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

General Information of Drug (ID: DM8NARQ)

• Drug Name: 1,3-Dibenzyl-[1,3]diazetidine-2,4-dione Drug Info
• Synonyms: CHEMBL47394; 1,3-dibenzyl-1,3-diazetidine-2,4-dione; GTPL6542; BDBM50101132; compound 1 [PMID: 11425539]

Indication

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

• Cross-matching ID:
  PubChem CID: 10038543
  TTD Drug ID: DM8NARQ

Molecule-Related Drug Atlas

Drug(s) Targeting Cationic trypsinogen (PRSS1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bortezomib	DMNO38U	Leukemia		Approved	[2]
MELAGATRAN	DM4W8RE	N. A.	N. A.	Phase 3	[3]
Ulinastatin	DMIQCFG	Premature labour	JB00	Phase 3	[4]
Alpha-1 antitrypsin	DM5EFXZ	Coagulation defect	3B10.0	Phase 2	[5]
Dermolastin	DM6WSU2	Atopic dermatitis	EA80	Discontinued in Phase 2	[6]
RWJ-56423	DM6BIHE	Asthma	CA23	Discontinued in Phase 1	[7]
Patamostat	DM6HBQJ	Hypotension	BA20-BA21	Terminated	[5]
BMY-44621	DM8R3N0	N. A.	N. A.	Terminated	[8]
Grassystatin a	DM1PWX2	Discovery agent	N.A.	Investigative	[9]
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine	DM3UMYD	Discovery agent	N.A.	Investigative	[10]

Drug(s) Targeting Cathepsin G (CTSG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
JNJ-10311795	DM7OTQS	Chronic obstructive pulmonary disease	CA22	Phase 2	[11]
Peptide analog 59	DMZAMNX	N. A.	N. A.	Patented	[12]
Peptide analog 61	DM45JMT	N. A.	N. A.	Patented	[12]
Peptide analog 55	DMVLP8H	N. A.	N. A.	Patented	[12]
Peptide analog 60	DMMSTNA	N. A.	N. A.	Patented	[12]
Peptide analog 70	DMN43Q5	N. A.	N. A.	Patented	[12]
Peptide analog 56	DMBCFJU	N. A.	N. A.	Patented	[12]
Peptide analog 57	DM6IQWE	N. A.	N. A.	Patented	[12]
Peptide analog 58	DM7X62M	N. A.	N. A.	Patented	[12]
Peptide analog 62	DM28NK0	N. A.	N. A.	Patented	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Cathepsin G (CTSG)	TTQAJF1	CATG_HUMAN	Inhibitor	[1]
Cationic trypsinogen (PRSS1)	TT2WR1T	TRY1_HUMAN	Inhibitor	[1]

References

• [1] Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1691-4.
• [2] Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. J Med Chem. 1995 Apr 28;38(9):1511-22.
• [3] Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
• [4] Intravenous administration of ulinastatin (human urinary trypsin inhibitor) in severe sepsis: a multicenter randomized controlled study. Intensive Care Med. 2014 Jun;40(6):830-8.
• [5] US patent application no. 2012,0251,516, PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING TRYPSINOGEN AND/OR CHYMOTRYPSINOGEN AND AN ACTIVE AGENT SELECTED FROM A SELENIUM COMPOUND, A VANILLOID COMPOUND AND A CYTOPLASMIC GLYCOLYSIS REDUCTION AGENT.
• [6] Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
• [7] Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G. J Med Chem. 2004 Feb 12;47(4):769-87.
• [8] Design and synthesis of conformationally constrained arginal thrombin inhibitors, Bioorg. Med. Chem. Lett. 7(17):2205-2210 (1997).
• [9] Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
• [10] Development of serine protease inhibitors displaying a multicentered short (<2.3 A) hydrogen bond binding mode: inhibitors of urokinase-type plasmi... J Med Chem. 2001 Aug 16;44(17):2753-71.
• [11] Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase. J Med Chem. 2007 Apr 19;50(8):1727-30.
• [12] Neutrophil elastase inhibitors: a patent review and potential applications for inflammatory lung diseases (2010 - 2014).Expert Opin Ther Pat. 2015;25(10):1145-58.