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) |
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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 | - | - | 7.8 | 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 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]
