A192621 [Ligand Id: 1009] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL332794 (A-192621)
  • ETA receptor/Endothelin receptor ET-A in Human [ChEMBL: CHEMBL252] [GtoPdb: 219] [UniProtKB: P25101]
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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 125I-labelled ET-1 saturation binding studies with EDNRA B 5.25 pKi 5600 nM Ki Data for DCP probe A-192621
ChEMBL Binding affinity towards human Endothelin A receptor (hET -A) B 5 pIC50 9900 nM IC50 J. Med. Chem. (1999) 42: 3668-3678 [PMID:10479298]
ChEMBL Binding affinity towards human Endothelin A receptor (hET -A) B 5.09 pIC50 8200 nM IC50 J. Med. Chem. (1999) 42: 3668-3678 [PMID:10479298]
ChEMBL Inhibition of 125I labeled ET-1 binding to EDNRA B 5.37 pIC50 4280 nM IC50 Data for DCP probe A-192621
ChEMBL EDNRA- dependent phosphatidylinositol hydrolysis assay B 6 pIC50 >1000 nM IC50 Data for DCP probe A-192621
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
GtoPdb - - 8.1 pKd 7.94 nM Kd J Med Chem (1999) 42: 3668-78 [PMID:10479298]
ChEMBL 125I-labelled ET-1 saturation binding studies with EDNRB B 8.06 pKi 8.8 nM Ki Data for DCP probe A-192621
ChEMBL Binding affinity towards human Endothelin B receptor (hET -B) B 7.92 pIC50 12 nM IC50 J. Med. Chem. (1999) 42: 3668-3678 [PMID:10479298]
ChEMBL Binding affinity towards human Endothelin B receptor (hET -B) B 8.19 pIC50 6.4 nM IC50 J. Med. Chem. (1999) 42: 3668-3678 [PMID:10479298]
ChEMBL Inhibition of 125I labeled ET-3 binding to EDNRB B 8.35 pIC50 4.5 nM IC50 Data for DCP probe A-192621
ChEMBL EDNRB- dependent phosphatidylinositol hydrolysis assay B 9.1 pIC50 0.8 nM IC50 Data for DCP probe A-192621

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]