Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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 | Darifenacin | 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 | Darifenacin | 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 | Darifenacin | 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 | Darifenacin | 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) | Darifenacin | 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 | Darifenacin | 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) | Darifenacin | Drug Info | EC50 = 39.81 nM | [12] |
References | Top | ||||
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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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