General Information of Drug (ID: DMCBV5F)

Drug Name
ZK-814048 Drug Info
Synonyms
ZK-814048; Thiophene-Anthranilamide, 10b; SCHEMBL6589576; CHEMBL227222; BDBM17090; CYFNXPSIQONWKY-UHFFFAOYSA-N; ZK814048; ZK 814048; N-(5-chloropyridin-2-yl)-2-[((4-((methylamino)methyl)-3-chlorothiophen-2-yl)carbonyl)amino]-3-methoxy-5-chlorobenzamide
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
16731825
TTD Drug ID
DMCBV5F

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Drug(s) Targeting Neutrophil elastase (NE)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sivelestat sodium hydrate DMOSJD0 Acute lung injury NB32.3 Phase 4 [2]
Epigallocatechin gallate DMCGWBJ Hepatic fibrosis DB93.0 Phase 3 [3]
Sivelestat DM6BZCV Crohn disease DD70 Phase 3 [4]
Tiprelestat DM1SB94 Myocardial infarction BA41-BA43 Phase 2 [5]
AZD9668 DMB87M3 Bronchiectasis CA24 Phase 2 [6]
L-694,458 DMA0DSJ Cystic fibrosis CA25 Phase 2 [7]
BAY 85-8501 DMCPUKG Bronchiectasis CA24 Phase 2 [8]
DX-890 DMBFZET Acute lung injury NB32.3 Phase 2 [2]
POL-6014 DM9B68S Cystic fibrosis CA25 Phase 1 [9]
AZD-9819 DMWYHXG Chronic obstructive pulmonary disease CA22 Phase 1 [10]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Plasma kallikrein (KLKB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ecallantide DMOF2C6 Retina venous occlusion 9B74.1 Approved [11]
Lanadelumab DMEH7YU Hereditary angioedema 4A00.14 Approved [12]
Berotralstat DMWA2DZ Hereditary angioedema 4A00.14 Approved [13]
KVD001 DMK4VOU Diabetic macular edema 9B71.02 Phase 2 [14]
KVD824 DM5N4OA Diabetic macular edema 9B71.02 Phase 2 [15]
THR-149 DMW8X05 Diabetic macular edema 9B71.02 Phase 2 [16]
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone DM31OSD Discovery agent N.A. Investigative [17]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone DMT9FZD Discovery agent N.A. Investigative [17]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide DMG5MNZ Discovery agent N.A. Investigative [17]
D-Pro-Phe-Arg chloromethyl ketone DMRJQ8X Discovery agent N.A. Investigative [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Coagulation factor Xa (F10)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Apixaban DM89JLN Thrombosis DB61-GB90 Approved [19]
Rivaroxaban DMQMBZ1 Deep vein thrombosis BD71 Approved [20]
DU-176b DMCIJBH Atrial fibrillation BC81.3 Approved [21]
Emicizumab DM0AQ83 Factor VIII deficiency 3B10 Approved [22]
BETRIXABAN DM2C4RF Venous thromboembolism BD72 Approved [23]
Lmw heparin DMJPD06 Coagulation defect 3B10.0 Approved [24]
Nadroparin calcium DMBNKST Coagulation defect 3B10.0 Approved [25]
Fondaparinux sodium DMWS3FH Deep vein thrombosis BD71 Approved [26]
Danaparoid DM6CLBN Deep venous clot BD71 Approved [27]
Coagulation Factor IX DM8HBJI Haemophilia B 3B11.0 Approved [28]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Coagulation factor Xa (F10) TTCIHJA FA10_HUMAN Inhibitor [1]
Neutrophil elastase (NE) TTPLTSQ ELNE_HUMAN Inhibitor [1]
Plasma kallikrein (KLKB1) TTMF8H9 KLKB1_HUMAN Inhibitor [1]

References

1 Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. J Med Chem. 2007 Jun 28;50(13):2967-80.
2 Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
3 Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
4 Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
5 Company report (Proteo Biotech AG)
6 Clinical pipeline report, company report or official report of AstraZeneca (2009).
7 Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
8 Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 5-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases. ChemMedChem. 2015 Jul;10(7):1163-73.
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: 2358).
10 Lipid Peroxide-Mediated Oxidative Rearrangement of the Pyrazinone Carboxamide Core of Neutrophil Elastase Inhibitor AZD9819 in Blood Plasma Samples. Drug Metab Dispos. 2015 Oct;43(10):1441-9.
11 Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery. Expert Opin Biol Ther. 2008 Aug;8(8):1187-99.
12 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
13 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
14 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
15 Clinical pipeline report, company report or official report of KalVista Pharmaceuticals.
16 Clinical pipeline report, company report or official report of Oxurion.
17 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. J Med Chem. 2007 Oct 4;50(20):4928-38.
18 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. J Med Chem. 2008 Jun 12;51(11):3077-80.
19 Pfizer. Product Development Pipeline. March 31 2009.
20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
21 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: 2359).
22 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
23 Company report (Portola)
24 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
25 Serum zinc concentrations: contamination from laboratory equipment. JPEN J Parenter Enteral Nutr. 1979 May-Jun;3(3):179-81.
26 Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002 Sep-Dec;32(5-6):218-24.
27 Effect of factor X inhibition on coagulation activation and cytokine induction in human systemic inflammation. J Infect Dis. 2002 Nov 1;186(9):1270-6.
28 Haemophilia B: Christmas disease. Expert Opin Pharmacother. 2005 Aug;6(9):1517-24.