Page last updated: 2024-11-11

uk-356,202

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

UK-356,202: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9885167
CHEMBL ID	111576
SCHEMBL ID	6437325
MeSH ID	M0534894

Synonyms (17)

Synonym
3-(4-chloro-1-guanidino-isoquinolin-7-yl)-benzoic acid
bdbm50147422
uk-356202
1-isoquinolinylguanidine 3
bdbm16129
3-{4-chloro-1-[(diaminomethylidene)amino]isoquinolin-7-yl}benzoic acid
3-[4-chloro-1-(diaminomethylideneamino)isoquinolin-7-yl]benzoic acid
CHEMBL111576 ,
AKOS015966399
uk-356,202
compound 13j [pmid: 15149680]
gtpl6543
SCHEMBL6437325
DTXSID40432402
223671-94-1
3-(4-chloro-1-guanidinoisoquinolin-7-yl)benzoic acid
Q27089077

Research Excerpts

Bioavailability

Excerpt	Reference	Relevance
" Subsequent optimization led to 15, a potent, selective, and orally bioavailable inhibitor of uPA."	( Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator. Callaghan, O; Chessari, G; Congreve, M; Cowan, SR; Frederickson, M; Matthews, JE; McMenamin, R; Smith, DM; Vinković, M; Wallis, NG, 2008)	0.35

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Plasminogen	Homo sapiens (human)	Ki	0.0170	0.0170	1.1560	4.4000	AID1797470
Urokinase-type plasminogen activator	Homo sapiens (human)	IC50 (µMol)	0.0370	0.0370	3.3859	10.0000	AID312586
Urokinase-type plasminogen activator	Homo sapiens (human)	Ki	0.0303	0.0170	2.6268	7.0000	AID1265737; AID1797470; AID215979
Tissue-type plasminogen activator	Homo sapiens (human)	Ki	0.0170	0.0170	3.7196	8.6000	AID1797470
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (40)

Process	via Protein(s)	Taxonomy
proteolysis	Plasminogen	Homo sapiens (human)
blood coagulation	Plasminogen	Homo sapiens (human)
negative regulation of cell population proliferation	Plasminogen	Homo sapiens (human)
negative regulation of cell-substrate adhesion	Plasminogen	Homo sapiens (human)
extracellular matrix disassembly	Plasminogen	Homo sapiens (human)
tissue regeneration	Plasminogen	Homo sapiens (human)
fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Plasminogen	Homo sapiens (human)
myoblast differentiation	Plasminogen	Homo sapiens (human)
muscle cell cellular homeostasis	Plasminogen	Homo sapiens (human)
tissue remodeling	Plasminogen	Homo sapiens (human)
biological process involved in interaction with symbiont	Plasminogen	Homo sapiens (human)
negative regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
positive regulation of fibrinolysis	Plasminogen	Homo sapiens (human)
trophoblast giant cell differentiation	Plasminogen	Homo sapiens (human)
labyrinthine layer blood vessel development	Plasminogen	Homo sapiens (human)
mononuclear cell migration	Plasminogen	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Plasminogen	Homo sapiens (human)
negative regulation of cell-cell adhesion mediated by cadherin	Plasminogen	Homo sapiens (human)
positive regulation of cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Urokinase-type plasminogen activator	Homo sapiens (human)
proteolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
chemotaxis	Urokinase-type plasminogen activator	Homo sapiens (human)
signal transduction	Urokinase-type plasminogen activator	Homo sapiens (human)
blood coagulation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of signaling receptor activity	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell migration	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell adhesion mediated by integrin	Urokinase-type plasminogen activator	Homo sapiens (human)
urokinase plasminogen activator signaling pathway	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of cell population proliferation	Urokinase-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of wound healing	Urokinase-type plasminogen activator	Homo sapiens (human)
regulation of smooth muscle cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
response to hypoxia	Tissue-type plasminogen activator	Homo sapiens (human)
proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
blood coagulation	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
plasminogen activation	Tissue-type plasminogen activator	Homo sapiens (human)
protein modification process	Tissue-type plasminogen activator	Homo sapiens (human)
fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of proteolysis	Tissue-type plasminogen activator	Homo sapiens (human)
negative regulation of fibrinolysis	Tissue-type plasminogen activator	Homo sapiens (human)
prevention of polyspermy	Tissue-type plasminogen activator	Homo sapiens (human)
trans-synaptic signaling by BDNF, modulating synaptic transmission	Tissue-type plasminogen activator	Homo sapiens (human)
platelet-derived growth factor receptor signaling pathway	Tissue-type plasminogen activator	Homo sapiens (human)
smooth muscle cell migration	Tissue-type plasminogen activator	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Process	via Protein(s)	Taxonomy
protease binding	Plasminogen	Homo sapiens (human)
endopeptidase activity	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Plasminogen	Homo sapiens (human)
signaling receptor binding	Plasminogen	Homo sapiens (human)
protein binding	Plasminogen	Homo sapiens (human)
serine-type peptidase activity	Plasminogen	Homo sapiens (human)
enzyme binding	Plasminogen	Homo sapiens (human)
kinase binding	Plasminogen	Homo sapiens (human)
protein domain specific binding	Plasminogen	Homo sapiens (human)
apolipoprotein binding	Plasminogen	Homo sapiens (human)
protein-folding chaperone binding	Plasminogen	Homo sapiens (human)
protein antigen binding	Plasminogen	Homo sapiens (human)
serine-type endopeptidase activity	Urokinase-type plasminogen activator	Homo sapiens (human)
protein binding	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase activity	Tissue-type plasminogen activator	Homo sapiens (human)
signaling receptor binding	Tissue-type plasminogen activator	Homo sapiens (human)
protein binding	Tissue-type plasminogen activator	Homo sapiens (human)
phosphoprotein binding	Tissue-type plasminogen activator	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Process	via Protein(s)	Taxonomy
extracellular region	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
plasma membrane	Plasminogen	Homo sapiens (human)
external side of plasma membrane	Plasminogen	Homo sapiens (human)
cell surface	Plasminogen	Homo sapiens (human)
platelet alpha granule lumen	Plasminogen	Homo sapiens (human)
collagen-containing extracellular matrix	Plasminogen	Homo sapiens (human)
extracellular exosome	Plasminogen	Homo sapiens (human)
blood microparticle	Plasminogen	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Plasminogen	Homo sapiens (human)
glutamatergic synapse	Plasminogen	Homo sapiens (human)
extracellular space	Plasminogen	Homo sapiens (human)
extracellular region	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
focal adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
external side of plasma membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
cell surface	Urokinase-type plasminogen activator	Homo sapiens (human)
specific granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Urokinase-type plasminogen activator	Homo sapiens (human)
tertiary granule membrane	Urokinase-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Urokinase-type plasminogen activator	Homo sapiens (human)
protein complex involved in cell-matrix adhesion	Urokinase-type plasminogen activator	Homo sapiens (human)
serine-type endopeptidase complex	Urokinase-type plasminogen activator	Homo sapiens (human)
extracellular space	Urokinase-type plasminogen activator	Homo sapiens (human)
collagen-containing extracellular matrix	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular region	Tissue-type plasminogen activator	Homo sapiens (human)
cytoplasm	Tissue-type plasminogen activator	Homo sapiens (human)
cell surface	Tissue-type plasminogen activator	Homo sapiens (human)
secretory granule	Tissue-type plasminogen activator	Homo sapiens (human)
apical part of cell	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular exosome	Tissue-type plasminogen activator	Homo sapiens (human)
serine protease inhibitor complex	Tissue-type plasminogen activator	Homo sapiens (human)
Schaffer collateral - CA1 synapse	Tissue-type plasminogen activator	Homo sapiens (human)
glutamatergic synapse	Tissue-type plasminogen activator	Homo sapiens (human)
extracellular space	Tissue-type plasminogen activator	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay ID	Title	Year	Journal	Article
AID312586	Inhibition of uPA	2008	Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2	Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.
AID215979	Inhibitory activity against human urokinase-type plasminogen activator was evaluated using S-2444 as substrate	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
AID210746	Inhibitory activity against human tissue type plasminogen activator was evaluated using S-2444 as substrate and tissue plasminogen activator stimulator at 100 mM	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
AID157835	Inhibitory activity against human plasmin was evaluated using chromozym-PL as substrate at 10 uM	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
AID1265737	Inhibition of human uPA using S-2444 as substrate	2015	Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23	Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.
AID1797470	Determination of Inhibitor Potency and Selectivity from Article 10.1021/jm061066t: \\Selective Urokinase-Type Plasminogen Activator Inhibitors. 4. 1-(7-Sulfonamidoisoquinolinyl)guanidines.\\	2007	Journal of medicinal chemistry, May-17, Volume: 50, Issue:10	Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (80.00)	29.6817
2010's	1 (20.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	12.50 (24.57)
Research Supply Index	1.79 (2.92)
Research Growth Index	4.30 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.50)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
bis(5-amidino-2-benzimidazolyl)methane bis(5-amidino-2-benzimidazolyl)methane: aromatic diamidine which has a significant suppressive effect on the cytopathology & yield of respiratory synctial (RS) virus; RN given refers to parent cpd	2.03	1
gabexate Gabexate: A serine proteinase inhibitor used therapeutically in the treatment of pancreatitis, disseminated intravascular coagulation (DIC), and as a regional anticoagulant for hemodialysis. The drug inhibits the hydrolytic effects of thrombin, plasmin, and kallikrein, but not of chymotrypsin and aprotinin.	2.11	1	benzoate ester
phenylguanidine phenylguanidine: RN given refers to parent cpd	2.11	1
amiloride Amiloride: A pyrazine compound inhibiting SODIUM reabsorption through SODIUM CHANNELS in renal EPITHELIAL CELLS. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with DIURETICS to spare POTASSIUM loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705). amiloride : A member of the class of pyrazines resulting from the formal monoacylation of guanidine with the carboxy group of 3,5-diamino-6-chloropyrazine-2-carboxylic acid.	2.11	1	aromatic amine; guanidines; organochlorine compound; pyrazines	diuretic; sodium channel blocker
n-alpha-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(l)-phenyl-alanine-4-ethoxycarbonyl-piperazide hydrochloride [no description available]	2.47	2

Condition	Relationship Strength	Studies
Chronic Illness [description not available]	2.03	1
Dermatoses [description not available]	2.03	1
Acute Disease Disease having a short and relatively severe course.	2.03	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.03	1
Skin Diseases Diseases involving the DERMIS or EPIDERMIS.	2.03	1
Ulcer A lesion on the surface of the skin or a mucous surface, produced by the sloughing of inflammatory necrotic tissue.	2.03	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	2.05	1

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