cenisertib [Ligand Id: 9927] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1614709 (AS-703569, R-763)
  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aurora B kinase by HTRF analysis in presence of 1 mM ATP B 7.27 pIC50 54 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4750-4755 [PMID:22695126]
GtoPdb In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM. - 7.27 pIC50 54 nM IC50 Bioorg Med Chem Lett (2012) 22: 4750-5 [PMID:22695126]
GtoPdb Measuring phosphorylation of AurB substrate histone H3 in A549 cells. - 8.15 pIC50 7 nM IC50 WO2005118544A2. Cycloalkyl substituted pyrimidinediamine compounds and their uses. (2005)
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
GtoPdb In a biochemical homogeneous time-resolved fluorescence (HTRF) kinase assay with an ATP concentration of 1 mM. - 7.02 pIC50 95 nM IC50 Bioorg Med Chem Lett (2012) 22: 4750-5 [PMID:22695126]
ChEMBL Inhibition of KDR by HTRF analysis in presence of 1 mM ATP B 7.02 pIC50 95 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4750-4755 [PMID:22695126]
ChEMBL Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells B 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4750-4755 [PMID:22695126]

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]