Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T09130 | Target Info | |||
| Target Name | Muscarinic acetylcholine receptor (CHRM) | ||||
| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Adrenergic receptor beta-2 (ADRB2) | Successful Target | ||||
| UniProt ID | ADRB2_HUMAN | |||||
| Gene Name | ADRB2 | |||||
| Synonyms |
Beta-2 adrenoreceptor; Beta-2 adrenoceptor; Beta-2 adrenergic receptor; B2AR; ADRB2R
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| Representative Drug(s) | Drug Info | EC50 = 0.7943 nM | [1] | |||
| Co-Target Name | Neuronal acetylcholine receptor alpha-4/beta-2 (CHRNA4/B2) | Successful Target | ||||
| UniProt ID | ACHA4_HUMAN-ACHB2_HUMAN | |||||
| Gene Name | CHRNA4-CHRNB2 | |||||
| Synonyms |
CHRN; nAChR
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| Representative Drug(s) | Acetylcholine | Drug Info | EC50 = 1.7 nM | [2] | ||
| Co-Target Name | Adrenergic receptor beta-1 (ADRB1) | Successful Target | ||||
| UniProt ID | ADRB1_HUMAN | |||||
| Gene Name | ADRB1 | |||||
| Synonyms |
Beta-1 adrenoreceptor; Beta-1 adrenoceptor; Beta-1 adrenergic receptor; B1AR; ADRB1R
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| Representative Drug(s) | Drug Info | EC50 = 39.81 nM | [3] | |||
| Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
| UniProt ID | KCNH2_HUMAN | |||||
| Gene Name | KCNH2 | |||||
| Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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| Representative Drug(s) | Drug Info | IC50 = 79.43 nM | [4] | |||
| Co-Target Name | Neuronal acetylcholine receptor alpha-7 (CHRNA7) | Successful Target | ||||
| UniProt ID | ACHA7_HUMAN | |||||
| Gene Name | CHRNA7 | |||||
| Synonyms |
Nicotinic acetylcholine receptor subunit alpha 7; Nicotinic acetylcholine receptor alpha7; CHRNA7; Alpha7 nicotinic receptor; Alpha7 nAChR; Alpha-7 nAChR; Alpha(7) nicotinic receptor
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| Representative Drug(s) | Acetylcholine | Drug Info | Ki = 501.19 nM | [5] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of (R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino)methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic antagonist and beta? agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD). J Med Chem. 2015 Mar 26;58(6):2609-22. | ||||
| REF 2 | Recent developments in novel antidepressants targeting alpha42-nicotinic acetylcholine receptors. J Med Chem. 2014 Oct 23;57(20):8204-23. | ||||
| REF 3 | Design-driven LO: the discovery of new ultra long acting dibasic beta2-adrenoceptor agonists. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4612-6. | ||||
| REF 4 | Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54. | ||||
| REF 5 | Identification of novel alpha7 nicotinic receptor ligands by in silico screening against the crystal structure of a chimeric alpha7 receptor ligand binding domain. Bioorg Med Chem. 2012 Oct 1;20(19):5992-6002. | ||||
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