IRL 2500 [Ligand Id: 3887] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL72410 (IRL-2500) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
| ChEMBL | Binding affinity to Endothelin A receptor | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2241-2246 [PMID:9873521] |
| ChEMBL | Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs | B | 7.03 | pIC50 | 94 | nM | IC50 | J Med Chem (2016) 59: 8168-8188 [PMID:27266371] |
| Endothelin receptor ET-A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4130] [UniProtKB: Q29010] | ||||||||
| ChEMBL | Ability to inhibit [125I]ET1 binding to the Endothelin A receptor from porcine lung membranes was evaluated | B | 6.36 | pKi | 440 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2323-2328 |
| ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
| GtoPdb | - | - | 7.2 | pKd | 63.1 | nM | Kd | Br J Pharmacol (1996) 119: 631-6 [PMID:8904635] |
| ChEMBL | Binding affinity to Endothelin B receptor | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 2241-2246 [PMID:9873521] |
| ChEMBL | Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2016) 59: 8168-8188 [PMID:27266371] |
| Endothelin receptor ET-B in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3949] [UniProtKB: P35463] | ||||||||
| ChEMBL | Ability to inhibit [125I]ET-3 binding to the Endothelin B receptor from porcine lung membranes was evaluated | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (1996) 6: 2323-2328 |
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]
