Compounds > oglemilast
Page last updated: 2024-08-02 19:50:45

oglemilast

Description

oglemilast: a PDE4 inhibitor and NSAID; no further info available 1/2006 [MeSH]

Cross-References

ID SourceID
PubMed CID11387409
CHEMBL ID4297520
SCHEMBL ID220245
MeSH IDM0493520

Synonyms (29)

Synonym
HY-15178
grc 3886
778576-62-8
oglemilast
67gxq6wcc6 ,
grc-3886
oglemilast [inn]
grc3886
unii-67gxq6wcc6
n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methylsulfonamido)dibenzo[b,d]furan-1-carboxamide
AKOS016005519
CS-0844
SCHEMBL220245
grc 3845
oglemilast [who-dd]
n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-((methylsulfonyl)amino)dibenzo(b,d)furan-1-carboxamide
NCGC00379066-01
DB12375
BCP21392
n-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-8-(methanesulfonamido)dibenzofuran-1-carboxamide
Q27264129
CHEMBL4297520
F84855
MS-29580
DTXSID70999058
n-(3,5-dichloropyridin-4(1h)-ylidene)-4-(difluoromethoxy)-8-[(methanesulfonyl)amino]dibenzo[b,d]furan-1-carboxamide
4-difluoromethoxy-8-methanesulfonylamino-dibenzofuran-1-carboxylic acid (3,5-dichloro-pyridin-4-yl)-amide
A853039
okfdrahpfkmajh-uhfffaoysa-n

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.3379AID1645841
GVesicular stomatitis virusPotency3.3786AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency11.9877AID1645840
Interferon betaHomo sapiens (human)Potency3.3786AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency3.3786AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency3.3786AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency3.3786AID1645842

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)IC500.1660AID1619495

Bioassays (7)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560		Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111		A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490		Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1713838Antiinflammatory activity in Swiss albino mouse model of LPS-induced sepsis assessed as reduction in TNFalpha production at 1 mg/kg, po administered 30 mins before LPS stimulation and measured after 90 min by ELISA relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ISSN: 1464-3391		In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors.
AID1713836Antiinflammatory activity in Swiss albino mouse model of LPS-induced sepsis assessed as reduction in TNFalpha production at 10 mg/kg, po administered 30 mins before LPS stimulation and measured after 90 min by ELISA relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
ISSN: 1464-3391		In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors.

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's2 (40.00)24.3611
2020's2 (40.00)2.80

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
roflumilast
1
aromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound		anti-asthmatic drug;
phosphodiesterase IV inhibitor		201620168.0high000010
apremilast
1
aromatic ether;
N-acetylarylamine;
phthalimides;
sulfone		non-steroidal anti-inflammatory drug;
phosphodiesterase IV inhibitor		201620168.0high000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
2-oxindole
1
gamma-lactam;
indolinone		2005200519.0high000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Arthritis, Rheumatoid0
1
2005200519.0low000100
Colitis, Granulomatous0
1
2005200519.0low000100
Congenital Zika Syndrome0
1
202020204.0low000010
Crohn Disease0
1
2005200519.0low000100
Disease Models, Animal0
2
2005202011.5medium000110
Inflammation0
1
2005200519.0low000100
Innate Inflammatory Response0
1
2005200519.0low000100
MS (Multiple Sclerosis)0
1
2005200519.0low000100
Multiple Sclerosis0
1
2005200519.0low000100
Rheumatoid Arthritis0
1
2005200519.0low000100
Zika Virus Infection0
1
202020204.0low000010

Bioavailability (1)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5		2019