sulfisoxazole [Ligand Id: 12700] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL453 (Entusil, Eryzole, Gantrisin, Neazolin, NSC-13120, NSC-683536, Pediazole, Sosol, Soxazole, Sulfafurazol, Sulfafurazole, Sulfalar, Sulfisoxazole, Sulphafurazole, Sulsoxin)
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
  • ETA receptor/Endothelin receptor ET-A in Rat [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
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  • ETB receptor/Endothelin receptor ET-B in Human [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
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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 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]