Target Validation Information
Target ID T28893
Target Name Muscarinic acetylcholine receptor M1
Target Type
Successful
Drug Potency against Target Atropine Drug Info Ki = 1 nM [552263]
2-(4-Diethylamino-but-2-ynyl)-isoindole-1,3-dione Drug Info Ki = 30 nM
GSK1034702 Drug Info KD = 0.1 nM [552674]
Ethopropazine Drug Info IC50 = 257000 nM [552771]
Benztropine Drug Info IC50 = 0.294 nM [552409]
FM1-43 Drug Info Ki = 44 nM [529178]
Linagliptin Drug Info IC50 = 295 nM [529188]
Sabcomeline Drug Info IC50 = 170 nM [534542]
6-Dimethylamino-2-methyl-hex-4-ynal oxime Drug Info IC50 = 13230 nM
2-Methyl-6-pyrrolidin-1-yl-hex-4-ynal oxime Drug Info IC50 = 1928 nM
3-Methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 5696 nM
1'-Benzyl-3-phenyl-[3,4']bipiperidinyl-2,6-dione Drug Info IC50 = 15 nM [533345]
Tolterodine Drug Info Ki = 3.98 nM [552263]
BRL-55473 Drug Info IC50 = 470 nM
ISOCLOZAPINE Drug Info IC50 = 55 nM [530313]
3-Tetrazol-2-yl-1-aza-bicyclo[2.2.2]octane Drug Info IC50 = 16000 nM [527344]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 5.6 nM [534645]
1-Methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Drug Info Ki = 10700 nM [527029]
ISOLOXAPINE Drug Info IC50 = 49 nM [533577]
N-methoxyquinuclidine-3-carboximidoyl fluoride Drug Info IC50 = 2000 nM
R-dimethindene Drug Info Ki = 2.4 nM [530300]
HIMBACINE Drug Info Ki = 48 nM [527126]
ACECLIDINE Drug Info IC50 = 510 nM [534044]
N-methoxyquinuclidine-3-carboximidoyl chloride Drug Info IC50 = 1100 nM
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 40.6 nM [528473]
7-Dimethylamino-hept-5-yn-2-one Drug Info IC50 = 68 nM
GNF-PF-5618 Drug Info Ki = 490 nM [527653]
DIFLUOROBENZTROPINE Drug Info Ki = 11.6 nM [528473]
2,8-Dimethyl-1-oxa-8-aza-spiro[4.5]decan-3-one Drug Info Ki = 6.7 nM [534723]
CARAMIPEN Drug Info Ki = 1.21 nM [529957]
AMINOBENZTROPINE Drug Info Ki = 1.12 nM [534349]
Propionic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 190 nM [525826]
7-Dimethylamino-3-methyl-hept-5-yn-2-one Drug Info IC50 = 101 nM
FLUMEZAPINE Drug Info IC50 = 80 nM [533165]
7-Pyrrolidin-1-yl-hept-5-yn-2-one Drug Info IC50 = 7280 nM
N-(4-Dimethylamino-but-2-ynyl)-N-methyl-acetamide Drug Info IC50 = 21.6 nM
FM1-10 Drug Info Ki = 34 nM [529178]
SULFOARECOLINE Drug Info IC50 = 1.4 nM [533450]
1,1-diphenyl-2-(3-tropanyl)ethanol Drug Info IC50 < 10 nM [530266]
Darifenacin Drug Info Ki = 15.8 nM [552263]
Pirenzepine Drug Info Ki = 6.3 nM [552263]
Benzoic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester Drug Info Ki = 440 nM [525826]
RR(17)PZ Drug Info Ki = 53.5 nM [527889]
Bo(15)PZ Drug Info Ki = 69.7 nM [527889]
CREMASTRINE Drug Info IC50 = 505 nM [527523]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [531079]
Action against Disease Model Trihexyphenidyl Affinity for the muscarinic receptors in the cerebral cortex IC50: 3.7 nM [553108] Drug Info
Pirenzepine Affinity for the muscarinic receptors in the cerebral cortex IC50: 14 nM [553108] Drug Info
Dicyclomine Affinity for the muscarinic receptors in the cerebral cortex(rat) IC50: 5.1 nM [553108] Drug Info
Glycopyrrolate IC50 of EFS-induced contraction in Guinea pig/h uMan trachea: 0.15 nM/0.44 nM [552190] Drug Info
References
Ref 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
Ref 552674Recent advances in the development of agonists selective for beta1-type thyroid hormone receptor. Mini Rev Med Chem. 2007 Jan;7(1):79-86.
Ref 552771Acetylcholinesterase in the sea urchin Lytechinus variegatus: characterization and developmental expression in larvae. Comp Biochem Physiol B Biochem Mol Biol. 2008 Mar;149(3):401-9. doi: 10.1016/j.cbpb.2007.10.014. Epub 2007 Nov 9.
Ref 552409Effects of N-substituted analogs of benztropine: diminished cocaine-like effects in dopamine transporter ligands. J Pharmacol Exp Ther. 2004 May;309(2):650-60. Epub 2004 Jan 30.
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 529188J Med Chem. 2007 Dec 27;50(26):6450-3. Epub 2007 Dec 1.8-(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.
Ref 534542J Med Chem. 1997 Dec 19;40(26):4265-80.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.
Ref 553108Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83-90.
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 552263Therapeutic opportunities from muscarinic receptor research. Trends Pharmacol Sci. 2001 Aug;22(8):409-14.
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 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 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 553108Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83-90.
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 530300J Med Chem. 2009 Sep 10;52(17):5307-10.Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
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 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 553108Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986 Sep;89(1):83-90.
Ref 528473J Med Chem. 2006 Oct 19;49(21):6391-9.Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
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 528473J Med Chem. 2006 Oct 19;49(21):6391-9.Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
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 529957J Med Chem. 1991 Oct;34(10):2984-9.Muscarinic receptor binding profile of para-substituted caramiphen analogues.
Ref 534349J Med Chem. 1997 Mar 14;40(6):851-7.3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.
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 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 533450J Med Chem. 1988 Jul;31(7):1312-6.Heterocyclic muscarinic agonists. Synthesis and biological activity of some bicyclic sulfonium arecoline bioisosteres.
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 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 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 552190Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways. Br J Pharmacol. 1999 May;127(2):413-20.
Ref 527889J Med Chem. 2005 Dec 1;48(24):7847-59.On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.
Ref 527889J Med Chem. 2005 Dec 1;48(24):7847-59.On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.
Ref 527523J Nat Prod. 2005 Apr;68(4):572-3.Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata.
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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