xamoterol [Ligand Id: 538] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL75753 (Xamoterol)
  • 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/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [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]
ChEMBL Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 7.09 pKd 81.28 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 7.75 pKd 17.78 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
GtoPdb - - 7 pKi 100 nM Ki Mol Pharmacol (1999) 56: 875-85 [PMID:10531390]
ChEMBL Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 7.96 pEC50 10.96 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 5.76 pKd 1737.8 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 6.18 pKd 660.69 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 6.15 pEC50 707.95 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 4.7 pKd 19952.62 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 4 pEC50 100000 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]