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Assay Detail

CHEMBL921787

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Binding
Inhibition of mouse COX2 for 17 mins pre-incubated before addition of [1-14C]arachidonic acid
20
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL4321)
Type SINGLE PROTEIN
Organism Mus musculus

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 11 - -
IC50 9 7.05 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139 DICLOFENAC 4.0 2 7.66
CHEMBL407109 2 7.48
CHEMBL76084 2 7.46
CHEMBL76154 2 7.32
CHEMBL259218 2 7.20
CHEMBL407368 2 7.03
CHEMBL259842 2 6.76
CHEMBL258738 2 6.62
CHEMBL408156 2 5.92
CHEMBL258969 1 -
CHEMBL260111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139 DICLOFENAC IC50 = 22.0 nM 7.66
CHEMBL407109 IC50 = 33.0 nM 7.48
CHEMBL76084 IC50 = 35.0 nM 7.46
CHEMBL76154 IC50 = 48.0 nM 7.32
CHEMBL259218 IC50 = 63.0 nM 7.20
CHEMBL407368 IC50 = 94.0 nM 7.03
CHEMBL259842 IC50 = 174.0 nM 6.76
CHEMBL258738 IC50 = 241.0 nM 6.62
CHEMBL408156 IC50 = 1200.0 nM 5.92
CHEMBL259218 Inhibition = 80.0 % -
CHEMBL407109 Inhibition = 90.0 % -
CHEMBL407368 Inhibition = 80.0 % -
CHEMBL258969 Inhibition = 40.0 % -
CHEMBL139 DICLOFENAC Inhibition = 85.0 % -
CHEMBL260111 Inhibition = 25.0 % -
CHEMBL259842 Inhibition = 85.0 % -
CHEMBL76084 Inhibition = 100.0 % -
CHEMBL408156 Inhibition = 50.0 % -
CHEMBL258738 Inhibition = 100.0 % -
CHEMBL76154 Inhibition = 100.0 % -