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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
