Page last updated: 2024-11-11

ticolubant

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

Description

Ticolubant: a leukotriene B4 antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6441619
CHEMBL ID90214
SCHEMBL ID1892766
SCHEMBL ID1230392
MeSH IDM0578262

Synonyms (26)

Synonym
sb-209247
CHEMBL90214 ,
(e)-3-[6-(2,6-dichloro-phenylsulfanylmethyl)-3-phenethyloxy-pyridin-2-yl]-acrylic acid
bdbm50052027
154413-61-3
D06140
ticolubant (usan/inn)
ticolubant
L012387
SCHEMBL1892766
c1fru4800p ,
unii-c1fru4800p
3-(6-((2,6-dichlorophenyl)thio)methyl)-3-((2-phenylethoxy)-2-pyridinyl)-2-propenoic acid
sb 209247
ticolubant [usan:inn]
(e)-6-(((2,6-dichlorophenyl)thio)methyl)-3-(phenethyloxy)-2-pyridineacrylic acid
2-propenoic acid, 3-(6(((2,6-dichlorophenyl)thio)methyl)-3-(2-phenylethoxy)-2-pyridinyl)-, (e)-
ZJLFOOWTDISDIO-ZRDIBKRKSA-N
(e)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2-pyridinyl]-2-propenoic acid
ticolubant [usan]
ticolubant [inn]
(e)-6-[[(2,6-dichlorophenyl)thio]methyl]-3-(phenethyloxy)-2-pyridineacrylic acid
SCHEMBL1230392
(e)-3-[6-[(2,6-dichlorophenyl)sulfanylmethyl]-3-(2-phenylethoxy)pyridin-2-yl]prop-2-enoic acid
Q27275056
AKOS040749649

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This method has utility in evaluating the pharmacodynamic action of either LTB(4) receptor antagonists or immune cell modulators in effecting CD11b integrin expression and granulocyte activation in human subjects administered such drugs."( Human granulocyte CD11b expression as a pharmacodynamic biomarker of inflammation.
Carpenter, DC; Davis, HM; Griswold, DE; Hynicka, WP; Stahl, JM; Zhang, W, 2000
)
0.31
[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)
Polyunsaturated fatty acid 5-lipoxygenaseRattus norvegicus (Norway rat)IC50 (µMol)8.20000.00462.018210.0000AID7203
Leukotriene B4 receptor 1Homo sapiens (human)IC50 (µMol)10.02500.00080.30913.2500AID102457; AID102458
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.00080.00010.51267.0000AID102637; AID102639
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (7)

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)
[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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
plasma membraneLeukotriene B4 receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay IDTitleYearJournalArticle
AID7203Concentration required to inhibit RBL-1 supernatant 5-lipoxygenase1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID102637Inhibition of [3H]LTB4 binding to human neutrophils1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID89256Compound was tested in vitro inhibitory activity against LTB4 induced neutrophil degranulation1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID225501Dose required to inhibit 50% of arachidonic acid-induced inflammation after topical administration obtained from dose-response curves1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID131180Compound was tested in vivo inhibitory activity against PMA induced ear edema1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID89244Compound was tested in vitro for inhibitory activity in LTB4 induced Ca mobilization.1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID89249Compound was tested in vitro inhibitory activity against 12-R-HETE induced Ca mobilization1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID225842Effect on Arachidonic Acid-Induced Mouse Ear Inflammation expressed as percent inhibition of MPO at 50 ug/ear of topical administration1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID131174Compound was tested in vivo inhibitory activity against AA induced ear edema (topically)1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID102458Inhibitory concentration against LTB4 with [3H]- fMLP in receptor binding assay1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID102457Inhibitory concentration LTB4 with [3H]LTD4 in LTD4 receptor binding assay1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID102639Compound was tested for binding affinity against human neutrophil LTB4 (leukotriene) receptor1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID225840Effect on Arachidonic Acid-Induced Mouse Ear Inflammation expressed as percent inhibition of MPO at 25 mg/kg of oral administration1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID160342Concentration required to block LTB4 induced calcium mobilization in human PMNs1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID160343Concentration required to block LTB4 induced degranulation in human PMNs1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
AID131177Compound was tested in vivo inhibitory activity against AA induced ear edema(orally)1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
Modulators of leukotriene biosynthesis and receptor activation.
AID225500Dose required to inhibit 50% of arachidonic acid-induced inflammation after oral administration obtained from dose-response curves1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
[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]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]