carazolol [Ligand Id: 569] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL324665 (BM 51052, BM-51052, Carazolol, Conducton, Suacron) |
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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 | - | - | 10.2 | 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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971] | ||||||||
| ChEMBL | Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Displacement of [3H]DHA from human beta2 adrenoceptor by liquid scintillation counter | B | 9.94 | pKi | 0.11 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5391-5395 [PMID:18829308] |
| GtoPdb | - | - | 10.5 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Bioorg Med Chem Lett (2008) 18: 5391-5 [PMID:18829308] |
| ChEMBL | Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay | B | 10.52 | pKi | 0.03 | nM | Ki | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| GtoPdb | - | - | 8.4 | pKi | 1.99 | nM | Ki | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| GtoPdb | - | - | 8.8 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421] |
| β3-adrenoceptor in Rat [GtoPdb: 30] [UniProtKB: P26255] | ||||||||
| GtoPdb | - | - | 7.7 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421] |
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]
