P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507568 | Binding affinity to INSRR | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1302368 | Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| 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. |
| AID1581228 | Inhibition of human c-KIT A loop exon 17 D816V single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 12-26, Volume: 62, Issue:24
| Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. |
| AID1387029 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID508038 | Binding affinity to PKN2 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435655 | Binding constant for ERK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID734141 | Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastati |
| 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. |
| AID446373 | Inhibition of human recombinant N-terminally GST-tagged SIRT1 at 50 uM after 4 hrs in presence of NAD+ by fluorescent deacetylase assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins). |
| AID1389788 | Antiproliferative activity against HUVEC after 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 04-01, Volume: 28, Issue:6
| Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents. |
| AID507665 | Binding affinity to PDGFRA | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1254835 | Inhibition of VEGFR2 (unknown origin) | 2015 | European journal of medicinal chemistry, Oct-20, Volume: 103 | Ynamide Click chemistry in development of triazole VEGFR2 TK modulators. |
| AID1386990 | Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay | 2018 | Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19
| Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. |
| AID507669 | Binding affinity to PFTK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID629477 | Cytotoxicity against human QSG7701 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID1395591 | Effect on c-MYC protein expression in human HT-29 cells assessed as c-MYC level at 25 uM after 48 hrs by ELISA | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| AID1218227 | Cmax in female Sprague-Dawley rat plasma at 5 mg/kg, iv administered as single dose by LC/MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID256621 | Average Binding Constant for CAMK2A; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1760970 | Antiproliferative activity against human MKN-45 cells assessed assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Design, synthesis, and in vitro and in vivo anti-angiogenesis study of a novel vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitor based on 1,2,3-triazole scaffold. |
| 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. |
| AID1563416 | Inhibition of AKT autophosphorylation at T308 residue in human GIST5R cells harboring c-KIT 560 to 578 deletion/T670I mutant at 0.1 uM measured after 2 hrs by Western blot analysis | | | |
| AID625057 | Binding constant for TYRO3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID256665 | Average Binding Constant for ABL1; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID1737709 | Inhibition of AMPK in human K562 cells assessed as p-ACC (Ser79) level at 5 uM in glucose free medium and in presence of 2-Deoxy-D-glucose measured after 3 hrs by ELISA relative to control | 2020 | European journal of medicinal chemistry, Jul-01, Volume: 197 | Substituted oxindol-3-ylidenes as AMP-activated protein kinase (AMPK) inhibitors. |
| AID1224785 | Delta TM value showing the stabilisation of PDK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID536881 | Inhibition of human PDGFRbeta after 30 mins by ELISA | 2010 | Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22
| Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. |
| AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436024 | Binding constant for MRCKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224781 | Delta TM value showing the stabilisation of PAK4 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1542976 | Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| AID1602362 | Inhibition of covalent binding of 50 uM (Z)-N-(2-(2-(4-(2,8-Diethyl-5,5-difluoro-1,3,7,9-tetramethyl-5H-4lambda4,5lambda4-dipyrrolo[1,2-c:2',1'-f ][1,3,2]diazaborinin-10-yl)phenoxy)-acetamido)ethyl)-2,4-dimethyl-5-((2-oxo-5-(vinylsulfon-amido)-indolin-3-y | 2019 | Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
| Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations. |
| AID665082 | Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| 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. |
| AID1217863 | Drug excretion in feces of male cynomolgus monkey at 6 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| AID27363 | In vitro cytotoxicity was determined | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID435831 | Binding constant for RPS6KA5(Kin.Dom.1 - C-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383297 | Inhibition of CAMK2gamma | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507804 | Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID538338 | Inhibition of recombinant VEGFR2 after 1 hr by fluorescence polarization assay | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
| Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors. |
