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Assay Detail

CHEMBL3240193

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant COX-2 by enzyme immunoassay
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of celecoxib and rofecoxib for the membrane permeabilizing activity.
Yamakawa N, Suzuki K, Yamashita Y, Katsu T, Hanaya K, Shoji M, Sugai T, Mizushima T.
Bioorg Med Chem (2014) 22 : 2529 -2534
PubMed 24650702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.56 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 7.16
CHEMBL3238416 1 6.96
CHEMBL241970 1 6.89
CHEMBL29920 1 6.80
CHEMBL3238415 1 6.52
CHEMBL122 ROFECOXIB 4.0 2 6.44
CHEMBL3238414 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 70.0 nM 7.16
CHEMBL3238416 IC50 = 110.0 nM 6.96
CHEMBL241970 IC50 = 130.0 nM 6.89
CHEMBL29920 IC50 = 160.0 nM 6.80
CHEMBL3238415 IC50 = 300.0 nM 6.52
CHEMBL122 ROFECOXIB IC50 = 360.0 nM 6.44
CHEMBL3238414 IC50 = 6840.0 nM 5.17
CHEMBL122 ROFECOXIB IC50 > 500000.0 nM -