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Assay Detail

CHEMBL917136

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

Binding
Activity of COX2 in human heparinized blood assessed as inhibition of LPS-induced PGE2 production after 24 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties.
Chegaev K, Lazzarato L, Tosco P, Cena C, Marini E, Rolando B, Carrupt PA, Fruttero R, Gasco A.
J Med Chem (2007) 50 : 1449 -1457
PubMed 17335184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.29 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117862 1 7.05
CHEMBL435381 CIMICOXIB 2.0 1 7.00
CHEMBL118 CELECOXIB 4.0 1 5.89
CHEMBL122 ROFECOXIB 4.0 1 5.82
CHEMBL223619 1 5.16
CHEMBL373819 1 4.85
CHEMBL376246 1 4.80
CHEMBL220113 1 4.70
CHEMBL223529 1 4.54
CHEMBL219893 1 4.25
CHEMBL373867 1 4.12
CHEMBL386006 1 -
CHEMBL219885 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117862 IC50 = 90.0 nM 7.05
CHEMBL435381 CIMICOXIB IC50 = 100.0 nM 7.00
CHEMBL118 CELECOXIB IC50 = 1300.0 nM 5.89
CHEMBL122 ROFECOXIB IC50 = 1500.0 nM 5.82
CHEMBL223619 IC50 = 6900.0 nM 5.16
CHEMBL373819 IC50 = 14000.0 nM 4.85
CHEMBL376246 IC50 = 16000.0 nM 4.80
CHEMBL220113 IC50 = 20000.0 nM 4.70
CHEMBL223529 IC50 = 29000.0 nM 4.54
CHEMBL219893 IC50 = 56000.0 nM 4.25
CHEMBL373867 IC50 = 76000.0 nM 4.12
CHEMBL386006 IC50 > 100000.0 nM -
CHEMBL219885 IC50 > 100000.0 nM -