| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1817045 | Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | | | |
| 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. |
| 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. |
| AID1387044 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) allografted in CB17 SCID mouse assessed as inhibition of tumor growth at 300 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. |
| AID1508902 | Inhibition of TEL fused c-KIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID374941 | Stabilization of human G4-telomeric quadruplex assessed as melting temperature by FRET assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID1532237 | Growth inhibition of human DU145 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID624735 | Binding constant for ANKK1 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. |
| AID512413 | Inhibition of human IGF-1R activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1611401 | Inhibition of wild type BCR/Abl (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| 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). |
| AID161423 | Inhibition of chimeric PDGF receptor with FLT-3 cytoplasmic domain phosphorylation in CHO cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID1563341 | Inhibition of c-KIT N822K mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1394581 | Antitumor activity against human EOL-1 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 25 mg/kg/day, ip | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID414739 | Cytotoxicity against human RKOp21 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID1338871 | Inhibition of Tel-fused c-KIT D816V mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1532196 | Growth inhibition of human HOP92 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID724672 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1443992 | Total Cmax in human administered as single dose | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
| Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| 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. |
| AID435564 | Binding constant for TRKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID511818 | Inhibition of BCR/ABL p210 autophosphorylation in human K562 cells after 2 hrs by Western blot analysis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
| Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase. |
| AID540210 | Clearance in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID435183 | Binding constant for PLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID414745 | Cytotoxicity against human A431 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID515837 | Antiproliferative activity against human GIST882 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| 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. |
| AID383090 | Inhibition of c-Kit 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. |
| AID387174 | Inhibition of c-kit | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Discovery of amido-benzisoxazoles as potent c-Kit inhibitors. |
| AID1524392 | Binding affinity to ANC-AS (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| AID1322184 | Effect on BCR-ABL protein levels in human K562 cells assessed as BCR-ABL to beta-tubulin ratio at 100 uM after 8 hrs in presence of MeBS by Western blot analysis relative to control | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand. |
| AID679626 | TP_TRANSPORTER: inhibition of ATPase activity in BCRP-expressing Sf9 cells | 2004 | Molecular pharmacology, Jun, Volume: 65, Issue:6
| High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. |
| 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. |
| AID414732 | Cytotoxicity against human H69 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435780 | Binding constant for BMPR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1394559 | Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID435795 | Binding constant for EPHA4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625064 | Binding constant for PIM2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624882 | Binding constant for PKAC-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624955 | Binding constant for EPHB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1126692 | Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1849608 | Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules. |
| AID624733 | Binding constant for SIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1524389 | Binding affinity to cSRC (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| AID1817046 | Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | | | |
| AID1705760 | Growth inhibition of human HCC 2998 cells measured after 48 hrs by SRB assay | | | |
| AID1338951 | Induction of apoptosis in human KU812 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID726977 | Antiproliferative activity against human K562 cells | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| New PAH derivatives functionalized by cyclic nitrone framework: synthetic design, anti-proliferative activity and interaction with DNA. |
| AID435516 | Binding constant for ADCK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435529 | Binding constant for LATS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1257225 | Inhibition of Trichomonas vaginalis adenosine-guanosine preferring ribohydrolase after 40 mins in presence of 0.01% triton X-100 | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target. |
| AID414986 | Cytotoxicity against human CCRF-CEM cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID457322 | Octanol-water partition coefficient, log P by RP-HPLC method | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity. |
| 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. |
| AID1705782 | Growth inhibition of human OVCAR-3 cells measured after 48 hrs by SRB assay | | | |
| AID721739 | Selectivity ratio of IC50 for human OCT3-mediated ASP+ uptake expressed in HEK293 cells to IC50 for human MATE1-mediated ASP+ uptake expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1338969 | Induction of apoptosis in human GIST48B cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID435924 | Binding constant for MARK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425024 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1832754 | Inhibition of wild type Bcr-Abl T315I mutant (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| 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. |
| 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. |
| 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. |
| AID1170647 | Cytotoxicity against HUVEC | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12
| Tetrahydroxanthene-1,3(2H)-dione derivatives from Uvaria valderramensis. |
| AID435783 | Binding constant for full-length BRSK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1464294 | Inhibition of AMPK alpha1/beta1/gamma1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID739103 | Cytotoxicity against mouse BA/F3 cells transfected with Bcr-Abl T315I mutant after 48 hrs by XTT assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| 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. |
| AID1358759 | Inhibition of SRC (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID624837 | Binding constant for IRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435521 | Binding constant for CAMKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625141 | Binding constant for RIOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624794 | Binding constant for MET kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624870 | Binding constant for NEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID414722 | Inhibition of c-Abl T315I mutant by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID624792 | Binding constant for KIT(V559D,T670I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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). |
| 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. |
| AID1394555 | Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1731535 | Permeability across apical to basolateral side in MDCK cells assessed as drug recovery at 1 uM after 2 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Tetrahydroindazole inhibitors of CDK2/cyclin complexes. |
| 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. |
| AID1508970 | Inhibition of c-KIT 560 to 578 deletion/T670I double mutant in human GIST5R cells assessed as reduction in STAT3 phosphorylation at 1 uM after 1 hr by Western blot analysis | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| 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. |
| AID1563328 | Inhibition of c-KIT V560D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| AID435280 | Binding constant for CSF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625116 | Binding constant for ADCK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435445 | Binding constant for ZAP70 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435184 | Binding constant for PTK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436014 | Binding constant for full-length DYRK1B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425110 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID624984 | Binding constant for ABL1(H396P)-phosphorylated 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. |
| AID1532207 | Growth inhibition of human KM12 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID625012 | Binding constant for GAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1865185 | Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as reduction in IL-6 level pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| 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). |
| AID435432 | Binding constant for MLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512390 | Inhibition of human PDK1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435793 | Binding constant for EPHA1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624944 | Binding constant for ALK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338879 | Antiproliferative activity against human MOLM14 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1444952 | Inhibition of TEL-fused cKIT N822K mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID624778 | Binding constant for ACVRL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID428367 | Inhibition of human carbonic anhydrase 2 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID625137 | Binding constant for MEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435195 | Binding constant for SRC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID721342 | Antitumor activity against mouse BA/F3 cells expressing BCR-ABL T315I mutant allografted in SCID mouse assessed as suppression of cell proliferation at 100 mg/kg/day, po qd for 10 days relative to untreated vehicle | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1865188 | Thermal stabilization of LPS-stimulated P38alpha in human THP-1 cells assessed as change in melting temperature at 5 uM pretreated for 1 hr followed by LPS-stimulation and measured after 15 mins by thermal proteome profiling analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID625135 | Binding constant for ADCK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1358757 | Inhibition of CDK16 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| 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. |
| 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. |
| AID663480 | Antiproliferative activity against HUVEC cells | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4
| Cytotoxic alkaloids from Fusarium incarnatum associated with the mangrove tree Aegiceras corniculatum. |
| AID624782 | Binding constant for FGFR3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1221965 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1394578 | Apparent volume of distribution in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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). |
| AID624896 | Binding constant for PRKR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424910 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID625111 | Binding constant for RIOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1860264 | Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay | | | |
| AID624732 | Binding constant for PYK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515826 | Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID624917 | Binding constant for MST3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1750904 | Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM after 48 hrs by MTT assay relative to control | | | |
| AID1612828 | Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| 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. |
| AID1247116 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib. |
| AID540213 | Half life in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| 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. |
| AID1358740 | Inhibition of ABL1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID624976 | Binding constant for PRKX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID343647 | Selectivity ratio of IC50 for Abl to IC50 for c-kit | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| AID435163 | Binding constant for full-length GSK3B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID591856 | Inhibition of human wild type PDGFRalpha assessed as [gamma33P]ATP incorporation into poly-Ala-Glu-Lys-Tyr after 60 mins by microplate scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1532199 | Growth inhibition of human NCI-H322M cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID624889 | Binding constant for JNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1338913 | Inhibition of c-KIT autophosphorylation at Y823 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID625024 | Binding constant for PRKD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID592014 | Binding affinity to human Flt3 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID625115 | Binding constant for PAK6 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. |
| 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. |
| 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. |
| AID1612812 | Inhibition of BTK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| AID512394 | Inhibition of human MST2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID512388 | Inhibition of human PKBalpha activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID414734 | Cytotoxicity against human MDA-MB-468 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID414743 | Cytotoxicity against human AsPC1 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID1659069 | Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects. |
| AID1743565 | Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID624748 | Binding constant for EPHA6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1301838 | Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
| Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. |
| AID1247115 | Inhibition of Bcr-Abl (unknown origin) after 1 hr by luminescence assay | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Expanding the structural diversity of Bcr-Abl inhibitors: Hybrid molecules based on GNF-2 and Imatinib. |
| AID317426 | Inhibition of human recombinant Abl | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents. |
| AID1422103 | Inhibition of heme oxygenase 1 in human K562R cell lysates assessed as decrease in bilirubin formation at 10 uM after 60 mins by spectrophotometric method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID94799 | Cytotoxic effect in K562 cells | 2003 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
| Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase. |
| 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. |
| AID436005 | Binding constant for ANKK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338853 | Inhibition of Tel-fused CSF1R (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID227573 | Relative resistance is the ratio of IC50 values of drug with JTV-519 to that without the reversing agent | 2004 | Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
| Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates. |
| AID1174981 | Antiproliferative activity against Bcr/Abl positive human K562 cells after 48 hrs by MTT method | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
| Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site. |
| 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. |
| AID435439 | Binding constant for PAK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1865196 | Thermal stabilization of LPS-stimulated MKK6 in human THP-1 cells assessed as upregulation of protein at 5 uM pretreated for 1 hr followed by Escherichia coli -stimulation and measured after 15 min by western blot analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID759134 | Growth inhibition of human LPS141 cells at 0.001 to 10 uM after 72 hrs by SRB 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. |
| 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. |
| AID512764 | Antiproliferative activity against mouse 32D cells transfected with p210 cells expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625132 | Binding constant for FGFR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1246534 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as cell viability at 250 nM incubated for 5 days (Rvb = 86.7%) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID625011 | Binding constant for FGR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625014 | Binding constant for PRKCE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1425140 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1584944 | Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID1394583 | Antitumor activity against human EOL-1 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg/day, ip | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| AID1444953 | Inhibition of TEL-fused cKIT D816V mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID624786 | Binding constant for KIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435910 | Binding constant for MAP4K4 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. |
| 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. |
| AID1322176 | Inhibition of BCR-ABL phosphorylation in human K562 cells at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand. |
| AID1714637 | Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors. |
| 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. |
| 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. |
| AID1277146 | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID1629557 | Inhibition of wild type cKIT in human GIST-T1 cells assessed as downregulation of ERK phosphorylation at T202//204 at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| AID1474049 | Ratio of drug concentration at steady state in human at 400 to 600 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| 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. |
| AID463624 | Inhibition of KIT | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID1532195 | Growth inhibition of human HOP62 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID435792 | Binding constant for EGFR(S752-I759del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625015 | Binding constant for ROCK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425128 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1563335 | Inhibition of c-KIT D816E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID767327 | Cytotoxicity against human QSG7701 cells assessed as growth inhibition at 100 uM after 48 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID435657 | Binding constant for full-length IKK-epsilon | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID592016 | Binding affinity to human Jak3 domain 10 assessed as residual binding at 1 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1422094 | Cytotoxicity against human K562R cells assessed as decrease in cell viability after 24 hrs by XTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID1444954 | Antiproliferative activity against CHL cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID414735 | Cytotoxicity against human MDA-MB-231 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| 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. |
| AID374943 | Stabilization of human G4-KIT1 DNA quadruplex assessed as melting temperature by FRET assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID1705785 | Growth inhibition of human OVCAR-8 cells measured after 48 hrs by SRB assay | | | |
| AID663481 | Cytotoxicity against human HeLa cells | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4
| Cytotoxic alkaloids from Fusarium incarnatum associated with the mangrove tree Aegiceras corniculatum. |
| AID512418 | Inhibition of human Flt-1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID709936 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| AID625051 | Binding constant for PRKCQ kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1221980 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID512371 | Inhibition of human SAPK4 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435319 | Binding constant for PKN1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1387052 | Antitumor activity against mouse BA/F3 cells expressing Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) allografted in CB17 SCID mouse assessed as tumor regression at 300 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. |
| 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. |
| 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. |
| AID262017 | Antiproliferative activity against U937 cells | 2006 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
| Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors. |
| 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. |
| AID1508899 | Inhibition of TEL fused c-KIT L576P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID1750944 | Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as early apoptotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 22.3%) | | | |
| AID428458 | Inhibition of mouse carbonic anhydrase 13 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1221982 | Fraction absorbed in human | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID624857 | Binding constant for HCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID705603 | Inhibition of CYP3A4-mediated midazolam 1'-hydroxylation | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
| AID724671 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1240407 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
| AID435202 | Binding constant for TRKC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1545699 | Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID414738 | Cytotoxicity against human A2780 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID625043 | Binding constant for PIK3CA(I800L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1464296 | Inhibition of Aurora A (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID1338941 | Cell cycle arrest in human GISTT1 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1444951 | Inhibition of TEL-fused cKIT D816H mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1262855 | Selectivity index, Ratio of IC50 for mouse BA/F3 cells expressing Bcr-Abl T315I mutant to IC50 for mouse BA/F3 cells expressing wild-type Bcr-Abl | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| AID624825 | Binding constant for BMPR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID364884 | Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
| AID1426835 | Toxicity in wild-type zebrafish AB assessed as mortality at 100 ug/ml | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| AID625056 | Binding constant for TESK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID414744 | Cytotoxicity against human CAL27 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| 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. |
| AID592104 | Binding affinity to human CSF1R cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1283269 | Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts. |
| 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. |
| 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. |
| AID1563342 | Inhibition of c-KIT Y823D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID1240405 | Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
| AID1865214 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as upregulation of CD44 expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID435932 | Binding constant for PKAC-alpha kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532224 | Growth inhibition of human OVCAR3 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID414733 | Cytotoxicity against human MCF7 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435205 | Selectivity for ABL1 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. |
| AID1425032 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624802 | Binding constant for PIM3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID590160 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
| Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors. |
| AID1424923 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID436006 | Binding constant for full-length AURKC | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1394604 | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y849 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID435822 | Binding constant for MEK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435160 | Binding constant for FER kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286571 | Antiproliferative activity against human CHL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| AID729373 | Inhibition of Abl1 kinase (unknown origin) using Tyr 6 peptide as substrate assessed as residual enzyme activity after every 10 secs measured for 15 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. |
| AID512380 | Inhibition of human TrkB activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1396812 | Inhibition of Bcr-Abl (unknown origin) | 2018 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 28, Issue:15
| ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups. |
| 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. |
| 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. |
| 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. |
| AID512775 | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-JAK1 kinase assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624994 | Binding constant for AKT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436055 | Binding constant for full-length YANK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625017 | Binding constant for TIE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1170648 | Cytotoxicity against human K562 cells | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12
| Tetrahydroxanthene-1,3(2H)-dione derivatives from Uvaria valderramensis. |
| 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. |
| AID435665 | Binding constant for NEK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1262841 | Growth inhibition of mouse BA/F3 cells expressing wild-type Bcr-Abl after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| 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. |
| AID435197 | Binding constant for TEC kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1286566 | Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| AID1507442 | Inhibition of SRC (unknown origin) at 10 uM after 15 mins by luminescence assay relative to control | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Design, synthesis and evaluation of azaacridine derivatives as dual-target EGFR and Src kinase inhibitors for antitumor treatment. |
| 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. |
| AID1508893 | Inhibition of wild type TEL fused c-KIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| 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. |
| AID1705744 | Growth inhibition of human CCRF-CEM cells measured after 48 hrs by SRB assay | | | |
| AID592021 | Binding affinity to human Vegfr2 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID624957 | Binding constant for EPHB6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID463625 | Inhibition of wild type Abl | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| 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. |
| AID625104 | Binding constant for MYO3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1699969 | Antiproliferative activity against human K562 cells by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
| Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells. |
| 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. |
| AID624941 | Binding constant for CDKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624704 | Binding constant for NEK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID591942 | Binding affinity to human CSF1R assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID435153 | Binding constant for full-length DAPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1508942 | Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant incubated for 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID513123 | Inhibition of phosphorylated Abl | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID592110 | Binding affinity to human Jnk2 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1358749 | Inhibition of ERK1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID624974 | Binding constant for PIK3CD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID759161 | Inhibition of ABL T315I mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr at 100 uM 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. |
| AID624814 | Binding constant for DCAMKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1750898 | Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay | | | |
| AID721745 | Ratio of Cmax unbound to IC50 for human MATE1-mediated ASP+ uptake expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID761194 | Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents. |
| 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. |
| AID1532217 | Growth inhibition of human MDA-MB-435 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1193745 | Cytotoxicity against human K562 cells after 72 hrs using Calcein AM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
| New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| 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. |
| AID721744 | Cmax in po dosed human | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID414627 | Drug level in rhesus monkey cerebrospinal fluid | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Discovery of N-(4-methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a potent apoptosis inducer and efficacious anticancer agent with high blood brain barrier penetration. |
| AID512393 | Inhibition of human NEK2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1563333 | Inhibition of c-KIT T670I/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID457326 | Binding affinity to HSA after 30 mins assessed as quenching of intrinsic HSA fluorescence emission by spectrofluorimetric assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity. |
| AID1832775 | Inhibition of Bcr-Abl phosphorylation in human K562 cells assessed as phosphorylated ABL protein level at 1 uM measured after 48 hrs by Western blot analysis (Rvb = 0.8783 to 0.9174 No_unit) | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| AID625010 | Binding constant for FER kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID1358750 | Inhibition of FAK (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| AID435678 | Binding constant for MUSK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID591943 | Binding affinity to human Fer assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1532230 | Growth inhibition of human ACHN cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID624840 | Binding constant for AXL kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1612827 | Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID1750903 | Reversal of BCRP-mediated multidrug resistance in MDCK-II cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay | | | |
| AID1394571 | Apparent volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1495933 | Stabilization of 5'-FAM/3'-TAMRA labeled c-KIT2 G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID1495931 | Stabilization of 5'-FAM/3'-TAMRA labeled human F21T G-quadruplex DNA assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID1584947 | Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1876320 | Antiviral activity against MERS-CoV | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| AID512386 | Inhibition of human PKCtheta activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1338874 | Antiproliferative activity against human KU812 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID625027 | Binding constant for MAP3K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1507439 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Design, synthesis and evaluation of azaacridine derivatives as dual-target EGFR and Src kinase inhibitors for antitumor treatment. |
| AID724677 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID374960 | Reduction in KIT protein expression in human GIST882 cells at 10 uM after 24 hrs by Western blot | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| 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. |
| AID435562 | Binding constant for STK36 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID721751 | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1425125 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624741 | Binding constant for LRRK2(G2019S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1338943 | Cell cycle arrest in human GIST882 cells assessed as accumulation at G0/G1 phase at 1 uM after 48 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID624822 | Binding constant for CDKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435310 | Binding constant for FLT3(ITD) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705783 | Growth inhibition of human OVCAR-4 cells measured after 48 hrs by SRB assay | | | |
| AID1445026 | Antitumor activity against mouse BAF3 cells harboring TEL-cKIT-T670I mutant allografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg, ip administered daily for 11 days relative to control | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1444961 | Antiproliferative activity against human MEG01 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID624869 | Binding constant for NEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1464295 | Inhibition of ASK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | | | |
| AID1286559 | Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1657795 | Octanol/water partition coefficient, log D of the compound at pH 2 | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID435297 | Binding constant for MLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425190 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID749516 | Inhibition of KIT K642E mutant autophosphorylation (unknown origin) expressed in human GIST882 cells by ELISA | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1903963 | Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| 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. |
| AID1303969 | Inhibition of Abl (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
| 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. |
| AID624975 | Binding constant for PLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425162 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624770 | Binding constant for CAMK2D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1358748 | Inhibition of EGFR (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| AID724650 | Inhibition of BCR-ABL T315I mutant in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID1865183 | Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as disappearance inflammatory phenotype at 5 uM pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID1338867 | Inhibition of Tel-fused c-KIT T670I/V559D double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1584976 | Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID592164 | Binding affinity to human Kit V559D/V654A mutant cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID1563327 | Inhibition of c-KIT V559G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID724678 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1240468 | Inhibition of wild type Bcr-Abl (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
| 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. |
| AID1495073 | Cytotoxicity in imatinib-resistant human K562R cells assessed as reduction cell viability incubated for 48 hrs by XTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
| Modular synthesis of new C-aryl-nucleosides and their anti-CML activity. |
| AID1705786 | Growth inhibition of human NCI/ADR-RES cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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. |
| 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. |
| 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). |
| 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. |
| AID625030 | Binding constant for LOK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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). |
| 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. |
| AID591949 | Binding affinity to human Flt1 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1832774 | Inhibition of Bcr-Abl phosphorylation in human K562 cells assessed as phosphorylated ABL protein level at 0.1 uM measured after 48 hrs by Western blot analysis (Rvb = 0.8783 to 0.9174 No_unit) | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| AID1705800 | Growth inhibition of human Hs-578T cells measured after 48 hrs by SRB assay | | | |
| AID228828 | Inhibition of Abl tyrosine kinase | 2003 | Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
| Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase. |
| AID414737 | Cytotoxicity against human SKOV3 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435318 | Binding constant for PAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1303957 | Inhibition of CDK2/Cyclin E (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
| AID625099 | Binding constant for TAOK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435939 | Binding constant for TIE2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705767 | Growth inhibition of human SF-295 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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. |
| AID625120 | Binding constant for EPHA8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1286552 | Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID435788 | Binding constant for CLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID384388 | Cytotoxicity against human PA1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID512416 | Inhibition of human Flt-4 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID625076 | Binding constant for PLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624982 | Binding constant for ABL1(F317L)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1630174 | Cytotoxicity against imatinib-resistant human K562 cells assessed as cell viability at 1 uM after 48 hrs by trypan blue exclusion assay relative to control | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. |
| 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. |
| 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). |
| AID295288 | Inhibition of human Lyn kinase expressed in Sf9 cells | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. |
| 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. |
| AID512385 | Inhibition of human PKD2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID414752 | Cytotoxicity against vincristine-resistant human CCRF-CEM/VCR1000 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID1337174 | Inhibition of recombinant human NQO2 using menadione/CMCDP as substrate/cofactor | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| 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. |
| 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. |
| AID435532 | Binding constant for MST3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625127 | Binding constant for RSK3(Kin.Dom.1-N-terminal) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1286562 | Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID709934 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| AID592017 | Binding affinity to human Kit assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1532209 | Growth inhibition of human SF268 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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). |
| 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. |
| AID435517 | Binding constant for AKT2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625038 | Binding constant for PIK3CA(E542K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624910 | Binding constant for TTK 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. |
| AID1612830 | Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| AID1358753 | Inhibition of FLT3 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| AID435285 | Binding constant for DMPK 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. |
| AID1705769 | Growth inhibition of human SNB-19 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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. |
| 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. |
| AID624874 | Binding constant for PCTK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624860 | Binding constant for VEGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1474047 | AUC in human at 400 to 600 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1705777 | Growth inhibition of human SK-MEL-28 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID435291 | Binding constant for FGFR3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624991 | Binding constant for ABL1-non phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1611407 | Inhibition of BCR/Abl F317I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID1495940 | Antiproliferative activity against imatinib-resistant human GIST48 cells harboring c-KIT V560D/D820A double mutant after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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. |
| AID435898 | Binding constant for ACVR1B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID451988 | Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
| 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. |
| 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. |
| AID1705771 | Growth inhibition of human U-251 cells measured after 48 hrs by SRB assay | | | |
| AID435404 | Binding constant for EPHB4 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 |
| AID624739 | Binding constant for GRK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID255004 | Inhibitory concentration against c-Kit wild type expressed in recombinant baculovirus | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. |
| AID271007 | Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | | | |
| AID624809 | Binding constant for MYLK4 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. |
| 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. |
| AID624797 | Binding constant for PHKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625094 | Binding constant for CDK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID513122 | Inhibition of unphosphorylated Abl | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| 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. |
| 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. |
| 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. |
| AID624768 | Binding constant for SRPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1750943 | Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as viable cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 52.8%) | | | |
| AID624726 | Binding constant for HIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1337171 | Inhibition of kinobead binding to ARG in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| AID435415 | Binding constant for MYLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1124818 | Activation of FXR (unknown origin) at 10 uM | 2014 | Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
| Some non-conventional biomolecular targets for diamidines. A short survey. |
| AID1567151 | Inhibition of wild type BCR/ABL (unknown origin) measured after 60 mins in presence of ATP by ADP-Glo kinase assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of novel Bcr-Abl |
| 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. |
| AID624743 | Binding constant for LTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1422101 | Induction of apoptosis in human K562R cells assessed as late apoptotic cells at 10 uM by Annexin V staining-based flow cytometry (Rvb = 9.49%) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID435551 | Binding constant for full-length p38-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1170649 | Cytotoxicity against human HeLa cells | 2014 | Journal of natural products, Dec-26, Volume: 77, Issue:12
| Tetrahydroxanthene-1,3(2H)-dione derivatives from Uvaria valderramensis. |
| AID1444940 | Inhibition of TEL-fused cKIT (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID435200 | Binding constant for full-length TNNI3K | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID436046 | Binding constant for PRKD2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1256161 | Inhibition of Bcr-Abl T315I mutant (unknown origin) by ADP-Glo assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
| AID435296 | Binding constant for MARK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625072 | Binding constant for TBK1 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. |
| 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. |
| AID1358760 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | | | |
| 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. |
| 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. |
| AID749501 | Drug metabolism in human liver microsomes assessed as formation of 4-(hydroxymethyl)-N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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). |
| AID1426838 | Cytotoxicity against CM-Dil-labeled human K562 cells xenografted in wild-type zebrafish AB assessed as cell growth inhibition at 50 ug/ml measured after 2 days by fluorescence microscopic method relative to control | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| AID1286557 | Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1246521 | Cytotoxicity against human U937 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID1886523 | Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| 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. |
| AID1584948 | Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1865190 | Thermal stabilization of LPS-stimulated P38alpha in human THP-1 cells assessed as thermal denaturation at 5 uM pretreated for 1 hr followed by LPS-stimulation and measured after 15 min by western blot based cellular thermal shift assay | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID1194049 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
| Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents. |
| AID1563436 | Inhibition of c-KIT V559D mutant in GIST patient-derived cells assessed as growth inhibition measured after 6 days by Celltiter-glo assay | | | |
| AID624932 | Binding constant for CLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID421455 | Inhibition of Lck | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. |
| AID624894 | Binding constant for MEK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1337170 | Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| 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 |
| AID1865234 | Binding affinity to P38alpha (unknown origin) measured at 2.54 to 50 uM after 360 secs by SPR analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID435162 | Binding constant for FLT3(N841I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338873 | Antiproliferative activity against human MEG01 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1358755 | Inhibition of JNK1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| 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. |
| AID435666 | Binding constant for full-length NEK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1705772 | Growth inhibition of human LOX IMVI cells measured after 48 hrs by SRB assay | | | |
| AID1283287 | Cytotoxicity against human K562/G cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
| 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. |
| AID625090 | Binding constant for ICK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532205 | Growth inhibition of human HCT15 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1563323 | Inhibition of c-KIT in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | | | |
| 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. |
| AID624714 | Binding constant for p38-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435204 | Binding constant for WEE1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID724981 | Inhibition of human recombinant wild type ABL1 expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1358745 | Inhibition of CDK1/cyclin A1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| AID624780 | Binding constant for CDK4-cyclinD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383901 | Cytotoxicity against human HCC1954 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID436015 | Binding constant for EPHA6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1519114 | Inhibition of recombinant human N-terminal His-tagged full length PDK1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID435290 | Binding constant for FGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID749498 | Terminal half life in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1272051 | Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Design, synthesis and evaluation of acridine derivatives as multi-target Src and MEK kinase inhibitors for anti-tumor treatment. |
| 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. |
| AID624779 | Binding constant for BTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID414748 | Cytotoxicity against human U87MG cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID1903975 | Inhibition of PDGFRbeta (unknown origin) by caliper mobility shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID436033 | Binding constant for PIK3CA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| 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. |
| 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. |
| AID1743562 | Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID1750899 | Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay | | | |
| AID624707 | Binding constant for DCAMKL3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID592098 | Binding affinity to human ABL1 phenylalanine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent 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. |
| 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. |
| 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. |
| AID624995 | Binding constant for CSF1R 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. |
| 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. |
| AID624992 | Binding constant for ABL1-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425034 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624747 | Binding constant for SgK110 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425192 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1358744 | Inhibition of CAMK2-alpha (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID436019 | Binding constant for FRK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID387176 | Selectivity ratio of IC50 for p38 to IC50 for c-kit | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Discovery of amido-benzisoxazoles as potent c-Kit inhibitors. |
| AID1316171 | Drug uptake in blood of rat monocrotaline model of pulmonary arterial hypertension at 100 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
| AID724667 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID767328 | Cytotoxicity against human HL7702 cells assessed as growth inhibition at 100 uM after 48 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| 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. |
| 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. |
| AID624718 | Binding constant for PFTAIRE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624931 | Binding constant for CLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1221964 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID512774 | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing TPR-MET kinase assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID310120 | Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID484276 | Colloidal aggregation in fed state simulated intestinal fluid by dynamic light scattering assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
| 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. |
| AID709996 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| 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. |
| 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. |
| AID497611 | Inhibition of mouse recombinant N-terminal His6-tagged Abl by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| 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. |
| 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. |
| AID624943 | Binding constant for ACVR1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1630173 | Cytotoxicity against imatinib-sensitive human K562 cells assessed as cell viability at 1 uM after 48 hrs by trypan blue exclusion assay relative to control | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells. |
| AID1524394 | Binding affinity to KIT (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| AID1262852 | Inhibition of human wild-type Abl after 30 mins by phosphocellulose paper disk assay using 0.1 mM EAIYAAPFAKKK peptide substrate | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| AID624990 | Binding constant for ABL1(Y253F)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435662 | Binding constant for MST2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624887 | Binding constant for ERK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625042 | Binding constant for PIK3CA(H1047Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512425 | Inhibition of human Met activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID484274 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
| AID625031 | Binding constant for MRCKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435169 | Binding constant for full-length MEK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1532202 | Growth inhibition of human COLO205 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1338832 | Inhibition of C-terminal His-tagged human ABL1 expressed in baculovirus infected SF9 cells using Tyr 02 peptide as substrate measured after 1 hr by FRET based Z'Lyte assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1221979 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| 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. |
| 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. |
| AID435899 | Binding constant for AKT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1532239 | Growth inhibition of human Hs 578T cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID1221971 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| AID721743 | Ratio of Cmax unbound to IC50 for human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| 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. |
| AID1358741 | Inhibition of ACVR2A (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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). |
| 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. |
| AID435518 | Binding constant for AURKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1629530 | Inhibition of His-tagged cKIT T670I mutant (544 to 935 residues) (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase 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 |
| 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. |
| AID663479 | Antiproliferative activity against human K562 cells | 2012 | Journal of natural products, Apr-27, Volume: 75, Issue:4
| Cytotoxic alkaloids from Fusarium incarnatum associated with the mangrove tree Aegiceras corniculatum. |
| AID1338855 | Inhibition of Tel-fused PDGFR-alpha (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID374959 | Reduction in KIT protein expression in human GIST882 cells at 5 uM after 24 hrs by Western blot | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID1903978 | Induction of cell cycle arrest in human MNNG/HOS cells assessed as accumulation of cells at G2/M phase at 0.4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID1508967 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as reduction in STAT3 phosphorylation at 1 uM after 1 hr by Western blot analysis | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| 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. |
| AID435400 | Binding constant for DDR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624973 | Binding constant for JAK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID374946 | Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID435781 | Binding constant for full-length BMX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624898 | Binding constant for GRK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1585050 | Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID624734 | Binding constant for YANK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435407 | Binding constant for FLT3(D835Y) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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). |
| AID1705793 | Growth inhibition of human SN12C cells measured after 48 hrs by SRB assay | | | |
| AID624951 | Binding constant for EPHA2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID436044 | Binding constant for PLK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID739091 | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated CrkL level after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| 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. |
| AID1394568 | MRT (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| AID624781 | Binding constant for CDK4-cyclinD3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1358761 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | | | |
| AID435561 | Binding constant for SRMS kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1286558 | Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1495936 | Stabilization of 5'-FAM/3'-TAMRA labeled duplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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. |
| AID1365580 | Inhibition of ABL T315I mutant in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
| AID1611403 | Inhibition of BCR/Abl Y253F mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID624795 | Binding constant for MET(M1250T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384409 | Cytotoxicity against human RERF-LC-KJ cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1750945 | Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as late apoptotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 17.9%) | | | |
| AID1256160 | Inhibition of wild type Bcr-Abl (unknown origin) by ADP-Glo assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
| AID1519115 | Inhibition of recombinant human N-terminal GST-tagged full length PRKG1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID1426834 | Toxicity in wild-type zebrafish AB assessed as mortality at 50 ug/ml | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| AID624738 | Binding constant for MLCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425078 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID591855 | Inhibition of human wild type KIT assessed as [gamma33P]ATP incorporation into polyGluTyr after 60 mins by microplate scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID282895 | Inhibition of BCRP expressed in mitoxantrone-resistant human HCT116 cells assessed as increase in mitoxantrone accumulation at 10 uM after 15 mins | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Piperazinobenzopyranones and phenalkylaminobenzopyranones: potent inhibitors of breast cancer resistance protein (ABCG2). |
| AID624965 | Binding constant for LZK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532221 | Growth inhibition of human UACC257 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1612813 | Inhibition of CSK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID724977 | Inhibition of human recombinant ABL1 G250E mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID1519098 | Inhibition of recombinant human N-terminal GST-tagged ALK1 (144 to end residues) expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID1563332 | Inhibition of c-KIT T670E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| AID624727 | Binding constant for FYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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 |
| AID435797 | Binding constant for ERBB4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624922 | Binding constant for CAMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435283 | Binding constant for DAPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1444946 | Inhibition of TEL-fused cKIT V559D mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID624880 | Binding constant for PIK4CB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624866 | Binding constant for MLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512383 | Inhibition of human Rsk1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1563495 | Antitumor activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant xenografted in BALB/c mouse assessed as tumor weight at 100 mg/kg/day, po administered via gavage for 28 days (Rvb = 4.59 g) | | | |
| AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1338866 | Inhibition of Tel-fused c-KIT N822K mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID767330 | Cytotoxicity against human QSG7701 cells assessed as growth inhibition at 50 uM after 48 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID435647 | Binding constant for CAMK2D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435912 | Binding constant for MRCKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1524391 | Binding affinity to SYK (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| AID435660 | Binding constant for full-length MELK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID592171 | Binding affinity to human DRAK1 valine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID435434 | Binding constant for RET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID592165 | Binding affinity to human LCK tyrosine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID624930 | Binding constant for TNK1 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. |
| AID1060677 | Inhibition of Bcr-Abl (unknown origin) phosphorylation by spectrophotometric assay | 2014 | Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
| Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level. |
| AID512373 | Inhibition of human SGK activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID624730 | Binding constant for CAMK2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1592401 | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents. |
| 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. |
| 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. |
| AID1532223 | Growth inhibition of human IGROV1 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1876321 | Antiviral activity against SARS-CoV-2 in african green monkey Vero cells pretreated with virus for 1 hr followed by cell addition measured after 1 to 8 hrs | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| 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. |
| AID624924 | Binding constant for RIPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID442505 | Inhibition of PTK | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
| Synthesis, antitumor activity and molecular docking study of novel sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives. |
| 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. |
| AID1338922 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID719837 | Displacement of (S)-N4-(2-(4-(4-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenylcarbamoyl)benzyl)piperazin-1-yl)ethyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2-(4-(3-(trifluoromethyl | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID435274 | Binding constant for ACVR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532222 | Growth inhibition of human UACC62 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1705774 | Growth inhibition of human M14 cells measured after 48 hrs by SRB assay | | | |
| AID512376 | Inhibition of human SAPK2a activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1508904 | Inhibition of TEL fused c-KIT D816H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID624753 | Binding constant for PKNB(M.tuberculosis) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1524396 | Binding affinity to ABL2 (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| AID1532206 | Growth inhibition of human HT-29 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1425101 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1337172 | Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| AID1611405 | Inhibition of BCR/Abl V299L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID428368 | Inhibition of human carbonic anhydrase 3 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID498532 | Cmax in chronic myeloid leukemia patient | 2009 | Nature chemical biology, Mar, Volume: 5, Issue:3
| A pulse at the heart of targeted therapy. |
| AID547622 | Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| 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. |
| AID1705756 | Growth inhibition of human NCI-H322M cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID435693 | Binding constant for TGFBR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1612817 | Inhibition of SRC (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624876 | Binding constant for PDPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID724976 | Inhibition of human recombinant ABL1 H396P mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID624952 | Binding constant for EPHA4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584970 | Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| 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. |
| AID1358742 | Inhibition of BRAF (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID435667 | Binding constant for full-length NLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1705794 | Growth inhibition of human TK-10 cells measured after 48 hrs by SRB assay | | | |
| AID721747 | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1386085 | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| 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. |
| AID1286570 | Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| AID515827 | Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| 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. |
| 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. |
| AID1495934 | Stabilization of 5'-FAM/3'-TAMRA labeled BCL-2 promoter G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID1657801 | Half life in human liver microsomes at 1 uM incubated prior to NADPH addition by LC-MS/MS analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID1246535 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as cell viability at 250 nM incubated for 8 days (Rvb = 89.4%) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| 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. |
| 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. |
| AID512382 | Inhibition of human PDGFR-beta activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435901 | Binding constant for BRAF kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624921 | Binding constant for MAP4K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435655 | Binding constant for ERK5 kinase domain | 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. |
| AID1737439 | Induction of cell death in human imatinib-resistant K562 cells assessed by cell viability at 1 uM measured after 72 hrs by Propidium iodide stain based FACS assay | 2020 | European journal of medicinal chemistry, Jun-01, Volume: 195 | Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells. |
| 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. |
| AID435147 | Binding constant for ACVR2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1465771 | Intrinsic clearance in mouse liver microsomes at 3 uM after 60 mins by LC-MS analysis | 2017 | Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
| Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. |
| AID1464298 | Inhibition of BRAF (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID1705781 | Growth inhibition of human IGROV-1 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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 |
| AID1508894 | Inhibition of TEL fused c-KIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID512438 | Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID771262 | Cytotoxicity against human MCF7 cells after 72 hrs by calcein-AM assay | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines. |
| AID625131 | Binding constant for FGFR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1454436 | Displacement of ALLO-1 from allosteric site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
| |
| AID1338877 | Antiproliferative activity against human GIST48B cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1876260 | Inhibition of Abl (unknown origin) | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinase Inhibitors as Underexplored Antiviral Agents. |
| AID435433 | Binding constant for full-length MST1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338939 | Cell cycle arrest in human MEG01 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1444931 | Inhibition of TEL-fused cKIT C674S mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID649626 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing assessed as cell viability at 0.1 uM 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. |
| AID435775 | Binding constant for ABL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338870 | Inhibition of Tel-fused c-KIT T670I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID435158 | Binding constant for EPHA5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1246526 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human U937 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| 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. |
| AID1563378 | Growth inhibition of human GIST48B cells after 72 hrs by CCK8 assay | | | |
| AID1612814 | Inhibition of Fyn A (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID435288 | Binding constant for EPHB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625060 | Binding constant for CAMKK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1625313 | Inhibition of imatinib-resistant PDGFR D842V mutant (unknown origin) expressed in mouse BA/F3 cells assessed as decrease in cell viability after 48 hrs by CellTiter 96 aqueous one solution cell proliferation assay | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID512429 | Inhibition of human CSK activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1563492 | Antitumor activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant xenografted in BALB/c mouse assessed as tumor growth inhibition at 100 mg/kg/day, po administered via gavage for 28 days relative to control | | | |
| AID591940 | Binding affinity to human Kit V559D mutant cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID435941 | Binding constant for ZAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435150 | Binding constant for ARK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624766 | Binding constant for p38-gamma kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID414720 | Cytotoxicity against human HeLa cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID463623 | Inhibition of PDGFR | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID1278602 | Inhibition of BCR/ABL in human K562 cells assessed as reduction in ABL protein level at IC50 incubated for 3 days by Western blot analysis relative to control | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. |
| AID1612815 | Inhibition of LCK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| AID1524397 | Binding affinity to ABL1 (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID709933 | Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1629556 | Inhibition of wild type cKIT in human GIST-T1 cells assessed as downregulation of S6 phosphorylation at S235/236 at 1 uM after 1 hr by Western blot analysis | 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 |
| AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | | | |
| AID262701 | Inhibition of PDGFR alpha phosphorylation in G292 cell | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. |
| 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. |
| AID624987 | Binding constant for ABL1(Q252H)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID271006 | Inhibition of wild type NPM/ALK autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| AID1524395 | Binding affinity to CSF1R (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| AID1705790 | Growth inhibition of human ACHN cells measured after 48 hrs by SRB assay | | | |
| AID1338914 | Inhibition of c-KIT autophosphorylation at Y703 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID761195 | Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Jul-15, Volume: 21, Issue:14
| Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents. |
| 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. |
| 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. |
| AID512409 | Inhibition of human PDGFRalpha activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1865216 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as suppression of CD14 expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID512389 | Inhibition of human PKA activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624905 | Binding constant for CDKL5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338831 | Growth inhibition of mouse BAF3 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1563338 | Inhibition of c-KIT D820E mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1612829 | Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID624823 | Binding constant for MKNK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425157 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID435398 | Binding constant for DAPK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID414746 | Cytotoxicity against human Hec1A cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID1445023 | Antitumor activity against human GISTT1 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg, ip administered daily for 28 days relative to control | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1705763 | Growth inhibition of human HT-29 cells measured after 48 hrs by SRB assay | | | |
| AID624947 | Binding constant for BRAF(V600E) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1262840 | Selectivity index, ratio of IC50 for Abl T315I mutant (unknown origin) to IC50 for human wild-type Abl | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| 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. |
| 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. |
| AID625067 | Binding constant for NDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1743567 | Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID624971 | Binding constant for DAPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1865194 | Thermal stabilization of LPS-stimulated MKK3 in human THP-1 cells assessed as upregulation of protein at 5 uM pretreated for 1 hr followed by LPS-stimulation and measured after 15 min by western blot analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID1563339 | Inhibition of c-KIT D820G mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID767332 | Antiproliferative activity against human HepG2 cells after 24 to 96 hrs by MTS assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID1629564 | Inhibition of cKIT T670I mutant in human GIST-5R cells assessed as downregulation of AKT phosphorylation at S473 at 1 uM after 1 hr by Western blot analysis | 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 |
| AID1244539 | Antiproliferative activity against imatinib-resistant human K562 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents. |
| AID1338863 | Inhibition of BCR/ABL p210 fusion protein F317I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1358746 | Inhibition of CK1alpha1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID457325 | Cytotoxicity against human HeLa cells after 72 hrs by methylene blue staining | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity. |
| 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. |
| AID1338953 | Induction of apoptosis in human KU812 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| 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. |
| AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | | | |
| 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. |
| AID1532189 | Growth inhibition of human HL-60(TB) cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID625129 | Binding constant for HIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID719847 | Competitive inhibition of human recombinant NQO2-mediated mitomycin C metabolism using NADH as cosubstrate incubated for 5 mins prior to NADH addition measured after 30 mins by Michaelis-Menten plot analysis | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID1714638 | Cytotoxicity against human 293T cells assessed as reduction in cell viability after 24 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors. |
| AID1474048 | Drug concentration at steady state in human at 400 to 600 mg, po QD after 24 hrs | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| 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. |
| AID512747 | Inhibition of Bcr-abl tyrosine phosphorylation in mouse BA/F3ells p210 Bcr-abl after 90 mins by ELISA | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624996 | Binding constant for EGFR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338852 | Inhibition of BCR-fused DDR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1338857 | Inhibition of Tel-fused VEGFR2 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID1300620 | Antiproliferative activity against human K562 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| AID721754 | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| 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. |
| AID590031 | Antiproliferative activity against human imatinib-resistant K562 cells | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
| Hybrid compounds as new Bcr/Abl 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. |
| 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. |
| 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. |
| AID592169 | Binding affinity to human PDGFRbeta cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID625078 | Binding constant for SRPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1246518 | Cytotoxicity against human K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID710013 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1277148 | Cytotoxicity against human G361 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID435431 | Binding constant for MAP4K1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624923 | Binding constant for MAPKAPK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435805 | Binding constant for MAP4K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425030 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID624961 | Binding constant for TGFBR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624928 | Binding constant for CDKL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1444950 | Inhibition of TEL-fused cKIT A829P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID435180 | Binding constant for MAPKAPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435808 | Binding constant for full-length MEK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID590030 | Antiproliferative activity against human KU812 cells | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
| Hybrid compounds as new Bcr/Abl inhibitors. |
| AID625047 | Binding constant for AMPK-alpha2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625119 | Binding constant for CAMK1G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID649623 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient 2 expressing FLT3-D835Y mutation assessed as cell viability at 15 uM 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. |
| AID1832777 | Inhibition of Bcr-Abl phosphorylation in human K562 cells assessed as phosphorylated ABL protein level at 10 uM measured after 48 hrs by Western blot analysis (Rvb = 0.8783 to 0.9174 No_unit) | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| AID414740 | Cytotoxicity against human HCT15 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID461860 | Cytotoxicity against human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Design, synthesis, and biological evaluation of novel water-soluble triptolide derivatives: Antineoplastic activity against imatinib-resistant CML cells bearing T315I mutant Bcr-Abl. |
| AID739092 | Inhibition of Bcr-Abl T315I mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction of phosphorylated STAT5 level after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| AID1464308 | Inhibition of NEK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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). |
| AID1286561 | Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| 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. |
| AID512769 | Antiproliferative activity against human SUP-B15 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID749493 | Ratio of AUC (0 to 48 hrs) in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose to AUC (0 to 48 hrs) in Sprague-Dawley rat assessed as N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-4-(1-piperazinylmethyl)benzamide at 1 mg/kg, iv | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1422102 | Induction of apoptosis in human K562R cells assessed as necrotic cells at 10 uM by Annexin V staining-based flow cytometry (Rvb = 0.87%) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID624926 | Binding constant for RIOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1386089 | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| AID1705795 | Growth inhibition of human UO-31 cells measured after 48 hrs by SRB assay | | | |
| AID435293 | Binding constant for JNK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624793 | Binding constant for KIT(V559D,V654A) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID590028 | Inhibition of Bcr/Abl by FRET-based Z-lyte assay | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
| Hybrid compounds as new Bcr/Abl inhibitors. |
| AID435663 | Binding constant for full-length MST4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435295 | Binding constant for MAP4K3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624970 | Binding constant for CDK5 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. |
| AID1904011 | Antiinvasive activity against human MG-63 cells assessed as expression of FAK by measuring fluorescence at 0.4 uM upto 48 hrs by DAPI staining based immunofluorescence microscopic analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| 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. |
| AID435807 | Binding constant for MARK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1743557 | Antiproliferative activity against human L132 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID435292 | Binding constant for ITK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID724668 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID1705791 | Growth inhibition of human CAKI-1 cells measured after 48 hrs by SRB assay | | | |
| AID592100 | Binding affinity to human BLK serine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID749507 | Half life in human liver microsomes by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| 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. |
| AID749497 | Mean residence time in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1584975 | Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1194048 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry, Apr-15, Volume: 23, Issue:8
| Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents. |
| AID497107 | Inhibition of human recombinant full-length N-terminal GST-tagged p38alpha expressed in Escherichia coli by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| 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. |
| AID1394602 | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y1018 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID435909 | Binding constant for full-length LKB1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1277149 | Induction of apoptosis in human G361 cells assessed as activation of caspases-3/7 at 50 uM using Ac-DEVD-AMC as substrate after 6 hrs by fluorescence microplate reader method relative to control | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID512403 | Inhibition of human IKKalpha activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625019 | Binding constant for AKT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID414717 | Inhibition of human recombinant HDAC1 expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID435198 | Binding constant for TIE1 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. |
| 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. |
| AID435785 | Binding constant for full-length CDK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1182700 | Antiproliferative activity against human HMC-1.2 cells carrying V560G, D816V mutant assessed as cell growth inhibition by MTT assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors. |
| AID1585052 | Antitumor activity against mouse BAF3 cells expressing BCR/ABL T315I mutant allografted in nu/nu mouse assessed as tumor weight at 100 mg/kg, po administered via gavage measured for 14 days (Rvb = 2.78 g) | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID463630 | Inhibition of wild type Bcr-Abl | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| 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. |
| 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. |
| 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. |
| AID1193744 | Cytotoxicity against human MCF7 cells after 72 hrs using Calcein AM by fluorescence assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
| New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID624820 | Binding constant for ACVR2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1464309 | Inhibition of p38alpha (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| 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. |
| AID436032 | Binding constant for MYO3B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435563 | Binding constant for TNIK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1750946 | Potentiation of adriamycin-induced apoptosis in human K562 cells assessed as necrotic cells at 5 uM incubated for 48 hrs in presence of 10 uM adriamycin by Annexin-V/FITC-based flow cytometry (Rvb = 7%) | | | |
| AID1532203 | Growth inhibition of human HCC2998 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID625007 | Binding constant for EGFR(T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1519110 | Inhibition of recombinant human N-terminal GST-tagged full length GSK3alpha expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID1743560 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID414741 | Cytotoxicity against human HCT116 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID624813 | Binding constant for MINK 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. |
| AID435832 | Binding constant for SLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338990 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1705759 | Growth inhibition of human COLO 205 cells measured after 48 hrs by SRB assay | | | |
| AID512374 | Inhibition of human SAPK3 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1625309 | In vivo inhibition of BCR-ABL/T315I mutant expressed in bone marrow cells transplanted in mouse assessed as level of cells expressing gatekeeper mutation at 100 mg/kg, bid measured after 15 days | 2016 | Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
| Development of Heat Shock Protein (Hsp90) Inhibitors To Combat Resistance to Tyrosine Kinase Inhibitors through Hsp90-Kinase Interactions. |
| AID1629565 | Inhibition of cKIT T670I mutant in human GIST-5R cells assessed as downregulation of S6 phosphorylation at S235/236 at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| AID719844 | Displacement of (S)-N4-(2-(4-(4-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenylcarbamoyl)benzyl)piperazin-1-yl)ethyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2-(4-(3-(trifluoromethyl | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID1339539 | Inhibition of full length human His6/GST-tagged NQO2 expressed in Escherichia coli Tuner(DE3)pLysS using menadione as substrate and CCHP as co-substrate preincubated with enzyme followed by substrate addition by MTT dye based continuous spectrophotometric | 2017 | ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2
| Affinity-Based Selectivity Profiling of an In-Class Selective Competitive Inhibitor of Acyl Protein Thioesterase 2. |
| AID624789 | Binding constant for KIT(D816V) 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. |
| 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. |
| AID1705755 | Growth inhibition of human NCI-H23 cells measured after 48 hrs by SRB assay | | | |
| AID1705751 | Growth inhibition of human EKVX cells measured after 48 hrs by SRB assay | | | |
| AID1903979 | Induction of cell cycle arrest in human MG-63 cells assessed as accumulation of cells at G0/G1 phase at 0.4 uM incubated for 48 hrs by propidium iodide staining based flow cytometry analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID624888 | Binding constant for ERK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435804 | Binding constant for LYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID384669 | Cytotoxicity against human NCI-H2087 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1338918 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in Stat3/5 phosphorylation at Y705/Y694 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1394556 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID625066 | Binding constant for IRAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1817042 | Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay | | | |
| AID1611404 | Inhibition of BCR/Abl E255K mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID1422095 | Inhibition of BCR-ABL in human K562R cells assessed as decrease in CrKL phosphorylation at 1 to 10 uM by immuno blot analysis | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID1338861 | Inhibition of BCR/ABL p210 fusion protein M356T mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1338947 | Induction of apoptosis in human K562 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID724648 | Inhibition of BCR-ABL T315I mutant-mediated STAT5 phosphorylation in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID512412 | Inhibition of human IR activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624830 | Binding constant for CDK9 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624855 | Binding constant for FRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID719835 | Displacement of (S)-N4-(2-(4-(4-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenylcarbamoyl)benzyl)piperazin-1-yl)ethyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2-(4-(3-(trifluoromethyl | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID1338851 | Inhibition of Tel-fused DDR1 (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID1386050 | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| AID1394603 | Inhibition of PDGF-induced PDGFRalpha autophosphorylation at Y754 residue in human NCI-H1703 cells at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| AID724984 | Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID343641 | Selectivity ratio of IC50 for p38alpha to IC50 for c-kit | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| 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. |
| AID1508897 | Inhibition of TEL fused c-KIT V559A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID515838 | Antiproliferative activity against mouse M-NFS-60 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID624962 | Binding constant for ASK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1444959 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID435152 | Binding constant for CAMK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1657816 | Protein binding in human plasma | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID1338856 | Inhibition of Tel-fused PDGFR-beta (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1422093 | Inhibition of heme oxygenase 1 in Sprague-Dawley rat spleen microsomal fraction assessed as decrease in bilirubin formation using biliverdin reductase as substrate after 60 mins by spectrophotometric method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID1508898 | Inhibition of TEL fused c-KIT V559G mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID1246522 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| AID1422092 | Cytotoxicity against imatinib-sensitive human K562 cells assessed as decrease in cell viability after 24 hrs by XTT assay | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| 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. |
| AID1412487 | Binding affinity to recombinant human CRK-2 nSH3 domain (1 to 304 residues) expressed in Escherichia coli assessed as inhibition of Abl T315I mutant-mediated CRK-2 phosphorylation at Y221 residue at 1 uM after 10 to 30 mins by PAGE analysis | 2018 | MedChemComm, Mar-01, Volume: 9, Issue:3
| Structure-guided design of a potent peptide inhibitor targeting the interaction between CRK and ABL kinase. |
| AID1338924 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1424892 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1743528 | Inhibition of BCR-ABL T315I mutant (unknown origin) incubated for 40 mins in presence of [gamma33P]ATP by scintillation method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| 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. |
| AID435405 | Binding constant for ERK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID255976 | Inhibitory concentration against IL-3 independent Ba/F3 Kit D816V cell line | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. |
| AID428366 | Inhibition of human carbonic anhydrase 1 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID1903970 | Antiproliferative activity against human MNNG/HOS cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID624775 | Binding constant for STK16 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1262854 | Growth inhibition of mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 48 hrs by MTT assay | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| AID625122 | Binding constant for RET(M918T) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID414719 | Inhibition of HDAC in human HeLa cells assessed as induction of cellular histone H3 hyperacetylation | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435546 | Binding constant for PRKG1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID721741 | Selectivity ratio of IC50 for human OCT1-mediated ASP+ uptake expressed in HEK293 cells to IC50 for human MATE1-mediated ASP+ uptake expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID625028 | Binding constant for ASK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515833 | Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID435826 | Binding constant for full-length PCTK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1916785 | Inhibition of HER2 (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery. |
| AID1338858 | Inhibition of BCR/ABL p210 fusion protein T315I mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1611402 | Inhibition of BCR/Abl Q252H mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID1563435 | Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion mutant measured after 72 hrs by CCK8 assay | | | |
| AID624858 | Binding constant for JAK1(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338959 | Induction of apoptosis in human MEG01 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID254803 | Inhibitory concentration against platelet-derived growth factor receptor | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
| Designed multiple ligands. An emerging drug discovery paradigm. |
| AID343642 | Inhibition of KDR | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| AID624918 | Binding constant for DYRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425046 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1394560 | Inhibition of TEL-fused c-KIT (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID512760 | Cytotoxic activity against mouse 32D cells transfected with p210 Bcr-abl | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID271010 | Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| 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. |
| AID414736 | Cytotoxicity against human SKBR3 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID624731 | Binding constant for CAMK2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID436018 | Binding constant for FLT4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID458671 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 1.4 uM 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. |
| 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. |
| AID1705788 | Growth inhibition of human 786-0 cells measured after 48 hrs by SRB assay | | | |
| AID1865202 | Inhibition of P38 MAPK pathway in Escherichia coli-stimulated human THP-1 cells assessed as reduction in IL-1beta expression at 5 uM pretreated for 1 hr followed by Escherichia coli stimulation and measured upto 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID435833 | Binding constant for full-length TNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624920 | Binding constant for MRCKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624729 | Binding constant for FAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435277 | Binding constant for full-length CDK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID540209 | Volume of distribution at steady state in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| AID435828 | Binding constant for full-length PIP5K2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID749513 | Inhibition of KIT K642E mutant (unknown origin) expressed in human GIST882 cells assessed as cell growth inhibition by ATP-depletion assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1743527 | Inhibition of wild type BCR-ABL (unknown origin) incubated for 40 mins in presence of [gamma33P]ATP by scintillation method | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID709990 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| AID591948 | Binding affinity to human Fgfr4 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID435650 | Binding constant for full-length CSNK1E | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID394659 | Inhibition of Abl with T315N mutant | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
| Kinase domain mutations in cancer: implications for small molecule drug design strategies. |
| AID625045 | Binding constant for PIK3CA(Q546K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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). |
| AID1629563 | Inhibition of cKIT T670I mutant autophosphorylation at Y823 in human GIST-5R cells at 1 uM after 1 hr by Western blot analysis | 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 |
| AID624963 | Binding constant for LATS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID254662 | Inhibitory concentration against c-Kit | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
| Designed multiple ligands. An emerging drug discovery paradigm. |
| AID435648 | Binding constant for CAMKK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435779 | Binding constant for ALK kinase domain | 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. |
| 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. |
| AID1532241 | Growth inhibition of human MDA-MB-468 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID515828 | Inhibition of PDGFRbeta autophosphorylation in human A31 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID721354 | Antitumor activity against mouse BA/F3 cells expressing wild type BCR-ABL allografted in SCID mouse assessed as inhibition of tumor growth at 50 mg/kg, po qd for 14 days | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| 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). |
| AID1611410 | Inhibition of BCR/Abl P190 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID1256162 | Cytotoxicity against human K562 cells expressing Bcr-Abl assessed as growth inhibition after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Nov-02, Volume: 104 | Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine. |
| 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. |
| AID343639 | Inhibition of c-kit | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| 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. |
| 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. |
| AID513129 | Inhibition of PDGFRbeta kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID360766 | Antiviral activity against Dengue virus infected in african green monkey Vero cells administered before viral challenge after 3 days by viral plaque assay | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Feb-27, Volume: 104, Issue:9
| c-Src protein kinase inhibitors block assembly and maturation of dengue virus. |
| 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. |
| 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 |
| AID624760 | Binding constant for PFPK5(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624939 | Binding constant for FLT3(N841I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1504524 | Inhibition of MAPK p38 (unknown origin) | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer. |
| AID1677058 | Anticancer activity against human K562 cells assessed as cell growth inhibition at 1 uM by MTT assay relative to control | 2020 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 30, Issue:23
| Benzylidene thiazolidinediones: Synthesis, in vitro investigations of antiproliferative mechanisms and in vivo efficacy determination in combination with Imatinib. |
| AID1246523 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| 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. |
| AID425653 | Renal clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Physicochemical determinants of human renal clearance. |
| AID282897 | Cytotoxicity against mitoxantrone-sensitive human HCT116 cells at 10 uM assessed as viable cells after 48 hrs | 2005 | Journal of medicinal chemistry, Nov-17, Volume: 48, Issue:23
| Piperazinobenzopyranones and phenalkylaminobenzopyranones: potent inhibitors of breast cancer resistance protein (ABCG2). |
| 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. |
| AID624758 | Binding constant for RIPK5 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). |
| 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. |
| 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. |
| AID625118 | Binding constant for CAMK1D kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624720 | Binding constant for HIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624812 | Binding constant for SBK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID503311 | Antiproliferative activity against human PC3 cells at 10 uM after 120 hrs by MTT assay relative to DMSO | 2006 | Nature chemical biology, Jun, Volume: 2, Issue:6
| Identifying off-target effects and hidden phenotypes of drugs in human cells. |
| 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. |
| 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 |
| AID625005 | Binding constant for EGFR(L861Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID749514 | Inhibition of human BCR-ABL1 autophosphorylation expressed in mouse BA/F3 cells by ELISA | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| 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. |
| 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. |
| AID1904009 | Antiinvasive activity against human MNNG/HOS cells assessed as expression of FAK by measuring fluorescence at 0.4 uM upto 48 hrs by DAPI staining based immunofluorescence microscopic analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID625130 | Binding constant for FGFR4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425173 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID749508 | Intrinsic clearance in human liver microsomes by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1257224 | Inhibition of Trichomonas vaginalis adenosine-guanosine preferring ribohydrolase after 40 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target. |
| AID1519099 | Inhibition of recombinant human C-terminal His-tagged full length AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative t | | | |
| 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. |
| AID625057 | Binding constant for TYRO3 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. |
| AID374945 | Antiproliferative activity against human GIST882 cells after 96 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| 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. |
| AID624717 | Binding constant for JNK2 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. |
| AID625022 | Binding constant for MUSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384366 | Cytotoxicity against human NCI-N87 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID625004 | Binding constant for EGFR(L858R,T790M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512402 | Inhibition of human IKK-beta activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1412486 | Binding affinity to recombinant human CRK-2 nSH3 domain (1 to 304 residues) expressed in Escherichia coli assessed as inhibition of interaction with Abl by measuring Abl-mediated CRK-2 phosphorylation at Y221 residue at 1 uM after 10 to 30 mins by PAGE an | 2018 | MedChemComm, Mar-01, Volume: 9, Issue:3
| Structure-guided design of a potent peptide inhibitor targeting the interaction between CRK and ABL kinase. |
| AID1221976 | Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1338876 | Antiproliferative activity against human GIST882 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1876322 | Binding affinity to SARS-CoV-2 spike protein receptor-binding domain by biolayer interferometry (BLI) assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| 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. |
| AID1532208 | Growth inhibition of human SW620 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID724975 | Inhibition of human recombinant ABL1 M351T mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID624816 | Binding constant for HPK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1444955 | Antiproliferative activity against CHO cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID625013 | Binding constant for LCK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1387048 | 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 300 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. |
| AID1338964 | Induction of apoptosis in human GIST882 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID649627 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing assessed as cell viability at 1 uM 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1495941 | Antiproliferative activity against imatinib-resistant human GIST62 cells after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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. |
| AID414725 | Inhibition of PKA by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435679 | Binding constant for PIM3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID515832 | Inhibition of BCR-ABL1 autophosphorylation in human K562 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID435651 | Binding constant for DCAMKL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435553 | Binding constant for PRKCD kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| 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). |
| AID625046 | Binding constant for PIK3CB 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. |
| 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. |
| AID435664 | Binding constant for MYLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425191 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID624854 | Binding constant for FLT4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624834 | Binding constant for DAPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1519105 | Inhibition of DYRK3 (unknown origin) assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID1532229 | Growth inhibition of human 786-0 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID512763 | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1650168 | Inhibition of ABL1 in human HEK293T cells assessed as reduction in cell viability at 3 uM measured after 48 hrs relative to control | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
| Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization. |
| AID1323076 | Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by XTT assay | 2016 | European journal of medicinal chemistry, Oct-04, Volume: 121 | Synthesis and antiproliferative evaluation of novel 2-(4H-1,2,4-triazole-3-ylthio)acetamide derivatives as inducers of apoptosis in cancer cells. |
| AID343645 | Selectivity ratio of IC50 for Lck to IC50 for c-kit | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| AID428373 | Inhibition of human carbonic anhydrase 7 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID724666 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID407628 | Inhibition of Src by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID1860259 | Antiproliferative activity against human K-562R cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | | | |
| AID1444932 | Inhibition of PDGFRalpha (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID161424 | Inhibition of chimeric PDGF receptor with c-kit cytoplasmic domain phosphorylation in CHO cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| 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. |
| 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. |
| AID512419 | Inhibition of human FGFR3 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625107 | Binding constant for DMPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625108 | Binding constant for MKNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID310122 | Inhibition of P-glycoprotein by Hoechst assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID721750 | Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID591946 | Binding affinity to human Fgfr2 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID262016 | Antiproliferative activity against K562 cells | 2006 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
| Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors. |
| 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. |
| AID484385 | Colloidal aggregation in fed state simulated intestinal fluid assessed as colloid radius at 100 uM by dynamic light scattering assay in presence of 1% DMSO | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
| AID625074 | Binding constant for IKK-epsilon kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID374953 | Reduction in KIT mRNA expression in human GIST882 cells after 24 hrs | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID625077 | Binding constant for DAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383647 | Cytotoxicity against human COLO 824 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1193747 | Inhibition of Abl (unknown origin) using GGEAIYAAPFKK peptide as substrate by [gamma-33P]ATP assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
| New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID1300622 | Antiproliferative activity against human EM2 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| AID435778 | Binding constant for full-length ADCK4 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1705766 | Growth inhibition of human SF-268 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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. |
| 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. |
| AID295287 | Inhibition of human Abl kinase expressed in Sf9 cells | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. |
| AID435802 | Binding constant for KIT(V559D,V654A) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512387 | Inhibition of human PKCalpha activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625087 | Binding constant for MELK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1743569 | Antiproliferative activity against human SR cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID513130 | Inhibition of Abl kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| AID767331 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| 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. |
| AID1303954 | Cytotoxicity against human K562 cells | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
| 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. |
| AID498533 | Antiproliferative activity against human CML cells | 2009 | Nature chemical biology, Mar, Volume: 5, Issue:3
| A pulse at the heart of targeted therapy. |
| AID435940 | Binding constant for full-length TSSK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID625018 | Binding constant for YES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394577 | Tmax in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1526708 | Antifibrotic activity in CCl4-induced BALB/c mouse model of liver fibrosis assessed as liver fibrosis area at 50 mg/kg, po administered for 6 weeks by picro-sirius red staining based microscopy | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. |
| AID595768 | Inhibition of human recombinant c-Src by filter-binding assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study. |
| AID709993 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1286556 | Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID435411 | Binding constant for KIT(D816V) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512411 | Inhibition of human KDR activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625065 | Binding constant for CIT kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID678801 | TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells | 2004 | Molecular pharmacology, Jun, Volume: 65, Issue:6
| High-affinity interaction of tyrosine kinase inhibitors with the ABCG2 multidrug transporter. |
| AID1126688 | Inhibition of recombinant Abl kinase (unknown origin) expressed in Sf9 cells using GGEAIYAAPFKK as substrate in presence of [gamma33P]ATP | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| AID624829 | Binding constant for CDK8 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1584943 | Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID625071 | Binding constant for STK39 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435930 | Binding constant for PHKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625093 | Binding constant for TNIK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394582 | Antitumor activity against human EOL-1 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 50 mg/kg/day, ip | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| 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. |
| AID435834 | Binding constant for YANK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID739097 | Cytotoxicity against human K562 cells | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| AID1286585 | Inhibition of BCR/ABL in human KU812 cells assessed as downregulation of CrkL phosphorylation at T207 site at 1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID624899 | Binding constant for ROS1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1464304 | Inhibition of FLT1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID709991 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| AID1584974 | Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| AID436034 | Binding constant for PRKCH kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1221958 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1508968 | Inhibition of c-KIT 560 to 578 deletion/T670I double mutant in human GISTT1 cells assessed as reduction in STAT3 phosphorylation at 1 uM after 1 hr by Western blot analysis | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID512766 | Antiproliferative activity against human HL60 Bcr-abl negative cells assessed as cell viability after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1394584 | Toxicity in nu/nu mouse xenografted with human EOL-1 cells assessed as change in body weight at 25 to 100 mg/kg/day, ip | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID625059 | Binding constant for YSK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID1524390 | Binding affinity to p38alpha (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| AID624891 | Binding constant for JNK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID759133 | Growth inhibition of human MPNST cells at 0.001 to 10 uM after 72 hrs by SRB 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. |
| AID435281 | Binding constant for full-length CSNK1A1L | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532228 | Growth inhibition of human NCI/ADR-RES cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID625035 | Binding constant for PHKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624925 | Binding constant for RIPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID729374 | Inhibition of Abl1 kinase (unknown origin) using Tyr 6 peptide as substrate assessed as residual enzyme activity after every 10 secs measured for 10 mins by platform assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. |
| 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. |
| 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. |
| AID624956 | Binding constant for EPHB4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338920 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| 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. |
| 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. |
| AID1903974 | Inhibition of PDGFRalpha (unknown origin) by caliper mobility shift assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID1584977 | Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| AID1532192 | Growth inhibition of human RPMI8226 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID435800 | Binding constant for FYN kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID443957 | Cytotoxicity against Philadelphia chromosome positive human ALL3 cells by Alamar Blue fluorescent assay | 2009 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
| Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors. |
| AID270711 | Apoptotic activity against human K562 cell line at 10 uM after 24 hrs | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant. |
| 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. |
| AID435554 | Binding constant for PRKD3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624706 | Binding constant for MLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| 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. |
| AID435410 | Binding constant for KIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID759157 | Inhibition of KIT T670I mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB 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. |
| 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. |
| AID435515 | Binding constant for ABL1(Q252H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1750897 | Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay | | | |
| AID435777 | Binding constant for ABL2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID592099 | Binding affinity to human ABL2 phenylalanine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1368034 | Binding affinity to recombinant full length human N-terminal GST-tagged Syk-KD (356 to 635 residues) cytoplasmic domain expressed in baculovirus infected Sf9 insect cells using poly EY 4:1 as substrate | 2017 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 27, Issue:24
| Drug-target interactions that involve the replacement or displacement of magnesium ions. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID719842 | Displacement of (S)-N4-(4-(3-(2-((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanamido)butyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2 | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| 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. |
| 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. |
| AID1532201 | Growth inhibition of human NCI-H522 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID1444943 | Inhibition of TEL-fused PDGFRalpha T674I mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1394567 | AUC (0 to infinity) in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| AID749496 | AUC in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1303956 | Inhibition of CDK1/Cyclin B (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
| AID624902 | Binding constant for MEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | | | |
| 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. |
| AID1865197 | Antiinflammatory activity against Escherichia coli induced human THP-1 cells assessed as reduction in proinflammatory phenotype at 1 uM for 1 hr followed by Escherichia coli stimulation and measured upto 24 hrs by MALDI-TOF MS analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID624913 | Binding constant for TYK2(JH2domain-pseudokinase) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532220 | Growth inhibition of human SK-MEL-5 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1519107 | Inhibition of recombinant human N-terminal GST-tagged EPHA1 (569 to end residues) expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID625033 | Binding constant for PCTK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID414731 | Cytotoxicity against human A549 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID624751 | Binding constant for PIP5K1C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1776900 | Antiproliferative activity against human K562 cells by MTS assay | | | |
| AID1394574 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID512768 | Antiproliferative activity against human Jurkat Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625098 | Binding constant for IRAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID428460 | Inhibition of mouse carbonic anhydrase 15 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID724985 | Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID625856 | Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as nuclear import of full-length c-Abl at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case. |
| AID1584973 | Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624799 | Binding constant for TIE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1705745 | Growth inhibition of human HL-60(TB) cells measured after 48 hrs by SRB assay | | | |
| AID484275 | Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100 | 2010 | Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
| Colloid formation by drugs in simulated intestinal fluid. |
| AID625134 | Binding constant for PIP5K2C kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1563343 | Inhibition of c-KIT A829P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID255987 | Inhibitory concentration against IL-3 independent Ba/F3 Kit cell line with SCF (kit-ligand) | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. |
| AID512770 | Antiproliferative activity against human M07e Bcr-abl negative cells expressing stem cell factor assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624711 | Binding constant for STK35 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394564 | Antiproliferative activity against human NCI-H1703 cells after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| AID435276 | Binding constant for BMPR1A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1386088 | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| 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. |
| AID1316176 | Anti-remodeling activity in rat monocrotaline model of pulmonary arterial hypertension assessed as reduction in MCT-induced muscularization of small blood vessels in lung at 100 mg/kg, po administered twice daily for 7 days by histological analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
| AID624945 | Binding constant for BMPR1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625113 | Binding constant for MARK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID724649 | Inhibition of BCR-ABL T315I mutant-mediated CRK1 phosphorylation in mouse BA/F3 cells after 4 hrs by Western blotting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID1338830 | Inhibition of Tel-fused c-KIT (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| 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. |
| 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. |
| AID624783 | Binding constant for FGFR3(G697C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID407625 | Inhibition of KDR by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID1221972 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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). |
| AID1300623 | Antiproliferative activity against human KCL22 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| 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. |
| 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. |
| AID435786 | Binding constant for full-length CLK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1519106 | Inhibition of EGFR (unknown origin) assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID749504 | Drug metabolism in rat liver microsomes assessed as formation of N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-4-(1-piperazinylmethyl)benzamide by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1126679 | In vitro antiproliferative activity against human K562 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| AID1338945 | Cell cycle arrest in human GIST48B cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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 |
| 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. |
| AID435528 | Binding constant for IRAK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512579 | Inhibition of Bcr-Abl | 2005 | Chemistry & biology, Jun, Volume: 12, Issue:6
| Features of selective kinase inhibitors. |
| AID1657796 | Octanol/water partition coefficient, log D of the compound at pH 11 | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| 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. |
| AID1865186 | Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as reduction in IL-1beta level pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID414749 | Cytotoxicity against human WM266.4 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID624710 | Binding constant for SRMS kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1705802 | Growth inhibition of human T47D cells measured after 48 hrs by SRB assay | | | |
| 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. |
| 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. |
| AID435801 | Binding constant for full-length GSK3A | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1750900 | Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay | | | |
| AID1860257 | Antiproliferative activity against human Adriamycin-resistant K562/Adr cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | | | |
| 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. |
| 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). |
| 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. |
| AID512384 | Inhibition of human ROCK-2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID436043 | Binding constant for PKMYT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435823 | Binding constant for full-length PAK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1394563 | Antiproliferative activity against human EOL-1 cells after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID457324 | Antiproliferative activity against human K562 cells after 72 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity. |
| AID1495942 | Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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). |
| 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. |
| 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 |
| AID1495935 | Stabilization of 5'-FAM/3'-TAMRA labeled 5'-UTR BCL-2 G-quadruplex RNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID625102 | Binding constant for PRKD2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624892 | Binding constant for p38-delta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1508944 | Antiproliferative activity against human GISTT1 cells harboring c-KIT 560 to 578 deletion/T670I double mutant incubated for 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID1286569 | Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID407623 | Inhibition of c-Kit by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID1705761 | Growth inhibition of human HCT-116 cells measured after 48 hrs by SRB assay | | | |
| AID624842 | Binding constant for BMX kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624737 | Binding constant for EPHA5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID658702 | Inhibition of BCR-ABL-mediated ERK1 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity. |
| 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. |
| AID684227 | Cytotoxicity against human K562 cells after 72 hrs by MTS assay | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Design and synthesis of diarylamines and diarylethers as cytotoxic antitumor agents. |
| AID724974 | Inhibition of human recombinant ABL1 Y253F mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1743558 | Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID624811 | Binding constant for PAK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID760008 | Downregulation of Gli1 mRNA expression in human DaOY cells at 2.5 uM relative to DMSO-treated control | 2013 | ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
| Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere. |
| AID435189 | Binding constant for full-length PDPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624916 | Binding constant for ULK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID547621 | Cytotoxicity against BESM cells after 88 hrs by HTS assay | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID1508945 | Antiproliferative activity against human GIST5R cells harboring c-KIT 560 to 578 deletion/T670I double mutant incubated for 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID436016 | Binding constant for full-length ERK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624875 | Binding constant for PDGFRB 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. |
| AID624724 | Binding constant for TAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1915539 | Inhibition of Abl (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
| 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. |
| 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. |
| AID1817043 | Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay | | | |
| AID1584949 | Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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. |
| AID1278603 | Cytotoxicity against human 293T cells assessed as growth inhibition | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. |
| AID512377 | Inhibition of human CaMK4 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID1876259 | Antiviral activity against SARS-CoV infected in african green monkey Vero E6 cells measured after 50 hrs by cell-titre glo assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinase Inhibitors as Underexplored Antiviral Agents. |
| 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. |
| AID1454437 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL (83 to 534 residues) (unknown origin) expressed in Escherichia coli co-expressing Protein Tyrosine Phosphatase 1b at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
| |
| AID709994 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID436017 | Binding constant for ERK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1750902 | Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by after 48 hrs by MTT assay relative to control | | | |
| 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. |
| 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. |
| AID512398 | Inhibition of human MAPKAP-K2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1443989 | Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell plasma membrane vesicles assessed as reduction in ATP-dependent [3H]-taurocholate uptake in to vesicles preincubated for 10 mins followed by ATP addition measured after 10 to | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
| Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID512746 | Antiproliferative activity against mouse BA/F3 cells expressing NPM-abl assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1394606 | Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in ERK phosphorylation at T202/Y204 residues at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID512765 | Antiproliferative activity against mouse 32D Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624847 | Binding constant for CSNK1E kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID329192 | Inhibition of LPS-induced Btk autophosphorylation on Tyr223 in human U937 cells after 1 hr | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Aug-14, Volume: 104, Issue:33
| The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. |
| AID624764 | Binding constant for CLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512431 | Inhibition of human Bmx activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625124 | Binding constant for RET(V804M) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512421 | Inhibition of human EGFR activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1444956 | Antiproliferative activity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| 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. |
| AID624827 | Binding constant for CAMK2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID658703 | Inhibition of BCR-ABL-mediated ERK2 phosphorylation in human K562 cells at 40 uM after 6 hrs by phospho-flow cytometry | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity. |
| 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. |
| 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. |
| 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. |
| AID592167 | Binding affinity to human Mark2 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID1286565 | Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID719845 | Displacement of (S)-N4-(4-(3-(2-((4-carbamimidoylphenylamino)methyl)-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)propanamido)butyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2 | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| 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. |
| AID632955 | Inhibition of Abl using DAIpYAAPFAKKK phosphopeptide as substrate by MALDI-MS analysis | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors. |
| AID592018 | Binding affinity to human PDGFRalpha assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1849609 | Inhibition of VEGFR3 (unknown origin) at 10 uM by ELISA relative to control | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules. |
| 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). |
| AID625126 | Binding constant for TAOK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624862 | Binding constant for LYN kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383595 | Cytotoxicity against human BICR 78 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| 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. |
| AID1394575 | MRT (0 to t) in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| AID624872 | Binding constant for PAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425004 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1739057 | Binding affinity to human ABL2 | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
| AID414723 | Inhibition of PDGFRbeta by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID477295 | Octanol-water partition coefficient, log P of the compound | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
| QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations. |
| AID624705 | Binding constant for MYLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384692 | Cytotoxicity against human HT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625053 | Binding constant for PRKG2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1303955 | Cytotoxicity against human MCF7 cells | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| RETRACTED: Design, synthesis, structure-activity relationship and kinase inhibitory activity of substituted 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ones. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1904010 | Antimigratory activity against human MG-63 cells assessed as expression of FAK by measuring fluorescence at 0.4 uM upto 48 hrs by DAPI staining based immunofluorescence microscopic analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID1519143 | Inhibition of recombinant human N-terminal GST-tagged BRAF (416 to 766 residues) expressed in baculovirus infected Sf9 insect cells incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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). |
| AID488075 | Selectivity ratio of Ki for human recombinant ABL T315I mutant to Ki for human recombinant ABL using abtide peptide as substrate | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms. |
| AID624915 | Binding constant for PIP5K2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425118 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| 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. |
| AID1286541 | Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1338965 | Induction of apoptosis in human GIST882 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID436023 | Binding constant for MERTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435522 | Binding constant for CDK11 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1221957 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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 |
| AID591944 | Binding affinity to human Fes assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1886524 | Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| AID1705773 | Growth inhibition of human Malme-3M cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID1524393 | Binding affinity to LCK (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| 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. |
| AID435649 | Binding constant for CDC2L2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625133 | Binding constant for CDC2L2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID681215 | TP_TRANSPORTER: cell accumulation/inhibition study by Ko-143 efflux in BCRP-expressing HEK293 cells | 2004 | Blood, Nov-01, Volume: 104, Issue:9
| Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump. |
| 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. |
| AID624801 | Binding constant for MAP3K15 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1699970 | Antiproliferative activity against human K562/A02 cells overexpressing P-gp by MTT assay | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
| Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells. |
| 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. |
| AID383340 | Inhibition of DDR 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. |
| 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 | | | |
| 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. |
| AID1860253 | Inhibition of Bcr-Abl T315I mutant (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay | | | |
| AID624777 | Binding constant for DDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1743561 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID592111 | Binding affinity to human Jnk3 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID414724 | Inhibition of VEGFR2 by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID624708 | Binding constant for CDC2L1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1444944 | Antiproliferative activity against mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID271011 | Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| AID512378 | Inhibition of rat AMPK activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1612816 | Inhibition of Lyn B (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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 |
| 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). |
| 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. |
| AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | | | |
| AID592103 | Binding affinity to human CAMKK2 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID624868 | Binding constant for MST1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | | | |
| 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. |
| AID1386087 | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| AID624826 | Binding constant for BMPR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394572 | Apparent clearance in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| AID1444947 | Inhibition of TEL-fused cKIT V654A mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1278598 | Antiproliferative activity against human K562 cells assessed as inhibition of cell survival after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. |
| 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. |
| AID1904007 | Antimigratory activity against human MNNG/HOS cells assessed as expression of FAK by measuring fluorescence at 0.4 uM upto 48 hrs by DAPI staining based immunofluorescence microscopic analysis | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID435190 | Binding constant for full-length PIP5K1A | 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. |
| AID374944 | Stabilization of human G4-KIT2 DNA quadruplex assessed as melting temperature by FRET assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID1126703 | Inhibition of Bcr/Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| AID1705776 | Growth inhibition of human SK-MEL-2 cells measured after 48 hrs by SRB assay | | | |
| AID724980 | Inhibition of human recombinant ABL1 T315I mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID705601 | Clearance in human at 400 mg, qd | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
| 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. |
| 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. |
| AID624784 | Binding constant for INSR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624964 | Binding constant for DYRK1B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532236 | Growth inhibition of human PC3 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID428371 | Inhibition of human carbonic anhydrase 5B by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1705748 | Growth inhibition of human RPMI-8226 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID1464300 | Inhibition of CK1alpha1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID1705752 | Growth inhibition of human HOP-62 cells measured after 48 hrs by SRB assay | | | |
| 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 |
| AID512767 | Antiproliferative activity against human K562 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID625121 | Binding constant for RET 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. |
| AID435776 | Binding constant for ABL1(Y253F) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID625049 | Binding constant for PRKCH kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384637 | Cytotoxicity against human MT3 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1338859 | Inhibition of BCR/ABL p210 fusion protein Y253H mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID739102 | Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| 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. |
| AID724670 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID435796 | Binding constant for ERBB2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID705602 | Inhibition of CYP3A4 in human at 400 to 600 mg, qd by erythromycin breath test | 2012 | Journal of medicinal chemistry, Jun-14, Volume: 55, Issue:11
| Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks. |
| AID435531 | Binding constant for MKNK2 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. |
| AID1508900 | Inhibition of TEL fused c-KIT V654A/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID625079 | Binding constant for NEK6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435188 | Binding constant for PAK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1508943 | Antiproliferative activity against human GIST882 cells harboring c-KIT K642E mutant incubated for 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| 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. |
| 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. |
| AID94815 | Inhibitory activity against human K562 cells growth using MTT assay | 2003 | Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21
| Identification of novel inhibitors of BCR-ABL tyrosine kinase via virtual screening. |
| AID1563325 | Inhibition of c-KIT V559A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624791 | Binding constant for KIT(V559D) 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. |
| AID1444941 | Inhibition of TEL-fused cKIT T670I mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1832755 | Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| 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. |
| AID435149 | Binding constant for AMPK-alpha2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1394580 | Apparent clearance in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| 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. |
| AID414747 | Cytotoxicity against human Saos2 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID625063 | Binding constant for PLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1629529 | Inhibition of His-tagged cKIT (unknown origin) expressed in Sf9 cells using Poly(4:1 Glu, Tyr) peptide as substrate after 1 hr by ADP-glo kinase 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 |
| AID1358756 | Inhibition of MET (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| 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. |
| AID1286551 | Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID625103 | Binding constant for MST4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435146 | Binding constant for ABL1(H396P) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1705764 | Growth inhibition of human KM12 cells measured after 48 hrs by SRB assay | | | |
| AID1425047 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1444960 | Antiproliferative activity against human KU812 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1705768 | Growth inhibition of human SF-539 cells measured after 48 hrs by SRB assay | | | |
| AID1743568 | Antiproliferative activity against human SR cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID1519102 | Inhibition of recombinant human N-terminal GST-tagged full length BLK expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID1705798 | Growth inhibition of human MCF7 cells measured after 48 hrs by SRB assay | | | |
| AID1545701 | Selectivity index, ratio of GI50 for human BJ cells to GI50 for FIP1L1-PDGFRA positive human EOL-1 cells after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID414718 | Inhibition of human recombinant HDAC6 expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID436052 | Binding constant for full-length SNF1LK2 | 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). |
| AID435555 | Binding constant for PRKR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1464310 | Inhibition of PDK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID624871 | Binding constant for PAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624853 | Binding constant for FLT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1545697 | Cytotoxicity against human CEM cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| 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. |
| AID624815 | Binding constant for ERBB4 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. |
| AID1246519 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| AID1221962 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1532240 | Growth inhibition of human BT549 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1286567 | Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1832753 | Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| AID625086 | Binding constant for SLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338957 | Induction of apoptosis in human GISTT1 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1731536 | Permeability across basolateral to apical side in MDCK cells at 1 uM after 2 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Tetrahydroindazole inhibitors of CDK2/cyclin complexes. |
| AID624772 | Binding constant for AURKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1592403 | Cytotoxicity against human MCF10A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents. |
| 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. |
| 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. |
| AID1854085 | Inhibition of BCR-ABL phosphorylation in human K562 cells | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | The progress of small-molecules and degraders against BCR-ABL for the treatment of CML. |
| 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. |
| AID624841 | Binding constant for BLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721350 | Antitumor activity against mouse BA/F3 cells expressing BCR-ABL T315I mutant allografted in SCID mouse assessed as inhibition of tumor growth at 100 mg/kg/day, po qd for 14 days | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID624856 | Binding constant for GSK3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425031 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID1584945 | Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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 |
| 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. |
| AID512428 | Inhibition of human c-SRC activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID724675 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| 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. |
| AID1545698 | Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| 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. |
| 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. |
| AID1705792 | Growth inhibition of human RXF 393 cells measured after 48 hrs by SRB assay | | | |
| AID1865195 | Thermal stabilization of LPS-stimulated MKK4 in human THP-1 cells assessed as upregulation of protein at 5 uM pretreated for 1 hr followed by LPS-stimulation and measured after 15 min by western blot analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| AID625128 | Binding constant for CSNK1G1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID749495 | AUC (0 to 48 hrs) in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| AID672486 | Cytotoxicity against human BCR-ABL positive K562 cells after 48 to 72 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16
| Design, synthesis and biological evaluation of novel acrylamide analogues as inhibitors of BCR-ABL kinase. |
| AID1629558 | Inhibition of wild type cKIT autophosphorylation at Y703 in human GIST-T1 cells at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| AID1394576 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID435902 | Binding constant for BRAF(V600E) 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. |
| AID1731534 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in MDCK cells at 1 uM after 2 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Tetrahydroindazole inhibitors of CDK2/cyclin complexes. |
| AID625095 | Binding constant for SIK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1422100 | Induction of apoptosis in human K562R cells assessed as early apoptotic cells at 10 uM by Annexin V staining-based flow cytometry (Rvb = 8.51%) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| 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. |
| 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. |
| 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. |
| AID435192 | Binding constant for ROS1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1739058 | Binding affinity to human FLT3 | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
| 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. |
| AID1584941 | Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID1532216 | Growth inhibition of human MALME-3M cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID624954 | Binding constant for EPHB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435527 | Binding constant for FGFR3(G697C) 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. |
| AID435326 | Binding constant for TYRO3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1422096 | Inhibition of BCR-ABL in imatinib-sensitive human K562 cells assessed as decrease in CrKL phosphorylation at 1 uM by immuno blot analysis | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| 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. |
| AID625062 | Binding constant for MAP3K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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). |
| AID1426831 | Toxicity in wild-type zebrafish AB assessed as mortality at 0.8 ug/ml | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | | | |
| 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. |
| AID1563330 | Inhibition of c-KIT V654A/V559D double mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624999 | Binding constant for EGFR(G719S) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624725 | Binding constant for NEK11 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512395 | Inhibition of human MKK6 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1338872 | Antiproliferative activity against human K562 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID455986 | Permeability across human Caco-2 cells | 2009 | Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
| Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain. |
| AID749509 | Half life in rat liver microsomes by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1519113 | Inhibition of recombinant human N-terminal GST-tagged full length p38alpha expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID512417 | Inhibition of human Flt-3 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625048 | Binding constant for PRKCD kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338865 | Inhibition of Tel-fused c-KIT V559D/V654A double mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID435443 | Binding constant for TXK 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. |
| 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. |
| 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. |
| 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. |
| AID1286550 | Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| 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. |
| AID512432 | Inhibition of human Axl activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1126704 | Inhibition of tyrosine phosphorylation of protein with molecular weight between 40 and 60 kDa in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| AID1519104 | Inhibition of CK1alpha1 (unknown origin) assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID711409 | Unbound Cmax in human plasma at 400 mg, po | 2012 | ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
| Minimizing Drug Exposure in the CNS while Maintaining Good Oral Absorption. |
| AID588975 | Substrates of transporters of clinical importance in the absorption and disposition of drugs, BCRP | 2010 | Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
| Membrane transporters in drug development. |
| AID435170 | Binding constant for MYO3A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435929 | Binding constant for PAK4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1278599 | Antiproliferative activity against human HL60 cells assessed as inhibition of cell survival after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. |
| AID1519108 | Inhibition of recombinant human N-terminal GST-tagged FLT1 (784 to end residues) expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID435171 | Binding constant for NEK9 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1221963 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID435438 | Binding constant for full-length p38-gamma | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID512397 | Inhibition of human MEK1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1673957 | Inhibition of BCR-ABL T315I mutant (unknown origin) | 2020 | Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
| Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations. |
| AID435646 | Binding constant for BLK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID370598 | Inhibition of human recombinant c-Src by filter-binding assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
| Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. |
| AID435430 | Binding constant for INSRR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID721742 | Ratio of Cmax unbound to IC50 for human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID749506 | Metabolic stability in rat liver microsomes assessed as compound remaining by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| 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. |
| AID515829 | Inhibition of human PDGFRalpha autophosphorylation in human A31 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| 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. |
| AID512404 | Inhibition of human GSK3-beta activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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). |
| AID1873208 | Inhibition of ABCG2 (unknown origin) expressed in human MCF7/MX cells mediated mitoxantrone efflux assessed as intracellular mitoxantrone level and measured after 30 mins by FACSflow cytometry analysis | 2022 | European journal of medicinal chemistry, Jul-05, Volume: 237 | Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators. |
| AID679104 | TP_TRANSPORTER: transepithelial transport in MDR1-transfected MDCKII cells | 2004 | Blood, Dec-01, Volume: 104, Issue:12
| Active transport of imatinib into and out of cells: implications for drug resistance. |
| AID1519116 | Inhibition of recombinant human N-terminal GST-tagged SGK1 (60 to end residues) expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID625089 | Binding constant for AAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624709 | Binding constant for MYLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435524 | Binding constant for full-length CSNK1D | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1563322 | Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay | | | |
| 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. |
| AID1860254 | Selectivity ratio of IC50 for inhibition of Bcr-Abl T315I mutant (unknown origin) to IC50 for inhibition of wild type Bcr-Abl (unknown origin) | | | |
| 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. |
| 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. |
| 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. |
| AID1338911 | Inhibition of c-KIT autophosphorylation at Y703 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1444957 | Antiproliferative activity against human GIST882 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1244538 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents. |
| 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. |
| AID435791 | Binding constant for EGFR(E746-A750del) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID710011 | Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | | | |
| AID1532190 | Growth inhibition of human K562 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID649633 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability at 0.3 nM after 72 hrs by luciferase assay in presence of 1 uM of N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin- | 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. |
| AID1422106 | Induction of ROS production in human K562R cells at 10 uM by DCFH-DA dye based spectrofluorometric method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID428459 | Inhibition of human carbonic anhydrase 14 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID624937 | Binding constant for FLT3(ITD) 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. |
| AID428372 | Inhibition of human carbonic anhydrase 6 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID291753 | Cytotoxicity against K562 cells by MTT assay | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties. |
| AID457323 | Antiproliferative activity against HUVEC after 72 hrs by resazurin dye reduction assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity. |
| AID1322166 | Inhibition of BCR-ABL signaling pathway in human K562 cells assessed as suppression of STAT5 phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand. |
| AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | | | |
| AID1338850 | Inhibition of Tel-fused BLK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID414726 | Cytotoxicity against human K562 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| 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. |
| AID1508946 | Antiproliferative activity against human GIST48B cells incubated for 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID370599 | Inhibition of human recombinant Abl by filter-binding assay | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
| Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. |
| AID1300624 | Antiproliferative activity against human JURL-MK1 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| 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. |
| AID435396 | Binding constant for CHEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1425205 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1776903 | Antiproliferative activity against human L02 cells by MTS assay | | | |
| 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. |
| AID435900 | Binding constant for AKT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1444442 | Binding affinity to c-KIT G-quadruplex DNA in human K562 cells assessed as reduction in c-KIT mRNA level at 0.5 uM after 48 hrs by RT-PCR analysis | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Synthesis and evaluation of 7-substituted-5,6-dihydrobenzo[c]acridine derivatives as new c-KIT promoter G-quadruplex binding ligands. |
| 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. |
| 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. |
| AID540211 | Fraction unbound in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| 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. |
| AID270709 | Apoptotic activity against human K562 cell line at 10 uM after 8 hrs | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant. |
| 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. |
| 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. |
| 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. |
| AID435311 | Binding constant for HCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338882 | Antiproliferative activity against human Rec1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID719848 | Inhibition of human alpha thrombin using Boc-Val-Pro-Arg-AMC as substrate after 2 hrs by fluorometric analysis | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID624744 | Binding constant for ZAP70 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1338881 | Antiproliferative activity against human HL60 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID591945 | Binding affinity to human Fgfr1 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID291752 | Inhibition of c-Abl | 2007 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 17, Issue:15
| Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties. |
| AID435148 | Binding constant for AMPK-alpha1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435403 | Binding constant for EPHB1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1623597 | Antiproliferative activity against human K562 cells after 72 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Discovery of potent, orally bioavailable ERK1/2 inhibitors with isoindolin-1-one structure by structure-based drug design. |
| 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. |
| AID625052 | Binding constant for PRKG1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1246532 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as cell viability at 250 nM incubated for 1 day (Rvb = 73.9%) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID1338880 | Antiproliferative activity against human U937 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID1338925 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6 phosphorylation at S235/236 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID458670 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 14 uM 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. |
| AID1532234 | Growth inhibition of human TK10 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID317425 | Inhibition of recombinant human c-Src | 2008 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
| Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents. |
| AID1394566 | AUC (0 to t) in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID624911 | Binding constant for TXK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435905 | Binding constant for full-length CSNK1G3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624977 | Binding constant for OSR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1443995 | Hepatotoxicity in human assessed as drug-induced liver injury | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
| Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID435413 | Binding constant for MLCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436004 | Binding constant for ACVR2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624881 | Binding constant for PKAC-alpha kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624740 | Binding constant for LRRK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1254379 | Inhibition of c-Kit (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
| Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
| 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. |
| AID1563324 | Inhibition of c-KIT T670I mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1584939 | Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID254663 | Inhibitory concentration against Src kinase | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
| Designed multiple ligands. An emerging drug discovery paradigm. |
| AID512375 | Inhibition of human SAPK2b activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1705753 | Growth inhibition of human HOP-92 cells measured after 48 hrs by SRB assay | | | |
| AID1257226 | Inhibition of Trichomonas vaginalis uridine ribohydrolase after 40 mins | 2015 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
| Adenosine/guanosine preferring nucleoside ribohydrolase is a distinct, druggable antitrichomonal target. |
| 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. |
| AID1705749 | Growth inhibition of human SR cells measured after 48 hrs by SRB assay | | | |
| AID624845 | Binding constant for CDK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705765 | Growth inhibition of human SW-620 cells measured after 48 hrs by SRB assay | | | |
| AID624867 | Binding constant for MLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515831 | Inhibition of autophosphorylation of BCR-ABL1 expressed in Ba/F cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID435645 | Binding constant for ACVRL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624818 | Binding constant for ULK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624904 | Binding constant for NEK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383927 | Cytotoxicity against human SEG1 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID1705746 | Growth inhibition of human K562 cells measured after 48 hrs by SRB assay | | | |
| AID1611406 | Inhibition of BCR/Abl F317L mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID1611411 | Inhibition of BCR/Abl P230 mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| 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. |
| 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. |
| AID1707040 | Induction of autophagy in human PANC-1 cells assessed as increase in LC3 expression at 25 uM measured after 24 hrs by muse cell analyzer based fluorescence assay relative to control | 2021 | European journal of medicinal chemistry, Feb-15, Volume: 212 | New derivatives of 4'-phenyl-2,2':6',2″-terpyridine as promising anticancer agents. |
| 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. |
| AID1743559 | Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID625112 | Binding constant for YANK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425161 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID512370 | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID624756 | Binding constant for MAP4K4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID387175 | Inhibition of p38 | 2008 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
| Discovery of amido-benzisoxazoles as potent c-Kit inhibitors. |
| 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. |
| AID625136 | Binding constant for YSK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512406 | Inhibition of human CK2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID435320 | Binding constant for PRKCE kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | | | |
| AID1262853 | Inhibition of Abl T315I mutant (unknown origin) after 30 mins by phosphocellulose paper disk assay using 0.1 mM EAIYAAPFAKKK peptide substrate | 2015 | Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
| Development of Alkyne-Containing Pyrazolopyrimidines To Overcome Drug Resistance of Bcr-Abl Kinase. |
| AID1611408 | Inhibition of BCR/Abl M351T mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| 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. |
| 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. |
| AID1508896 | Inhibition of TEL fused c-KIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| 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. |
| AID436045 | Binding constant for PRKD1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID592109 | Binding affinity to human Jnk1 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID624935 | Binding constant for FLT3(D835H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1221968 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1286555 | Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1221973 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1495072 | Cytotoxicity in drug sensitive human K562 cells assessed as reduction cell viability incubated for 48 hrs by XTT assay | 2018 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 28, Issue:10
| Modular synthesis of new C-aryl-nucleosides and their anti-CML activity. |
| AID435402 | Binding constant for EGFR(G719S) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383084 | Inhibition of Bcr-abl 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. |
| AID1532232 | Growth inhibition of human RXF393 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1193746 | Inhibition of CDK2/Cyclin E (unknown origin) using histone H1 as substrate by [gamma-33P]ATP assay | 2015 | Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
| New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity. |
| AID624821 | Binding constant for YANK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394596 | Inhibition of PDGFRalpha autophosphorylation at Y754 residue in human EOL-1 cells at 100 nM after 2 hrs by Western blot method | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| AID1629561 | Inhibition of cKIT T670I mutant autophosphorylation at Y703 in human GIST-5R cells at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| 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. |
| AID435289 | Binding constant for ERK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1322175 | Inhibition of BCR-ABL in signaling pathway human K562 cells assessed as suppression of CrkL phosphorylation at 100 uM after 8 hrs in presence of MeBS by Western blot analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
| Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand. |
| 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. |
| AID595769 | Inhibition of human recombinant c-Abl by filter-binding assay | 2011 | Journal of medicinal chemistry, Apr-28, Volume: 54, Issue:8
| Design, synthesis, biological activity, and ADME properties of pyrazolo[3,4-d]pyrimidines active in hypoxic human leukemia cells: a lead optimization study. |
| AID435409 | Binding constant for full-length JNK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338864 | Inhibition of Tel-fused c-KIT V559D mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID254706 | Inhibitory concentration against v-Abl tyrosine kinase | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
| Designed multiple ligands. An emerging drug discovery paradigm. |
| AID1532204 | Growth inhibition of human HCT116 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID435526 | Binding constant for FGFR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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). |
| AID435907 | Binding constant for EGFR(L861Q) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1338878 | Antiproliferative activity against human MV4-11 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID512762 | Antiproliferative activity against mouse BA/F3 cells transfected with p210 Bcr-abl assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435534 | Binding constant for NEK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532193 | Growth inhibition of human SR cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1394579 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1519103 | Inhibition of recombinant human N-terminal GST-tagged full length CDK2/CyclinA1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | | | |
| AID1563329 | Inhibition of c-KIT L576P mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1705775 | Growth inhibition of human MDA-MB-435 cells measured after 48 hrs by SRB assay | | | |
| AID435799 | Binding constant for FLT3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1495932 | Stabilization of 5'-FAM/3'-TAMRA labeled c-KIT1 G-quadruplex DNA (unknown origin) assessed as change in melting temperature at 0.5 uM by FRET assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID435692 | Binding constant for STK16 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1507440 | Antiproliferative activity against human A549 cells after 48 hrs by MTT assay | 2017 | European journal of medicinal chemistry, Aug-18, Volume: 136 | Design, synthesis and evaluation of azaacridine derivatives as dual-target EGFR and Src kinase inhibitors for antitumor treatment. |
| AID1705750 | Growth inhibition of human A549 cells measured after 48 hrs by SRB assay | | | |
| AID1495943 | Antiproliferative activity against human HGC27 cells after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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. |
| AID1750901 | Reversal of P-gp-mediated multidrug resistance in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity at 5 uM by measuring adriamycin IC50 after 48 hrs by MTT assay | | | |
| AID343640 | Inhibition of p38alpha | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| 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. |
| AID624771 | Binding constant for TLK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID343646 | Inhibition of Abl | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| AID624762 | Binding constant for DLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | | | |
| AID749500 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| AID1338916 | Inhibition of c-KIT autophosphorylation at Y823 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID625125 | Binding constant for CLK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1592402 | Cytotoxicity against human MDA-MB-453 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents. |
| AID407624 | Inhibition of SCF-induced phosphorylation of c-Kit in MO7e cells by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID435286 | Binding constant for EPHA7 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| 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. |
| AID1545695 | Cytotoxicity against FIP1L1-PDGFRA positive human EOL-1 cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID436013 | Binding constant for DMPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625143 | Binding constant for CAMKK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1386090 | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| AID624702 | Binding constant for BRSK1 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. |
| 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. |
| AID435282 | Binding constant for full-length CSNK1G2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1424893 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624846 | Binding constant for CSNK1A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625092 | Binding constant for NDR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435533 | Binding constant for NEK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1495944 | Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| AID435556 | Binding constant for RAF1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624776 | Binding constant for PCTK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624850 | Binding constant for DDR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID625084 | Binding constant for HUNK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425015 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID435182 | Binding constant for full-length PKAC-beta | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1424934 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| 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. |
| AID414750 | Cytotoxicity against human EOL-1 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID724978 | Inhibition of human recombinant ABL1 Q252H mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID271009 | Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| AID724674 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1221970 | Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID624828 | Binding constant for CDK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338919 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID625061 | Binding constant for MAP4K5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1699971 | Resistance index, ratio of of IC50 for human K562/A02 cells to IC50 for human K562 cells | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
| Discovery of thiosemicarbazone-containing compounds with potent anti-proliferation activity against drug-resistant K562/A02 cells. |
| 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. |
| AID624721 | Binding constant for MEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705778 | Growth inhibition of human SK-MEL-5 cells measured after 48 hrs by SRB assay | | | |
| AID161421 | Inhibition of chimeric PDGF receptor with CSF-1R cytoplasmic domain phosphorylation in CHO cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID512422 | Inhibition of human ZAP-70 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1657805 | Permeability across apical to basolateral side in human Caco2 cells measured up to 2 hrs by LC-MS/MS analysis or scintillation counting method | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID591854 | Inhibition of human wild type ABL1 assessed as [gamma33P]ATP incorporation into poly-Ala-Glu-Lys-Tyr after 60 mins by microplate scintillation counting | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID512379 | Inhibition of human aurora-A activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID310121 | Inhibition of P-glycoprotein expressed in MDCK-MDR1 cells by calcein AM assay | 2007 | Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
| New functional assay of P-glycoprotein activity using Hoechst 33342. |
| AID1386091 | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| 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. |
| AID515840 | Toxicity in chronic CML patient assessed as cytogenetic response | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID1394565 | Antiproliferative activity against human NCI-H1703 cells after 72 hrs in presence of PDGF-AA by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1338883 | Antiproliferative activity against CHO cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1817039 | Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay | | | |
| AID435323 | Binding constant for RET(M918T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID658699 | Inhibition of BCR-ABL-mediated STAT5 phosphorylation in human K562 cells after 6 hrs by phospho-flow cytometry | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
| Small molecule STAT5-SH2 domain inhibitors exhibit potent antileukemia activity. |
| 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. |
| 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. |
| AID624865 | Binding constant for MAP3K3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625100 | Binding constant for NLK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624831 | Binding constant for CHEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1126682 | In vitro antiproliferative activity against human CCRF-CEM cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| 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. |
| AID1563374 | Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| 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. |
| AID1246525 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for human THP1 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| AID1886527 | Cytotoxicity against human iPSC-CM cells assessed as reduction in contractile alterations or amplitude in cell voltage by VF2.1.Cl dye based assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| 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. |
| 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. |
| AID436042 | Binding constant for full-length PHKG1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1567153 | Antiproliferative activity against human BCR/ABL positive K562 cells assessed as growth inhibition measured after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of novel Bcr-Abl |
| 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. |
| AID1865184 | Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as reduction in TNFalpha level pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| AID1903967 | Antiproliferative activity against human MG-63 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| 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. |
| AID435164 | Binding constant for IGF1R kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1394569 | Half life in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| AID1563375 | Inhibition of c-KIT K642E mutant in human GIST882 cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID624763 | Binding constant for RIPK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1731533 | Apparent permeability across basolateral to apical side in MDCK cells at 1 uM after 2 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Tetrahydroindazole inhibitors of CDK2/cyclin complexes. |
| 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. |
| AID435159 | Binding constant for EPHB3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624934 | Binding constant for FLT3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1532226 | Growth inhibition of human OVCAR5 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID451987 | Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
| Novel lead for potent inhibitors of breast cancer resistance protein (BCRP). |
| 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. |
| AID759135 | Growth inhibition of human LMS676 cells at 0.001 to 10 uM after 72 hrs by SRB 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. |
| AID1338937 | Cell cycle arrest in human KU812 cells assessed as accumulation at G0/G1 phase at 1 uM after 12 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1585048 | Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID624897 | Binding constant for RAF1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID512433 | Inhibition of mouse Abl activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1464307 | Inhibition of MSK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID1705757 | Growth inhibition of human NCI-H460 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID625110 | Binding constant for TRPM6 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1743556 | Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID1705762 | Growth inhibition of human HCT-15 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID1267742 | Induction of apoptosis in human K562 cells after 48 hrs by annexinV and propidium iodide staining based flow cytometry | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation. |
| AID435654 | Binding constant for full-length ERK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624852 | Binding constant for FES kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435675 | Binding constant for KIT(V559D,T670I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435545 | Binding constant for NEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435321 | Binding constant for PRKCQ kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624745 | Binding constant for PKN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624804 | Binding constant for ERBB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID625037 | Binding constant for PIK3CA(C420R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338961 | Induction of apoptosis in human GISTT1 cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID374948 | Antiproliferative activity against human MCF7 cells after 96 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID1865213 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as upregulation of MMP9 expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID435789 | Binding constant for full-length CSNK2A2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID407645 | Inhibition of Abl by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID1464305 | Inhibition of GRK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID435312 | Binding constant for MET kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532235 | Growth inhibition of human UO31 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID612169 | Antiproliferative activity against human K562 cells after 48 hrs by MTT assay | 2011 | Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
| Exploration of acridine scaffold as a potentially interesting scaffold for discovering novel multi-target VEGFR-2 and Src kinase inhibitors. |
| 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. |
| AID624798 | Binding constant for LKB1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1544925 | Antiproliferative activity against human K562 cells assessed as inhibition of cell viability incubated for 72 hrs by real time live-cell imaging technique | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Design and synthesis of novel 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4-thiadiazol- 2-yl)urea derivatives with potent anti-CML activity throughout PI3K/AKT signaling pathway. |
| 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. |
| AID1532213 | Growth inhibition of human SNB75 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1860252 | Inhibition of wild type Bcr-Abl (unknown origin) incubated for 1 hr in presence of ATP by ADP-Glo kinase assay | | | |
| 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. |
| AID428374 | Inhibition of human carbonic anhydrase 9 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID1526713 | Effect on plasma AST level in CCl4-induced BALB/c mouse model of liver fibrosis at 50 mg/kg, po administered for 6 weeks | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. |
| 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. |
| AID1532215 | Growth inhibition of human LOXIMVI cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID435393 | Binding constant for CAMK1D kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1338915 | Inhibition of c-KIT autophosphorylation at Y719 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| 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. |
| AID625139 | Binding constant for SNARK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID592102 | Binding affinity to human CAMKK1 isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID624817 | Binding constant for MYO3B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1277145 | Inhibition of CDK2/Cyclin E (unknown origin) expressed in baculoviral infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| AID625106 | Binding constant for MARK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532210 | Growth inhibition of human SF295 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID624851 | Binding constant for ERBB3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID624942 | Binding constant for DRAK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435904 | Binding constant for full-length CSK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624969 | Binding constant for ROCK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID771263 | Cytotoxicity against human K562 cells after 72 hrs by calcein-AM assay | 2013 | European journal of medicinal chemistry, Oct, Volume: 68 | Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines. |
| AID1657802 | Stability in human liver microsomes at 1 uM incubated prior to NADPH addition by LC-MS/MS analysis relative to hepatic blood flow | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID624728 | Binding constant for NIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1316177 | Anti-remodeling activity in rat monocrotaline model of pulmonary arterial hypertension assessed as reduction in MCT-induced muscularization of small blood vessels in lung at 25 mg/kg, po administered twice daily for 7 days by histological analysis | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
| 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. |
| AID1300641 | Antitumor activity against human K562 cells over expressing eIF4E xenografted in NOD-SCID mouse assessed as tumor growth inhibition at 200 mg/kg, po qd administered through oral gavage for 14 days relative to control | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| AID463627 | Inhibition of Abl T315I mutant | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID625101 | Binding constant for TAOK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID270712 | Apoptotic activity against human K562 cell line at 10 uM after 48 hrs | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant. |
| 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. |
| 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. |
| AID1286586 | Inhibition of BCR/ABL in human MEG01 cells assessed as downregulation of CrkL phosphorylation at T207 site at 1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| AID435442 | Binding constant for SYK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1247413 | Anticancer activity against human HCT116 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Recent developments regarding the use of thieno[2,3-d]pyrimidin-4-one derivatives in medicinal chemistry, with a focus on their synthesis and anticancer properties. |
| 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. |
| AID1705770 | Growth inhibition of human SNB-75 cells measured after 48 hrs by SRB assay | | | |
| AID1394554 | Cytotoxicity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID625020 | Binding constant for ITK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1126680 | In vitro antiproliferative activity against human BV173 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| AID435154 | Binding constant for DDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624886 | Binding constant for ERK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1731532 | Apparent permeability across apical to basolateral side in MDCK cells at 1 uM after 2 hrs by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Mar-15, Volume: 214 | Tetrahydroindazole inhibitors of CDK2/cyclin complexes. |
| 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. |
| AID271008 | Inhibition of wild type NPM/ALK kinase activity in BaF3 cells by radioenzymatic assay | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and homology modeling. |
| AID624757 | Binding constant for PKMYT1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625854 | Inhibition of 14-3-3sigma in human Ba/F3 cells expressing wild type Bcr-Abl construct assessed as release of full-length c-Abl from cytoplasmic complex with 14-3-3sigma at 1 uM after 24 hrs by immunoprecipitation/immunoblot technique | 2011 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
| Computational techniques are valuable tools for the discovery of protein-protein interaction inhibitors: the 14-3-3σ case. |
| 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. |
| AID1246524 | Therapeutic index, ratio of CC50 for HEK293 cells to IC50 for imatinib resistant human IR-K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| AID624774 | Binding constant for QSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID767455 | Inhibition of PDGFRA (unknown origin) | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
| Selectivity data: assessment, predictions, concordance, and implications. |
| AID759163 | Inhibition of cSRC T338M mutant (unknown origin)-mediated phosphorylation of biotinylated poly-Glu-Tyr at 100 uM 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. |
| AID435557 | Binding constant for RIPK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512420 | Inhibition of FGFR-1 kinase activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435156 | Binding constant for EGFR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624959 | Binding constant for MAP4K2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625117 | Binding constant for PAK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID428369 | Inhibition of human carbonic anhydrase 4 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| 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. |
| AID435897 | Binding constant for ABL1(T315I) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1358764 | Antiproliferative activity against human WM793B cells after 72 hrs by MTT assay | | | |
| AID1849695 | Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules. |
| AID256551 | Inhibitory concentration against c-Kit D816V type expressed in recombinant baculovirus | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
| Molecular modeling of wild-type and D816V c-Kit inhibition based on ATP-competitive binding of ellipticine derivatives to tyrosine kinases. |
| AID1358747 | Inhibition of c-KIT (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID1584950 | Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID435794 | Binding constant for EPHA3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1286564 | Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1916784 | Inhibition of EGFR (unknown origin) incubated for 1 hr in presence of ATP by Kinase-Glo Plus luminescence kinase assay | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery. |
| AID1865215 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as suppression of CD11c expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs by flow cytometric analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID625096 | Binding constant for STK36 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435324 | Binding constant for full-length RIOK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624833 | Binding constant for CSNK1G2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435408 | Binding constant for INSR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435284 | Binding constant for DCAMKL1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1629566 | Inhibition of cKIT T670I mutant in human GIST-5R cells assessed as downregulation of ERK phosphorylation at T202/204 at 1 uM after 1 hr by Western blot analysis | 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 |
| AID624765 | Binding constant for TRKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435688 | Binding constant for full-length PCTK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1221969 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID624752 | Binding constant for SNRK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID351489 | Inhibition of recombinant Syk | 2009 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
| Pharmacophore modeling study based on known spleen tyrosine kinase inhibitors together with virtual screening for identifying novel inhibitors. |
| AID435429 | Binding constant for FLT1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435559 | Binding constant for SNARK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID461859 | Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTT assay | 2010 | Bioorganic & medicinal chemistry, Mar-01, Volume: 18, Issue:5
| Design, synthesis, and biological evaluation of novel water-soluble triptolide derivatives: Antineoplastic activity against imatinib-resistant CML cells bearing T315I mutant Bcr-Abl. |
| AID512372 | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624908 | Binding constant for TEC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID724664 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID592170 | Binding affinity to human PDGFRalpha cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1386051 | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| 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. |
| 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. |
| AID1612811 | Inhibition of BRK (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| 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. |
| 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. |
| AID1849610 | In vivo inhibition of VEGFR2 in Swiss albino mouse implanted with mouse Ehrlich cells incubated for 24 hrs by immunohistochemical staining based analysis relative to control | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules. |
| 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. |
| AID512392 | Inhibition of human p70S6K activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID625075 | Binding constant for INSRR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID512773 | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | | | |
| AID343644 | Inhibition of Lck | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| AID414721 | Inhibition of wild-type c-Abl by liquid scintillation counting | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID435196 | Binding constant for full-length SRPK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID624788 | Binding constant for KIT(D816H) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
| A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
| AID512772 | Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing FIt3-ITD kinase assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID1338829 | Inhibition of human BCR/ABL p210 fusion protein expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1629562 | Inhibition of cKIT T670I mutant autophosphorylation at Y719 in human GIST-5R cells at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| AID407646 | Inhibition of PDGFRalpha by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID374942 | Stabilization of synthetic duplex DNA assessed as melting temperature by FRET assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| 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. |
| 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. |
| 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. |
| AID1508901 | Inhibition of TEL fused c-KIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID624968 | Binding constant for DRAK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1886530 | Inhibition of ABL1 (unknown origin) | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| AID1464301 | Inhibition of DYRK3 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID1705758 | Growth inhibition of human NCI-H522 cells measured after 48 hrs by SRB assay | | | |
| AID592019 | Binding affinity to human PDGFRbeta assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID624914 | Binding constant for WEE1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625041 | Binding constant for PIK3CA(H1047L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID591947 | Binding affinity to human Fgfr3 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID625044 | Binding constant for PIK3CA(M1043I) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1358758 | Inhibition of PCK-beta2 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID1338875 | Antiproliferative activity against human GISTT1 cells measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID624859 | Binding constant for JAK1(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1286554 | Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1394605 | Inhibition of PDGFRalpha in human EOL-1 cells assessed as decrease in STAT5 phosphorylation at Y694 residue at 1 uM after 2 hrs in presence of PDGF-AA by Western blot analysis | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1532194 | Growth inhibition of human A549 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID436049 | Binding constant for PTK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1563336 | Inhibition of c-KIT D816H mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1567152 | Inhibition of BCR/ABL T315I mutant (unknown origin) measured after 60 mins in presence of ATP by ADP-Glo kinase assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of novel Bcr-Abl |
| AID592107 | Binding affinity to human DDR2 phenylalanine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID724665 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| 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. |
| 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 | | | |
| 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. |
| AID1865201 | Inhibition of P38 MAPK pathway in Escherichia coli-stimulated human THP-1 cells assessed as reduction in IL-6 expression at 5 uM pretreated for 1 hr followed by Escherichia coli stimulation and measured up to 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| AID1386086 | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| 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. |
| AID624769 | Binding constant for AURKC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1464312 | Inhibition of SGK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID1278600 | Antiproliferative activity against human KG1a cells assessed as inhibition of cell survival after 72 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
| Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib. |
| AID435644 | Binding constant for ABL1(E255K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624938 | Binding constant for FLT3(K663Q) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID739095 | Inhibition of Bcr-Abl T315I mutant (unknown origin) phosphorylation transfected in mouse Ba/F3 cells after 1 hr by Western blot analysis | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| AID1519101 | Inhibition of recombinant human N-terminal GST-tagged full length Aurora A expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID739098 | Cytotoxicity against mouse BA/F3 cells after 48 hrs by XTT assay | 2013 | Journal of medicinal chemistry, May-09, Volume: 56, Issue:9
| Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant. |
| AID1563334 | Inhibition of c-KIT S709F mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID724669 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| AID512745 | Antiproliferative activity against mouse BA/F3 cells expressing Tel-SH3-SH2-KD assessed as cell viability at 5 to 10 uM after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435821 | Binding constant for GAK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532214 | Growth inhibition of human U251 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID649625 | Cytotoxicity against human TF1 cells expressing c-KIT mutation assessed as cell viability | 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. |
| AID435414 | Binding constant for MLK3 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624759 | Binding constant for PFCDPK1(P.falciparum) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625008 | Binding constant for EPHA1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435523 | Binding constant for CIT kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624972 | Binding constant for MTOR kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1338862 | Inhibition of BCR/ABL p210 fusion protein F317L mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1338923 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in ERK1/2 phosphorylation at T202/Y204 in human GIST882 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID767333 | Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID407626 | Inhibition of p38 by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID624832 | Binding constant for IKK-alpha 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. |
| AID463658 | Inhibition of HDAC | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| 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. |
| AID1705797 | Growth inhibition of human DU-145 cells measured after 48 hrs by SRB assay | | | |
| AID624755 | Binding constant for ZAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512771 | Antiproliferative activity against human M07e Bcr-abl negative cells expressing granulocyte-macrophage colony stimulating factor assessed as proliferation after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624861 | Binding constant for LIMK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID414742 | Cytotoxicity against human PC3 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID343643 | Selectivity ratio of IC50 for KDR to IC50 for c-kit | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| 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. |
| AID624873 | Binding constant for PAK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID436054 | Binding constant for TLK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1612810 | Inhibition of ABL1 (unknown origin) at 0.5 uM preincubated for 10 mins followed by substrate addition and measured after 1 hr by ADP-Glo luminescence assay relative to control | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID625140 | Binding constant for MARK4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624929 | Binding constant for BRSK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1584951 | Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1508905 | Inhibition of TEL fused c-KIT D820E mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID624978 | Binding constant for ABL1(E255K)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID625006 | Binding constant for EGFR(S752-I759del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424999 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID435397 | Binding constant for CSNK1G1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435166 | Binding constant for full-length JNK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1526716 | Antifibrotic activity in bleomycin-induced C57BL/6 mouse model of lung fibrosis assessed as reduction in Ashcroft score at 50 mg/kg, ip administered on day 7 to 27 and measured on day 28 by H and E staining based microscopy | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. |
| AID1221978 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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). |
| AID1629559 | Inhibition of wild type cKIT autophosphorylation at Y719 in human GIST-T1 cells at 1 uM after 1 hr by Western blot analysis | 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 |
| AID435676 | Binding constant for LCK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID343658 | Inhibition of stem cell factor-induced histamine release in C57BL/6 mouse model of mast cell activation and systemic anaphylaxis at 100 mg/kg, po after 15 mins by ELISA | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
| Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases. |
| 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. |
| 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). |
| 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. |
| 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. |
| AID625023 | Binding constant for HIPK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1338854 | Inhibition of Tel-fused LCK (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID749510 | Intrinsic clearance in rat liver microsomes by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID1705747 | Growth inhibition of human MOLT-4 cells measured after 48 hrs by SRB assay | | | |
| AID1532218 | Growth inhibition of human SK-MEL-2 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1705787 | Growth inhibition of human SK-OV-3 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID721749 | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1532227 | Growth inhibition of human OVCAR8 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1860262 | Antiproliferative activity against mouse BaF3 cells expressing wild type Bcr-Abl assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay | | | |
| AID383092 | Inhibition of PDGFRalpha 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. |
| AID1817044 | Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay | | | |
| AID592168 | Binding affinity to human Mst2 lysine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID436012 | Binding constant for full-length CSNK2A1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID384860 | Cytotoxicity against human JHH4 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID512415 | Inhibition of HER-1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID1444948 | Inhibition of TEL-fused cKIT V559D/V654A double mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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). |
| AID1563340 | Inhibition of c-KIT D820Y mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| 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. |
| AID1358762 | Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay | | | |
| AID1425186 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID414730 | Cytotoxicity against human H460 cells after 72 hrs by alamar-blue cell viability assay | 2009 | Journal of medicinal chemistry, Apr-23, Volume: 52, Issue:8
| Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. |
| AID625114 | Binding constant for GSK3A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1657804 | Equilibrium thermodynamic aqueous solubility of the compound in pH 6.8 buffer incubated for 24 hrs by UV-spectroscopy based shake flask method | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID1444949 | Inhibition of TEL-fused cKIT V559D/T670I double mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1519111 | Inhibition of recombinant human N-terminal GST-tagged full length MSK1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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. |
| AID435287 | Binding constant for EPHA8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436025 | Binding constant for NDR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID592101 | Binding affinity to human BRAF V600E mutant isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID592106 | Binding affinity to human EPHA8 tyrosine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID1174980 | Inhibition of BCR/ABL (unknown origin) after 40 mins by ADP-Glo kinase assay | 2014 | Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
| Discovery of novel Bcr-Abl inhibitors targeting myristoyl pocket and ATP site. |
| AID1776901 | Antiproliferative activity against imatinib-resistant human K562R cells by MTS assay | | | |
| AID1221966 | Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID1240469 | Inhibition of Bcr-Abl T315I mutant (unknown origin) using Tyr2 peptide substrate after 2 hrs by FRET-based Z'-lyte assay | 2015 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 25, Issue:17
| Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant. |
| AID625009 | Binding constant for EPHA3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID547804 | Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells | 2010 | Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
| Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. |
| AID435925 | Binding constant for PCTK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID721740 | Selectivity ratio of IC50 for human OCT2-mediated ASP+ uptake expressed in HEK293 cells to IC50 for human MATE1-mediated ASP+ uptake expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID592166 | Binding affinity to human LYN tyrosine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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). |
| AID512434 | Inhibition of human Abl activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID749499 | Volume of distribution at steady state in Sprague-Dawley rat at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| AID1426832 | Toxicity in wild-type zebrafish AB assessed as mortality at 4 ug/ml | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| 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. |
| AID1338917 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in AKT phosphorylation at S473 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID625097 | Binding constant for TNNI3K kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1358751 | Inhibition of FGFR1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| AID709935 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1657806 | Efflux ratio of permeability in human Caco2 cells measured up to 2 hrs by LC-MS/MS analysis or scintillation counting method | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID1338968 | Induction of apoptosis in human GIST48B cells assessed as cleavage of PARP at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1267741 | Antiproliferative activity against human K562 cells after 48 hrs by trypan blue dye exclusion assay | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Novel iodoacetamido benzoheterocyclic derivatives with potent antileukemic activity are inhibitors of STAT5 phosphorylation. |
| 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. |
| AID624993 | Binding constant for ABL2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID709938 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| 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. |
| 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. |
| AID435560 | Binding constant for SNF1LK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625054 | Binding constant for MST2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID759158 | Inhibition of KIT in human GISTT1 cells assessed as growth inhibition after 72 hrs by SRB 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. |
| AID1246520 | Cytotoxicity against human THP1 cells assessed as reduction in cell viability | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID1611409 | Inhibition of BCR/Abl H396P mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CellTiter-Glo luminescent cell viability assay | 2019 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
| Structure-based analysis and biological characterization of imatinib derivatives reveal insights towards the inhibition of wild-type BCR-ABL and its mutants. |
| AID435395 | Binding constant for CDC2L1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1244537 | Inhibition of Bcr-Abl (unknown origin) after 60 mins by luminescent kinase assay | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and biological evaluation of novel aromatic-heterocyclic biphenyls as potent anti-leukemia agents. |
| AID435201 | Binding constant for TRKA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID435896 | Binding constant for AAK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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). |
| AID435911 | Binding constant for MEK6 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID590029 | Antiproliferative activity against human K562 cells | 2011 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
| Hybrid compounds as new Bcr/Abl inhibitors. |
| AID1629571 | Induction of apoptosis in human GIST5R cells assessed as increase in cleaved PARP levels after at 1 uM 24 hrs by Western blot analysis | 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 |
| AID624909 | Binding constant for TGFBR2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID701071 | Inhibition of SYK | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Discovery and development of spleen tyrosine kinase (SYK) inhibitors. |
| 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. |
| AID719839 | Displacement of (S)-N4-(2-(4-(4-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenylcarbamoyl)benzyl)piperazin-1-yl)ethyl)-N1-(15-oxo-19-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10-trioxa-14-azanonadecyl)-2-(4-(3-(trifluoromethyl | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID435157 | Binding constant for EGFR(G719C) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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). |
| 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. |
| AID512423 | Inhibition of human Syk activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624998 | Binding constant for EGFR(G719C) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID749494 | AUC (0 to 48 hrs) in Sprague-Dawley rat assessed as N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-4-(1-piperazinylmethyl)benzamide at 1 mg/kg, iv administered as bolus dose | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| 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. |
| AID1532197 | Growth inhibition of human NCI-H226 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1254380 | Inhibition of Abl (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
| Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
| 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. |
| AID1286584 | Inhibition of BCR/ABL in human K562 cells assessed as downregulation of CrkL phosphorylation at T207 site at 1 uM after 1 hr by immunoblotting method | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| 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. |
| AID1567156 | Antiproliferative activity against human K562R cells expressing BCR/ABL T315I mutant assessed as growth inhibition measured after 48 hrs by MTT assay | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | Discovery of novel Bcr-Abl |
| 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. |
| AID719846 | Inhibition of human recombinant NQO2-mediated mitomycin C metabolism using NADH as cosubstrate incubated for 5 mins prior to NADH addition measured after 30 mins by spectrophotometric analysis | 2012 | Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
| Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). |
| AID435401 | Binding constant for full-length DRAK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID436047 | Binding constant for full-length PRKX | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1508903 | Inhibition of TEL fused c-KIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID624879 | Binding constant for PIK3CG kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID383579 | Cytotoxicity against human A549 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1508907 | Inhibition of TEL fused c-KIT A829P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID512408 | Inhibition of human CDK1/cyclinB activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID436053 | Binding constant for full-length STK33 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625068 | Binding constant for NEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1876318 | Antiviral activity against MERS-CoV infected in 1 hr pretreated african green monkey Vero E6 cells measured after 48 hrs by fluorescence based plate reader method | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| AID624835 | Binding constant for ERN1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625040 | Binding constant for PIK3CA(E545K) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721748 | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID593557 | Binding affinity to human active site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. |
| 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. |
| 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. |
| AID435191 | Binding constant for full-length RIOK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID435936 | Binding constant for full-length SRPK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512761 | Cytotoxic activity against mouse 32D Bcr-abl negative cells | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID512369 | Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID512407 | Inhibition of human CHK2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1394573 | Cmax in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID512427 | Inhibition of human Fes activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID436008 | Binding constant for full-length BTK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID512426 | Inhibition of human Lck activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1444942 | Inhibition of TEL-fused PDGFRalpha (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1202712 | Inhibition of DDR1b (unknown origin) assessed as reduction in collagen-induced DDR1b activation | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
| 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. |
| AID435938 | Binding constant for TGFBR1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID624754 | Binding constant for NEK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721752 | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1286553 | Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID1202713 | Inhibition of DDR2 (unknown origin) assessed as reduction in collagen-induced DDR2 activation | 2015 | Journal of medicinal chemistry, Apr-23, Volume: 58, Issue:8
| Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. |
| AID1743564 | Antiproliferative activity against human MOLT-4 cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| AID435519 | Binding constant for AURKB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID384641 | Cytotoxicity against human NCI-H1435 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID364887 | Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay | 2008 | Bioorganic & medicinal chemistry, Sep-01, Volume: 16, Issue:17
| Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2). |
| 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. |
| AID625069 | Binding constant for TLK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID592105 | Binding affinity to human DDR1 phenylalanine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID513131 | Inhibition of c-Kit | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| 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. |
| AID1338912 | Inhibition of c-KIT autophosphorylation at Y719 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1443980 | Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch | 2010 | Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
| Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. |
| AID1464303 | Inhibition of EPHA1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID749503 | Drug metabolism in human liver microsomes assessed as formation of N-[4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]-4-(1-piperazinylmethyl)benzamide by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| AID749502 | Drug metabolism in rat liver microsomes assessed as formation of 4-(hydroxymethyl)-N-(4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl)benzamide by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID435327 | Binding constant for VEGFR2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1221961 | Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| AID458672 | Inhibition of CSF1-stimulated human FMS autophosphorylation expressed in growth factor dependent mouse FDC-P1 cells assessed as phosphorylated receptor level at 0.14 uM 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. |
| AID649622 | Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability at 15 uM 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. |
| 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). |
| 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. |
| AID624966 | Binding constant for DCAMKL1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1394570 | Tmax in Sprague-Dawley rat at 1 mg/kg, iv | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID1444438 | Induction of apoptosis in human K562 cells assessed as late apoptotic cells at 0.5 uM after 48 hrs by flow cytometric method (Rvb = 0.1 %) | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Synthesis and evaluation of 7-substituted-5,6-dihydrobenzo[c]acridine derivatives as new c-KIT promoter G-quadruplex binding ligands. |
| AID624844 | Binding constant for CDK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1286560 | Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID624838 | Binding constant for ACVR2A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID709992 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1903971 | Antiproliferative activity against human SAOS-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID624761 | Binding constant for CDC2L5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID729372 | Inhibition of Abl1 kinase (unknown origin) | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7
| Rapid discovery of a novel series of Abl kinase inhibitors by application of an integrated microfluidic synthesis and screening platform. |
| AID624703 | Binding constant for MAPKAPK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624946 | Binding constant for BRAF kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID1283297 | Resistance index, ratio IC50 for human K562/G cells to IC50 for human K562 cells | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
| AID624878 | Binding constant for PIM1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| 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. |
| AID1526711 | Effect on plasma ALT level in CCl4-induced BALB/c mouse model of liver fibrosis at 50 mg/kg, po administered for 6 weeks | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. |
| AID1519100 | Inhibition of recombinant human N-terminal GST-tagged ASK1 (649 to 946 residues) expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID624849 | Binding constant for CSNK2A2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721364 | Antitumor activity against human K562 cells xenografted in mouse assessed as induction of tumor stasis at 50 mg/kg, po qd for 6 days | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID435694 | Binding constant for TNK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625138 | Binding constant for STK33 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1283286 | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay | 2016 | Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
| Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A. |
| AID1563331 | Inhibition of c-KIT V654A mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1705780 | Growth inhibition of human UACC-62 cells measured after 48 hrs by SRB assay | | | |
| AID436022 | Binding constant for full-length MEK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1254381 | Inhibition of PDGFR (unknown origin) | 2015 | Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
| Synthesis and biological evaluation of di-aryl urea derivatives as c-Kit inhibitors. |
| AID1338860 | Inhibition of BCR/ABL p210 fusion protein H369P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1705789 | Growth inhibition of human A498 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID1705801 | Growth inhibition of human BT-549 cells measured after 48 hrs by SRB assay | | | |
| AID1338984 | Anticancer activity against human K562 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 100 mg/kg administered daily via oral gavage measured 28 days post compound treatment relative to vehicle-treated control | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID624997 | Binding constant for EGFR(E746-A750del) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515839 | Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3 | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID436007 | Binding constant for AXL kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625080 | Binding constant for EIF2AK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID435167 | Binding constant for KIT(V559D) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1714636 | Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 24 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 26, Issue:23
| Design, synthesis, and biological activity of 4-(imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-phenylbenzamide derivatives as BCR-ABL kinase inhibitors. |
| AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | | | |
| AID593558 | Binding affinity to human remote site of N-terminal hexahistidine-tagged ABL2 expressed in Trichoplusia ni infected Sf9 cells by isothermal titration calorimetric assay | 2011 | Journal of medicinal chemistry, Apr-14, Volume: 54, Issue:7
| Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. |
| AID1532238 | Growth inhibition of human MCF7 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID436009 | Binding constant for full-length CAMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| 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. |
| 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. |
| AID1286568 | Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| 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. |
| 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. |
| AID513124 | Inhibition of Syk kinase | 2006 | Nature chemical biology, Jul, Volume: 2, Issue:7
| Rational design of inhibitors that bind to inactive kinase conformations. |
| 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. |
| AID435322 | Binding constant for PRKG2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID161395 | Inhibition of wild type Platelet-derived growth factor receptor beta phosphorylation in CHO cells | 2002 | Journal of medicinal chemistry, Aug-15, Volume: 45, Issue:17
| Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. |
| AID512400 | Inhibition of human JNK2alpha2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID512424 | Inhibition of human Ros activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| 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. |
| AID1221960 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| AID407627 | Inhibition of Lck by TR-FRET assay | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
| Discovery of aryl aminoquinazoline pyridones as potent, selective, and orally efficacious inhibitors of receptor tyrosine kinase c-Kit. |
| AID709937 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1584940 | Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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 |
| AID767329 | Cytotoxicity against human HL7702 cells assessed as growth inhibition at 50 uM after 48 hrs by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry, Sep-15, Volume: 21, Issue:18
| Exploration of N-(2-aminoethyl)piperidine-4-carboxamide as a potential scaffold for development of VEGFR-2, ERK-2 and Abl-1 multikinase inhibitor. |
| AID1338935 | Cell cycle arrest in human K562 cells assessed as accumulation at G0/G1 phase at 1 uM after 24 hrs by propidium iodide/RNase staining based flow cytometry | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID383339 | Inhibition of DDR | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID1338833 | Inhibition of recombinant C-terminal polyhistidine-tagged human c-KIT expressed in mammalian expression system using Tyr 06 peptide as substrate measured after 1hr by FRET based Z'Lyte assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID624800 | Binding constant for IGF1R kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1865218 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as suppression of CD54 expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs by flow cytometric analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| AID624712 | Binding constant for DYRK1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424988 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID1532198 | Growth inhibition of human NCI-H23 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID1532200 | Growth inhibition of human NCI-H460 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID435406 | Binding constant for FLT3(D835H) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID1358743 | Inhibition of CAMK1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID1338949 | Induction of apoptosis in human K562 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID1743566 | Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition at 10 uM measured after 48 hrs by SRB assay relative to control | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID749512 | Inhibition of human BCR-ABL1 (unknown origin) expressed in mouse 32D cells | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| AID624877 | Binding constant for PIK3C2B kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID384193 | Cytotoxicity against human NCI-H2444 cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| AID435151 | Binding constant for CAMK1G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID724673 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID1705779 | Growth inhibition of human UACC-257 cells measured after 48 hrs by SRB 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. |
| AID724676 | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID709997 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1464302 | Inhibition of EGFR (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID624989 | Binding constant for ABL1(T315I)-phosphorylated kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1865219 | Inhibition of cell adhesion in human Escherichia coli stimulated-THP-1 cells by crystal violet staining based assay | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| 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. |
| AID1524398 | Binding affinity to DDR1 (unknown origin) | 2019 | Journal of medicinal chemistry, 03-28, Volume: 62, Issue:6
| Electrostatic Complementarity as a Fast and Effective Tool to Optimize Binding and Selectivity of Protein-Ligand Complexes. |
| AID512381 | Inhibition of human Tie2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1584971 | Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID540212 | Mean residence time in human after iv administration | 2008 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
| Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. |
| 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. |
| AID624936 | Binding constant for FLT3(D835Y) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1865217 | Inhibition of human Escherichia coli stimulated monocyte activation in human THP-1 cells assessed as suppression of CD49a expression level at 5 uM pretreated for 1 hr and measured up to 24 hrs by flow cytometric analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| AID1221977 | Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| AID1387056 | 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 300 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. |
| AID1338869 | Inhibition of Tel-fused c-KIT L576P mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID512391 | Inhibition of human PAK2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID624890 | Binding constant for p38-beta kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID624907 | Binding constant for SYK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1272050 | Cytotoxicity against human K562 cells after 48 hrs by MTT assay | 2016 | Bioorganic & medicinal chemistry, Jan-15, Volume: 24, Issue:2
| Design, synthesis and evaluation of acridine derivatives as multi-target Src and MEK kinase inhibitors for anti-tumor treatment. |
| AID435278 | Binding constant for full-length CDK7 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID624906 | Binding constant for S6K1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435199 | Binding constant for TLK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1629560 | Inhibition of wild type cKIT autophosphorylation at Y823 in human GIST-T1 cells at 1 uM after 1 hr by Western blot analysis | 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 |
| 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. |
| AID624715 | Binding constant for ERK8 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. |
| 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 |
| 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. |
| AID488074 | Selectivity ratio of Ki for human recombinant ABL T315I mutant to Ki for human recombinant ABL using ATP as substrate | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
| Dual Src and Abl inhibitors target wild type Abl and the AblT315I Imatinib-resistant mutant with different mechanisms. |
| AID624885 | Binding constant for ERK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID592112 | Binding affinity to human Kit cysteine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID1519109 | Inhibition of GRK1 (unknown origin) assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| 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). |
| 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. |
| AID625083 | Binding constant for LATS2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624787 | Binding constant for KIT(A829P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624839 | Binding constant for AKT2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID425652 | Total body clearance in human | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
| Physicochemical determinants of human renal clearance. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID435656 | Binding constant for FGFR4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1705796 | Growth inhibition of human PC-3 cells measured after 48 hrs by SRB assay | | | |
| AID435514 | Binding constant for ABL1(M351T) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532211 | Growth inhibition of human SF539 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID624803 | Binding constant for CHEK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1424971 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| 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. |
| AID592015 | Binding affinity to human Flt4 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| AID625036 | Binding constant for PIK3CA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1316153 | Inhibition of PDGFR-beta driven proliferation of rat A10 cells after 68 hrs in presence of rat recombinant PDGF-BB by cell titer-glo luminescence assay | 2016 | Journal of medicinal chemistry, 09-08, Volume: 59, Issue:17
| Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension. |
| AID624773 | Binding constant for AMPK-alpha1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624912 | Binding constant for TYK2(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425017 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1545700 | Cytotoxicity against human BJ cells assessed as growth inhibition after 72 hrs by resazurin dye-based fluorescence analysis | 2019 | European journal of medicinal chemistry, Nov-15, Volume: 182 | Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity. |
| AID1563337 | Inhibition of c-KIT D816V mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID1532225 | Growth inhibition of human OVCAR4 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1705799 | Growth inhibition of human MDA-MB-231 cells measured after 48 hrs by SRB assay | | | |
| AID749505 | Metabolic stability in human liver microsomes assessed as compound remaining by capillary-HPLC/MS analysis | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| 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. |
| 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. |
| AID624824 | Binding constant for PIP5K1A kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435203 | Binding constant for TTK kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID515830 | Inhibition of human KIT autophosphorylation in human GIST882 cells by ELISA | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID1584972 | Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| 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 |
| AID726978 | Antiproliferative activity against human MCF7 cells | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| New PAH derivatives functionalized by cyclic nitrone framework: synthetic design, anti-proliferative activity and interaction with DNA. |
| AID1338955 | Induction of apoptosis in human MEG01 cells assessed as increase in cleaved caspase-3 level at 1 uM by Western blot analysis | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID463626 | Inhibition of Abl Y253F mutant | 2010 | Journal of medicinal chemistry, Feb-25, Volume: 53, Issue:4
| Selectively nonselective kinase inhibition: striking the right balance. |
| AID1860255 | Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay | | | |
| AID1705754 | Growth inhibition of human NCI-H226 cells measured after 48 hrs by SRB assay | | | |
| AID1444933 | Inhibition of VEGFR2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1338868 | Inhibition of Tel-fused c-KIT V654A mutant (unknown origin) expressed in BAF3 cells assessed as growth inhibition measured after 72 hrs by CellTiter-Glo or CCK8 assay | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| 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. |
| AID374947 | Antiproliferative activity against human HT-29 cells after 96 hrs by SRB assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| AID625142 | Binding constant for TSSK1B 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. |
| 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. |
| AID624933 | Binding constant for PLK3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1464297 | Inhibition of BLK (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID625021 | Binding constant for LIMK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515841 | Toxicity in chronic CML patient assessed as maximum tolerated dose | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID1532212 | Growth inhibition of human SNB19 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID624750 | Binding constant for PRP4 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1425201 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID435329 | Binding constant for YSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1886532 | Vasculo-toxicity in human HMVEC cells assessed as reduction in vascular structure integrity by measuring AUC measured after 6 hrs by calcein AM dye based fluorescence assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| 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. |
| AID1758303 | Inhibition of NFkappaB transcriptional activity in LPS-stimulated mouse RAW264.7 cells | 2021 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 41 | Design and development of 1,3,5-triazine derivatives as protective agent against spinal cord injury in rat via inhibition of NF-ĸB. |
| AID624790 | Binding constant for KIT(L576P) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID721340 | Antitumor activity against mouse BA/F3 cells expressing BCR-ABL T315I mutant allografted in SCID mouse assessed as increased survival at 100 mg/kg/day, po qd for 10 days | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| AID436011 | Binding constant for full-length CLK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1286543 | Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| 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. |
| AID1358754 | Inhibition of HER2 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| AID1464311 | Inhibition of PRKG1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID428370 | Inhibition of human carbonic anhydrase 5A by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| 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. |
| AID436010 | Binding constant for full-length CDK5 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1444935 | Inhibition of cKIT (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition in presence of ATP by mobility shift assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID709995 | Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant. |
| AID1585047 | Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID383341 | Inhibition of DDR1 | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| AID625109 | Binding constant for BIKE kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1876319 | Antiviral activity against SARS-CoV in 2 hrs pretreated african green monkey Vero E6 cells measured after 48 hrs by CellTireGlo luminescent cell viability assay | 2022 | Journal of medicinal chemistry, 01-27, Volume: 65, Issue:2
| Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy. |
| AID1612826 | Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay | 2019 | European journal of medicinal chemistry, Feb-01, Volume: 163 | The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. |
| AID512410 | Inhibition of human c-kit activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID435294 | Binding constant for full-length LIMK2 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID435784 | Binding constant for CAMK2G kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID1422099 | Induction of apoptosis in human K562R cells assessed as viable cells at 10 uM by Annexin V staining-based flow cytometry (Rvb = 81.13%) | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | | | |
| 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. |
| AID435782 | Binding constant for BRSK1 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435412 | Binding constant for MAP3K5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625016 | Binding constant for SRC kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID435525 | Binding constant for EGFR(L858R) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435806 | Binding constant for MAPKAPK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624864 | Binding constant for CTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435926 | Binding constant for PDGFRB kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID262702 | Inhibition of c-kit receptor phosphorylation in M07e cell | 2006 | Journal of medicinal chemistry, Apr-06, Volume: 49, Issue:7
| Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. |
| AID1532219 | Growth inhibition of human SK-MEL-28 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID625055 | Binding constant for MST1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1509031 | Antitumor activity against human GIST5R cells xenografted in nude mouse assessed as tumor weight at 100 mg/kg, po administered as single dose via gavage for 28 days (Rvb = 0.59g) | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID1365579 | Inhibition of ABL in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTT assay | 2017 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 27, Issue:21
| Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors. |
| AID624948 | Binding constant for CSK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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). |
| AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | | | |
| AID624796 | Binding constant for MET(Y1235D) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID435908 | Binding constant for EPHA2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435935 | Binding constant for RIPK2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1584946 | Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| AID1657803 | Aqueous solubility of the compound in pH 6.8 buffer incubated for 24 hrs under shaking condition by UV-HPLC analysis | 2020 | Journal of medicinal chemistry, 07-09, Volume: 63, Issue:13
| Phosphine Oxides from a Medicinal Chemist's Perspective: Physicochemical and |
| AID1886533 | Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| 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. |
| AID624749 | Binding constant for CASK 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. |
| 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. |
| AID435691 | Binding constant for SgK085 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. |
| AID625003 | Binding constant for EGFR(L858R) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1904063 | Toxicity in BALB/c nude mouse xenograted with human MNNG/HOS cells assessed as kidney lesion at 30 mg/kg/day, po for 14 days by hematoxylin and eosin staining method | 2022 | Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
| Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. |
| AID724979 | Inhibition of human recombinant ABL1 E255K mutant expressed in insect cells after 30 mins by FRET assay | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. |
| 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. |
| 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. |
| AID435903 | Binding constant for CDK8 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID383393 | Cytotoxicity against human 639-V cells assessed as fraction of viable cells after 72 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Dec-11, Volume: 104, Issue:50
| Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID624746 | Binding constant for WEE2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624742 | Binding constant for NEK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512430 | Inhibition of human BTK activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID436021 | Binding constant for LATS2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435659 | Binding constant for full-length MARK3 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID632954 | Inhibition of Abl at 10 uM using DAIpYAAPFAKKK phosphopeptide as substrate by MALDI-MS analysis | 2011 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 21, Issue:23
| Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors. |
| 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. |
| 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. |
| 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. |
| AID512405 | Inhibition of human c-RAF activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1394558 | Inhibition of TEL-fused PDGFRbeta (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| AID749515 | Inhibition of human BCR-ABL1 expressed in mouse BA/F3 cells assessed as cell growth inhibition by ATP-depletion assay | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11
| The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588. |
| AID592108 | Binding affinity to human GAK isoleucine residue assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| AID1563326 | Inhibition of c-KIT V559D mutant in mouse BAF3(transformed) cells assessed as growth inhibition after 72 hrs by CCK8 assay | | | |
| AID721746 | Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis | 2013 | Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3
| Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. |
| AID1915540 | Inhibition of Abl T3151 (unknown origin) | 2021 | European journal of medicinal chemistry, Jan-01, Volume: 209 | Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors. |
| AID1277147 | Cytotoxicity against human MCF7 cells assessed as cell viability after 72 hrs by fluorescence microplate reader method | 2016 | European journal of medicinal chemistry, Jan-27, Volume: 108 | Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors. |
| 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. |
| AID512399 | Inhibition of human MAPK1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1286563 | Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay | 2016 | Journal of medicinal chemistry, Mar-10, Volume: 59, Issue:5
| Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le |
| AID624785 | Binding constant for JAK3(JH1domain-catalytic) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID759155 | Growth inhibition of human GIST48B cells after 72 hrs by SRB 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. |
| AID435552 | Binding constant for PIK3CA(E545K) kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID625032 | Binding constant for TRKB kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435161 | Binding constant for FES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1126681 | In vitro antiproliferative activity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| AID1705784 | Growth inhibition of human OVCAR-5 cells measured after 48 hrs by SRB assay | | | |
| AID1865198 | Inhibition of P38 MAPK pathway in Escherichia coli-stimulated human THP-1 cells assessed as reduction in TNFalpha expression at 5 uM pretreated for 1 hr followed by Escherichia coli stimulation and measured up to 24 hrs by ELISA analysis | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18
| A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia. |
| 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. |
| AID435328 | Binding constant for YES kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| AID625088 | Binding constant for ARK5 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID624950 | Binding constant for DMPK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1246533 | Cytotoxicity against imatinib resistant human IR-K562 cells assessed as cell viability at 250 nM incubated for 3 days (Rvb = 79.5%) | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| 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. |
| AID1519112 | Inhibition of recombinant human N-terminal GST-tagged full length NEK1 expressed in baculovirus infected Sf9 insect cells assessed as enzyme activity incubated for 15 mins by [gamma-33]ATP based scintillation counting method relative to control | | | |
| AID515836 | Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID1394557 | AUC (0 to t) in Sprague-Dawley rat at 10 mg/kg, po | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Discovery of 4-((N-(2-(dimethylamino)ethyl)acrylamido)methyl)-N-(4-methyl-3-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)benzamide (CHMFL-PDGFR-159) as a highly selective type II PDGFRα kinase inhibitor for PDGFRα driving chronic eosinophilic leukemia. |
| 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. |
| 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. |
| AID435520 | Binding constant for CAMK2A kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1443991 | Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay | 2014 | Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
| Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump. |
| AID435394 | Binding constant for CAMK2B kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1444958 | Antiproliferative activity against human GIST48B cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| AID1464299 | Inhibition of CDK2/Cyclin A (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| 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. |
| AID435803 | Binding constant for full-length LIMK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1886531 | Inhibition of ABL1 T315I mutant (unknown origin) | 2022 | Journal of medicinal chemistry, 08-25, Volume: 65, Issue:16
| Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety. |
| AID270710 | Apoptotic activity against human K562 cell line at 10 uM after 16 hrs | 2006 | Journal of medicinal chemistry, Sep-21, Volume: 49, Issue:19
| Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1358752 | Inhibition of FLT1 (unknown origin) at 10 uM by [33P]-ATP radiometric assay | | | |
| 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. |
| 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. |
| AID436048 | Binding constant for full-length PTK2B | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| 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. |
| AID435687 | Binding constant for PAK7/PAK5 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID435440 | Binding constant for PIM2 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1464293 | Inhibition of ALK1 (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID624719 | Binding constant for GRK7 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID624919 | Binding constant for AURKA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1221959 | Efflux ratio of permeability from apical to basolateral over basolateral to apical side of MDCK cells expressing MDR1 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| AID1737438 | Induction of cell death in human K562 cells assessed by cell viability at 1 uM measured after 72 hrs by Propidium iodide stain based FACS assay | 2020 | European journal of medicinal chemistry, Jun-01, Volume: 195 | Identification and development of non-cytotoxic cell death modulators: Impact of sartans and derivatives on PPARγ activation and on growth of imatinib-resistant chronic myelogenous leukemia cells. |
| AID624807 | Binding constant for TNK2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID672485 | Inhibition of recombinant BCR-ABL using EAIYAAPFAKKK as substrate after 15 mins by [gamma-32P] isotope incorporation assay | 2012 | Bioorganic & medicinal chemistry letters, Aug-15, Volume: 22, Issue:16
| Design, synthesis and biological evaluation of novel acrylamide analogues as inhibitors of BCR-ABL kinase. |
| 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. |
| AID435181 | Binding constant for full-length p38-alpha | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID254715 | Inhibitory concentration against protein kinase C alpha | 2005 | Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21
| Designed multiple ligands. An emerging drug discovery paradigm. |
| AID624883 | Binding constant for PRKCI kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID515835 | Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| 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. |
| AID668693 | Cytotoxicity against human K562 cells after 24 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry letters, Jul-01, Volume: 22, Issue:13
| Thieno[3,2-c]pyran-4-one based novel small molecules: their synthesis, crystal structure analysis and in vitro evaluation as potential anticancer agents. |
| 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. |
| AID624949 | Binding constant for CSNK1G3 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID512396 | Inhibition of mouse MKK4 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID1425041 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID624848 | Binding constant for CSNK2A1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1519117 | Inhibition of CDK2 (unknown origin) incubated for 40 mins by ADP-glo assay | | | |
| AID1221956 | Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| 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. |
| AID625058 | Binding constant for VRK2 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. |
| AID624767 | Binding constant for MERTK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID625070 | Binding constant for PFTK1 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1246527 | Resistance index, ratio of IC50 for imatinib resistant human IR-K562 cells to IC50 for human K562 cells | 2015 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
| Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia. |
| AID435798 | Binding constant for FGR kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1705803 | Growth inhibition of human MDA-MB-468 cells measured after 48 hrs by SRB assay | | | |
| 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. |
| AID743664 | Inhibition of BCR-ABL kinase (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
| BCR-ABL tyrosine kinase inhibitor pharmacophore model derived from a series of phenylaminopyrimidine-based (PAP) derivatives. |
| AID625034 | Binding constant for PDGFRA kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID1126702 | Inhibition of Abl kinase tyrosine phosphorylation in human K562 cells at 10 uM after 1 hr by immunoblot analysis | 2014 | European journal of medicinal chemistry, May-06, Volume: 78 | Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines. |
| AID512414 | Inhibition of HER-2 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID592020 | Binding affinity to human Pyk2 assessed as residual binding at 10 uM by site dependent competitive binding assay | 2011 | Journal of medicinal chemistry, Mar-10, Volume: 54, Issue:5
| Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. |
| 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. |
| 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). |
| AID624713 | Binding constant for ERK2 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. |
| AID435530 | Binding constant for MAP3K4 kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative 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. |
| AID371451 | Inhibition of PDGFR autophosphorylation in mouse Swiss 3T3 fibroblast by immunoblotting | 2008 | European journal of medicinal chemistry, Jul, Volume: 43, Issue:7
| Inhibition of PDGFR tyrosine kinase activity by a series of novel N-(3-(4-(pyridin-3-yl)-1H-imidazol-2-ylamino)phenyl)amides: a SAR study on the bioisosterism of pyrimidine and imidazole. |
| AID1508906 | Inhibition of TEL fused c-KIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay | 2019 | Journal of medicinal chemistry, 05-23, Volume: 62, Issue:10
| Discovery of ( E)- N |
| AID1426833 | Toxicity in wild-type zebrafish AB assessed as mortality at 20 ug/ml | 2017 | Journal of medicinal chemistry, 02-09, Volume: 60, Issue:3
| Total Syntheses and Biological Activities of Vinylamycin Analogues. |
| 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. |
| AID428457 | Inhibition of human carbonic anhydrase 12 by stopped flow CO2 hydration assay | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
| The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. |
| AID1585049 | Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants includi |
| 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. |
| AID512401 | Inhibition of human JNK1alpha1 activity at 10 uM by radiometric assay | 2006 | Nature chemical biology, Feb, Volume: 2, Issue:2
| Allosteric inhibitors of Bcr-abl-dependent cell proliferation. |
| AID375196 | Cytotoxicity against human GIST48 cells assessed as effect on cell viability after 3 to 6 days by luciferase based luminescence assay | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Targeting human gastrointestinal stromal tumor cells with a quadruplex-binding small molecule. |
| 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. |
| AID1337173 | Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method | 2017 | Nature reviews. Drug discovery, Jun, Volume: 16, Issue:6
| Non-kinase targets of protein kinase inhibitors. |
| AID1425204 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry | 2017 | Science (New York, N.Y.), 12-01, Volume: 358, Issue:6367
| The target landscape of clinical kinase drugs. |
| AID1338921 | Inhibition of c-KIT mediated signaling pathways assessed as reduction in S6K phosphorylation at T389 in human GISTT1 cells at 1 uM measured after 2 hrs by immunoblotting | 2017 | Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
| Discovery of 4-Methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((1-nicotinoylpiperidin-4-yl)oxy)benzamide (CHMFL-ABL/KIT-155) as a Novel Highly Potent Type II ABL/KIT Dual Kinase Inhibitor with a Distinct Hinge Binding. |
| AID625123 | Binding constant for RET(V804L) kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID624819 | Binding constant for ACVR1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| 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. |
| AID435933 | Binding constant for PKN2 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. |
| AID1532233 | Growth inhibition of human SN12C cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID1358763 | Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay | | | |
| AID1629555 | Inhibition of wild type cKIT in human GIST-T1 cells assessed as downregulation of AKT phosphorylation at S473 at 1 uM after 1 hr by Western blot analysis | 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 |
| AID1454442 | Displacement of CAT-1 from catalytic site of N-terminal His6-tagged ABL T315I mutant (unknown origin) at 25 uM by 19F NMR spectroscopy based dual-site competition assay | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
| |
| 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. |
| AID435155 | Binding constant for full-length DLK | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1832773 | Antiproliferative activity against T315I mutant expressing human K-562R cells assessed as inhibition of cell proliferation at 100 uM incubated for 48 hrs by MTT assay relative to control | 2021 | Bioorganic & medicinal chemistry, 10-15, Volume: 48 | Design, synthesis, and biological evaluation of novel Bcr-Abl |
| AID624893 | Binding constant for MEK1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1386084 | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. |
| AID1444945 | Inhibition of TEL-fused cKIT L576P mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay | 2017 | Journal of medicinal chemistry, 06-22, Volume: 60, Issue:12
| Discovery of Potent, Selective Stem Cell Factor Receptor/Platelet Derived Growth Factor Receptor Alpha (c-KIT/PDGFRα) Dual Inhibitor for the Treatment of Imatinib-Resistant Gastrointestinal Stromal Tumors (GISTs). |
| 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. |
| AID1739059 | Binding affinity to human FLT4 | 2020 | European journal of medicinal chemistry, Aug-01, Volume: 199 | A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone. |
| 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 |
| AID1221975 | Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
| Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model. |
| 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. |
| AID1300621 | Antiproliferative activity against human BV173 cells after 48 hrs by Cell-Titer-Glo luminescent cell viability assay | 2016 | Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7
| Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells. |
| AID624884 | Binding constant for PRKD1 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1495939 | Antiproliferative activity against imatinib-susceptible human GIST882 cells harboring c-KIT K642E mutant after 96 hrs by SRB assay | 2018 | Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
| A naphthalene diimide G-quadruplex ligand inhibits cell growth and down-regulates BCL-2 expression in an imatinib-resistant gastrointestinal cancer cell line. |
| 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). |
| 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. |
| 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. |
| AID1526725 | Antifibrotic activity in CCl4-induced BALB/c mouse model of liver fibrosis assessed as reduction in liver fibrosis area at 50 mg/kg, po administered for 6 weeks by alpha-SMA staining based microscopy | 2019 | Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
| Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-like 2/3. |
| 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. |
| AID624958 | Binding constant for PIK3C2G kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive 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. |
| AID625105 | Binding constant for EPHB2 kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1544927 | Induction of apoptosis in human K562 cells assessed as increase in apoptotic cells at 10 uM incubated for 48 hrs by Caspase-3/7 reagent-based fluorescence assay | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14
| Design and synthesis of novel 1-phenyl-3-(5-(pyrimidin-4-ylthio)-1,3,4-thiadiazol- 2-yl)urea derivatives with potent anti-CML activity throughout PI3K/AKT signaling pathway. |
| AID1743563 | Antiproliferative activity against human HL-60(TB) cells assessed as cell growth inhibition measured after 48 hrs by SRB assay | 2020 | European journal of medicinal chemistry, Dec-01, Volume: 207 | Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity. |
| 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. |
| AID435827 | Binding constant for PDGFRA kinase domain | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| 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. |
| 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. |
| AID1464306 | Inhibition of GSK3alpha (unknown origin) at 10 uM using [33P]-ATP after 20 to 40 mins by scintillation counting method | | | |
| AID515834 | Antiproliferative activity against human K562 cells | 2010 | Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
| Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. |
| AID497610 | Inhibition of human recombinant full-length GST-tagged B-Raf by radiometric kinase assay | 2010 | Bioorganic & medicinal chemistry, Aug-01, Volume: 18, Issue:15
| The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: a structural analysis of the binding interactions of Gleevec, Nexavar, and BIRB-796. |
| 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. |
| AID649624 | Cytotoxicity against human TF1 cells expressing FLT3 mutation assessed as cell viability | 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. |
| AID625025 | Binding constant for MAK kinase domain | 2011 | Nature biotechnology, Oct-30, Volume: 29, Issue:11
| Comprehensive analysis of kinase inhibitor selectivity. |
| AID1532188 | Growth inhibition of human CCRF-CEM cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| AID1532191 | Growth inhibition of human MOLT4 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| AID777467 | Cytotoxicity against HGC27 cells assessed as cell viability after 48 hrs by MTT assay | 2013 | ACS medicinal chemistry letters, Oct-10, Volume: 4, Issue:10
| Synthesis and Evaluation of Quinazolone Derivatives as a New Class of c-KIT G-Quadruplex Binding Ligands. |
| AID1422104 | Inhibition of heme oxygenase 1 in human K562R cells assessed as decrease in HO-1 mRNA levels at 10 uM by qRT-PCR method | 2018 | European journal of medicinal chemistry, Oct-05, Volume: 158 | Targeting heme Oxygenase-1 with hybrid compounds to overcome Imatinib resistance in chronic myeloid leukemia cell lines. |
| 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. |
| 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. |
| AID435689 | Binding constant for full-length PFTK1 | 2008 | Nature biotechnology, Jan, Volume: 26, Issue:1
| A quantitative analysis of kinase inhibitor selectivity. |
| AID1532231 | Growth inhibition of human Caki1 cells at 10 uM after 48 hrs by SRB assay relative to control | 2019 | European journal of medicinal chemistry, Jan-01, Volume: 161 | Natural products hybrids: 3,5,4'-Trimethoxystilbene-5,6,7-trimethoxyflavone chimeric analogs as potential cytotoxic agents against diverse human cancer cells. |
| 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. |
| 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. |
| AID1347117 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347112 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347128 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347124 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347121 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347127 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| 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. |
| AID1347114 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347119 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347126 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347115 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347122 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347129 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1745855 | NCATS anti-infectives library activity on the primary C. elegans qHTS viability assay | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| AID1347110 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1347109 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745854 | NCATS anti-infectives library activity on HEK293 viability as a counter-qHTS vs the C. elegans viability qHTS | 2023 | Disease models & mechanisms, 03-01, Volume: 16, Issue:3
| In vivo quantitative high-throughput screening for drug discovery and comparative toxicology. |
| 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. |
| 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. |
| AID1347118 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347116 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347111 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| 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. |
| 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. |
| AID1347125 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347113 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347123 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4
| Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| 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. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID493040 | Navigating the Kinome | 2011 | Nature chemical biology, Apr, Volume: 7, Issue:4
| Navigating the kinome. |
| 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. |
| 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. |
| AID1800098 | EC50 Test from Article 10.1021/cb400430t: \\Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor.\\ | 2013 | ACS chemical biology, Oct-18, Volume: 8, Issue:10
| Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. |
| AID1804127 | No assay is provided from Article 10.1002/med.21724: \\The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.\\ | 2021 | Medicinal research reviews, 01, Volume: 41, Issue:1
| The recent outbreaks of human coronaviruses: A medicinal chemistry perspective. |
| AID1799577 | Kinase Assay from Article 10.1111/j.1747-0285.2007.00556.x: \\Crystal structure of the T315I mutant of AbI kinase.\\ | 2007 | Chemical biology & drug design, Sep, Volume: 70, Issue:3
| Crystal structure of the T315I mutant of AbI kinase. |
| AID1801733 | Kinome-Wide Inhibitor Profiling for Phosphorylated c-Abl from Article 10.1021/acschembio.5b01018: \\Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5
| Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity. |
| AID1799800 | Radiometric Assay from Article 10.1074/jbc.M109.005694: \\Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.\\ | 2009 | The Journal of biological chemistry, Jun-05, Volume: 284, Issue:23
| Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. |
| 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. |
| AID1802830 | LRRK2 Kinase Assay from Article 10.1074/jbc.M113.537811: \\The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity.\\ | 2014 | The Journal of biological chemistry, May-09, Volume: 289, Issue:19
| The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity. |
| AID1801731 | Kinome-Wide Inhibitor Profiling from Article 10.1021/acschembio.5b01018: \\Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.\\ | 2016 | ACS chemical biology, 05-20, Volume: 11, Issue:5
| Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity. |
| AID1799511 | Enzymatic Assay from Article 10.1016/j.chembiol.2006.05.008: \\MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells.\\ | 2006 | Chemistry & biology, Jul, Volume: 13, Issue:7
| MASPIT: three-hybrid trap for quantitative proteome fingerprinting of small molecule-protein interactions in mammalian cells. |
| AID1799514 | Biochemcial Assay from Article 10.1016/j.chembiol.2006.05.015: \\A general strategy for creating "inactive-conformation" abl inhibitors.\\ | 2006 | Chemistry & biology, Jul, Volume: 13, Issue:7
| A general strategy for creating "inactive-conformation" abl inhibitors. |
| AID1799515 | Biochemcial Assay from Article 10.1016/j.chembiol.2006.05.015: \\A general strategy for creating "inactive-conformation" abl inhibitors.\\ | 2006 | Chemistry & biology, Jul, Volume: 13, Issue:7
| A general strategy for creating "inactive-conformation" abl inhibitors. |
| AID1799755 | Inhibition Assay from Article 10.1021/cb300128b: \\Targeting GSK3 from Ustilago maydis: Type-II Kinase Inhibitors as Potential Antifungals.\\ | 2012 | ACS chemical biology, Jul-20, Volume: 7, Issue:7
| Targeting GSK3 from Ustilago maydis: type-II kinase inhibitors as potential antifungals. |
| AID1345606 | Human ABL proto-oncogene 1, non-receptor tyrosine kinase (Abl family) | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10
| Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. |
| AID1345562 | Human discoidin domain receptor tyrosine kinase 1 (Type XVI RTKs: DDR (collagen receptor) family) | 2013 | ACS chemical biology, Oct-18, Volume: 8, Issue:10
| Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. |
| AID1345524 | Human discoidin domain receptor tyrosine kinase 2 (Type XVI RTKs: DDR (collagen receptor) family) | 2013 | ACS chemical biology, Oct-18, Volume: 8, Issue:10
| Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. |
| AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2002 | Cancer research, Aug-01, Volume: 62, Issue:15
| Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2002 | Cancer research, Aug-01, Volume: 62, Issue:15
| Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). |
| AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2004 | The Journal of biological chemistry, Dec-31, Volume: 279, Issue:53
| A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. |
| AID1811 | Experimentally measured binding affinity data derived from PDB | 2004 | The Journal of biological chemistry, Dec-31, Volume: 279, Issue:53
| A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |