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ChEMBL ligand: CHEMBL453 (Entusil, Eryzole, Gantrisin, Neazolin, NSC-13120, NSC-683536, Pediazole, Sosol, Soxazole, Sulfafurazol, Sulfafurazole, Sulfalar, Sulfisoxazole, Sulphafurazole, Sulsoxin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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ETA receptor/Endothelin receptor ET-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101] | ||||||||
ChEMBL | DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) | B | 4.87 | pKi | 13465 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Endothelin ETA radioligand binding (ligand: [125I] Endothelin-1) | B | 4.66 | pIC50 | 21880 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Binding affinity against human Endothelin A receptor in TE 671(ATCC# HTB 139) cell membrane preparation | B | 6.07 | pIC50 | 850 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2393-2398 |
ChEMBL | Inhibitory concentration against Endothelin A receptor | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (2004) 47: 1303-1314 [PMID:14998318] |
ChEMBL | Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (1994) 37: 329-331 [PMID:8308857] |
ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684] | ||||||||
ChEMBL | Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor | B | 5.05 | pIC50 | 9000 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1875-1878 [PMID:10969989] |
ChEMBL | Inhibition of [125I]endothelin-l binding to endothelin A receptor of rat thoracic aorta smooth muscle cells | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1995) 38: 659-668 [PMID:7861414] |
ChEMBL | Antagonism of [125 I]ET-1 binding to the rat endothelin receptor in vascular smooth muscle VSM-A10 cells. | B | 6.11 | pIC50 | 780 | nM | IC50 | J Med Chem (1995) 38: 1344-1354 [PMID:7731020] |
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530] | ||||||||
ChEMBL | Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation | B | 4.62 | pIC50 | 24000 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2393-2398 |
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]