cenisertib [Ligand Id: 9927] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1614709 (AS-703569, R-763) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
