Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMNY8H7)

• Drug Name: AF-DX-384 Drug Info
• Synonyms: MZDYABXXPZNUCT-UHFFFAOYSA-N; AF-DX 384; AFDX384; 118290-27-0; CHEMBL279453; N-(2-(2-((Dipropylamino)methyl)piperidin-1-yl)ethyl)-6-oxo-5H-benzo[e]pyrido[3,2-b][1,4]diazepine-11(6H)-carboxamide; N-[2-[2-[(Dipropylamino)methyl]-1-piperidinyl]ethyl]-5,6-dihydro-6-oxo-11H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide; AFDX-384; N-[2-[2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide; [3H]AF-DX 384; [3H]AF DX-384; AC1L3ONW; GTPL368; 118290-26-9; SCHEMBL9824222; AF-DX-384

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 119357
  ChEBI ID: CHEBI:110176
  TTD Drug ID: DMNY8H7

Molecule-Related Drug Atlas

Drug(s) Targeting Muscarinic acetylcholine receptor (CHRM)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Acetylcholine	DMDF79Z	Cataract	9B10	Approved	[4]
Tiotropium	DMFDC0Q	Chronic obstructive pulmonary disease	CA22	Approved	[5]
Darifenacin	DMWXLYZ	Overactive bladder	GC50.0	Approved	[6]
Methylscopolamine	DM5VWOB	Peptic ulcer	DA61	Approved	[7]
Clidinium	DMUMQZ0	Abdominal stomach pain	DD91.4	Approved	[8]
Oxybutynin hydrochloride	DMF2KLU	Urinary incontinence	MF50.2	Approved	[9]
Incruse Ellipta	DM32GSJ	Chronic obstructive pulmonary disease	CA22	Approved	[10]
Revefenacin	DMMP5SI	Chronic obstructive pulmonary disease	CA22	Approved	[11]
Scopolamine	DMOM8AL	Addictive disorder	6C50-6C5Z	Approved	[12]
Isopropamide iodide	DMQYV60	Allergic rhinitis	CA08.0	Approved	[13]

Drug(s) Targeting Muscarinic acetylcholine receptor M4 (CHRM4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ACECLIDINE	DMOLNCZ	Glaucoma/ocular hypertension	9C61	Approved	[14]
Methacholine Chloride	DMGS4QH	Asthma	CA23	Approved	[15]
Tropicamide	DM1D90W	Mydriasis	LA11.62	Approved	[16]
Diphenidol	DMHPWOM	Nausea	MD90	Approved	[17]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	DMM9X0G	Discovery agent	N.A.	Investigative	[18]
A-987306	DMU34BK	Discovery agent	N.A.	Investigative	[19]
ISOCLOZAPINE	DM52CPU	Discovery agent	N.A.	Investigative	[20]
FLUMEZAPINE	DMW0HOG	Discovery agent	N.A.	Investigative	[21]
ISOLOXAPINE	DMH1BN4	Discovery agent	N.A.	Investigative	[22]
Acetic acid 8-aza-bicyclo[3.2.1]oct-6-yl ester	DMVEH40	Discovery agent	N.A.	Investigative	[15]

Drug(s) Targeting Muscarinic acetylcholine receptor M2 (CHRM2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ACECLIDINE	DMOLNCZ	Glaucoma/ocular hypertension	9C61	Approved	[14]
Methacholine Chloride	DMGS4QH	Asthma	CA23	Approved	[15]
SMT-D002	DM1I93C	Seborrhea	ED91.2	Approved	[23]
Methylscopolamine	DM5VWOB	Peptic ulcer	DA61	Approved	[24]
Gallamine Triethiodide	DMPO0MS	Stabilize muscle contraction	FB3Z	Approved	[25]
FP-1097	DMC1F2T	Urinary incontinence	MF50.2	Phase 2	[26]
PSD-506	DMT0KB1	Overactive bladder	GC50.0	Discontinued in Phase 2	[27]
Otenzepad	DMRXHAC	Heart failure	BD10-BD13	Discontinued in Phase 2	[28]
SCH-211803	DM92E0W	Parkinson disease	8A00.0	Discontinued in Phase 1	[29]
Alvameline	DMLN0Y5	Alzheimer disease	8A20	Terminated	[30]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Muscarinic acetylcholine receptor (CHRM)	TTOXS3C	NOUNIPROTAC	Antagonist	[2]
Muscarinic acetylcholine receptor M2 (CHRM2)	TTYEG6Q	ACM2_HUMAN	Modulator	[3]
Muscarinic acetylcholine receptor M4 (CHRM4)	TTQ3JTF	ACM4_HUMAN	Modulator	[3]

References

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• [7] Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. J Pharmacol Exp Ther. 2002 Oct;303(1):29-35.
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• [9] Effects of propiverine hydrochloride (propiverine) on the muscarinic receptor binding affinity in guinea pig tissues and on salivation in conscious dogs. Nihon Yakurigaku Zasshi. 1999 Mar;113(3):157-66.
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• [11] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
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• [13] Competitive and non-competitive antagonism exhibited by 'selective' antagonists at atrial and ileal muscarinic receptor subtypes. Br J Pharmacol. 1987 Apr;90(4):701-7.
• [14] 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.
• [15] 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. J Med Chem. 1998 Jun 4;41(12):2047-55.
• [16] The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 rec... Psychopharmacology (Berl). 2007 Oct;194(3):347-59.
• [17] Diphenidol-related diamines as novel muscarinic M4 receptor antagonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2972-6.
• [18] 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.
• [19] 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.
• [20] Chloro-substituted, sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents. J Med Chem. 1990 Feb;33(2):809-14.
• [21] 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.
• [22] 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.
• [23] Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol. 2004 Nov;172(5 Pt 1):2059-64.
• [24] Methylacridinium and its cholinergic properties. Neurotox Res. 2009 Nov;16(4):372-7.
• [25] Cholinergic regulation of the corpora allata in adult male loreyi leafworm Mythimna loreyi. Arch Insect Biochem Physiol. 2002 Apr;49(4):215-24.
• [26] Clinical pipeline report, company report or official report of FemmePharma.
• [27] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [28] Beneficial effect of muscarinic-2 antagonist on dilated cardiomyopathy induced by autoimmune mechanism against muscarinic-2 receptor. J Cardiovasc Pharmacol. 2001 Oct;38 Suppl 1:S43-9.
• [29] 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.
• [30] In vivo muscarinic cholinergic mediated effects of Lu 25-109, a M1 agonist and M2/M3 antagonist in vitro. Psychopharmacology (Berl). 1998 Jun;137(3):233-40.