Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T79961 | Target Info | |||
| Target Name | Muscarinic acetylcholine receptor M5 (CHRM5) | ||||
| Synonyms |
CHRM5
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| Target Type | Successful Target | ||||
| Gene Name | CHRM5 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | Muscarinic acetylcholine receptor M3 (CHRM3) | Successful Target | ||||
| UniProt ID | ACM3_HUMAN | |||||
| Gene Name | CHRM3 | |||||
| Synonyms |
M3 receptor; CHRM3
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| Representative Drug(s) | Umeclidinium | Drug Info | Ki = 0.06 nM | Click to Show More | [1] | |
| 2 | Hyoscyamine | Drug Info | Ki = 0.2692 nM | [3] | ||
| 3 | Atropine | Drug Info | Ki = 0.5 nM | [2] | ||
| 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) | Umeclidinium | Drug Info | Ki = 0.15 nM | Click to Show More | [1] | |
| 2 | Atropine | Drug Info | Ki = 0.344 nM | [4] | ||
| 3 | Atropine | Drug Info | Ki = 0.683 nM | [4] | ||
| 4 | Hyoscyamine | Drug Info | Ki = 2.818 nM | [5] | ||
| 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) | Umeclidinium | Drug Info | Ki = 0.16 nM | Click to Show More | [1] | |
| 2 | Atropine | Drug Info | Ki = 0.25 nM | [2] | ||
| 3 | Hyoscyamine | Drug Info | Ki = 0.2692 nM | [3] | ||
| 4 | Atropine | Drug Info | Ki = 0.683 nM | [4] | ||
| 5 | Pilocarpine | Drug Info | EC50 = 17.5 nM | [6] | ||
| 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) | Atropine | Drug Info | Ki = 0.34 nM | [2] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists. J Med Chem. 2009 Apr 23;52(8):2493-505. | ||||
| REF 2 | Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes. J Med Chem. 2002 Feb 14;45(4):984-7. | ||||
| REF 3 | The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds. Bioorg Med Chem Lett. 2014 Jan 15;24(2):576-9. | ||||
| REF 4 | Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen. J Med Chem. 1991 Apr;34(4):1436-40. | ||||
| REF 5 | Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity. J Med Chem. 2014 Aug 14;57(15):6739-50. | ||||
| REF 6 | Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1546-51. | ||||
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