| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T20709 | ||||
| Target Name | Muscarinic acetylcholine receptor M4 (CHRM4) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Atropine | Drug Info | Ki = 1.25 nM | [17] | |
| Darifenacin | Drug Info | Ki = 19.9 nM | [17] | ||
| Pirenzepine | Drug Info | Ki = 39.8 nM | [17] | ||
| Tolterodine | Drug Info | Ki = 12.5 nM | [17] | ||
| Tropicamide | Drug Info | IC50 = 8 nM | [18] | ||
| 1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione | Drug Info | IC50 = 15 nM | [11] | ||
| 1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea | Drug Info | Ki = 10700 nM | [2] | ||
| 2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one | Drug Info | Ki = 6.7 nM | [16] | ||
| 2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime | Drug Info | IC50 = 1928 nM | |||
| 3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one | Drug Info | IC50 = 5696 nM | |||
| 3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane | Drug Info | IC50 = 16000 nM | [3] | ||
| 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [9] | ||
| 6-Dimethylamino-2-methyl-hex-4-ynal oxime | Drug Info | IC50 = 13230 nM | |||
| 7-Dimethylamino-3-methyl-hept-5-yn-2-one | Drug Info | IC50 = 101 nM | |||
| 7-Dimethylamino-hept-5-yn-2-one | Drug Info | IC50 = 68 nM | |||
| 7-Pyrrolidin-1-yl-hept-5-yn-2-one | Drug Info | IC50 = 7280 nM | |||
| ACECLIDINE | Drug Info | IC50 = 510 nM | [14] | ||
| Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester | Drug Info | Ki = 33 nM | [15] | ||
| Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester | Drug Info | Ki = 440 nM | [1] | ||
| BRL-55473 | Drug Info | IC50 = 470 nM | |||
| Cremastrine | Drug Info | IC50 = 498 nM | [4] | ||
| FLUMEZAPINE | Drug Info | IC50 = 80 nM | [10] | ||
| FM1-10 | Drug Info | Ki = 121 nM | [6] | ||
| FM1-43 | Drug Info | Ki = 103 nM | [6] | ||
| GNF-PF-5618 | Drug Info | Ki = 140 nM | [5] | ||
| ISOCLOZAPINE | Drug Info | IC50 = 55 nM | [8] | ||
| ISOLOXAPINE | Drug Info | IC50 = 49 nM | [13] | ||
| Methacholine Chloride | Drug Info | Ki = 1600 nM | [15] | ||
| N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide | Drug Info | IC50 = 21.6 nM | |||
| N-DESMETHYLCLOZAPINE | Drug Info | Ki = 290 nM | [9] | ||
| N-methoxyquinuclidine-3-carboximidoyl chloride | Drug Info | IC50 = 1100 nM | |||
| N-methoxyquinuclidine-3-carboximidoyl fluoride | Drug Info | IC50 = 2000 nM | |||
| PF-3409409 | Drug Info | Ki = 4300 nM | [7] | ||
| Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester | Drug Info | Ki = 85 nM | [1] | ||
| SULFOARECOLINE | Drug Info | IC50 = 1.4 nM | [12] | ||
| References | |||||
| REF 1 | 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 2 | Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. J Med Chem. 1992 Aug 21;35(17):3270-9. | ||||
| REF 3 | Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives. J Med Chem. 1992 Apr 3;35(7):1280-90. | ||||
| REF 4 | Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata. J Nat Prod. 2005 Apr;68(4):572-3. | ||||
| REF 5 | Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. J Nat Prod. 2005 Jul;68(7):1061-5. | ||||
| REF 6 | Design and synthesis of a fluorescent muscarinic antagonist. Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. | ||||
| REF 7 | Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. | ||||
| REF 8 | Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. J Med Chem. 1990 Feb;33(2):809-14. | ||||
| 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 | Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. J Med Chem. 1989 Dec;32(12):2573-82. | ||||
| REF 11 | Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist. J Med Chem. 1989 May;32(5):1057-62. | ||||
| REF 12 | Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. J Med Chem. 1988 Jul;31(7):1312-6. | ||||
| REF 13 | Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6. | ||||
| REF 14 | Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. J Med Chem. 1993 Apr 2;36(7):842-7. | ||||
| REF 15 | 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. J Med Chem. 1998 Jun 4;41(12):2047-55. | ||||
| REF 16 | Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone. J Med Chem. 1998 Oct 22;41(22):4181-5. | ||||
| REF 17 | Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14. | ||||
| REF 18 | A novel assay of Gi/o-linked G protein-coupled receptor coupling to potassium channels provides new insights into the pharmacology of the group III metabotropic glutamate receptors. Mol Pharmacol. 2008 Apr;73(4):1213-24. | ||||
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