[3H]CGP12177 [Ligand Id: 5387] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL420746 (CGP-12177) |
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| 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 | Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs | F | 7.91 | pEC50 | 12.3 | nM | EC50 | J Med Chem (2013) 56: 3852-3865 [PMID:23614528] |
| 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 | 7.72 | pKd | 19 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| ChEMBL | Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting | B | 9.7 | pKd | 0.2 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| GtoPdb | - | - | 9.8 | pKd | - | - | - | Br J Pharmacol (2002) 137: 400-8 [PMID:12237261] |
| GtoPdb | Binding to human &beta2-adrenoceptor expressed in CHO-K1 cells, in a whole cell binding assay. | - | 9.84 | pKd | 0.14 | nM | Kd | Br J Pharmacol (2002) 137: 400-8 [PMID:12237261] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| GtoPdb | - | - | 7 | pKd | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells | F | 5.7 | pEC50 | 2000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 219-224 |
ChEMBL data shown on this page come from version 35:
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]
