Target Validation Information
TTD ID T46185
Target Name Muscarinic acetylcholine receptor M2 (CHRM2)
Type of Target
Successful
Drug Potency against Target Atropine Drug Info Ki = 1.58 nM [22]
Darifenacin Drug Info Ki = 100 nM [22]
Gallamine Triethiodide Drug Info IC50 = 590nM [20]
Methylscopolamine Drug Info ED50 = 5.0 ug/kg [21]
Pirenzepine Drug Info Ki = 316 nM [22]
Scopolamine Drug Info IC50 = 2.2 nM
Tolterodine Drug Info Ki = 7.94 nM [22]
1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info IC50 = 15 nM [14]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info IC50 < 10 nM [10]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info Ki = 10700 nM [3]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info Ki = 6.7 nM [19]
2-(4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione Drug Info Ki = 100 nM
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info IC50 = 5500 nM
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 6500 nM
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info IC50 = 16000 nM [5]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [12]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info IC50 = 13230 nM
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info IC50 = 101 nM
7-Dimethylamino-hept-5-yn-2-one Drug Info IC50 = 18900 nM
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 7280 nM
ACECLIDINE Drug Info IC50 = 510 nM [17]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info IC50 = 120 nM [18]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 440 nM [1]
BRL-55473 Drug Info IC50 = 470 nM
CARAMIPEN Drug Info Ki = 31.7 nM [9]
FLUMEZAPINE Drug Info IC50 = 80 nM [13]
FM1-10 Drug Info Ki = 38 nM [7]
FM1-43 Drug Info Ki = 55 nM [7]
GNF-PF-5618 Drug Info Ki = 630 nM [6]
HIMBACINE Drug Info Ki = 4.5 nM [4]
ISOCLOZAPINE Drug Info IC50 = 55 nM [11]
ISOLOXAPINE Drug Info IC50 = 49 nM [16]
Methacholine Chloride Drug Info IC50 = 5200 nM [18]
METHOCTRAMINE Drug Info Ki = 36 nM [8]
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info IC50 = 4460 nM
N-DESMETHYLCLOZAPINE Drug Info Ki = 250 nM [12]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info IC50 = 1100 nM
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info IC50 = 2000 nM
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 190 nM [1]
SCH-211803 Drug Info Ki = 0.89 nM [2]
SULFOARECOLINE Drug Info IC50 = 1.4 nM [15]
References
REF 1 6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. J Med Chem. 2000 Jun 29;43(13):2514-22.
REF 2 Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists. J Med Chem. 2002 Dec 5;45(25):5415-8.
REF 3 Urea and 2-imidazolidone derivatives of the muscarinic agents oxotremorine and N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. J Med Chem. 1992 Aug 21;35(17):3270-9.
REF 4 Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations. Bioorg Med Chem Lett. 2004 Aug 2;14(15):3967-70.
REF 5 Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives. J Med Chem. 1992 Apr 3;35(7):1280-90.
REF 6 Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. J Nat Prod. 2005 Jul;68(7):1061-5.
REF 7 Design and synthesis of a fluorescent muscarinic antagonist. Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7.
REF 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... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 9 Muscarinic receptor binding profile of para-substituted caramiphen analogues. J Med Chem. 1991 Oct;34(10):2984-9.
REF 10 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 acetylch... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2.
REF 11 Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. J Med Chem. 1990 Feb;33(2):809-14.
REF 12 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 13 Synthesis and pharmacological evaluation of a series of 4-piperazinylpyrazolo[3,4-b]- and -[4,3-b][1,5]benzodiazepines as potential anxiolytics. J Med Chem. 1989 Dec;32(12):2573-82.
REF 14 Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist. J Med Chem. 1989 May;32(5):1057-62.
REF 15 Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres. J Med Chem. 1988 Jul;31(7):1312-6.
REF 16 Synthesis of clozapine analogues and their affinity for clozapine and spiroperidol binding sites in rat brain. J Med Chem. 1981 Sep;24(9):1021-6.
REF 17 Design, synthesis, and neurochemical evaluation of 5-(3-alkyl-1,2,4- oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists. J Med Chem. 1993 Apr 2;36(7):842-7.
REF 18 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. J Med Chem. 1998 Jun 4;41(12):2047-55.
REF 19 Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone. J Med Chem. 1998 Oct 22;41(22):4181-5.
REF 20 Neuromuscular relaxants as antagonists for M2 and M3 muscarinic receptors. Anesthesiology. 1998 Mar;88(3):744-50.
REF 21 Impaired atrial M(2)-cholinoceptor function in obesity-related hypertension. Hypertension. 1999 Nov;34(5):1066-72.
REF 22 Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.

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