Proteins > Muscarinic acetylcholine receptor M3
Page last updated: 2024-08-07 16:09:03
Muscarinic acetylcholine receptor M3
A muscarinic acetylcholine receptor M3 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P20309]
Synonyms
Research
Bioassay Publications (127)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 7 (5.51) | 18.7374 |
| 1990's | 15 (11.81) | 18.2507 |
| 2000's | 37 (29.13) | 29.6817 |
| 2010's | 56 (44.09) | 24.3611 |
| 2020's | 12 (9.45) | 2.80 |
Compounds (167)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 1.2550 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.2660 | 1 | 0 |
| amiodarone | Homo sapiens (human) | IC50 | 3.2010 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 0.6790 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0260 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0054 | 1 | 0 |
| amoxapine | Homo sapiens (human) | IC50 | 1.7810 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.3780 | 1 | 0 |
| 1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester | Homo sapiens (human) | Ki | 0.8511 | 1 | 1 |
| arecoline | Homo sapiens (human) | IC50 | 34.5000 | 2 | 2 |
| arecoline | Homo sapiens (human) | Ki | 24.3500 | 2 | 2 |
| astemizole | Homo sapiens (human) | IC50 | 0.8400 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.1780 | 1 | 0 |
| bethanechol | Homo sapiens (human) | Ki | 0.0970 | 1 | 1 |
| biperiden | Homo sapiens (human) | Ki | 0.0060 | 1 | 1 |
| carbamylcholine | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| chloroquine | Homo sapiens (human) | Ki | 3.3113 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.2060 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0440 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | IC50 | 14.9470 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 3.1680 | 1 | 0 |
| clomipramine | Homo sapiens (human) | IC50 | 0.1700 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0360 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 9.9280 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 2.1040 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0460 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0068 | 2 | 1 |
| dicyclomine | Homo sapiens (human) | IC50 | 0.0044 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | Ki | 0.0009 | 1 | 0 |
| diphenidol | Homo sapiens (human) | IC50 | 0.2450 | 1 | 0 |
| diphenidol | Homo sapiens (human) | Ki | 0.0520 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | IC50 | 0.6470 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 0.1370 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0690 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0150 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.6475 | 1 | 0 |
| ebastine | Homo sapiens (human) | Ki | 0.1372 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 1.7890 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 0.3790 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 4.7280 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 1.0020 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | IC50 | 3.5950 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | Ki | 0.7620 | 1 | 0 |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester | Homo sapiens (human) | IC50 | 0.0002 | 2 | 2 |
| haloperidol | Homo sapiens (human) | Ki | 4.6700 | 1 | 1 |
| hydroxychloroquine | Homo sapiens (human) | Ki | 4.7863 | 1 | 1 |
| ketotifen | Homo sapiens (human) | IC50 | 2.2090 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 0.4680 | 1 | 0 |
| maprotiline | Homo sapiens (human) | IC50 | 0.4730 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.1000 | 1 | 0 |
| methoctramine | Homo sapiens (human) | Ki | 0.4009 | 2 | 2 |
| n-methylcarbamylcholine | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| 5-methylfurtrethonium | Homo sapiens (human) | Ki | 6.1659 | 1 | 1 |
| mianserin | Homo sapiens (human) | IC50 | 1.4050 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 0.2980 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 3.1540 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 0.6680 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.1710 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0360 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | IC50 | 0.1750 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 0.0370 | 1 | 0 |
| oxotremorine | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| oxybutynin | Homo sapiens (human) | IC50 | 0.0027 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | Ki | 0.0010 | 4 | 3 |
| perhexiline | Homo sapiens (human) | IC50 | 3.1186 | 1 | 0 |
| perhexiline | Homo sapiens (human) | Ki | 0.6610 | 1 | 0 |
| pirenzepine | Homo sapiens (human) | IC50 | 0.9556 | 1 | 1 |
| pirenzepine | Homo sapiens (human) | Ki | 0.2453 | 3 | 3 |
