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Assay Detail

CHEMBL921732

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Binding
Inhibition of ovine COX1 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
15
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 1 (CHEMBL2949)
Type SINGLE PROTEIN
Organism Ovis aries

Publication

Molecular determinants for the selective inhibition of cyclooxygenase-2 by lumiracoxib.
Blobaum AL, Marnett LJ.
J Biol Chem (2007) 282 : 16379 -16390
PubMed 17434872 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 9 - -
IC50 6 6.69 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76084 2 7.24
CHEMBL139 DICLOFENAC 4.0 2 7.17
CHEMBL407109 2 7.11
CHEMBL76154 2 6.63
CHEMBL258738 2 6.16
CHEMBL259842 2 5.80
CHEMBL259218 1 -
CHEMBL408156 1 -
CHEMBL260111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76084 IC50 = 58.0 nM 7.24
CHEMBL139 DICLOFENAC IC50 = 67.0 nM 7.17
CHEMBL407109 IC50 = 77.0 nM 7.11
CHEMBL76154 IC50 = 234.0 nM 6.63
CHEMBL258738 IC50 = 696.0 nM 6.16
CHEMBL259842 IC50 = 1600.0 nM 5.80
CHEMBL259218 Inhibition = 40.0 % -
CHEMBL259842 Inhibition = 55.0 % -
CHEMBL76154 Inhibition = 90.0 % -
CHEMBL258738 Inhibition = 80.0 % -
CHEMBL408156 Inhibition = 35.0 % -
CHEMBL76084 Inhibition = 100.0 % -
CHEMBL260111 Inhibition = 30.0 % -
CHEMBL139 DICLOFENAC Inhibition = 90.0 % -
CHEMBL407109 Inhibition = 75.0 % -