Bookmark and Share
BioAssay: AID 160863

Inhibition of PGE-2 production in 3T3 (murine fibroblast) cell culture.

Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5-lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the arachidonic acid-induced murine ear edema model. On the basis of their promising profile of in vitro and more ..
_
   
 Tested Compounds
 Tested Compounds
All(23)
 
 
Active(11)
 
 
Unspecified(12)
 
 
 Tested Substances
 Tested Substances
All(23)
 
 
Active(11)
 
 
Unspecified(12)
 
 
 Related BioAssays
 Related BioAssays
AID: 160863
Data Source: ChEMBL (158122)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-21
Modify Date: 2014-05-19

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 11
Description:
Title: Dibenzoxepinone hydroxylamines and hydroxamic acids: dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity.

Abstract: Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5-lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the arachidonic acid-induced murine ear edema model. On the basis of their promising profile of in vitro and in vivo activities, hydroxamic acids 24h, 3-(6,11-dihydro-11-oxodibenz[b,e]oxepin-2-yl)-N-hydroxy-N-++ +methylpropanamide (HP 977), and 25, 3-(6,11-dihydrodibenz[b,e]oxepin-2-yl)-N-hydroxy-N- methylpropanamide (P10294), were selected as developmental candidates for the topical treatment of inflammatory skin disorders.
(PMID: 8568814)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Putative Target:
ChEMBL Target ID: 105051
Target Type: PROTEIN FAMILY
Pref Name: Prostaglandin G/H synthase (cyclooxygenase)
Synonyms: COX-1;Cyclooxygenase-1;PGH synthase 1;PGHS-1;PHS 1;Prostaglandin G/H synthase 1;Prostaglandin H2 synthase 1;Prostaglandin-endoperoxide synthase 1;COX-2;Cyclooxygenase-2;Glucocorticoid-regulated inflammatory cyclooxygenase;Gripghs;Macrophage activation-associated marker protein P71/73;PES-2;PGH synthase 2;PGHS-2;PHS II;Prostaglandin G/H synthase 2;Prostaglandin H2 synthase 2;Prostaglandin-endoperoxide synthase 2;TIS10 protein;
Gene Name: Cox-1 ;Cox1;Ptgs1;Cox-2 ;Cox2;Pghs-b;Ptgs2;Tis10;
Protein Accession: P22437;Q05769;
Protein GI: 129900;548483;
Organism: Mus musculus
Tax ID: 10090
Target Classification: enzyme
Confidence: Multiple homologous protein targets may be assigned
Relationship Type: Homologous protein target assigned
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Assay Data Source: Scientific Literature
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2IC50 activity commentIC50 activity commentString
3IC50 standard flagIC50 standard flagInteger
4IC50 qualifierIC50 qualifierString
5IC50 published valueIC50 published valueFloatμM
6IC50 standard valueIC50 standard valueFloatnM
7Inhibition activity commentInhibition activity commentString
8Inhibition standard flagInhibition standard flagInteger
9Inhibition qualifierInhibition qualifierString
10Inhibition published valueInhibition published valueFloat%
11Inhibition standard valueInhibition standard valueFloat%

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
PageFrom: