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Assay Detail

CHEMBL665718

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

Binding
In vitro inhibition of the production of PGE-2 in arachidonic acid stimulated chinese hamster ovary (CHO) cells transfected with human cyclooxygenase-2
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
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 5,6-diarylimidazo[2.1-b]thiazole as selective COX-2 inhibitors
Therien M, Brideau C, Chan CC, Cromlish WA, Gauthier JY, Gordon R, Greig G, Kargman S, Lau CK, Leblanc Y, Li C, O'Neill GP, Riendeau D, Roy P, Wang Z, Xu L, Prasit P
Bioorg Med Chem Lett (1997) 7 : 47 -52
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.74 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42485 DUP-697 1 8.70
CHEMBL423576 1 7.92
CHEMBL358609 1 7.92
CHEMBL148976 1 7.85
CHEMBL146742 1 7.80
CHEMBL148708 1 7.80
CHEMBL6 INDOMETHACIN 4.0 1 7.58
CHEMBL149040 1 6.85
CHEMBL359143 1 6.38
CHEMBL149936 1 6.05
CHEMBL149167 1 6.00
CHEMBL149076 1 5.52
CHEMBL150006 1 5.49
CHEMBL149597 1 5.44
CHEMBL358482 1 5.30
CHEMBL148666 1 5.30
CHEMBL345333 1 -
CHEMBL356206 1 -
CHEMBL424313 1 -
CHEMBL358666 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42485 DUP-697 IC50 = 2.0 nM 8.70
CHEMBL423576 IC50 = 12.0 nM 7.92
CHEMBL358609 IC50 = 12.0 nM 7.92
CHEMBL148976 IC50 = 14.0 nM 7.85
CHEMBL146742 IC50 = 16.0 nM 7.80
CHEMBL148708 IC50 = 16.0 nM 7.80
CHEMBL6 INDOMETHACIN IC50 = 26.0 nM 7.58
CHEMBL149040 IC50 = 140.0 nM 6.85
CHEMBL359143 IC50 = 420.0 nM 6.38
CHEMBL149936 IC50 = 900.0 nM 6.05
CHEMBL149167 IC50 = 1000.0 nM 6.00
CHEMBL149076 IC50 = 3000.0 nM 5.52
CHEMBL150006 IC50 = 3210.0 nM 5.49
CHEMBL149597 IC50 = 3600.0 nM 5.44
CHEMBL358482 IC50 = 5000.0 nM 5.30
CHEMBL148666 IC50 = 5000.0 nM 5.30
CHEMBL345333 IC50 > 5000.0 nM -
CHEMBL356206 IC50 > 5000.0 nM -
CHEMBL424313 IC50 > 5000.0 nM -
CHEMBL358666 IC50 > 5000.0 nM -