cyanopindolol [Ligand Id: 132] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| 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 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]
