Proteins > Muscarinic acetylcholine receptor M1
Page last updated: 2024-08-07 15:54:13
Muscarinic acetylcholine receptor M1
A muscarinic acetylcholine receptor M1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P11229]
Synonyms
Research
Bioassay Publications (174)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 7 (4.02) | 18.7374 |
| 1990's | 30 (17.24) | 18.2507 |
| 2000's | 50 (28.74) | 29.6817 |
| 2010's | 79 (45.40) | 24.3611 |
| 2020's | 8 (4.60) | 2.80 |
Compounds (185)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 1.4890 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.3590 | 1 | 0 |
| tacrine | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 2.6130 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 0.6290 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0110 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0027 | 1 | 0 |
| amoxapine | Homo sapiens (human) | IC50 | 1.1920 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.2870 | 1 | 0 |
| 1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester | Homo sapiens (human) | Ki | 1.0407 | 2 | 2 |
| arecoline | Homo sapiens (human) | IC50 | 81.4038 | 4 | 4 |
| arecoline | Homo sapiens (human) | Ki | 19.5087 | 3 | 3 |
| astemizole | Homo sapiens (human) | IC50 | 1.0660 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.2570 | 1 | 0 |
| azelastine | Homo sapiens (human) | IC50 | 6.3096 | 1 | 1 |
| bethanechol | Homo sapiens (human) | Ki | 0.0970 | 1 | 1 |
| biperiden | Homo sapiens (human) | Ki | 0.0024 | 1 | 1 |
| carbamylcholine | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| carbetapentane | Homo sapiens (human) | Ki | 0.0760 | 2 | 3 |
| chloroquine | Homo sapiens (human) | Ki | 9.1201 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.0830 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.0729 | 2 | 1 |
| clomipramine | Homo sapiens (human) | IC50 | 0.0910 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0220 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 6.8690 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 1.6540 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0160 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0040 | 2 | 1 |
| dicyclomine | Homo sapiens (human) | IC50 | 0.0035 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | Ki | 0.0008 | 1 | 0 |
| diphenidol | Homo sapiens (human) | IC50 | 0.3240 | 1 | 0 |
| diphenidol | Homo sapiens (human) | Ki | 0.0780 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | IC50 | 0.3460 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 0.0830 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.0770 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0180 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.8734 | 2 | 2 |
| ebastine | Homo sapiens (human) | Ki | 0.1012 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 2.6420 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 0.6360 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 2.6830 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 0.6460 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | IC50 | 3.2030 | 1 | 0 |
| fluoxetine | Homo sapiens (human) | Ki | 0.7710 | 1 | 0 |
| gallamine triethiodide | Homo sapiens (human) | Ki | 8.5114 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 5.5000 | 2 | 2 |
| haloperidol | Homo sapiens (human) | Ki | 2.6233 | 3 | 3 |
| hydroxychloroquine | Homo sapiens (human) | Ki | 15.4882 | 1 | 1 |
| ketotifen | Homo sapiens (human) | IC50 | 1.1120 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 0.2680 | 1 | 0 |
| loxapine | Homo sapiens (human) | IC50 | 5.5000 | 1 | 1 |
| maprotiline | Homo sapiens (human) | IC50 | 0.5930 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.1430 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | IC50 | 4.7730 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 1.1500 | 1 | 0 |
| methoctramine | Homo sapiens (human) | Ki | 0.0665 | 2 | 2 |
| n-methylcarbamylcholine | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| 5-methylfurtrethonium | Homo sapiens (human) | Ki | 7.9433 | 1 | 1 |
| mianserin | Homo sapiens (human) | IC50 | 1.4230 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 0.3430 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 3.9710 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 0.9560 | 1 | 0 |
| minaprine | Homo sapiens (human) | Ki | 17.0000 | 1 | 1 |
| mitoxantrone | Homo sapiens (human) | IC50 | 0.7487 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | Ki | 0.1803 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.0820 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.0200 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | IC50 | 0.1480 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 0.0360 | 1 | 0 |
| oxotremorine | Homo sapiens (human) | IC50 | 12.0341 | 3 | 3 |
| oxotremorine | Homo sapiens (human) | Ki | 0.0091 | 2 | 2 |
| oxybutynin | Homo sapiens (human) | IC50 | 0.0035 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | Ki | 0.0014 | 3 | 2 |
| perhexiline | Homo sapiens (human) | IC50 | 2.7105 | 1 | 0 |
| perhexiline | Homo sapiens (human) | Ki | 0.6528 | 1 | 0 |
| pirenzepine | Homo sapiens (human) | IC50 | 0.0291 | 14 | 14 |
| pirenzepine | Homo sapiens (human) | Ki | 0.0566 | 13 | 13 |
| prochlorperazine | Homo sapiens (human) | IC50 | 1.0130 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 0.2440 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 0.4870 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.1170 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.0140 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.0033 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| pyridostigmine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| quetiapine | Homo sapiens (human) | IC50 | 2.6150 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 0.4408 | 5 | 4 |
