BMS-193884 [Ligand Id: 13016] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL24461 (BMS-193884)
  • 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]
  • ETB receptor/Endothelin receptor ET-B in Rat [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451]
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  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
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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]
GtoPdb - - 8.85 pKi 1.4 nM Ki J Med Chem (2000) 43: 3111-7 [PMID:10956219]
ChEMBL Compound was evaluated for its binding affinity towards human Endothelin A receptor B 8.85 pKi 1.4 nM Ki J Med Chem (2002) 45: 3829-3835 [PMID:12190306]
ChEMBL Inhibitory concentration against Endothelin A receptor B 8.85 pKi 1.4 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to CHO cells stably expressing human Endothelin A receptor. B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2002) 12: 517-520 [PMID:11844662]
ChEMBL Inhibitory activity against human endothelin A receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki J Med Chem (2003) 46: 125-137 [PMID:12502366]
ChEMBL Inhibition of Human Endothelin A receptor expressed in CHO Cells. B 8.85 pKi 1.4 nM Ki J Med Chem (2000) 43: 3111-3117 [PMID:10956219]
ChEMBL Binding affinity to ETA receptor B 8.85 pKi 1.4 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
ETA receptor/Endothelin receptor ET-A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4566] [GtoPdb: 219] [UniProtKB: P26684]
ChEMBL Binding affinity towards Endothelin A receptor B 8.85 pKi 1.4 nM Ki J Med Chem (2004) 47: 1969-1986 [PMID:15055997]
ChEMBL Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method B 8.85 pKi 1.4 nM Ki Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
ETB receptor/Endothelin receptor ET-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1785] [GtoPdb: 220] [UniProtKB: P24530]
ChEMBL Inhibitory concentration against endotheline ETB receptor F 4.73 pKi 18700 nM Ki J Med Chem (2004) 47: 1303-1314 [PMID:14998318]
ChEMBL Binding affinity to CHO cells stably expressing human Endothelin B receptor. B 4.73 pKi 18700 nM Ki Bioorg Med Chem Lett (2002) 12: 517-520 [PMID:11844662]
ChEMBL Inhibitory activity against human endothelin B receptor expressed in CHO cells B 4.73 pKi 18700 nM Ki J Med Chem (2003) 46: 125-137 [PMID:12502366]
ChEMBL Inhibition of Human Endothelin B receptor expressed in CHO Cells. B 4.73 pKi 18700 nM Ki J Med Chem (2000) 43: 3111-3117 [PMID:10956219]
GtoPdb - - 4.73 pKi 18700 nM Ki J Med Chem (2000) 43: 3111-7 [PMID:10956219]
ETB receptor/Endothelin receptor ET-B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4631] [GtoPdb: 220] [UniProtKB: P21451]
ChEMBL Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method B 5.72 pKi 1900 nM Ki Bioorg Med Chem Lett (2016) 26: 3381-3394 [PMID:27321813]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Binding affinity to AT1 receptor B 5 pKi >10000 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]

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]