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ChEMBL ligand: CHEMBL378501 (Cyanopindolol) |
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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 in Human [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
GtoPdb | - | - | 10.5 | pKd | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Mol Pharmacol (2015) 88: 1024-34 [PMID:26385885] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells | F | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells | F | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells | F | 9.9 | pKi | 0.13 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
ChEMBL | Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells | F | 10.3 | pKi | 0.05 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
ChEMBL | Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells | F | 10.4 | pKi | 0.04 | nM | Ki | J Med Chem (2006) 49: 3467-3477 [PMID:16759089] |
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 | 9.15 | pKd | 0.7 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
5-HT1B receptor in Mouse [GtoPdb: 2] [UniProtKB: P28334] | ||||||||
GtoPdb | - | - | 8.1 | pKi | - | - | - | Proc Natl Acad Sci USA (1992) 89: 3020-4 [PMID:1557407] |
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
GtoPdb | - | - | 7.1 | pKi | - | - | - | Mol Pharmacol (1991) 40: 143-8 [PMID:1652050] |
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]