| AID638910 | Inhibition of Flt-1 at 10 uM | 2012 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 22, Issue:1
| Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1337499 | Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Design, synthesis, and biological evaluation of (2E)-(2-oxo-1, 2-dihydro-3H-indol-3-ylidene)acetate derivatives as anti-proliferative agents through ROS-induced cell apoptosis. |
| 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. |
| AID1224793 | Delta TM value showing the stabilisation of RSK2a produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1631794 | Cytotoxicity against human A549 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Design and synthesis of 4'-O-alkylamino-tethered-benzylideneindolin-2-ones as potent cytotoxic and apoptosis inducing agents. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID729552 | Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells at 5 uM by TR-FRET based binding assay | 2013 | European journal of medicinal chemistry, Mar, Volume: 61 | Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. |
| AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1896637 | Binding affinity to human RIP1 assessed as dissociation constant by competitive binding assay | 2022 | Journal of medicinal chemistry, 11-24, Volume: 65, Issue:22
| Small-Molecule Receptor-Interacting Protein 1 (RIP1) Inhibitors as Therapeutic Agents for Multifaceted Diseases: Current Medicinal Chemistry Insights and Emerging Opportunities. |
| AID1542972 | Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay | 2019 | ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
| Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids. |
| 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. |
| AID508133 | Binding affinity to YANK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1586439 | Inhibition of VEGFR2 internalization in HMEC1 cells assessed as total VEGFR2 level at 14 uM after 24 hrs by flow cytometry (Rvb = 100%) | 2019 | European journal of medicinal chemistry, Jan-15, Volume: 162 | Synthesis and biological evaluation as antiangiogenic agents of ureas derived from 3'-aminocombretastatin A-4. |
| AID479741 | Inhibition of ROCK2 | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| 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. |
| AID508041 | Binding affinity to PLK3 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID507603 | Binding affinity to MAP4K4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| 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. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507969 | Binding affinity to HIPK1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID256577 | Average Binding Constant for CLK4; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID612497 | Inhibition of VEGF-A induced HUVEC cell sprouting after 24 hrs by angiogenesis assay | 2011 | Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
| Arthrinins A-D: novel diterpenoids and further constituents from the sponge derived fungus Arthrinium sp. |
| AID665083 | Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay | 2012 | European journal of medicinal chemistry, Jul, Volume: 53 | 2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines. |
| AID1550019 | Effect on VEGFR2 in human A549 cells assessed as membrane VEGFR2 level at 10 uM incubated for 24 hrs by flow cytometric analysis relative to control | 2019 | European journal of medicinal chemistry, May-15, Volume: 170 | Novel multitarget inhibitors with antiangiogenic and immunomodulator properties. |
| AID1158369 | Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay | 2014 | Bioorganic & medicinal chemistry, Jul-15, Volume: 22, Issue:14
| The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents. |
| AID1421405 | Inhibition of recombinant human PDGFRbeta at 1000 nM after 60 mins by ELISA relative to control | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR. |
| 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. |
| AID256579 | Average Binding Constant for MAP3K5; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID513986 | Inhibition of EGFR expressed in human A431 cells | 2010 | Bioorganic & medicinal chemistry, Jul-15, Volume: 18, Issue:14
| Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents. |
| 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. |
| AID491754 | Inhibition of KDR at 0.1 uM | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
| Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. |
| AID1599415 | Antiviral activity against DENV2 infected in BHK-21 cells assessed as viral titer by plaque assay | 2019 | European journal of medicinal chemistry, Aug-15, Volume: 176 | Recent update on anti-dengue drug discovery. |
| AID1808764 | Selectivity index, ratio of IC50 for cytotoxicity in HUVEC cells to IC50 for antivascular activity against HUVEC assessed as inhibition of tube formation incubated for 6 hrs by inverted microscopy | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Novel Small-Molecule Antiangiogenesis Agents to Treat Diabetic Retinopathy. |
| AID459252 | Growth inhibition of mouse BaPTC2 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting | 2010 | Bioorganic & medicinal chemistry, Feb-15, Volume: 18, Issue:4
