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ChEMBL ligand: CHEMBL3039530 (Abediterol, LAS-100977, LAS100977) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]