CGP 12177 [Ligand Id: 532] 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] | ||||||||
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 525-32 [PMID:15060759]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; Pharmacol Res Perspect (2016) 4: e00250 [PMID:27588207] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - |
Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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 | - | - | 9.4 | pKi | - | - | - |
Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528]; 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 | - | - | 7.3 | pKi | 50.1 | nM | Ki |
Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020]; Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421]; Mol Pharmacol (1993) 44: 1094-104 [PMID:7903415]; Br J Pharmacol (1997) 120: 165-76 [PMID:9117106] |
| 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 |
| β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962] | ||||||||
| GtoPdb | - | - | 6.8 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421] |
| β3-adrenoceptor in Rat [GtoPdb: 30] [UniProtKB: P26255] | ||||||||
| GtoPdb | - | - | 6.8 | 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]
