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

General Information of Drug (ID: DM6BIHE)

Drug Name
RWJ-56423 Drug Info
Synonyms
RWJ-56423; CHEMBL256892; CHEMBL124571; (2S,4R)-1-ACETYL-N-[(1S)-4-[(AMINOIMINOMETHYL)AMINO]-1-(2-BENZOTHIAZOLYLCARBONYL)BUTYL]-4-HYDROXY-2-PYRROLIDINECARBOXAMIDE; (2S,4R)-1-acetyl-N-[(2S)-1-(1,3-benzothiazol-2-yl)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-4-hydroxypyrrolidine-2-carboxamide; AC1NR9Y0; SCHEMBL4314345; GTPL9333; VXDAVYUFYPFGDX-SNPRPXQTSA-N; BDBM50228764; BDBM50131977; DB02812; (2S)-6; (4R)-1-acetyl-N-[(1S)-1-(1,3-benzothiazol-2-ylcarbonyl)-4-carbamimidamidobutyl]-4-hydroxy-L-prolinamide
Indication
Disease Entry ICD 11 Status REF
Asthma CA23 Discontinued in Phase 1 [1]
Cross-matching ID
PubChem CID
5287596
TTD Drug ID
DM6BIHE

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Cationic trypsinogen (PRSS1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Bortezomib DMNO38U Leukemia Approved [3]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [4]
Ulinastatin DMIQCFG Premature labour JB00 Phase 3 [5]
Alpha-1 antitrypsin DM5EFXZ Coagulation defect 3B10.0 Phase 2 [6]
Dermolastin DM6WSU2 Atopic dermatitis EA80 Discontinued in Phase 2 [7]
Patamostat DM6HBQJ Hypotension BA20-BA21 Terminated [6]
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]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine DME3PUT Discovery agent N.A. Investigative [11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Cationic trypsinogen (PRSS1) TT2WR1T TRY1_HUMAN Inhibitor [2]

References

1 Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone. J Med Chem. 2003 Aug 28;46(18):3865-76.
2 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.
3 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.
4 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
5 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.
6 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.
7 Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
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 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.