General Information of Drug (ID: DM31OSD)

Drug Name
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info
Synonyms
AC1LDSCF; N-Benzoylpyrazole deriv., 7; CHEMBL244909; ZINC37188; BDBM23705; MolPort-002-174-815; AKOS000576906; 4-bromopyrazolyl 4-methylphenyl ketone; MCULE-8194486011; ST033225; AB00100488-01; (4-bromopyrazol-1-yl)-(4-methylphenyl)methanone; SR-01000521427; SR-01000521427-1
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
674656
TTD Drug ID
DM31OSD

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)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pro-urokinase DMGKT2L Thrombin deficiency 3B14.Z Approved [2]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [3]
PAI-1 DMY2AEF N. A. N. A. Phase 4 [4]
Amediplase DM4FPM3 Myocardial infarction BA41-BA43 Phase 3 [5]
Upamostat DMFZULI Breast cancer 2C60-2C65 Phase 2 [6]
Saruplase DM1M0PR Thrombosis DB61-GB90 Phase 2 [7]
HTU-PA DMNHE43 Cerebrovascular ischaemia 8B1Z Phase 1/2 [8]
PMID18163548C4 DMHPME3 Myocardial ischemia BA6Z Clinical trial [9]
UK-356202 DMSRK2A Myocardial hypertrophy BC45 Clinical trial [10]
PAI-2 DMRSMW8 N. A. N. A. Discontinued in Phase 2 [11]
⏷ Show the Full List of 10 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 [12]
Epigallocatechin gallate DMCGWBJ Hepatic fibrosis DB93.0 Phase 3 [13]
Sivelestat DM6BZCV Crohn disease DD70 Phase 3 [14]
Tiprelestat DM1SB94 Myocardial infarction BA41-BA43 Phase 2 [15]
AZD9668 DMB87M3 Bronchiectasis CA24 Phase 2 [16]
L-694,458 DMA0DSJ Cystic fibrosis CA25 Phase 2 [17]
BAY 85-8501 DMCPUKG Bronchiectasis CA24 Phase 2 [18]
DX-890 DMBFZET Acute lung injury NB32.3 Phase 2 [12]
POL-6014 DM9B68S Cystic fibrosis CA25 Phase 1 [19]
AZD-9819 DMWYHXG Chronic obstructive pulmonary disease CA22 Phase 1 [20]
⏷ 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 [21]
Lanadelumab DMEH7YU Hereditary angioedema 4A00.14 Approved [22]
Berotralstat DMWA2DZ Hereditary angioedema 4A00.14 Approved [23]
KVD001 DMK4VOU Diabetic macular edema 9B71.02 Phase 2 [24]
KVD824 DM5N4OA Diabetic macular edema 9B71.02 Phase 2 [25]
THR-149 DMW8X05 Diabetic macular edema 9B71.02 Phase 2 [26]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone DMT9FZD Discovery agent N.A. Investigative [1]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide DMG5MNZ Discovery agent N.A. Investigative [1]
D-Pro-Phe-Arg chloromethyl ketone DMRJQ8X Discovery agent N.A. Investigative [27]
(3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone DMNVDLI Discovery agent N.A. Investigative [1]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Coagulation factor IIa (F2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Argatroban DMFI46A Thrombosis DB61-GB90 Approved [28]
Pyridoxal Phosphate DMO2K0J Malnutrition 5B50-5B71 Approved [29]
Bivalirudin DMECRX1 Thrombocytopenia 3B64 Approved [30]
Ximelegatran DMU8ANS Myocardial infarction BA41-BA43 Approved [5]
Dabigatran DMDI6R4 Stroke 8B20 Approved [31]
Desirudin Recombinant DM2BTFN Coagulation defect 3B10.0 Approved [3]
Human prothrombin complex concentrate DMPHVQ1 Bleeding disorder GA20-GA21 Approved [32]
Lepirudin DM1I3D5 Thrombocytopenia 3B64 Approved [33]
Anisindione DM2C48U Coagulation defect 3B10.0 Approved [34]
ATryn antithrombin DM79Y2T Multiple sclerosis 8A40 Approved [35]
⏷ 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 IIa (F2) TT6L509 THRB_HUMAN Inhibitor [1]
Neutrophil elastase (NE) TTPLTSQ ELNE_HUMAN Inhibitor [1]
Plasma kallikrein (KLKB1) TTMF8H9 KLKB1_HUMAN Inhibitor [1]
Urokinase-type plasminogen activator (PLAU) TTGY7WI UROK_HUMAN Inhibitor [1]

References

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3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4 Urokinase-type plasminogen activator and its inhibitor PAI-1: predictors of poor response to tamoxifen therapy in recurrent breast cancer. J Natl Cancer Inst. 1995 May 17;87(10):751-6.
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6 Phase II randomised proof-of-concept study of the urokinase inhibitor upamostat (WX-671) in combination with gemcitabine compared with gemcitabine alone in patients with non-resectable, locally advanced pancreatic cancer. Br J Cancer. 2013 Mar 5;108(4):766-70.
7 Pharmacokinetics and pharmacodynamics of saruplase, an unglycosylated single-chain urokinase-type plasminogen activator, in patients with acute myocardial infarction. Thromb Haemost. 1994 Nov;72(5):740-4.
8 Characterization of the dexamethasone-induced inhibitor of plasminogen activator in HTC hepatoma cells. J Biol Chem. 1986 Mar 25;261(9):4352-7.
9 Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. J Med Chem. 2008 Jan 24;51(2):183-6.
10 Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3227-30.
11 Topological localization of plasminogen activator inhibitor type 2. Cytometry. 2000 May 1;40(1):32-41.
12 Emerging therapies for treatment of acute lung injury and acute respiratory distress syndrome. Expert Opin Emerg Drugs. 2007 Sep;12(3):461-77.
13 Evaluation of human neutrophil elastase inhibitory effect of iridoid glycosides from Hedyotis diffusa. Bioorg Med Chem Lett. 2010 Jan 15;20(2):513-5.
14 Neutrophil elastase inhibitor (sivelestat) reduces the levels of inflammatory mediators by inhibiting NF-kB. Inflamm Res. 2009 Apr;58(4):198-203.
15 Company report (Proteo Biotech AG)
16 Clinical pipeline report, company report or official report of AstraZeneca (2009).
17 Neutrophil elastase inhibitors as treatment for COPD. Expert Opin Investig Drugs. 2002 Jul;11(7):965-80.
18 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.
19 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).
20 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.
21 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.
22 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
23 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
24 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
25 Clinical pipeline report, company report or official report of KalVista Pharmaceuticals.
26 Clinical pipeline report, company report or official report of Oxurion.
27 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. J Med Chem. 2008 Jun 12;51(11):3077-80.
28 Studies on the different modes of action of the anticoagulant protease inhibitors DX-9065a and Argatroban. I. Effects on thrombin generation. J Biol Chem. 2002 Dec 27;277(52):50439-44.
29 New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
30 New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
31 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
32 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: 2362).
33 Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
34 Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
35 Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.