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 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]
