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Assay Detail

CHEMBL769643

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

Binding
Inhibitory activity against human recombinant Prostaglandin G/H synthase 2 expressed in microsomes taken from baculovirus infected Sf9 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf9
Subcellular Microsomes
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 inhibitors. part II: Replacing the heterocycle
Gauthier JY, Leblanc Y, Cameron Black W, Chan C, Cromlish WA, Gordon R, Kennedey BP, Lau CK, Leger S, Wang Z, Ethier D, Guay J, Mancini J, Riendeau D, Tagari P, Vickers P, Wong E, Xu L, Prasit P
Bioorg Med Chem Lett (1996) 6 : 87 -92
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.18 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42485 DUP-697 1 8.15
CHEMBL328837 1 7.52
CHEMBL274893 SC-57666 1 6.80
CHEMBL274990 SC-58125 1 6.70
CHEMBL274473 1 6.51
CHEMBL16850 1 6.51
CHEMBL319306 1 6.33
CHEMBL355263 1 5.92
CHEMBL366807 1 5.68
CHEMBL171646 1 5.29
CHEMBL367778 1 5.23
CHEMBL368409 1 5.19
CHEMBL355771 1 4.52
CHEMBL355781 1 -
CHEMBL174009 1 -
CHEMBL170591 1 -
CHEMBL173961 1 -
CHEMBL43165 1 -
CHEMBL366886 1 -
CHEMBL97935 1 -
CHEMBL171360 1 -
CHEMBL443819 1 -
CHEMBL367885 1 -
CHEMBL170639 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42485 DUP-697 IC50 = 7.0 nM 8.15
CHEMBL328837 IC50 = 30.0 nM 7.52
CHEMBL274893 SC-57666 IC50 = 160.0 nM 6.80
CHEMBL274990 SC-58125 IC50 = 200.0 nM 6.70
CHEMBL274473 IC50 = 310.0 nM 6.51
CHEMBL16850 IC50 = 310.0 nM 6.51
CHEMBL319306 IC50 = 470.0 nM 6.33
CHEMBL355263 IC50 = 1200.0 nM 5.92
CHEMBL366807 IC50 = 2100.0 nM 5.68
CHEMBL171646 IC50 = 5100.0 nM 5.29
CHEMBL367778 IC50 = 5900.0 nM 5.23
CHEMBL368409 IC50 = 6500.0 nM 5.19
CHEMBL355771 IC50 = 30000.0 nM 4.52
CHEMBL355781 IC50 > 10000.0 nM -
CHEMBL174009 IC50 > 10000.0 nM -
CHEMBL170591 IC50 > 30000.0 nM -
CHEMBL173961 IC50 > 30000.0 nM -
CHEMBL43165 IC50 > 30000.0 nM -
CHEMBL366886 IC50 > 30000.0 nM -
CHEMBL97935 IC50 > 30000.0 nM -
CHEMBL171360 IC50 > 30000.0 nM -
CHEMBL443819 IC50 > 30000.0 nM -
CHEMBL367885 IC50 > 30000.0 nM -
CHEMBL170639 IC50 > 30000.0 nM -