Target Validation Information
Target ID T67684
Target Name Muscarinic acetylcholine receptor M3
Target Type
Successful
Drug Potency against Target 7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 7280 nM
7-Dimethylamino-hept-5-yn-2-one Drug Info IC50 = 68 nM
Nocardimicin C Drug Info Ki = 1000 nM [527653]
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 5696 nM
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info IC50 = 13230 nM
Succinylcholine Drug Info Ki = 18450 nM [552407]
CREMASTRINE Drug Info IC50 = 126 nM [527523]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info IC50 = 101 nM
Darifenacin Drug Info Ki = 1.58 nM [552263]
FLUMEZAPINE Drug Info IC50 = 80 nM [533165]
FM1-43 Drug Info Ki = 30 nM [529178]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info IC50 < 10 nM [530266]
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]
Tolterodine Drug Info Ki = 6.3 nM [552263]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info IC50 = 16000 nM [527344]
FM1-10 Drug Info Ki = 24 nM [529178]
NOCARDIMICIN A Drug Info Ki = 1250 nM [527653]
GNF-PF-5618 Drug Info Ki = 130 nM [527653]
Nocardimicin F Drug Info Ki = 1330 nM [527653]
Pirenzepine Drug Info Ki = 125 nM [552263]
UCB-101333-3 Drug Info Ki = 3.2 nM [528765]
BRL-55473 Drug Info IC50 = 470 nM
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info IC50 = 1928 nM
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info Ki = 6.7 nM [534723]
ACECLIDINE Drug Info IC50 = 510 nM [534044]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info Ki = 10700 nM [527029]
Atropine Drug Info Ki = 0.5 nM [552263]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 680 nM [534645]
Noccardimicin E Drug Info Ki = 970 nM [527653]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info IC50 = 1100 nM
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info IC50 = 21.6 nM
1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info IC50 = 15 nM [533345]
Nocardimicin D Drug Info Ki = 230 nM [527653]
ISOCLOZAPINE Drug Info IC50 = 55 nM [530313]
SULFOARECOLINE Drug Info IC50 = 1.4 nM [533450]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 11400 nM [525826]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info IC50 = 2000 nM
N-DESMETHYLCLOZAPINE Drug Info Ki = 90 nM [531079]
Action against Disease Model Tiotropium Tiotropi uM concentration-dependently inhibited pulmonary neutrophilic inflammation with IC50: 0.058 mg/mL Drug Info
References
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 552407Receptor binding thermodynamics at the neuronal nicotinic receptor. Curr Top Med Chem. 2004;4(3):361-8.
Ref 527523J Nat Prod. 2005 Apr;68(4):572-3.Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.
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 529178Bioorg Med Chem Lett. 2008 Jan 15;18(2):825-7. Epub 2007 Nov 17.Design and synthesis of a fluorescent muscarinic antagonist.
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 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 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 527344J Med Chem. 1992 Apr 3;35(7):1280-90.Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
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 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 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 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 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 528765Bioorg Med Chem Lett. 2007 Jun 1;17(11):3077-80. Epub 2007 Mar 19.Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives.
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 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 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 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 534645J Med Chem. 1998 Jun 4;41(12):2047-55.6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
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 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 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 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 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 533450J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
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 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.

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