arformoterol [Ligand Id: 7479] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1363 (Arformoterol, Formoterol r,r-form)
  • 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]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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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 - - 6.5 pKi 319 nM Ki Bioorg Med Chem Lett (2010) 20: 5302-7 [PMID:20655218]
ChEMBL Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology F 6.96 pEC50 109 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 - - 8.59 pKi 2.6 nM Ki Bioorg Med Chem Lett (2004) 14: 4705-10 [PMID:15324892]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology F 8.58 pEC50 2.63 nM EC50 J Med Chem (2020) 63: 15218-15242 [PMID:33213146]
ChEMBL Agonist activity at beta2-adrenergic receptor (unknown origin) F 9.5 pEC50 0.32 nM EC50 Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734]
Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
ChEMBL Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction B 9.89 pEC50 0.13 nM EC50 Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734]
ChEMBL Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction B 9.9 pEC50 0.13 nM EC50 Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734]

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]