eltrombopag [Ligand Id: 6961] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL461101 (Eltrombopag, Revolade, SB497115)
  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
ChEMBL Inhibition of human ABCG2 expressed in dog MDCK-II-BCRP cells membrane vesicles mediated transport of 3[H]-methotrexate for 5 mins using [3H]-methotrexate as substrate by radiometric scintillation analysis B 5.51 pIC50 3100 nM IC50 Eur J Med Chem (2022) 237: 114346-114346 [PMID:35483322]
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 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]