cyanopindolol [Ligand Id: 132] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL378501 (Cyanopindolol)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • 5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells F 6.5 pKi 316.23 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells F 9.5 pKi 0.32 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells F 9.9 pKi 0.13 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells F 10.3 pKi 0.05 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells F 10.4 pKi 0.04 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 9.15 pKd 0.7 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting B 9.15 pKd 0.7 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334]
GtoPdb - - 8.1 pKi - - - Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 7.1 pKi - - - Mol Pharmacol (1991) 40: 143-8 [PMID:1652050]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]