Page last updated: 2024-12-06

ro 24-4736

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

Description

Ro 24-4736: structure given in first source; platelet activating factor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60775
CHEMBL ID277650
SCHEMBL ID7528667
MeSH IDM0193802

Synonyms (21)

Synonym
ro 24-4736
CHEMBL277650 ,
5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)phenanthridin-6(5h)-one
ro-24-4736
125030-71-9
bdbm50011638
5-{3-[4-(2-chloro-phenyl)-9-methyl-6h-1-thia-5,7,8,9a-tetraaza-cyclopenta[e]azulen-2-yl]-prop-2-ynyl}-5h-phenanthridin-6-one
SCHEMBL7528667
i2mj13sofo ,
6(5h)-phenanthridinone, 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propynyl)-
unii-i2mj13sofo
DTXSID80154550
HY-19097
CS-6683
5-[3-[7-(2-chlorophenyl)-13-methyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-4-yl]prop-2-ynyl]phenanthridin-6-one
ro24-4736
6(5h)-phenanthridinone, 5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-2-yl)-2-propyn-1-yl)-
5-(3-(4-(2-chlorophenyl)-9-methyl-6h-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)-diazepin-2-yl)-2-propynyl)phenanthridin-6(5h)-one
ro-244736
ro 244736
AKOS040742561

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Peak plasma and tissue concentrations were seen at 5 minutes after dosing except for the small intestine (4 hrs) and abdominal fat, stomach and large intestine (4 hrs)."( Disposition and metabolism of Ro 24-4736 in the rat.
Anastasi, EM; Chang, D; Liberato, DJ; Loh, AC; Sasso, GJ; Williams, TH, 1994
)
0.58
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Platelet-activating factor receptorHomo sapiens (human)IC50 (µMol)0.01300.00030.63183.7000AID59351
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (29)

Processvia Protein(s)Taxonomy
positive regulation of cellular extravasationPlatelet-activating factor receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIPlatelet-activating factor receptorHomo sapiens (human)
chemotaxisPlatelet-activating factor receptorHomo sapiens (human)
inflammatory responsePlatelet-activating factor receptorHomo sapiens (human)
immune responsePlatelet-activating factor receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
parturitionPlatelet-activating factor receptorHomo sapiens (human)
response to symbiotic bacteriumPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide-mediated signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of interleukin-6 productionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of tumor necrosis factor productionPlatelet-activating factor receptorHomo sapiens (human)
inositol trisphosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of neutrophil degranulationPlatelet-activating factor receptorHomo sapiens (human)
transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of translationPlatelet-activating factor receptorHomo sapiens (human)
negative regulation of blood pressurePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processPlatelet-activating factor receptorHomo sapiens (human)
cellular response to gravityPlatelet-activating factor receptorHomo sapiens (human)
cellular response to cAMPPlatelet-activating factor receptorHomo sapiens (human)
cellular response to fatty acidPlatelet-activating factor receptorHomo sapiens (human)
response to dexamethasonePlatelet-activating factor receptorHomo sapiens (human)
positive regulation of leukocyte tethering or rollingPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of transcytosisPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of maternal process involved in parturitionPlatelet-activating factor receptorHomo sapiens (human)
positive regulation of gastro-intestinal system smooth muscle contractionPlatelet-activating factor receptorHomo sapiens (human)
cellular response to 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholinePlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
lipopolysaccharide bindingPlatelet-activating factor receptorHomo sapiens (human)
lipopolysaccharide immune receptor activityPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled receptor activityPlatelet-activating factor receptorHomo sapiens (human)
platelet activating factor receptor activityPlatelet-activating factor receptorHomo sapiens (human)
protein bindingPlatelet-activating factor receptorHomo sapiens (human)
phospholipid bindingPlatelet-activating factor receptorHomo sapiens (human)
mitogen-activated protein kinase bindingPlatelet-activating factor receptorHomo sapiens (human)
G protein-coupled purinergic nucleotide receptor activityPlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membranePlatelet-activating factor receptorHomo sapiens (human)
membranePlatelet-activating factor receptorHomo sapiens (human)
secretory granule membranePlatelet-activating factor receptorHomo sapiens (human)
tertiary granule membranePlatelet-activating factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID76987Inhibition of PAF-induced bronchoconstriction in the guinea pig after intravenous administration1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
AID77482Inhibitory activity at 0.03 mg/kg was determined against PAF-induced bronchoconstriction in guinea pig1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
AID76854Inhibition of PAF-induced bronchoconstriction in guinea pig after oral administration after two-hour pretreatment time1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
AID59351PAF-antagonist activity determined in dog platelets by PAF-binding assay1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's12 (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: 11.81

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 Index11.81 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (8.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (91.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]