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

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ChEMBL ligand: CHEMBL461101 (Eltrombopag, Revolade, SB497115)
  • ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/METTL3/METTL14 in Human [ChEMBL: CHEMBL4106140] [GtoPdb: 3181] [UniProtKB: Q86U44Q9HCE5]
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  • methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/N6-adenosine-methyltransferase catalytic subunit in Human [ChEMBL: CHEMBL4739695] [GtoPdb: 3181] [UniProtKB: Q86U44]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCG2/Broad substrate specificity ATP-binding cassette transporter ABCG2 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]
methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/METTL3/METTL14 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106140] [GtoPdb: 3181] [UniProtKB: Q86U44Q9HCE5]
ChEMBL Binding affinity to METTL3/METTL14 (unknown origin) assessed as dissociation constant by SPR analysis B 4.88 pKd 13200 nM Kd J Med Chem (2023) 66: 1654-1677 [PMID:36692498]
ChEMBL Inhibition of METTL3/METTL14 (unknown origin) by mass spectrometry-based assay B 5.34 pIC50 4550 nM IC50 J Med Chem (2023) 66: 1654-1677 [PMID:36692498]
ChEMBL Inhibition of METTL3/METTL14 (unknown origin) by bioluminescence assay B 5.44 pIC50 3650 nM IC50 J Med Chem (2023) 66: 1654-1677 [PMID:36692498]
ChEMBL Inhibition of human recombinant METTL3/METTL14 extracted from baculovirus infected Hi-5 cells using SAM and 5'-ACGAGUCCUGGACUGAAACGGACUUGU-3' as substrates incubated for 1 hr by MTase-Glo bioluminescence assay B 5.44 pIC50 3650 nM IC50 ACS Med Chem Lett (2024) 15: 1491-1499 [PMID:39291017]
methyltransferase 3, N6-adenosine-methyltransferase complex catalytic subunit/N6-adenosine-methyltransferase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739695] [GtoPdb: 3181] [UniProtKB: Q86U44]
ChEMBL Binding affinity to METTL3 (unknown origin) assessed as dissociation constant by SPR assay B 4.88 pKd 13200 nM Kd Eur J Med Chem (2024) 274: 116526-116526 [PMID:38805939]
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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]