| risperidone | Homo sapiens (human) | Ki | 4.2667 | 3 | 3 |
| spiperone | Homo sapiens (human) | Ki | 49.6000 | 1 | 1 |
| sulconazole | Homo sapiens (human) | IC50 | 3.6750 | 1 | 0 |
| sulconazole | Homo sapiens (human) | Ki | 0.8850 | 1 | 0 |
| terfenadine | Homo sapiens (human) | IC50 | 2.9000 | 1 | 2 |
| thioridazine | Homo sapiens (human) | IC50 | 0.0070 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0017 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | IC50 | 0.0056 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | Ki | 0.0014 | 1 | 0 |
| tropicamide | Homo sapiens (human) | IC50 | 0.2810 | 1 | 0 |
| tropicamide | Homo sapiens (human) | Ki | 0.0680 | 1 | 0 |
| carbachol | Homo sapiens (human) | IC50 | 41.1368 | 4 | 4 |
| carbachol | Homo sapiens (human) | Ki | 135.4539 | 18 | 18 |
| pilocarpine | Homo sapiens (human) | Ki | 7.2751 | 2 | 2 |
| (4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride | Homo sapiens (human) | Ki | 1.9498 | 2 | 2 |
| mepazine | Homo sapiens (human) | IC50 | 0.0790 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.0190 | 1 | 0 |
| cyclizine | Homo sapiens (human) | IC50 | 0.6750 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.1630 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 0.4120 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.0990 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 0.0330 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.0079 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| muscarine | Homo sapiens (human) | Ki | 9.1265 | 2 | 2 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 0.4510 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 0.1090 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 1.0950 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.2640 | 1 | 0 |
| glycopyrrolate | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| Berberine chloride (TN) | Homo sapiens (human) | IC50 | 3.0800 | 1 | 0 |
| Berberine chloride (TN) | Homo sapiens (human) | Ki | 0.7420 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 18.0130 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 4.3380 | 1 | 0 |
| 2-chloro-11-(4-methyl-1-piperazinyl)-5h-dibenzo(b,e)(1,4)diazepine | Homo sapiens (human) | IC50 | 0.0060 | 2 | 2 |
| benzetimide | Homo sapiens (human) | IC50 | 5.0005 | 1 | 2 |
| dimethindene | Homo sapiens (human) | Ki | 0.2630 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | Ki | 0.0002 | 4 | 6 |
| clemastine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| pizotyline | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 1.3830 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 0.3330 | 1 | 0 |
| butaclamol | Homo sapiens (human) | Ki | 5.2000 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 0.1450 | 1 | 0 |
| paroxetine | Homo sapiens (human) | Ki | 0.0350 | 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 |
| xanomeline | Homo sapiens (human) | IC50 | 1.3967 | 6 | 6 |
| xanomeline | Homo sapiens (human) | Ki | 0.6829 | 10 | 10 |
| ziprasidone | Homo sapiens (human) | Ki | 6.7000 | 3 | 3 |
| mizolastine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| trihexyphenidyl hydrochloride | Homo sapiens (human) | IC50 | 0.0013 | 1 | 1 |
| diphenidol hydrochloride | Homo sapiens (human) | Ki | 0.4266 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 1.2882 | 1 | 0 |
| sertraline | Homo sapiens (human) | Ki | 0.3102 | 1 | 0 |
| esaprazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| aprofen | Homo sapiens (human) | Ki | 0.0235 | 5 | 5 |
| n-methylscopolamine | Homo sapiens (human) | IC50 | 0.0018 | 1 | 1 |
| n-methylscopolamine | Homo sapiens (human) | Ki | 0.0002 | 6 | 6 |
| gr 127935 | Homo sapiens (human) | Ki | 4.0000 | 3 | 3 |
| afdx 116 | Homo sapiens (human) | Ki | 0.5370 | 1 | 1 |
| 7-methoxytacrine | Homo sapiens (human) | IC50 | 3.7100 | 1 | 1 |
| afdx 384 | Homo sapiens (human) | Ki | 0.0309 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 0.2670 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.0640 | 1 | 0 |
| l 670548 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| azaprophen | Homo sapiens (human) | Ki | 0.0002 | 2 | 2 |
| aq-ra 741 | Homo sapiens (human) | Ki | 0.0395 | 2 | 2 |
| bibn 99 | Homo sapiens (human) | Ki | 1.0715 | 1 | 1 |
| tripitramine | Homo sapiens (human) | Ki | 0.0026 | 2 | 2 |
| solifenacin | Homo sapiens (human) | Ki | 0.0513 | 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 | 0.0015 | 1 | 0 |
| atropine | Homo sapiens (human) | Ki | 0.0010 | 14 | 16 |
| sb 203580 | Homo sapiens (human) | IC50 | 10.6660 | 1 | 0 |
| sb 203580 | Homo sapiens (human) | Ki | 2.5690 | 1 | 0 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| solifenacin succinate | Homo sapiens (human) | IC50 | 0.0635 | 1 | 1 |
| 5-((4-(4-(diethylamino)butyl)-1-piperidinyl)acetyl)-10,11-dihydrobenzo(b,e)(1,4)diazepine-11-one | Homo sapiens (human) | Ki | 0.0031 | 4 | 4 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| terconazole | Homo sapiens (human) | IC50 | 5.7090 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 1.3750 | 1 | 0 |
| brucine | Homo sapiens (human) | Ki | 44.6684 | 1 | 1 |
| tolterodine | Homo sapiens (human) | Ki | 0.0014 | 1 | 1 |
| darifenacin | Homo sapiens (human) | Ki | 0.0055 | 2 | 2 |
