Page last updated: 2024-12-11

cp 195543

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

Description

CP 195543: a potent & selective leukotriene B4 antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9823886
CHEMBL ID301829
SCHEMBL ID896066
MeSH IDM0291499

Synonyms (25)

Synonym
cp-195,543
cp-195543
CHEMBL301829 ,
cp195543
cp 195543
gtpl6155
2-[(3s,4r)-4-hydroxy-3-(phenylmethyl)chroman-7-yl]-4-(trifluoromethyl)benzoic acid
204981-48-6
benzoic acid, 2-((3s,4r)-3,4-dihydro-4-hydroxy-3-(phenylmethyl)-2h-1-benzopyran-7-yl)-4-(trifluoromethyl)-
YB1F0V77MK ,
SCHEMBL896066
(3s,4r)-2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoicacid
(3s,4r)-2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoic acid
(3s, 4r)-2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoicacid
(3s, 4r)-2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoic acid
unii-yb1f0v77mk
2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoic acid
DB13053
bdbm50215854
Q27076890
2-[(3s,4r)-3-benzyl-4-hydroxy-3,4-dihydro-2h-chromen-7-yl]-4-(trifluoromethyl)benzoic acid
2-((3s,4r)-3-benzyl-4-hydroxychroman-7-yl)-4-(trifluoromethyl)benzoic acid
CS-0063240
HY-112742
AKOS040751267
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
B2 bradykinin receptorHomo sapiens (human)IC50 (µMol)0.28000.00040.02120.2800AID90992
Leukotriene B4 receptor 1Homo sapiens (human)IC50 (µMol)0.05250.00080.30913.2500AID101316; AID90992; AID90993
Leukotriene B4 receptor 2Homo sapiens (human)IC50 (µMol)0.05250.00200.53022.9000AID101316; AID90992; AID90993
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (24)

Processvia Protein(s)Taxonomy
smooth muscle contractionB2 bradykinin receptorHomo sapiens (human)
inflammatory responseB2 bradykinin receptorHomo sapiens (human)
cell surface receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayB2 bradykinin receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationB2 bradykinin receptorHomo sapiens (human)
blood circulationB2 bradykinin receptorHomo sapiens (human)
response to salt stressB2 bradykinin receptorHomo sapiens (human)
regulation of vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
negative regulation of peptidyl-serine phosphorylationB2 bradykinin receptorHomo sapiens (human)
vasoconstrictionB2 bradykinin receptorHomo sapiens (human)
vasodilationB2 bradykinin receptorHomo sapiens (human)
regulation of vascular permeabilityB2 bradykinin receptorHomo sapiens (human)
arachidonic acid secretionB2 bradykinin receptorHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediatorB2 bradykinin receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayB2 bradykinin receptorHomo sapiens (human)
muscle contractionLeukotriene B4 receptor 1Homo sapiens (human)
inflammatory responseLeukotriene B4 receptor 1Homo sapiens (human)
immune responseLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 1Homo sapiens (human)
chemotaxisLeukotriene B4 receptor 2Homo sapiens (human)
negative regulation of adenylate cyclase activityLeukotriene B4 receptor 2Homo sapiens (human)
keratinocyte migrationLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protease bindingB2 bradykinin receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityB2 bradykinin receptorHomo sapiens (human)
bradykinin receptor activityB2 bradykinin receptorHomo sapiens (human)
protein bindingB2 bradykinin receptorHomo sapiens (human)
type 1 angiotensin receptor bindingB2 bradykinin receptorHomo sapiens (human)
protein heterodimerization activityB2 bradykinin receptorHomo sapiens (human)
nucleotide bindingLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 1Homo sapiens (human)
leukotriene receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
leukotriene B4 receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
G protein-coupled peptide receptor activityLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
endosomeB2 bradykinin receptorHomo sapiens (human)
Golgi apparatusB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
intracellular membrane-bounded organelleB2 bradykinin receptorHomo sapiens (human)
plasma membraneB2 bradykinin receptorHomo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
nucleoplasmLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
membraneLeukotriene B4 receptor 2Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (8)

Assay IDTitleYearJournalArticle
AID90993Ability to inhibit LTB4-induced chemotaxis of isolated human neutrophils.1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID90992Ability to inhibit LTB4-induced CD11b up-regulation on isolated human neutrophils1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID101316Ability to inhibit LTB4 binding to LTB receptors on isolated human neutrophils.1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID21881Compound was evaluated for its lipophilicity1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID91155Ability to inhibit LTB4-induced CD11b up-regulation on isolated human neutrophils in whole blood1998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID232097Ratio of CD11b(WB) IC50 to CD11b (IC)IC501998Bioorganic & medicinal chemistry letters, Jul-21, Volume: 8, Issue:14
trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor.
AID1346072Human BLT1 receptor (Leukotriene receptors)1998The Journal of pharmacology and experimental therapeutics, Jun, Volume: 285, Issue:3
The preclinical pharmacological profile of the potent and selective leukotriene B4 antagonist CP-195543.
AID1346050Human BLT2 receptor (Leukotriene receptors)2001The Journal of biological chemistry, Apr-13, Volume: 276, Issue:15
Hydroxyeicosanoids bind to and activate the low affinity leukotriene B4 receptor, BLT2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (60.00)18.2507
2000's2 (40.00)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: 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.

MetricThis Compound (vs All)
Research Demand Index12.50 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.50)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]