Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T67684 Target Info
Target Name Muscarinic acetylcholine receptor M3 (CHRM3)
Synonyms
M3 receptor; CHRM3
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Target Type Successful Target
Gene Name CHRM3
Biochemical Class GPCR rhodopsin
UniProt ID
ACM3_HUMAN
Co-Targets of This Target  Top
Co-Target Name Muscarinic acetylcholine receptor M2 (CHRM2) Successful Target
UniProt ID ACM2_HUMAN
Gene Name CHRM2
Synonyms
M2 receptor; CHRM2
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Representative Drug(s) LAS-34273 Drug Info IC50 < 0.03981 nM Click to Show More [1]
2 Methylscopolamine Drug Info Ki = 0.0631 nM [2]
3 Tolterodine Drug Info Ki = 2.7 nM [9]
4 Drug Info Ki = 47 nM [10]
5 Tarafenacin Drug Info IC50 = 97.3 nM [8]
6 Solifenacin Drug Info Ki = 120.23 nM [13]
7 Solifenacin Drug Info IC50 = 573.7 nM [8]
Co-Target Name Muscarinic acetylcholine receptor M1 (CHRM1) Successful Target
UniProt ID ACM1_HUMAN
Gene Name CHRM1
Synonyms
M1 receptor
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Representative Drug(s) LAS-34273 Drug Info Ki = 0.08 nM Click to Show More [3]
2 Methylscopolamine Drug Info Ki = 0.0955 nM [4]
3 Tarafenacin Drug Info IC50 = 0.9 nM [8]
4 Tolterodine Drug Info Ki = 1.4 nM [9]
5 Drug Info Ki = 5.5 nM [10]
6 Solifenacin Drug Info Ki = 51.29 nM [13]
7 Solifenacin Drug Info IC50 = 63.5 nM [8]
Co-Target Name Muscarinic acetylcholine receptor M4 (CHRM4) Successful Target
UniProt ID ACM4_HUMAN
Gene Name CHRM4
Synonyms
M4 receptor; CHRM4
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Representative Drug(s) Methylscopolamine Drug Info Ki = 0.1413 nM Click to Show More [5]
2 LAS-34273 Drug Info IC50 = 0.1995 nM [6]
3 Tolterodine Drug Info Ki = 3.1 nM [9]
4 Drug Info Ki = 8.6 nM [10]
5 Solifenacin Drug Info Ki = 128.82 nM [13]
Co-Target Name Muscarinic acetylcholine receptor M5 (CHRM5) Successful Target
UniProt ID ACM5_HUMAN
Gene Name CHRM5
Synonyms
CHRM5
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Representative Drug(s) LAS-34273 Drug Info IC50 = 0.1585 nM Click to Show More [6]
2 Methylscopolamine Drug Info Ki = 0.2089 nM [5]
3 Tolterodine Drug Info Ki = 2.2 nM [9]
4 Drug Info Ki = 2.3 nM [10]
5 Solifenacin Drug Info Ki = 43.65 nM [13]
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 [7]
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) Tolterodine Drug Info IC50 = 12.59 nM Click to Show More [11]
2 Drug Info IC50 = 79.43 nM [11]
3 Solifenacin Drug Info IC50 = 251.19 nM [11]
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 [12]
References  Top
REF 1 The discovery of AZD9164, a novel muscarinic M3 antagonist. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7440-6.
REF 2 Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M. J Med Chem. 2017 Apr 27;60(8):3314-34.
REF 3 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for... J Med Chem. 2009 Aug 27;52(16):5076-92.
REF 4 Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors. J Med Chem. 2012 Mar 8;55(5):2125-43.
REF 5 Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure. J Med Chem. 2007 Mar 22;50(6):1409-13.
REF 6 The discovery of new spirocyclic muscarinic M3 antagonists. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7458-61.
REF 7 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 8 Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3457-61.
REF 9 Design and synthesis of a fluorescent muscarinic antagonist. Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7.
REF 10 Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes. J Med Chem. 2002 Feb 14;45(4):984-7.
REF 11 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 12 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 13 Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments. Eur J Med Chem. 2017 Sep 8;137:327-37.

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