| diethylstilbestrol | Homo sapiens (human) | IC50 | 15.1710 | 1 | 0 |
| diethylstilbestrol | Homo sapiens (human) | Ki | 3.6540 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | IC50 | 4.5050 | 1 | 0 |
| (1S,2R)-2-(octylamino)-1-[4-(propan-2-ylthio)phenyl]-1-propanol | Homo sapiens (human) | Ki | 1.0850 | 1 | 0 |
| ipratropium bromide anhydrous | Homo sapiens (human) | IC50 | 0.0028 | 2 | 2 |
| ipratropium bromide anhydrous | Homo sapiens (human) | Ki | 0.0010 | 2 | 2 |
| methamilane methiodide | Homo sapiens (human) | Ki | 10.9648 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | IC50 | 0.0004 | 1 | 1 |
| 4,4-dicarboxy-5-pyridoxylproline | Homo sapiens (human) | Ki | 19.9526 | 1 | 1 |
| flunarizine | Homo sapiens (human) | IC50 | 2.9360 | 1 | 0 |
| flunarizine | Homo sapiens (human) | Ki | 0.7070 | 1 | 0 |
| benztropine | Homo sapiens (human) | IC50 | 0.0005 | 1 | 0 |
| benztropine | Homo sapiens (human) | Ki | 0.0001 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | IC50 | 2.5130 | 1 | 0 |
| cinnarizine | Homo sapiens (human) | Ki | 0.6050 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 1.6280 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 0.3920 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 2.8290 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 0.6810 | 1 | 0 |
| vicriviroc | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | IC50 | 0.0045 | 1 | 1 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | Ki | 0.0011 | 1 | 1 |
| ml012 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Homo sapiens (human) | Ki | 0.0116 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| montelukast | Homo sapiens (human) | IC50 | 8.0450 | 1 | 0 |
| montelukast | Homo sapiens (human) | Ki | 1.9380 | 1 | 0 |
| trospium chloride | Homo sapiens (human) | Ki | 0.0035 | 1 | 1 |
| oxiconazole | Homo sapiens (human) | IC50 | 4.7364 | 1 | 0 |
| oxiconazole | Homo sapiens (human) | Ki | 1.1407 | 1 | 0 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | IC50 | 0.1310 | 1 | 0 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | Ki | 0.0320 | 1 | 0 |
| himbacine | Homo sapiens (human) | IC50 | 0.5482 | 1 | 1 |
| himbacine | Homo sapiens (human) | Ki | 0.0851 | 4 | 5 |
| fm1 43 | Homo sapiens (human) | Ki | 0.0440 | 1 | 1 |
| milameline | Homo sapiens (human) | Ki | 5.6234 | 1 | 1 |
| sabcomeline | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| sabcomeline | Homo sapiens (human) | Ki | 0.2291 | 1 | 1 |
| pd 144418 | Homo sapiens (human) | Ki | 31.6228 | 1 | 1 |
| lissamine rhodamine b | Homo sapiens (human) | Ki | 1,000.0000 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | IC50 | 3.9811 | 1 | 1 |
| linagliptin | Homo sapiens (human) | IC50 | 0.2967 | 3 | 3 |
| iperoxo | Homo sapiens (human) | IC50 | 0.0013 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | IC50 | 0.8793 | 2 | 2 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 0.3162 | 1 | 1 |
| 6-chlorotacrine | Homo sapiens (human) | IC50 | 6.0900 | 1 | 1 |
| PB28 | Homo sapiens (human) | Ki | 23.4423 | 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 | 0.0001 | 3 | 3 |
| tiotropium bromide | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| aclidinium bromide | Homo sapiens (human) | IC50 | 0.0001 | 2 | 2 |
| aclidinium bromide | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| scopolamine hydrobromide | Homo sapiens (human) | IC50 | 0.0026 | 5 | 5 |
| scopolamine hydrobromide | Homo sapiens (human) | Ki | 0.0075 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| srt1720 | Homo sapiens (human) | IC50 | 8.0200 | 1 | 1 |
| pf 3246799 | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| entecavir | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
| entecavir | Homo sapiens (human) | Ki | 0.0970 | 1 | 0 |
| clozapine | Homo sapiens (human) | IC50 | 0.0096 | 3 | 2 |
| clozapine | Homo sapiens (human) | Ki | 0.0079 | 6 | 5 |
| olanzapine | Homo sapiens (human) | Ki | 0.0107 | 4 | 4 |
| norclozapine | Homo sapiens (human) | Ki | 0.0603 | 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 |
| oxybutynin | Homo sapiens (human) | Kb | 0.0100 | 1 | 1 |
| pirenzepine | Homo sapiens (human) | KA | 0.0110 | 1 | 1 |
| carbachol | Homo sapiens (human) | ED50 | 5.6000 | 2 | 2 |
| uridine triphosphate | Homo sapiens (human) | Km | 15.0000 | 1 | 1 |
| metergoline | Homo sapiens (human) | Activity | 0.0012 | 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 |
| afdx 116 | Homo sapiens (human) | KA | 6.8100 | 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 |
| atropine | Homo sapiens (human) | Kb | 0.0004 | 1 | 1 |
| 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | Homo sapiens (human) | Activity | 0.6600 | 3 | 3 |
| 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | Homo sapiens (human) | IP | 0.7235 | 8 | 8 |
| 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid | Homo sapiens (human) | Kb | 26.5000 | 2 | 2 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | KA | 0.0210 | 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
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
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 In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
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
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
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
Design, synthesis and binding affinity of acetylcholine carbamoyl analogues.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 23, Issue:23, 2013
Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
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
