General Information of Drug (ID: DM3UMYD)

Drug Name
2-(2-Hydroxy-phenyl)-1H-indole-5-carboxamidine Drug Info
Synonyms
2-(2-hydroxy-phenyl)-1h-indole-5-carboxamidine; amino[2-(2-hydroxyphenyl)-1H-indol-5-yl]methaniminium; AC1L1BMI; BDBM13942; CTK8A0256; APC-8328; DB02463; [amino-[2-(2-hydroxyphenyl)-1H-indol-5-yl]methylidene]azanium
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
1507
TTD Drug ID
DM3UMYD

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 Name Drug ID Indication ICD 11 Highest Status REF
Bortezomib DMNO38U Leukemia Approved [12]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [13]
Ulinastatin DMIQCFG Premature labour JB00 Phase 3 [14]
Alpha-1 antitrypsin DM5EFXZ Coagulation defect 3B10.0 Phase 2 [15]
Dermolastin DM6WSU2 Atopic dermatitis EA80 Discontinued in Phase 2 [16]
RWJ-56423 DM6BIHE Asthma CA23 Discontinued in Phase 1 [17]
Patamostat DM6HBQJ Hypotension BA20-BA21 Terminated [15]
BMY-44621 DM8R3N0 N. A. N. A. Terminated [18]
Grassystatin a DM1PWX2 Discovery agent N.A. Investigative [19]
4-(4-Benzyloxy-3-methoxy-benzylamino)-benzamidine DME3PUT Discovery agent N.A. Investigative [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aminocaproic Acid DMFGND4 Bleeding disorder GA20-GA21 Approved [21]
1-guanidino-N-phenyl-7-isoquinolinesulphonamide DMTF1HL Discovery agent N.A. Investigative [22]
BMS-344577 DM9WRUG Discovery agent N.A. Investigative [23]
N-(4-Chloro-7-p-tolyl-isoquinolin-1-yl)-guanidine DMNO46U Discovery agent N.A. Investigative [10]
5-(DIMETHYLAMINO)-2-NAPHTHALENESULFONIC ACID DMPFX0S Discovery agent N.A. Investigative [24]
N-(4-Phenyl-pyridin-2-yl)-guanidine DMYD4PC Discovery agent N.A. Investigative [25]
N-(7-Benzyloxy-isoquinolin-1-yl)-guanidine DMPMBC2 Discovery agent N.A. Investigative [10]
N-(5-Benzyloxy-isoquinolin-1-yl)-guanidine DMGAITY Discovery agent N.A. Investigative [10]
⏷ Show the Full List of 8 Drug(s)
Drug(s) Targeting Plasminogen (PLG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ranolazine DM0C9IL Acute coronary syndrome BA41 Approved [26]
Aminocaproic Acid DMFGND4 Bleeding disorder GA20-GA21 Approved [27]
Streptokinase DM5JQ0D Pulmonary embolism BB00 Approved [28]
Tranexamic Acid DMFI8A7 Excessive bleeding GA30.02 Approved [29]
Alteplase DMRJ3YX Acute myocardial infarction BA41 Approved [30]
Tenecteplase DMJYN25 Acute myocardial infarction BA41 Approved [30]
Anistreplase DM6Q4B0 Acute coronary syndrome BA41 Approved [31]
Reteplase DML0D1P Heart attack BA41 Approved [32]
MELAGATRAN DM4W8RE N. A. N. A. Phase 3 [13]
Desmoteplase DMDLU4Z Ischemic stroke 8B11.5Z Phase 3 [33]
⏷ 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 [34]
Pyridoxal Phosphate DMO2K0J Malnutrition 5B50-5B71 Approved [35]
Bivalirudin DMECRX1 Thrombocytopenia 3B64 Approved [36]
Ximelegatran DMU8ANS Myocardial infarction BA41-BA43 Approved [5]
Dabigatran DMDI6R4 Stroke 8B20 Approved [37]
Desirudin Recombinant DM2BTFN Coagulation defect 3B10.0 Approved [3]
Human prothrombin complex concentrate DMPHVQ1 Bleeding disorder GA20-GA21 Approved [38]
Lepirudin DM1I3D5 Thrombocytopenia 3B64 Approved [39]
Anisindione DM2C48U Coagulation defect 3B10.0 Approved [40]
ATryn antithrombin DM79Y2T Multiple sclerosis 8A40 Approved [41]
⏷ 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
Cationic trypsinogen (PRSS1) TT2WR1T TRY1_HUMAN Inhibitor [1]
Coagulation factor IIa (F2) TT6L509 THRB_HUMAN Inhibitor [1]
Plasminogen (PLG) TTP86E2 PLMN_HUMAN Inhibitor [1]
Tissue-type plasminogen activator (PLAT) TTXAGYU TPA_HUMAN Inhibitor [1]
Urokinase-type plasminogen activator (PLAU) TTGY7WI UROK_HUMAN Inhibitor [1]

References

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2 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: 2393).
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.
5 Emerging drugs in peripheral arterial disease. Expert Opin Emerg Drugs. 2006 Mar;11(1):75-90.
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 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.
13 Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety. Bioorg Med Chem Lett. 2006 May 15;16(10):2641-7.
14 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.
15 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.
16 Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.
17 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.
18 Design and synthesis of conformationally constrained arginal thrombin inhibitors, Bioorg. Med. Chem. Lett. 7(17):2205-2210 (1997).
19 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.
20 Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22.
21 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
22 Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51.
23 Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9.
24 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
25 Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines. Bioorg Med Chem Lett. 2002 Jan 21;12(2):181-4.
26 Tranexamic acid in trauma: how should we use it. J Trauma Acute Care Surg. 2013 Jun;74(6):1575-86.
27 The blockage of the high-affinity lysine binding sites of plasminogen by EACA significantly inhibits prourokinase-induced plasminogen activation. Biochim Biophys Acta. 2002 Apr 29;1596(2):182-92.
28 Acute anuric renal failure with streptokinase therapy in a patient with acute venous thromboembolic disease and the review of renal side effects of streptokinase. Tuberk Toraks. 2008;56(4):456-61.
29 Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8.
30 Thrombolytic therapies: the current state of affairs. J Endovasc Ther. 2005 Apr;12(2):224-32.
31 Evaluation of thrombolytic agents. Drugs. 1997;54 Suppl 3:11-6; discussion 16-7.
32 Fibrin binding and the regulation of plasminogen activators during thrombolytic therapy. Cardiovasc Hematol Agents Med Chem. 2008 Jul;6(3):212-23.
33 Vampire bat salivary plasminogen activator (desmoteplase): a unique fibrinolytic enzyme that does not promote neurodegeneration. Stroke. 2003 Feb;34(2):537-43.
34 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.
35 New antithrombotic drugs (excluding plasminogen activators. Arch Mal Coeur Vaiss. 2001 Nov;94(11 Suppl):1225-32.
36 New anticoagulants. Am Heart J. 2001 Aug;142(2 Suppl):S3-8.
37 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
38 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).
39 Recombinant hirudin (lepirudin) as anticoagulant in intensive care patients treated with continuous hemodialysis. Kidney Int Suppl. 1999 Nov;(72):S46-50.
40 Anticoagulation with anisindione in a patient with a warfarin-induced skin eruption. Pharmacotherapy. 2003 Apr;23(4):533-6.
41 Antithrombin III Utilization in a Large Teaching Hospital. P T. 2013 December; 38(12): 764-767, 779.