dubermatinib [Ligand Id: 8863] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2022968 (Dubermatinib, HCl-2084, Tp 0903, Tp-0903, TP-0903, TP0903) |
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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] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| ChEMBL | Inhibition of Aurora A | B | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| 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 | B | 7.91 | pIC50 | 12.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| GtoPdb | - | - | 7.91 | pIC50 | 12.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of human recombinant His-tagged AXL kinase using fluorescein-labelled poly-GT as substrate after 60 mins by TR-FRET analysis | B | 7.57 | pIC50 | 27 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| GtoPdb | - | - | 7.57 | pIC50 | 27 | nM | IC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| ChEMBL | Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA | B | 6.52 | pEC50 | 305 | nM | EC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
| ChEMBL | Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA | B | 6.65 | pEC50 | 222 | nM | EC50 | ACS Med Chem Lett (2011) 2: 907-912 [PMID:22247788] |
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]