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
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
Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
[no title available],
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 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
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
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 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.European journal of medicinal chemistry, , Mar-06, Volume: 92, 2015
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 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
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
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
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
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
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
On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Identification and characterization of m1 selective muscarinic receptor antagonists1.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.Bioorganic & medicinal chemistry letters, , Oct-04, Volume: 9, Issue:19, 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
Amide, urea, and carbamate analogues of the muscarinic agent [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride.Journal of medicinal chemistry, , Jul-24, Volume: 35, Issue:15, 1992
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
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
[no title available],
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
Fluorination of Photoswitchable Muscarinic Agonists Tunes Receptor Pharmacology and Photochromic Properties.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DJournal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
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
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
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
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
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
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 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
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 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
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
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
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
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
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
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
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
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
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.Bioorganic & medicinal chemistry letters, , Jul-19, Volume: 9, Issue:14, 1999
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
1,2,5-Thiadiazole analogues of aceclidine as potent m1 muscarinic agonists.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
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
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
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
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
Amide, urea, and carbamate analogues of the muscarinic agent [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride.Journal of medicinal chemistry, , Jul-24, Volume: 35, Issue:15, 1992
[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
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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
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
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
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
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
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
Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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
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
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
Synthesis and Pharmacological Evaluation of Heterocyclic Carboxamides: Positive Allosteric Modulators of the MJournal of medicinal chemistry, , 04-12, Volume: 61, Issue:7, 2018
MK-7622: A First-in-Class MACS medicinal chemistry letters, , Jul-12, Volume: 9, Issue:7, 2018
The discovery of VU0486846: steep SAR from a series of MBioorganic & medicinal chemistry letters, , 07-01, Volume: 28, Issue:12, 2018
4-Phenylpyridin-2-one Derivatives: A Novel Class of Positive Allosteric Modulator of the M1 Muscarinic Acetylcholine Receptor.Journal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 25, Issue:2, 2015
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Synthesis and pharmacological evaluation of analogues of benzyl quinolone carboxylic acid (BQCA) designed to bind irreversibly to an allosteric site of the M ₁ muscarinic acetylcholine receptor.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 24, Issue:5, 2014
Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.ACS medicinal chemistry letters, , May-08, Volume: 5, Issue:5, 2014
Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.ACS medicinal chemistry letters, , Dec-13, Volume: 3, Issue:12, 2012
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
N-heterocyclic derived M1 positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
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
Amide, urea, and carbamate analogues of the muscarinic agent [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride.Journal of medicinal chemistry, , Jul-24, Volume: 35, Issue:15, 1992
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
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
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 9, Issue:6, 1999
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 25, Issue:7, 2015
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
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
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
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 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
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
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
Fluorination of Photoswitchable Muscarinic Agonists Tunes Receptor Pharmacology and Photochromic Properties.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Rational design of partial agonists for the muscarinic m1 acetylcholine receptor.Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 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
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
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
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
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine DJournal of medicinal chemistry, , 04-26, Volume: 61, Issue:8, 2018
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
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
Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 25, Issue:2, 2015
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 23, Issue:2, 2013
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Discovery of ML326: The first sub-micromolar, selective M5 PAM.Bioorganic & medicinal chemistry letters, , May-15, Volume: 23, Issue:10, 2013
Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 21, Issue:21, 2011
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
Multi-receptor drug design: Haloperidol as a scaffold for the design and synthesis of atypical antipsychotic agents.Bioorganic & medicinal chemistry, , Feb-01, Volume: 20, Issue:3, 2012
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.Journal of medicinal chemistry, , Jun-17, Volume: 42, Issue:12, 1999
Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
[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
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
Current and novel approaches to the drug treatment of schizophrenia.Journal of medicinal chemistry, , Feb-15, Volume: 44, Issue:4, 2001
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
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
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 4 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] |
| 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 8 target(s):
| Target | Category | Definition |
|---|
| 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
| Schaffer collateral - CA1 synapse | cellular component | A synapse between the Schaffer collateral axon of a CA3 pyramidal cell and a CA1 pyramidal cell. [PMID:16399689] |
| postsynaptic density membrane | cellular component | The membrane component of the postsynaptic density. This is the region of the postsynaptic membrane in which the population of neurotransmitter receptors involved in synaptic transmission are concentrated. [GOC:dos] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
| cholinergic synapse | cellular component | A synapse that uses acetylcholine as a neurotransmitter. [GOC:dos] |
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] |
| 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] |
| 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] |
Involved In
This protein is involved in 18 target(s):
| Target | Category | Definition |
|---|
| 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] |
| protein kinase C-activating 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 with activation of protein kinase C (PKC). PKC is activated by second messengers including diacylglycerol (DAG). [GOC:mah, GOC:signaling] |
| 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] |
| neuromuscular synaptic transmission | biological process | The process of synaptic transmission from a neuron to a muscle, across a synapse. [GOC:dos, GOC:jl, MeSH:D009435] |
| 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] |
| regulation of locomotion | biological process | Any process that modulates the frequency, rate or extent of locomotion of a cell or organism. [GOC:ems] |
| 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] |
| cognition | biological process | The operation of the mind by which an organism becomes aware of objects of thought or perception; it includes the mental activities associated with thinking, learning, and memory. [ISBN:0721619908] |
| regulation of postsynaptic membrane potential | biological process | Any process that modulates the potential difference across a post-synaptic membrane. [GOC:dph, GOC:ef] |
| regulation of glial cell proliferation | biological process | Any process that modulates the frequency, rate or extent of glial cell proliferation. [GOC:dph, GOC:tb] |
| positive regulation of intracellular protein transport | biological process | Any process that activates or increases the frequency, rate or extent of the directed movement of proteins within cells. [GOC:tb] |
| 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] |
| postsynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the postsynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| 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] |