| Synthesis, structure-activity relationship and crystallographic studies of 3-substituted indolin-2-one RET inhibitors. |
| 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. |
| 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. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID507868 | Binding affinity to CDK7 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID436051 | Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1629525 | Inhibition of wild type cKIT in human GIST-T1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kina |
| AID507635 | Binding affinity to MST4 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID507579 | Binding affinity to KIT | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID479499 | Inhibition of gamma secretase in HEK293 cells assessed as amyloid beta secretion | 2010 | Bioorganic & medicinal chemistry letters, May-01, Volume: 20, Issue:9
| Inhibition of gamma-secretase by the CK1 inhibitor IC261 does not depend on CK1delta. |
| AID507959 | Binding affinity to FRK | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1395539 | Induction of apoptosis in human HT-29 cells assessed as necrotic cells at 25000 nM after 48 hrs by Annexin V-FITC staining-based flow cytometric analysis (Rvb = 2 +/- 6%) | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Arylureas derived from colchicine: Enhancement of colchicine oncogene downregulation activity. |
| 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. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1587940 | Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID1217922 | Drug excretion in urine of female Sprague-Dawley rat at 15 mg/kg, po administered as single dose by liquid scintillation counting | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
| Pharmacokinetics, distribution, and metabolism of [14C]sunitinib in rats, monkeys, and humans. |
| 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. |
| AID256575 | Average Binding Constant for NEK6; NA=Not Active at 10 uM | 2005 | Nature biotechnology, Mar, Volume: 23, Issue:3
| A small molecule-kinase interaction map for clinical kinase inhibitors. |
| AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1224784 | Delta TM value showing the stabilisation of PCTK1 produced by compound binding | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-18, Volume: 104, Issue:51
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. |
| AID1302357 | Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Discovery of N-(3-((1-Isonicotinoylpiperidin-4-yl)oxy)-4-methylphenyl)-3-(trifluoromethyl)benzamide (CHMFL-KIT-110) as a Selective, Potent, and Orally Available Type II c-KIT Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID759170 | Inhibition of chicken wild-type cSRC (251 to 533)-mediated phosphorylation of biotinylated poly-Glu-Tyr expressed in Escherichia coli BL21(DE3) preincubated for 30 to 60 mins prior to substrate addition by TR-FRET assay | 2013 | Journal of medicinal chemistry, Jul-25, Volume: 56, Issue:14
| Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design. |
| 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. |
| AID629516 | Inhibition of human VEGFR2 preincubated for 10 mins before ATP addition measured after 45 mins | 2011 | European journal of medicinal chemistry, Dec, Volume: 46, Issue:12
| Synthesis and biological evaluation of 2-indolinone derivatives as potential antitumor agents. |
| AID624910 | Binding constant for TTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID649472 | Antitumor activity against mouse BA/F3 cells expressing FLT3-ITD mutant xenografted in BALB/c mouse myeloproliferative model assessed as increase in host survival days at 60 mg/kg, po qd relative to control (Rvb = 20 days) | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| 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. |
| AID436020 | Binding constant for GCN2(Kin.Dom.2,S808G) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID435790 | Binding constant for DRAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425194 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID507945 | Binding affinity to FGFR1 | 2009 | Blood, Oct-01, Volume: 114, Issue:14
| AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). |
| AID1600271 | Cytotoxicity against human HepG2 cells assessed as reduction in cell growth after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Oct-01, Volume: 179 | Synthesis and biological evaluation of novel benzylidene-succinimide derivatives as noncytotoxic antiangiogenic inhibitors with anticolorectal cancer activity in vivo. |
| AID1895666 | Inhibition of PDGFRalpha (unknown origin) | 2021 | Journal of medicinal chemistry, 08-26, Volume: 64, Issue:16
| Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development. |
| 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. |
| AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435900 | Binding constant for AKT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1406764 | Antiproliferative activity against human HepG2 cells by MTT assay | 2018 | European journal of medicinal chemistry, Aug-05, Volume: 156 | Diterpenoid lead stevioside and its hydrolysis products steviol and isosteviol: Biological activity and structural modification. |