| prochlorperazine | Homo sapiens (human) | IC50 | 1.5140 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.3210 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.4160 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.0880 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.0200 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.0041 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| pyridostigmine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| quetiapine | Homo sapiens (human) | Ki | 1.0200 | 1 | 1 |
| risperidone | Homo sapiens (human) | IC50 | 55.0000 | 2 | 2 |
| risperidone | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| spiperone | Homo sapiens (human) | Ki | 49.6000 | 1 | 1 |
| sulconazole | Homo sapiens (human) | IC50 | 3.4040 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 0.7210 | 1 | 0 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0900 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | IC50 | 0.0150 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | Ki | 0.0032 | 1 | 0 |
| tropicamide | Homo sapiens (human) | IC50 | 0.1420 | 1 | 0 |
| tropicamide | Homo sapiens (human) | Ki | 0.0300 | 1 | 0 |
| carbachol | Homo sapiens (human) | IC50 | 4.9900 | 2 | 2 |
| carbachol | Homo sapiens (human) | Ki | 30.1886 | 10 | 10 |
| (4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride | Homo sapiens (human) | Ki | 2.3988 | 2 | 2 |
| mepazine | Homo sapiens (human) | IC50 | 0.1910 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.0400 | 1 | 0 |
| mepenzolate bromide | Homo sapiens (human) | Ki | 0.0040 | 2 | 2 |
| cyclizine | Homo sapiens (human) | IC50 | 0.7480 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.1590 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 0.3830 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.0810 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.0073 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 0.4470 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 0.0950 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 4.3300 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.9180 | 1 | 0 |
| glycopyrrolate | Homo sapiens (human) | IC50 | 0.0003 | 1 | 1 |
| glycopyrrolate | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 19.0040 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 4.0280 | 1 | 0 |
| benzetimide | Homo sapiens (human) | IC50 | 5.0005 | 1 | 2 |
| dimethindene | Homo sapiens (human) | Ki | 0.1906 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | Ki | 0.0002 | 4 | 6 |
| clemastine | Homo sapiens (human) | IC50 | 0.0390 | 1 | 0 |
| clemastine | Homo sapiens (human) | Ki | 0.0322 | 2 | 1 |
| danazol | Homo sapiens (human) | IC50 | 17.7470 | 1 | 0 |
| danazol | Homo sapiens (human) | Ki | 3.7620 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 2.5790 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 0.5470 | 1 | 0 |
| butaclamol | Homo sapiens (human) | Ki | 5.2000 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 0.1790 | 1 | 0 |
| paroxetine | Homo sapiens (human) | Ki | 0.0380 | 1 | 0 |
| n-methyl-n-(1-methyl-4-pyrrolidino-2-butynyl)acetamide | Homo sapiens (human) | Ki | 0.3300 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| aripiprazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| xanomeline | Homo sapiens (human) | Ki | 0.0449 | 4 | 4 |
| ziprasidone | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| trihexyphenidyl hydrochloride | Homo sapiens (human) | IC50 | 0.0263 | 1 | 1 |
| diphenidol hydrochloride | Homo sapiens (human) | Ki | 1.1220 | 1 | 1 |
| esaprazole | Homo sapiens (human) | IC50 | 87.0000 | 1 | 1 |
| aprofen | Homo sapiens (human) | Ki | 1.9604 | 4 | 4 |
| n-methylscopolamine | Homo sapiens (human) | IC50 | 0.0011 | 1 | 1 |
| n-methylscopolamine | Homo sapiens (human) | Ki | 0.0001 | 3 | 3 |
| enpiperate | Homo sapiens (human) | Ki | 0.0011 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 4.0000 | 2 | 3 |
| afdx 116 | Homo sapiens (human) | Ki | 2.0890 | 1 | 1 |
| afdx 384 | Homo sapiens (human) | Ki | 0.0661 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 0.4460 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.0950 | 1 | 0 |
| l 670548 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| azaprophen | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| aq-ra 741 | Homo sapiens (human) | Ki | 0.0816 | 2 | 2 |
| bibn 99 | Homo sapiens (human) | Ki | 0.7762 | 1 | 1 |
| tripitramine | Homo sapiens (human) | Ki | 0.0930 | 2 | 2 |
| solifenacin | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| solifenacin | Homo sapiens (human) | Ki | 0.0132 | 1 | 1 |
| hyoscyamine | Homo sapiens (human) | Ki | 0.0003 | 1 | 2 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| atropine | Homo sapiens (human) | IC50 | 0.0021 | 1 | 0 |
| atropine | Homo sapiens (human) | Ki | 0.0011 | 10 | 11 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| solifenacin succinate | Homo sapiens (human) | IC50 | 0.1308 | 1 | 1 |
