Target Validation Information
Target ID T46185
Target Name Muscarinic acetylcholine receptor M2
Target Type
Successful
Drug Potency against Target 7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info IC50 = 101 nM
Pirenzepine Drug Info Ki = 316 nM [552263]
BRL-55473 Drug Info IC50 = 470 nM
Darifenacin Drug Info Ki = 100 nM [552263]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info Ki = 10700 nM [527029]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
SCH-211803 Drug Info Ki = 0.89 nM [526473]
FM1-43 Drug Info Ki = 55 nM [529178]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 190 nM [525826]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info Ki = 6.7 nM [534723]
Gallamine Triethiodide Drug Info IC50 = 590nM [538090]
Scopolamine Drug Info IC50 = 2.2 nM
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info IC50 = 1100 nM
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info IC50 = 4460 nM
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info IC50 = 13230 nM
GNF-PF-5618 Drug Info Ki = 630 nM [527653]
METHOCTRAMINE Drug Info Ki = 36 nM [529789]
2-(4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione Drug Info Ki = 100 nM
Tolterodine Drug Info Ki = 7.94 nM [552263]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 6500 nM
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info IC50 = 2000 nM
FLUMEZAPINE Drug Info IC50 = 80 nM [533165]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info IC50 = 16000 nM [527344]
METHACHOLINE Drug Info IC50 = 5200 nM [534645]
1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info IC50 = 15 nM [533345]
N-DESMETHYLCLOZAPINE Drug Info Ki = 250 nM [531079]
CARAMIPEN Drug Info Ki = 31.7 nM [529957]
SULFOARECOLINE Drug Info IC50 = 1.4 nM [533450]
ACECLIDINE Drug Info IC50 = 510 nM [534044]
Atropine Drug Info Ki = 1.58 nM [552263]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info IC50 < 10 nM [530266]
ISOCLOZAPINE Drug Info IC50 = 55 nM [530313]
HIMBACINE Drug Info Ki = 4.5 nM [527126]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 7280 nM
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info IC50 = 5500 nM
FM1-10 Drug Info Ki = 38 nM [529178]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 440 nM [525826]
ISOLOXAPINE Drug Info IC50 = 49 nM [533577]
7-Dimethylamino-hept-5-yn-2-one Drug Info IC50 = 18900 nM
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info IC50 = 120 nM [534645]
Methylscopolamine Drug Info ED50 = 5.0 ug/kg [552206]
References
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 527029J Med Chem. 1992 Aug 21;35(17):3270-9.Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.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.
Ref 526473J Med Chem. 2002 Dec 5;45(25):5415-8.Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Ref 529178Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist.
Ref 525826J Med Chem. 2000 Jun 29;43(13):2514-22.6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.
Ref 534723J Med Chem. 1998 Oct 22;41(22):4181-5.Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.
Ref 538090Neuromuscular relaxants as antagonists for M2 and M3 muscarinic receptors. Anesthesiology. 1998 Mar;88(3):744-50.
Ref 527653J Nat Prod. 2005 Jul;68(7):1061-5.Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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.
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 533165J Med Chem. 1989 Dec;32(12):2573-82.Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics.
Ref 527344J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
Ref 534645J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Ref 533345J Med Chem. 1989 May;32(5):1057-62.Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.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.
Ref 529957J Med Chem. 1991 Oct;34(10):2984-9.Muscarinic receptor binding profile of para-substituted caramiphen analogues.
Ref 533450J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
Ref 534044J Med Chem. 1993 Apr 2;36(7):842-7.Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 530266Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2. Epub 2009 Jul 8.Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.
Ref 530313J Med Chem. 1990 Feb;33(2):809-14.Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
Ref 527126Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70.Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Ref 529178Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist.
Ref 525826J Med Chem. 2000 Jun 29;43(13):2514-22.6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.
Ref 533577J Med Chem. 1981 Sep;24(9):1021-6.Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain.
Ref 534645J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Ref 552206Impaired atrial M(2)-cholinoceptor function in obesity-related hypertension. Hypertension. 1999 Nov;34(5):1066-72.

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