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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]