Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
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
NOUNIPROTAC
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) Darifenacin 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) Darifenacin 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) Darifenacin 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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