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

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ChEMBL ligand: CHEMBL378501 (Cyanopindolol)
  • β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588]
  • 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 in Human [GtoPdb: 28] [UniProtKB: P08588]
GtoPdb - - 10.5 pKd - - - Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599];
Mol Pharmacol (2015) 88: 1024-34 [PMID:26385885]
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]
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]