Home
Drugs
Targets
Pathways
Ontologies
Cyp450s
Adv.search
Help/FAQ

Drug-Target Interaction

Drug

show drug details
PubChem ID:116545
Structure:
Synonyms:
"2-[((2′,6′-dichloro-4′-hydroxy)phenyl)amino]benzeneacetic acid"
"4′-ohd"
"diclofenac, 4′-hydroxy-"
(o-(2,6-Dichloro-4-hydroxyanilino)phenyl)acetic acid
2-[((2′,6′-Dichloro-4′-hydroxy)phenyl)amino]benzeneaceti
2-[((2′,6′-Dichloro-4′-hydroxy)phenyl)amino]benzeneacetic Acid
2-[2-(2,6-dichloro-4-hydroxyanilino)phenyl]acetic acid
4′-OHD
4'-Hydroxy Diclofenac
4'-HYDROXY-DICLOFENAC
4'-Hydroxydiclofenac
4'-OH DCF
64118-84-9
66161-65-7
AC1L3J5M
AC1Q3QSP
Acetic acid, (o-(2,6-dichloro-4-hydroxyanilino)phenyl)-
AR-1A9418
Benzeneacetic acid, 2-((2,6-dichloro-4-hydroxyphenyl)amino)-
Benzeneacetic acid, 2-[(2,6-dichloro-4-hydroxyphenyl)amino]-
BRN 4198042
C108036
CHEBI:59613
CHEMBL1030
CID116545
Diclofenac, 4′-Hydroxy-
H3661_SIGMA
IN1359
KST-1B7071
LS-11596
{2-[(2,6-dichloro-4-hydroxyphenyl)amino]phenyl}acetic acid

Target

show target details
Uniprot ID:Q6LCE7_HUMAN
Synonyms:
Cyclooxygenase-1
EC-Numbers:1.14.99.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

9226412
Aceclofenac blocks prostaglandin E2 production following its intracellular conversion into cyclooxygenase inhibitors.. R Yamazaki; S Kawai; T Matsuzaki; N Kaneda; S Hashimoto; T Yokokura; R Okamoto; T Koshino; Y Mizushima (1997) European journal of pharmacology display abstract
Aceclofenac, 2-[(2,6-dichlorophenyl) amino] phenylacetoxyacetic acid, is a novel non-steroidal anti-inflammatory drug. We investigated the effects of aceclofenac on prostaglandin E2 production by several kinds of human cells. Aceclofenac inhibited interleukin-1beta-induced prostaglandin E2 production by human rheumatoid synovial cells, but had no inhibitory effect on cyclooxygenase-1 or cyclooxygenase-2 activities by itself. We also observed that part of the aceclofenac was converted into diclofenac, the cyclooxygenase-1 and cyclooxygenase-2 inhibitor, when aceclofenac was incubated with human rheumatoid synovial cells. Aceclofenac was also converted into diclofenac and 4'-hydroxy diclofenac by human polymorphonuclear leukocytes and monocytes. 4'-Hydroxy diclofenac suppressed prostaglandin E2 production specifically by blocking cyclooxygenase-2 activity. These findings suggested that aceclofenac can be metabolized to cyclooxygenase inhibitors (diclofenac and/or 4'-hydroxy diclofenac) by these inflammatory cells. Although detailed examinations in non-inflammatory cells remain to be studied, we concluded that aceclofenac is shown to be a new type of non-steroidal anti-inflammatory drug which is intracellulary converted into active metabolites that inhibit the prostaglandin E2 production.