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Assay Detail

CHEMBL4187828

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

Binding
Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, biological evaluation and docking study of a new series of di-substituted benzoxazole derivatives as selective COX-2 inhibitors and anti-inflammatory agents.
Kaur A, Pathak DP, Sharma V, Wakode S.
Bioorg Med Chem (2018) 26 : 891 -902
PubMed 29373271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.89 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205552 1 7.40
CHEMBL118 CELECOXIB 4.0 1 6.82
CHEMBL4212341 1 6.80
CHEMBL4210463 1 6.36
CHEMBL4210856 1 6.34
CHEMBL4215506 1 6.03
CHEMBL521 IBUPROFEN 4.0 1 5.97
CHEMBL4203006 1 5.92
CHEMBL4204840 1 5.86
CHEMBL4211316 1 5.86
CHEMBL4212465 1 5.85
CHEMBL4208086 1 5.81
CHEMBL4212716 1 5.65
CHEMBL4206180 1 5.57
CHEMBL4213903 1 5.32
CHEMBL4202666 1 5.13
CHEMBL4216007 1 4.97
CHEMBL4209915 1 4.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205552 IC50 = 40.0 nM 7.40
CHEMBL118 CELECOXIB IC50 = 150.0 nM 6.82
CHEMBL4212341 IC50 = 160.0 nM 6.80
CHEMBL4210463 IC50 = 440.0 nM 6.36
CHEMBL4210856 IC50 = 460.0 nM 6.34
CHEMBL4215506 IC50 = 930.0 nM 6.03
CHEMBL521 IBUPROFEN IC50 = 1080.0 nM 5.97
CHEMBL4203006 IC50 = 1210.0 nM 5.92
CHEMBL4204840 IC50 = 1390.0 nM 5.86
CHEMBL4211316 IC50 = 1390.0 nM 5.86
CHEMBL4212465 IC50 = 1400.0 nM 5.85
CHEMBL4208086 IC50 = 1560.0 nM 5.81
CHEMBL4212716 IC50 = 2240.0 nM 5.65
CHEMBL4206180 IC50 = 2700.0 nM 5.57
CHEMBL4213903 IC50 = 4840.0 nM 5.32
CHEMBL4202666 IC50 = 7400.0 nM 5.13
CHEMBL4216007 IC50 = 10590.0 nM 4.97
CHEMBL4209915 IC50 = 45540.0 nM 4.34