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

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ChEMBL ligand: CHEMBL3039530 (Abediterol, LAS-100977, LAS100977)
  • 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 34:

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]