| 5-((4-(4-(diethylamino)butyl)-1-piperidinyl)acetyl)-10,11-dihydrobenzo(b,e)(1,4)diazepine-11-one | Homo sapiens (human) | Ki | 0.0100 | 3 | 3 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| terconazole | Homo sapiens (human) | IC50 | 14.5370 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 3.0810 | 1 | 0 |
| tolterodine | Homo sapiens (human) | Ki | 0.0035 | 4 | 4 |
| darifenacin | Homo sapiens (human) | Ki | 2.5007 | 4 | 4 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 18.4320 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 3.9070 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 4.6238 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 0.9800 | 1 | 0 |
| ipratropium bromide anhydrous | Homo sapiens (human) | IC50 | 0.0019 | 2 | 2 |
| ipratropium bromide anhydrous | Homo sapiens (human) | Ki | 0.0004 | 5 | 5 |
| ipratropium | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| methamilane methiodide | Homo sapiens (human) | Ki | 13.4896 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | IC50 | 0.0009 | 1 | 1 |
| 4,4-dicarboxy-5-pyridoxylproline | Homo sapiens (human) | Ki | 19.9526 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 1.4790 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.3130 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.0106 | 2 | 1 |
| benztropine | Homo sapiens (human) | Ki | 0.0003 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 0.7620 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.1620 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 2.0710 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.4390 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 2.9740 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 0.6300 | 1 | 0 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | IC50 | 0.0014 | 9 | 9 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | Ki | 0.0007 | 7 | 7 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 6.6260 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 1.4040 | 1 | 0 |
| trospium chloride | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| oxiconazole | Homo sapiens (human) | IC50 | 4.5310 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 0.9604 | 1 | 0 |
| n-methylscopolamine bromide | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| tiotropium bromide | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| tiotropium | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | IC50 | 0.0760 | 1 | 0 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
| himbacine | Homo sapiens (human) | IC50 | 0.3336 | 1 | 1 |
| himbacine | Homo sapiens (human) | Ki | 0.0971 | 2 | 3 |
| fm1 43 | Homo sapiens (human) | Ki | 0.0300 | 1 | 1 |
| sabcomeline | Homo sapiens (human) | IC50 | 0.0600 | 1 | 1 |
| pd 144418 | Homo sapiens (human) | Ki | 23.9883 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.9000 | 2 | 2 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | IC50 | 2.3221 | 1 | 2 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | Ki | 0.4300 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 1.2023 | 1 | 1 |
| batefenterol | Homo sapiens (human) | IC50 | 0.0016 | 1 | 1 |
| batefenterol | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| PB28 | Homo sapiens (human) | Ki | 19.4985 | 1 | 1 |
| amd 070 | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| tiotropium bromide | Homo sapiens (human) | IC50 | 0.0002 | 5 | 5 |
| tiotropium bromide | Homo sapiens (human) | Ki | 0.0000 | 17 | 17 |
| aclidinium bromide | Homo sapiens (human) | IC50 | 0.0001 | 4 | 4 |
| aclidinium bromide | Homo sapiens (human) | Ki | 0.0003 | 2 | 2 |
| td-4208 | Homo sapiens (human) | Ki | 0.0050 | 2 | 0 |
| scopolamine hydrobromide | Homo sapiens (human) | Ki | 0.0065 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| alamethicin | Homo sapiens (human) | Ki | 0.6190 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pf 3246799 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| azd9164 | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| entecavir | Homo sapiens (human) | Ki | 0.8900 | 1 | 0 |
| clozapine | Homo sapiens (human) | IC50 | 0.0780 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.0255 | 2 | 1 |
| olanzapine | Homo sapiens (human) | IC50 | 0.3920 | 1 | 0 |
| olanzapine | Homo sapiens (human) | Ki | 0.0545 | 2 | 1 |
| norclozapine | Homo sapiens (human) | Ki | 0.0900 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nifedipine | Homo sapiens (human) | ID50 | 700,000.0050 | 2 | 2 |
| carbachol | Homo sapiens (human) | ED50 | 1.3000 | 2 | 2 |
| metergoline | Homo sapiens (human) | Activity | 0.0038 | 1 | 1 |
| 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester | Homo sapiens (human) | ID50 | 4,000,000.0000 | 1 | 1 |
