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Assay Detail

CHEMBL869264

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

Functional
Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Selective COX-2 inhibitors. Part 1: synthesis and biological evaluation of phenylazobenzenesulfonamides.
Tsai WJ, Shiao YJ, Lin SJ, Chiou WF, Lin LC, Yang TH, Teng CM, Wu TS, Yang LM.
Bioorg Med Chem Lett (2006) 16 : 4440 -4443
PubMed 16814546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.32 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 7.44
CHEMBL118 CELECOXIB 4.0 1 6.48
CHEMBL17161 1 5.69
CHEMBL213326 1 5.37
CHEMBL377353 SALAZOSULFAMIDE 2.0 1 5.05
CHEMBL212918 1 4.96
CHEMBL215872 1 4.95
CHEMBL386992 1 4.91
CHEMBL213939 1 4.91
CHEMBL213267 1 4.83
CHEMBL214710 1 4.77
CHEMBL165 RESVERATROL 3.0 1 4.48
CHEMBL379206 1 -
CHEMBL213266 1 -
CHEMBL277836 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 36.0 nM 7.44
CHEMBL118 CELECOXIB IC50 = 330.0 nM 6.48
CHEMBL17161 IC50 = 2040.0 nM 5.69
CHEMBL213326 IC50 = 4280.0 nM 5.37
CHEMBL377353 SALAZOSULFAMIDE IC50 = 8890.0 nM 5.05
CHEMBL212918 IC50 = 11070.0 nM 4.96
CHEMBL215872 IC50 = 11340.0 nM 4.95
CHEMBL386992 IC50 = 12420.0 nM 4.91
CHEMBL213939 IC50 = 12370.0 nM 4.91
CHEMBL213267 IC50 = 14630.0 nM 4.83
CHEMBL214710 IC50 = 16850.0 nM 4.77
CHEMBL165 RESVERATROL IC50 = 33150.0 nM 4.48
CHEMBL379206 IC50 - -
CHEMBL213266 IC50 - -
CHEMBL277836 IC50 - -