Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T28893 | Target Info | |||
| Target Name | Muscarinic acetylcholine receptor M1 (CHRM1) | ||||
| Synonyms |
M1 receptor
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| Target Type | Successful Target | ||||
| Gene Name | CHRM1 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Glycopyrrolate | Drug Info | IC50 = 0.1585 nM | Click to Show More | [1] | |
| 2 | Pirenzepine | Drug Info | IC50 = 1.148 nM | [3] | ||
| 3 | Arecoline | Drug Info | Ki = 26 nM | [6] | ||
| 4 | Biperiden | Drug Info | Ki = 32.1 nM | [4] | ||
| 5 | N-DESMETHYLCLOZAPINE | Drug Info | Ki = 290 nM | [9] | ||
| 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) | Glycopyrrolate | Drug Info | IC50 = 0.1995 nM | Click to Show More | [1] | |
| 2 | Pirenzepine | Drug Info | Ki = 35.48 nM | [7] | ||
| 3 | N-DESMETHYLCLOZAPINE | Drug Info | Ki = 51 nM | [9] | ||
| 4 | Arecoline | Drug Info | EC50 = 600 nM | [5] | ||
| 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) | Glycopyrrolate | Drug Info | IC50 = 0.2512 nM | Click to Show More | [1] | |
| 2 | Biperiden | Drug Info | Ki = 5.95 nM | [4] | ||
| 3 | Pirenzepine | Drug Info | Ki = 47.86 nM | [8] | ||
| 4 | N-DESMETHYLCLOZAPINE | Drug Info | Ki = 90 nM | [9] | ||
| 5 | Arecoline | Drug Info | EC50 = 100 nM | [10] | ||
| Co-Target Name | Thyroid hormone receptor beta (THRB) | Successful Target | ||||
| UniProt ID | THB_HUMAN | |||||
| Gene Name | THRB | |||||
| Synonyms |
c-erbA-beta; c-erbA-2; THR1; Nuclear receptor subfamily 1 group A member 2; NR1A2; ERBA2
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| Representative Drug(s) | B7-2/GM-CSF | Drug Info | Ki = 0.32 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) | Glycopyrrolate | Drug Info | IC50 = 0.5012 nM | Click to Show More | [1] | |
| 2 | Biperiden | Drug Info | Ki = 13.7 nM | [4] | ||
| 3 | Arecoline | Drug Info | EC50 = 25 nM | [5] | ||
| 4 | Pirenzepine | Drug Info | Ki = 173.78 nM | [8] | ||
| 5 | N-DESMETHYLCLOZAPINE | Drug Info | Ki = 250 nM | [9] | ||
| Co-Target Name | Thyroid hormone receptor alpha (THRA) | Successful Target | ||||
| UniProt ID | THA_HUMAN | |||||
| Gene Name | THRA | |||||
| Synonyms |
V-erbA-related protein 7; THRA2; THRA1; Nuclear receptor subfamily 1 group A member 1; NR1A1; ERBA1; EAR7; EAR-7; C-erbA-alpha; C-erbA-1
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| Representative Drug(s) | B7-2/GM-CSF | Drug Info | Ki = 1.09 nM | [2] | ||
| Co-Target Name | Dopamine transporter (DAT) | Successful Target | ||||
| UniProt ID | SC6A3_HUMAN | |||||
| Gene Name | SLC6A3 | |||||
| Synonyms |
Solute carrier family 6 member 3; Sodium-dependent dopamine transporter; DAT1; DAT; DA transporter
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| Representative Drug(s) | Benztropine | Drug Info | IC50 = 312 nM | [11] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | The discovery of new spirocyclic muscarinic M3 antagonists. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7458-61. | ||||
| REF 2 | Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. J Med Chem. 2008 Nov 27;51(22):7075-93. | ||||
| REF 3 | Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). J Med Chem. 2014 Nov 13;57(21):9065-77. | ||||
| REF 4 | Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods. Bioorg Med Chem. 2013 May 1;21(9):2651-62. | ||||
| REF 5 | Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. J Med Chem. 1995 Jun 9;38(12):2188-95. | ||||
| REF 6 | 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. J Med Chem. 2000 Jun 29;43(13):2514-22. | ||||
| REF 7 | Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. Bioorg Med Chem. 2007 Dec 15;15(24):7626-37. | ||||
| REF 8 | Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics. Bioorg Med Chem. 2008 Aug 1;16(15):7311-20. | ||||
| REF 9 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | ||||
| REF 10 | A novel class of conformationally restricted heterocyclic muscarinic agonists. J Med Chem. 1986 Jun;29(6):1004-9. | ||||
| REF 11 | The discovery of an unusually selective and novel cocaine analog: difluoropine. Synthesis and inhibition of binding at cocaine recognition sites. J Med Chem. 1994 Jun 24;37(13):2001-10. | ||||
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