Compounds > ns 004
Page last updated: 2024-11-10

ns 004

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

Cross-References

ID SourceID
PubMed CID5311330
CHEMBL ID375448
SCHEMBL ID3102522
SCHEMBL ID8911620
MeSH IDM0221509

Synonyms (22)

Synonym
ns004 ,
EC-000.2036
ns-004
CHEMBL375448
ns-o04
3-(5-chloro-2-hydroxyphenyl)-6-(trifluoromethyl)-1h-benzimidazol-2-one
2h-benzimidazol-2-one, 1-(5-chloro-2-hydroxyphenyl)-1,3-dihydro-5-(trifluoromethyl)-
1-(5-chloro-2-hydroxyphenyl)-5-(trifluoromethyl)-2,3-dihydro-1h-1,3-benzodiazol-2-one
gtpl4271
SCHEMBL3102522
SCHEMBL8911620
1-[2-hydroxy-5-chlorophenyl]-5-trifluoromethyl-2-benzimidazolone
1,3-dihydro-1-(5-chloro-2-hydroxyphenyl)-5-trifluoromethyl-2h-benzimidazol-2-one
1-(5-chloro-2-hydroxyphenyl)-5-trifluoromethyl-1,3-dihydrobenzoimidazol-2-one
141797-92-4
Q27088041
1-(5-chloro-2-hydroxy-phenyl)-5-trifluoromethyl-1,3-dihydro-benzoimidazol-2-one
F79305
1-(5-cl-2-oh-phenyl)-5-cf3-benzimidazolin-2-one
1-(5-chloro-2-hydroxyphenyl)-5-trifluoromethyl-benzimidazolin-2-one
AB91058
AKOS040749041
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID277717Brain to plasma ration in Sprague-Dawley rat after 2 hrs2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.
AID26347pKa value was determined2003Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8
Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.
AID95622Maxi-K opening activity on cloned human (hSlo) large- conductance (BK) Ca(2+)-activated K+ channel expressed in Xenopus laevis oocytes at concentration of 20 uM2003Bioorganic & medicinal chemistry letters, Apr-17, Volume: 13, Issue:8
Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.
AID221843Effect on Maxi-K-Mediated outward current in Xenopus laevis oocytes expressing cloned mSlo maxi-K channels at 20 uM2002Journal of medicinal chemistry, Mar-28, Volume: 45, Issue:7
Synthesis and structure-activity relationships of 3-aryloxindoles: a new class of calcium-dependent, large conductance potassium (maxi-K) channel openers with neuroprotective properties.
AID161271Compound was tested for its effect on maxi-K-mediated outward current in Xenopus laevis oocytes expressing the cloned maxi-K channel mslo at a concentration of 20 uM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and structure-activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel opener targeted for urge urinary incontinence.
AID277716Brain to plasma ratio in Sprague-Dawley rat after 15 mins2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.
AID182548Compound was tested for percentage inhibition of isometric force in response to a test compound in isolated rat bladder strips pre-contracted with carbachol at a concentration of 20 uM2002Bioorganic & medicinal chemistry letters, Apr-08, Volume: 12, Issue:7
The synthesis and structure-activity relationships of 1,3-diaryl 1,2,4-(4H)-triazol-5-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel opener targeted for urge urinary incontinence.
AID219759Effect of compound (20 uM) on maxi-K-mediated outward current in Xenopus laevis oocytes expressing the cloned hSlo maxi-K channels was determined2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction.
AID277712Opening of cloned human maxi-K ion channel expressed in Xenopus laevis oocytes measured as outward current at 20 uM relative to control by voltage clamp method2007Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3
3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR.
AID252347Effect on maxi-K mediated outward current in xenopus laevis oocytes at 20 uM2004Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17
4-Aryl-3-(mercapto)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle.
AID166651Percentage inhibition of isometric force in response to 10 uM compound in isolated rabbit corpus cavernosum precontracted with 3 uM phenylephrine2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
4-Aryl-3-(hydroxyalkyl)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle targeted for erectile dysfunction.
AID108448Percent opening of mouse maxi-K channel expressed in xenopus oocyte at a concentration of 20 umolar under voltage clamp.2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
4,5-diphenyltriazol-3-ones: openers of large-conductance Ca(2+)-activated potassium (maxi-K) channels.
AID251710Percentage inhibition by the compound in isolated rabbit corpus cavernosum at 10 uM2004Bioorganic & medicinal chemistry letters, Sep-06, Volume: 14, Issue:17
4-Aryl-3-(mercapto)quinolin-2-ones: novel maxi-K channel opening relaxants of corporal smooth muscle.
AID219774Tested for the effect on maxi-K-mediated outward current (mSlo) in Xenopus laevis oocytes at 20 uM2002Bioorganic & medicinal chemistry letters, Jul-08, Volume: 12, Issue:13
The synthesis and structure-activity relationships of 4-aryl-3-aminoquinolin-2-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel openers targeted for post-stroke neuroprotection.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's8 (100.00)29.6817
2010's0 (0.00)24.3611
2020's0 (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: 26.35

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.35 (24.57)
Research Supply Index2.20 (2.92)
Research Growth Index4.36 (4.65)
Search Engine Demand Index35.52 (26.88)
Search Engine Supply Index2.89 (0.95)

This Compound (26.35)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
bithionol
Bithionol: Halogenated anti-infective agent that is used against trematode and cestode infestations.. bithionol : An aryl sulfide that is diphenyl sulfide in which each phenyl group is substituted at position 2 by hydroxy and at positions 3 and 5 by chlorine. A fungicide and anthelmintic, it was used in various topical drug products for the treatment of liver flukes, but withdrawn after being shown to be a potent photosensitizer with the potential to cause serious skin disorders.		2.0110aryl sulfide;
bridged diphenyl antifungal drug;
bridged diphenyl fungicide;
dichlorobenzene;
organochlorine pesticide;
polyphenol		antifungal agrochemical;
antiplatyhelmintic drug
dichlorophen
Dichlorophen: Nontoxic laxative vermicide effective for taenia infestation. It tends to produce colic and nausea. It is also used as a veterinary fungicide, anthelmintic, and antiprotozoan. (From Merck, 11th ed.)		2.0110bridged diphenyl fungicide;
diarylmethane
hexachlorophene
Hexachlorophene: A chlorinated bisphenol antiseptic with a bacteriostatic action against Gram-positive organisms, but much less effective against Gram-negative organisms. It is mainly used in soaps and creams and is an ingredient of various preparations used for skin disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p797). hexachlorophene : An organochlorine compound that is diphenylmethane in which each of the phenyl groups is substituted by chlorines at positions 2, 3, and 5, and by a hydroxy group at position 6. An antiseptic that is effective against Gram-positive organisms, it is used in soaps and creams for the treatment of various skin disorders. It is also used in agriculture as an acaricide and fungicide, but is not approved for such use within the European Union.		2.0110bridged diphenyl fungicide;
polyphenol;
trichlorobenzene		acaricide;
antibacterial agent;
antifungal agrochemical;
antiseptic drug
ns 1619
NS 1619: structure given in first source. NS 1619 : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca).		2.4220(trifluoromethyl)benzenes;
benzimidazoles;
phenols		potassium channel opener
ns 1608
NS 1608: a BK(Ca) channel opener		2.0110ureas
bms 191011
3-((5-chloro-2-hydroxyphenyl)methyl)-5-(4-(trifluoromethyl)phenyl)-1,3,4-oxadiazol-2(3H)-one: a maxi-K channel opener; structure in first source		2.0310(trifluoromethyl)benzenes
ConditionIndicatedRelationship StrengthStudiesTrials
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		02.4220
Urinary Incontinence
Involuntary loss of URINE, such as leaking of urine. It is a symptom of various underlying pathological processes. Major types of incontinence include URINARY URGE INCONTINENCE and URINARY STRESS INCONTINENCE.		02.0110
Apoplexy
[description not available]		02.4220
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0110
Stroke
A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)		02.4220
Impotence
[description not available]		02.0110
Erectile Dysfunction
The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.		02.0110