| 1,4-dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester | Homo sapiens (human) | ID50 | 3,200,000.0000 | 1 | 1 |
| atropine | Homo sapiens (human) | ED50 | 0.0001 | 2 | 2 |
| atropine | Homo sapiens (human) | ID50 | 0.0001 | 1 | 1 |
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
The discovery of AZD9164, a novel muscarinic M3 antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.Bioorganic & medicinal chemistry, , Mar-15, Volume: 15, Issue:6, 2007
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Synthesis and calcium channel antagonist activity of dialkyl 4- (dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylates.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
Synthesis and calcium channel antagonist activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pyridinyl)-3,5-pyridinedicarboxylates.Journal of medicinal chemistry, , Volume: 29, Issue:12, 1986
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
[no title available],
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Identification and characterization of m1 selective muscarinic receptor antagonists1.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Structure-Based Design and Discovery of New MJournal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 19, Issue:3, 2011
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bindJournal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.Bioorganic & medicinal chemistry, , Jul-01, Volume: 22, Issue:13, 2014
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 40, Issue:23, 1997
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
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).Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
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 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bindJournal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.Bioorganic & medicinal chemistry, , May-01, Volume: 21, Issue:9, 2013
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).Journal of medicinal chemistry, , Apr-03, Volume: 35, Issue:7, 1992
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.Journal of medicinal chemistry, , Volume: 30, Issue:5, 1987
1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human MBioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.Bioorganic & medicinal chemistry, , May-01, Volume: 21, Issue:9, 2013
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 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 40, Issue:23, 1997
Synthesis and antimuscarinic activity of some 1-cycloalkyl-1-hydroxy-1-phenyl-3-(4-substituted piperazinyl)-2-propanones and related compounds.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Enantioselectivity of muscarinic antagonists. 2,2-Dicyclohexyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides and related 3-oxides.Journal of medicinal chemistry, , Volume: 31, Issue:9, 1988
Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.Journal of medicinal chemistry, , Volume: 30, Issue:5, 1987
[no title available],
[no title available]European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
[no title available]RSC medicinal chemistry, , Jul-01, Volume: 11, Issue:7, 2020
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-β₂-agonist for the treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , May-01, Volume: 21, Issue:9, 2011
Design and synthesis of a fluorescent muscarinic antagonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
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 pharmacJournal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
Discovery of MJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.Journal of medicinal chemistry, , 01-12, Volume: 60, Issue:1, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.Bioorganic & medicinal chemistry, , Dec-15, Volume: 15, Issue:24, 2007
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Discovery of MJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
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 pharmacJournal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
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 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).Journal of medicinal chemistry, , 07-11, Volume: 62, Issue:13, 2019
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 pharmacJournal of medicinal chemistry, , Mar-26, Volume: 58, Issue:6, 2015
Discovery of ACS medicinal chemistry letters, , May-10, Volume: 9, Issue:5, 2018
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
The discovery of AZD9164, a novel muscarinic M3 antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
The design of a novel series of muscarinic receptor antagonists leading to AZD8683, a potential inhaled treatment for COPD.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
