xamoterol [Ligand Id: 538] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL75753 (ICI-118,587, ICI-118587, Xamoterol) |
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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 | - | - | 7.2 | pKi | - | - | - |
Mol Pharmacol (1999) 56: 875-85 [PMID:10531390]; Br J Pharmacol (2005) 144: 317-22 [PMID:15655528] |
| 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 33:
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]
