eltrombopag [Ligand Id: 6961] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL461101 (Eltrombopag, Revolade, SB497115) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG channel tail current | B | 6.16 | pIC50 | 690 | nM | IC50 | Bioorg Med Chem (2016) 24: 1419-1430 [PMID:26935940] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | F | 6.2 | pIC50 | 630.96 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Thrombopoietin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1864] [GtoPdb: 1722] [UniProtKB: P40238] | ||||||||
| GtoPdb | - | - | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5259-62 [PMID:18783949] |
| ChEMBL | Agonist activity at human thrombopoietin receptor expressed in mouse Ba/F3 cells by kinase activation based reporter gene assay | F | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5259-5262 [PMID:18783949] |
| ChEMBL | Agonist activity at human thrombopoietin receptor in Ba/F3 cells assessed as activation of Stat5 response element-driven reporter gene expression | F | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5255-5258 [PMID:18778936] |
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]
