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ChEMBL ligand: CHEMBL471 (Betapace, C07AA07, Darob mite, Dl-sotalol, MJ-1999, Sorine, Sotalol) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.08 | pKi | 833.5 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 6.1 | pKi | - | - | - |
Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; National Toxicology Program: Dept of Health and Human Services.. DrugMatrix |
ChEMBL | In vitro Beta-1 adrenergic receptor affinity in partially purified membrane fractions from canine cardiac tissue using [SH]dihydroalprenolol (4.5 nM) | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (1990) 33: 1087-1090 [PMID:2319556] |
ChEMBL | Binding affinity for Beta-1 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine ventricular muscle in the presence of 1 uM zinterol | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (1992) 35: 743-750 [PMID:1347318] |
ChEMBL | Tested for Beta-1 adrenergic receptor selectivity in canine cardiac tissue in anesthetized dogs | B | 5.05 | pIC50 | 8900 | nM | IC50 | J Med Chem (1990) 33: 2883-2891 [PMID:1976812] |
ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 5.84 | pIC50 | 1443.4 | nM | IC50 | DrugMatrix in vitro pharmacology data |
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.53 | pKi | 298.3 | nM | Ki | DrugMatrix in vitro pharmacology data |
GtoPdb | - | - | 6.9 | pKi | - | - | - |
Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; National Toxicology Program: Dept of Health and Human Services.. DrugMatrix |
ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.36 | pIC50 | 433.9 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833] | ||||||||
ChEMBL | Tested for Beta-2 adrenergic receptor selectivity in canine lung tissue in anesthetized dogs | B | 5.28 | pIC50 | 5200 | nM | IC50 | J Med Chem (1990) 33: 2883-2891 [PMID:1976812] |
ChEMBL | In vitro Beta-2 adrenergic receptor affinity in partially purified membrane fractions from canine lung tissue using [SH]dihydroalprenolol (4.5 nM) | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1990) 33: 1087-1090 [PMID:2319556] |
ChEMBL | Binding affinity towards Beta-2 adrenergic receptor by displacing [3H]dihydroalprenolol, in partially purified membrane fractions from canine lung tissue in the presence of 0.1 uM metoprolol | B | 5.3 | pIC50 | 5000 | nM | IC50 | J Med Chem (1992) 35: 743-750 [PMID:1347318] |
Beta-2 adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3373] [UniProtKB: Q28044] | ||||||||
ChEMBL | Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) | B | 6.24 | pKd | 580 | nM | Kd | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
ChEMBL | Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) | B | 6.57 | pKd | 6.57 | - | -Log KD | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
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]