| AID649619 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay | 2012 | Journal of medicinal chemistry, Jan-26, Volume: 55, Issue:2
| VX-322: a novel dual receptor tyrosine kinase inhibitor for the treatment of acute myelogenous leukemia. |
| AID1587970 | Inhibition of human c-KIT A loop exon 18 A829P single mutant at 100 nM using poly (Glu,Tyr) 4:1 as substrate in presence of 33P-gamma-ATP by hotspot kinase assay relative to control | 2019 | Journal of medicinal chemistry, 04-25, Volume: 62, Issue:8
| Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1508612 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling | 2017 | Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
| Highly predictive and interpretable models for PAMPA permeability. |
| 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. |
| 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. |
| AID1645871 | NCATS Parallel Artificial Membrane Permeability Assay (PAMPA) Profiling in pH 5 buffer | 2022 | Bioorganic & medicinal chemistry, 02-15, Volume: 56 | Using in vitro ADME data for lead compound selection: An emphasis on PAMPA pH 5 permeability and oral bioavailability. |
| AID1797044 | Kinase Assay and Binding Constant Measurement from Article 10.1073/pnas.0504952102: \\Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.\\ | 2005 | Proceedings of the National Academy of Sciences of the United States of America, Aug-02, Volume: 102, Issue:31
| Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. |
| AID1795684 | Tyrosine Kinase Assay from Article 10.1021/jm0204183: \\Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothe | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1796237 | Homogeneous Time-resolved Fluorescence (HTRF) Assay from Article 10.1021/jm050458h: \\Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.\\ | 2005 | Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
| Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. |
| AID1798514 | PLK Kinase Assay from Article 10.1021/bi7008745: \\Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.\\ | 2007 | Biochemistry, Aug-21, Volume: 46, Issue:33
| Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity. |
| AID1799799 | Inhibition Assay from Article 10.1002/cbic.201200316: \\A Novel Approach to the Discovery of Small-Molecule Ligands of CDK2.\\ | 2012 | Chembiochem : a European journal of chemical biology, Sep-24, Volume: 13, Issue:14
| A novel approach to the discovery of small-molecule ligands of CDK2. |
| AID1801133 | KinEASE-STK Assay from Article 10.1021/cb500908d: \\Identification and further development of potent TBK1 inhibitors.\\ | 2015 | ACS chemical biology, Jan-16, Volume: 10, Issue:1
| Identification and further development of potent TBK1 inhibitors. |
| AID1795685 | Autophosphorylation Assay from Article 10.1021/jm0204183: \\Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular end | 2003 | Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
| Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosi |
| AID1801568 | Enzyme-linked Immunosorbent Assay (ELISA) from Article 10.1111/cbdd.12703: \\Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation.\\ | 2016 | Chemical biology & drug design, May, Volume: 87, Issue:5
| Discovery of 1,3-Diaryl-pyridones as Potent VEGFR-2 Inhibitors: Design, Synthesis, and Biological Evaluation. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| 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. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
| Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
| 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. |
| 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. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 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. |
| AID1347151 | Optimization of GU AMC 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. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7
| Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID364089 | Inhibition of CSF1R | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer. |
| AID1179255 | Antiangiogenic activity in chicken chorioallantoic membrane assessed as inhibition of VEGF-induced blood vessel formation treated 30 mins after VEGF addition measured after 3 days | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
| Synthesis and antiangiogenic activity of 6-amido-2,4,5-trimethylpyridin-3-ols. |
| AID1179254 | Antiangiogenic activity in chicken chorioallantoic membrane assessed as inhibition of VEGF-induced blood vessel formation at 0.01 nmol/CAM treated 30 mins after VEGF addition measured after 3 days relative to control | 2014 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
| Synthesis and antiangiogenic activity of 6-amido-2,4,5-trimethylpyridin-3-ols. |
| AID364090 | Antiproliferative activity against mouse 3T3 cells expressing human CSF1R after 72 hrs by Celltiter assay | 2008 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 18, Issue:17
| Pyridyl and thiazolyl bisamide CSF-1R inhibitors for the treatment of cancer. |
| AID1187639 | Cytotoxicity against human ACHN cells after 72 hrs by MTT assay | 2014 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 24, Issue:17
| Phorbaketals L-N, cytotoxic sesterterpenoids isolated from the marine sponge of the genus Phorbas. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |