gandotinib [Ligand Id: 7909] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2107823 (Ly2784544, Ly-2784544, LY2784544, LY-2784544, Gandotinib)
  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674]
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  • Janus kinase 3 in Human [GtoPdb: 2049] [UniProtKB: P52333]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Further kinetic evaluation of compounds supplied by Sanofi against AuroraA within a BIAcore3000 instrument B 7.82 pKd 15.05 nM Kd K4DD drug target binding kinetics data
Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb - - 8.4 pIC50 4 nM IC50 Blood Cancer J (2013) 3: e109 [PMID:23584399]
Janus kinase 3 in Human [GtoPdb: 2049] [UniProtKB: P52333]
GtoPdb - - 7.32 pIC50 48 nM IC50 Blood Cancer J (2013) 3: e109 [PMID:23584399]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]