Compounds > rg 14893
Page last updated: 2024-11-07

rg 14893

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

Description

RG 14893: structure in first source; leukotriene B4 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132379
CHEMBL ID328712
SCHEMBL ID1894401
MeSH IDM0208580

Synonyms (17)

Synonym
rg-14893
CHEMBL328712 ,
rg14893
4-(2-(methyl(2-phenethyl)amino)-2-oxoethyl)-8-(phenylmethoxy)-2-naphthalenecarboxylic acid
2-naphthalenecarboxylic acid, 4-(2-(methyl(2-phenylethyl)amino)-2-oxoethyl)-8-(phenylmethoxy)-
141835-49-6
4-(2-(methyl(2-phenylethyl)amino)-2-oxoethyl)-8-(phenylmethoxy)-2-naphthalenecarboxylic acid
rg 14893
L006851
8-benzyloxy-4-[(methyl-phenethyl-carbamoyl)-methyl]-naphthalene-2-carboxylic acid (rg14893)
8-benzyloxy-4-[(methyl-phenethyl-carbamoyl)-methyl]-naphthalene-2-carboxylic acid
bdbm50001609
SCHEMBL1894401
2-naphthalenecarboxylicacid, 4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-
DTXSID30161835
4-[2-[methyl(2-phenylethyl)amino]-2-oxoethyl]-8-phenylmethoxynaphthalene-2-carboxylic acid
AKOS040749291
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Leukotriene B4 receptor 1Homo sapiens (human)IC50 (µMol)0.00480.00080.30913.2500AID102317; AID102318; AID102456; AID102654; AID160327
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.00150.00010.51267.0000AID102305; AID102491; AID102633; AID102635
Leukotriene B4 receptor 2Homo sapiens (human)IC50 (µMol)0.00470.00200.53022.9000AID102318
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
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 (4)

Processvia Protein(s)Taxonomy
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 (3)

Processvia Protein(s)Taxonomy
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 (15)

Assay IDTitleYearJournalArticle
AID160327Concentration inhibiting 1 nM LTB4-induced aggregation in GP polymorphonuclear (PMN) leukocytes.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102304Antagonistic activity against LTB4 receptor using guinea pig (GP) spleen cell membrane1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID160326Dose of the compound (administered orally) required to inhibit chemotaxis of [111In]-labeled PMNs to LTB4-induced wheals in guinea pig1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102287LTB4 receptor binding from radioligand binding assay using guinea pig spleen cell membrane1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain.
AID147700Effect on LTB4-induced neutrophil function (neutrophilia) after systemic administration of 0.3 micro/kg to cynomolgus monkey.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102317Compound tested for binding affinity against Leukotriene B4 receptor using radioligand binding assay from Human PMN cells1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships.
AID102654Antagonistic activity against monkey neutrophil LTB4 receptor 2 min after an iv dose of 3 mg/kg. 1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID147699Effect on LTB4-induced neutrophil function (neutropenia) after systemic administration of 0.3 micro/kg to cynomolgus monkey.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102491Affinity for human PMN LTB-4 receptors.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102635Binding affinity at leukotriene B4 receptor on intact human PMNs by displacement of [3H]LTB4.1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.
AID102305Affinity for guinea pig PMN LTB-4 receptors.1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID102456Concentration inhibiting the binding of [3H]LTB4 to human whole cell neutrophils1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
AID99773Binding affinity for Leukotriene B4 receptor of guinea pig spleen membranes1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships.
AID102318LTB4 receptor binding from radioligand binding assay using human intact neutrophils PMN1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
Structure-activity relationships study of two series of leukotriene B4 antagonists: novel indolyl and naphthyl compounds substituted with a 2-[methyl(2-phenethyl)amino]-2-oxoethyl side chain.
AID102633Binding affinity against LTB4 receptors in human PMNs using [3H]LTB4 as radioligand1993Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.
[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's5 (100.00)18.2507
2000's0 (0.00)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: 12.66

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 Index12.66 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.66)

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]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
2-naphthol
2-naphthol: RN given refers to parent cpd. 2-naphthol : A naphthol carrying a hydroxy group at position 2.. naphthols : Any hydroxynaphthalene derivative that has a single hydroxy substituent.		2.3920naphtholantinematodal drug;
genotoxin;
human urinary metabolite;
human xenobiotic metabolite;
mouse metabolite;
radical scavenger
sc 41930
SC 41930: leukotriene B4 receptor antagonist; structure in first source		2.3820
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		2.3920dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
sb 201993
(E)-3-((((6-(2-carboxyethenyl)-5-((8-(4-methoxyphenyl)octyl)oxy)-2-pyridinyl)methyl)thio)methyl)benzoic acid: structure given in first source; a competitive LTB(4) receptor antagonist		2.3920
ono 4057
ONO-LB 457: LTB4 receptor antagonist; structure given in first source		2.3920
ly 223982
LY 223982: RN & structure in first source; leukotriene B4 antagonist		2.6730
ConditionIndicatedRelationship StrengthStudiesTrials
Innate Inflammatory Response
[description not available]		01.9810
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		01.9810