The discovery of AZD9164, a novel muscarinic M3 antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Discovery of ML326: The first sub-micromolar, selective M5 PAM.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.Journal of medicinal chemistry, , Jun-11, Volume: 52, Issue:11, 2009
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
[no title available],
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
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 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Enables
This protein enables 6 target(s):
| Target | Category | Definition |
|---|
| phosphatidylinositol phospholipase C activity | molecular function | Catalysis of the reaction: 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate + H2O = 1,2-diacylglycerol + 1D-myo-inositol 1,4,5-trisphosphate + H+. [EC:3.1.4.11, RHEA:33179] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| G protein-coupled acetylcholine receptor activity | molecular function | Combining with acetylcholine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:fj, GOC:mah] |
| signaling receptor activity | molecular function | Receiving a signal and transmitting it in the cell to initiate a change in cell activity. A signal is a physical entity or change in state that is used to transfer information in order to trigger a response. [GOC:bf, GOC:signaling] |
| acetylcholine binding | molecular function | Binding to acetylcholine, an acetic acid ester of the organic base choline that functions as a neurotransmitter, released at the synapses of parasympathetic nerves and at neuromuscular junctions. [GOC:ai] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 19 target(s):
| Target | Category | Definition |
|---|
| smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. Smooth muscle differs from striated muscle in the much higher actin/myosin ratio, the absence of conspicuous sarcomeres and the ability to contract to a much smaller fraction of its resting length. [GOC:ef, GOC:jl, GOC:mtg_muscle, ISBN:0198506732] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway | biological process | A phospholipase C-activating G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled acetylcholine receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a ligand binding to an acetylcholine receptor on the surface of a target cell, and ends with regulation of a downstream cellular process, e.g. transcription. [GOC:mah, ISBN:0815316194] |
| synaptic transmission, cholinergic | biological process | The vesicular release of acetylcholine from a presynapse, across a chemical synapse, the subsequent activation of dopamine receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:dos, Wikipedia:Cholinergic] |
| nervous system development | biological process | The process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh] |
| positive regulation of insulin secretion | biological process | Any process that activates or increases the frequency, rate or extent of the regulated release of insulin. [GOC:mah] |
| protein modification process | biological process | The covalent alteration of one or more amino acids occurring in proteins, peptides and nascent polypeptides (co-translational, post-translational modifications). Includes the modification of charged tRNAs that are destined to occur in a protein (pre-translation modification). [GOC:bf, GOC:jl] |
| positive regulation of smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| saliva secretion | biological process | The regulated release of saliva from the salivary glands. In man, the saliva is a turbid and slightly viscous fluid, generally of an alkaline reaction, and is secreted by the parotid, submaxillary, and sublingual glands. In the mouth the saliva is mixed with the secretion from the buccal glands. In man and many animals, saliva is an important digestive fluid on account of the presence of the peculiar enzyme, ptyalin. [GOC:curators, UBERON:0001836] |
| acetylcholine receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of an acetylcholine receptor binding to one of its physiological ligands. [GOC:mah] |
| G protein-coupled serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| ion channel modulating, G protein-coupled receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand, where the pathway proceeds through activation or inhibition of an ion channel. [GOC:dos] |
| ligand-gated ion channel signaling pathway | biological process | The series of molecular signals initiated by activation of a ligand-gated ion channel on the surface of a cell. The pathway begins with binding of an extracellular ligand to a ligand-gated ion channel and ends with a molecular function that directly regulates a downstream cellular process, e.g. transcription. [GOC:bhm, PMID:25869137] |
| regulation of smooth muscle contraction | biological process | Any process that modulates the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |