Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL471 (Betapace, C07AA07, Darob mite, Dl-sotalol, MJ-1999, Sorine, Sotalol) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
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 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]