endothelin-1 [Ligand Id: 989] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3775234 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin-1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Binding affinity to ETA receptor (unknown origin) assessed as inhibition constant | B | 10.47 | pKi | 0.03 | nM | Ki | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| GtoPdb | - | - | 8.5 | pIC50 | - | - | - | Br J Pharmacol (1995) 115: 191-7 [PMID:7647976] |
| ChEMBL | Inhibition of ETA receptor (unknown origin) | B | 10.57 | pIC50 | 0.03 | nM | IC50 | ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908] |
| ChEMBL | Displacement of [125I]Endothelin-1 from human recombinant Endothelin-1 receptor expressed in CHO cells | B | 10.64 | pIC50 | 0.02 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Displacement of [125I]endothelin-1 from human recombinant ETA receptor expressed in CHO cells measured after 120 mins by scintillation counting method | B | 10.64 | pIC50 | 0.02 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ETA receptor/Endothelin-1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
| ChEMBL | Agonist activity to ETA receptor in Sprague-Dawley rat aorta assessed as induction of vessel ring contraction | F | 8.96 | pEC50 | 1.1 | nM | EC50 | Eur J Pharmacol (1999) 366: 189-201 [PMID:10082200] |
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]
