bisoprolol [Ligand Id: 7129] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL645 (Bisoprolol, CL 297,939, CL-297939, EMD 33 512, EMD-33-512, Zebeta, Ziac)
  • β1-adrenoceptor in Human [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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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 - - 8 pKi 10 nM Ki FASEB J (2017) 31: 3150-3166 [PMID:28400472]
β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
ChEMBL Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes B 8.28 pKi 5.3 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
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 4.48 pKd 33000 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 by liquid scintillation counting B 6.82 pKd 150 nM Kd J Med Chem (2016) 59: 5780-5789 [PMID:27239696]
ChEMBL Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes B 6.6 pKi 250 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]

ChEMBL data shown on this page come from version 32:

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]