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 human Axl using KKSRGDYMTMQIG as substrate incubated for 40 mins in the presence of [gamma33P]ATP by scintillation counting analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | RSC Med Chem (2022) 13: 1246-1264 [PMID:36325401] |
| 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 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]
