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

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ChEMBL ligand: CHEMBL645 (CL 297,939, Bisoprolol, CL-297939, EMD 33 512, Zebeta, Ziac, EMD-33-512)
  • 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/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 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]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 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]