abediterol [Ligand Id: 9326] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3039530 (Abediterol, LAS100977, LAS-100977)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
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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 Membrane radioligand displacement assay using [3H]CGP12177 as tracer. - 7.44 pIC50 36.2 nM IC50 J Pharmacol Exp Ther (2012) 342: 497-509 [PMID:22588259]
ChEMBL Inhibition of 3H]CGP12177 binding to human beta1 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method B 7.44 pEC50 36.2 nM EC50 J Med Chem (2020) 63: 15218-15242 [PMID:33213146]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
GtoPdb Membrane radioligand displacement assay using [3H]CGP12177 as tracer. - 9.22 pIC50 0.6 nM IC50 J Pharmacol Exp Ther (2012) 342: 497-509 [PMID:22588259]
ChEMBL Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation F 8.72 pEC50 1.9 nM EC50 J Med Chem (2020) 63: 15218-15242 [PMID:33213146]
ChEMBL Inhibition of 3H]CGP12177 binding to human beta2 adrenoceptor expressed in sf9 cell membranes incubated for 60 mins by scintillation counting method B 9.22 pEC50 0.6 nM EC50 J Med Chem (2020) 63: 15218-15242 [PMID:33213146]
β3-adrenoceptor in Human [GtoPdb: 30] [UniProtKB: P13945]
GtoPdb - - 5.52 pIC50 3001 nM IC50 J Pharmacol Exp Ther (2012) 342: 497-509 [PMID:22588259]

ChEMBL data shown on this page come from version 32:

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]