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ChEMBL ligand: CHEMBL509336 (Ractopamine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting | B | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2009) 52: 1773-1777 [PMID:19245211] |
GtoPdb | Inhibitory constant determined from a standard radioligand displacement assay using human β2-adrenoceptors expressed in Sf-9 cells and [3H]CGP1217 as tracer. | - | 6.9 | pKi | - | - | - |
Mol Pharmacol (1999) 56: 875-85 [PMID:10531390]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Br J Pharmacol (2022) 179: 4692-4708 [PMID:35732075] |
ChEMBL | Displacement of [3H]CGP1217 from human recombinant adrenergic beta2 receptor transfected in insect Sf9 cells by scintillation counting | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2009) 52: 1773-1777 [PMID:19245211] |
GtoPdb | - | - | 7.8 | pEC50 | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Br J Pharmacol (2022) 179: 4692-4708 [PMID:35732075] |
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
ChEMBL | Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction | F | 8.21 | pEC50 | 6.2 | nM | EC50 | J Med Chem (2009) 52: 1773-1777 [PMID:19245211] |
TA1 receptor in Mouse [GtoPdb: 364] [UniProtKB: Q923Y8] | ||||||||
GtoPdb | Measuring chloride conductance in oocytes coexpressing hCFTR and mTAAR1, as a as a sensor for intracellular cAMP modulation. | - | 4.8 | pEC50 | 16000 | nM | EC50 | J Pharmacol Exp Ther (2014) 350: 124-9 [PMID:24799633] |
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]