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] |
| Dynamin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4958] [UniProtKB: Q05193] | ||||||||
| ChEMBL | Inhibition of phosphotidylserine liposome-stimulated Dynamin 1 (unknown origin) GTPase activity by malachite green assay | B | 4.1 | pIC50 | 79700 | nM | IC50 | Eur J Med Chem (2023) 247: 115001-115001 [PMID:36577213] |
| 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 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]
