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Assay Detail

CHEMBL875404

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

Binding
Inhibitory activity against human COX-2 expressed in baculovirus infected Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 and Cox-1 inhibitors
Leblanc Y, Gauthier J, Ethier D, Guay J, Mancini J, Riendeau D, Tagari P, Vickers P, Wong E, Prasit P
Bioorg Med Chem Lett (1995) 5 : 2123 -2128
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.59 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42485 DUP-697 1 8.30
CHEMBL417204 1 8.00
CHEMBL65155 1 7.70
CHEMBL303688 1 7.52
CHEMBL303870 1 7.16
CHEMBL305060 1 6.60
CHEMBL308682 1 6.39
CHEMBL69053 1 6.26
CHEMBL67447 1 6.17
CHEMBL303674 1 5.80
CHEMBL66445 1 5.37
CHEMBL63706 1 5.27
CHEMBL292948 1 5.14
CHEMBL303036 1 -
CHEMBL302543 1 -
CHEMBL66630 1 -
CHEMBL294050 1 -
CHEMBL63286 1 -
CHEMBL302663 1 -
CHEMBL302687 1 -
CHEMBL293229 1 -
CHEMBL416687 1 -
CHEMBL302950 1 -
CHEMBL63283 1 -
CHEMBL66821 1 -
CHEMBL307983 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42485 DUP-697 IC50 = 5.0 nM 8.30
CHEMBL417204 IC50 = 10.0 nM 8.00
CHEMBL65155 IC50 = 20.0 nM 7.70
CHEMBL303688 IC50 = 30.0 nM 7.52
CHEMBL303870 IC50 = 70.0 nM 7.16
CHEMBL305060 IC50 = 250.0 nM 6.60
CHEMBL308682 IC50 = 410.0 nM 6.39
CHEMBL69053 IC50 = 550.0 nM 6.26
CHEMBL67447 IC50 = 670.0 nM 6.17
CHEMBL303674 IC50 = 1600.0 nM 5.80
CHEMBL66445 IC50 = 4300.0 nM 5.37
CHEMBL63706 IC50 = 5400.0 nM 5.27
CHEMBL292948 IC50 = 7200.0 nM 5.14
CHEMBL303036 IC50 > 30000.0 nM -
CHEMBL302543 IC50 > 30000.0 nM -
CHEMBL66630 IC50 > 30000.0 nM -
CHEMBL294050 IC50 > 30000.0 nM -
CHEMBL63286 IC50 > 30000.0 nM -
CHEMBL302663 IC50 > 30000.0 nM -
CHEMBL302687 IC50 > 30000.0 nM -
CHEMBL293229 IC50 > 30000.0 nM -
CHEMBL416687 IC50 > 30000.0 nM -
CHEMBL302950 IC50 > 30000.0 nM -
CHEMBL63283 IC50 > 30000.0 nM -
CHEMBL66821 IC50 > 30000.0 nM -
CHEMBL307983 IC50 > 30000.0 nM -