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

General Information of Drug (ID: DMHKTGX)

Drug Name

BAY 1142524 Drug Info

Synonyms

Fulacimstat; UNII-VIR72PP4ZU; VIR72PP4ZU; BAY1142524; 1488354-15-9; 1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid; 1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-; 2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-; Fulacimstat [INN]; Fulacimstat; BAY1142524; Fulacimstat(BAY 1142524); CHEMBL4297596; SCHEMBL16701233; EX-A2732; DB15085; BAY-1142524; HY-109059; CS-0032987; (R)-1-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)-2,4-dioxo-3-(4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid; 1-(2,3-Dihydro-3-methyl-2-oxo-6-benzoxazolyl)-3-((1R)-2,3-dihydro-4-(trifluoromethyl)-1H-inden-1-yl)-1,2,3,4-tetrahydro-2,4-dioxo-5-pyrimidinecarboxylic acid; 1-(3-methyl-2-oxo-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]pyrimidine-5-carboxylic acid; 1-(3-Methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-((1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl)-1,2,3,4-tetrahydro-5-pyrimidinecarboxylic acid; 1-(3-Methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid; 5-Pyrimidinecarboxylic acid, 1-(2,3-dihydro-3-methyl-2-oxo-6-benzoxazolyl)-3-((1R)-2,3-dihydro-4-(trifluoromethyl)-1H-inden-1-yl)-1,2,3,4-tetrahydro-2,4-dioxo-

Indication

Disease Entry	ICD 11	Status	REF
Myocardial infarction	BA41-BA43	Phase 2	[1]

Cross-matching ID

PubChem CID: 91758792
CAS Number: CAS 1488354-15-9
TTD Drug ID: DMHKTGX

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Investigative Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Chymase (CYM)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SUN13834	DMPK34E	Gram-positive bacterial infection	1B74-1G40	Phase 2	[3]
JNJ-10311795	DM7OTQS	Chronic obstructive pulmonary disease	CA22	Phase 2	[4]
ASB17061	DMNVU28	Atopic dermatitis	EA80	Phase 2	[5]
BAY 11-42524	DM8SNEM	Left ventricular dysfunction	BD11	Phase 2	[6]
2-(N-Morpholino)-Ethanesulfonic Acid	DMZVHSB	Discovery agent	N.A.	Investigative	[7]
Benzylsulfinic Acid	DM7XK28	Discovery agent	N.A.	Investigative	[8]
KM-01221	DMG594K	Cardiovascular disease	BA00-BE2Z	Investigative	[9]
Y-40613	DM412IV	Discovery agent	N.A.	Investigative	[10]
Rac-2q	DMD5TPH	Discovery agent	N.A.	Investigative	[11]
Phenylalanylmethane	DMZNFT2	Discovery agent	N.A.	Investigative	[7]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Chymase (CYM)	TT8VUE0	CMA1_HUMAN	Inhibitor	[2]

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References

1	ClinicalTrials.gov (NCT02976467) A Double-blind Study to Investigate Efficacy, Safety and Tolerability of BAY 1142524 in Patients After Acute Myocardial Infarction With Left-ventricular Dysfunction (CHIARA MIA 2). U.S. National Institutes of Health.
2	Pharmacokinetics, Safety, and Tolerability of the Novel Chymase Inhibitor BAY 1142524 in Healthy Male Volunteers. Clin Pharmacol Drug Dev. 2019 May;8(4):467-479.
3	Oral chymase inhibitor SUN13834 ameliorates skin inflammation as well as pruritus in mouse model for atopic dermatitis.Eur J Pharmacol.2008 Dec 28;601(1-3):186-91.
4	Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.
5	Immunology of atopic eczema: overcoming the Th1/Th2 paradigm. Allergy. 2013 Aug;68(8):974-82.
6	ClinicalTrials.gov (NCT02452515) A Single-blind Pilot Study to Investigate Safety and Tolerability of the Chymase Inhibitor BAY1142524 in Clinically Stable Patients With Left-ventricular Dysfunction.
7	How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
8	The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
9	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2340).
10	Therapeutic potential of a specific chymase inhibitor in atopic dermatitis. Jpn J Pharmacol. 2002 Nov;90(3):214-7.
11	Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3431-4.