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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 |
|---|---|---|---|---|---|---|---|---|
| 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: Q86U44, Q9HCE5] | ||||||||
| 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]