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Assay Detail

CHEMBL763346

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

Binding
Inhibition of PGE-2 production by arachidonic acid-stimulated CHO cells expressing human Prostaglandin G/H synthase 2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel 1,2-diarylcyclobutenes: Selective and orally active cox-2 inhibitors
Friesen RW, Dube D, Fortin R, Frenette R, Prescott S, Cromlish W, Greig GM, Kargman S, Wong E, Chan CC, Gordon R, Xu LJ, Riendeau D
Bioorg Med Chem Lett (1996) 6 : 2677 -2682
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.90 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92154 1 8.96
CHEMBL91118 1 8.92
CHEMBL42485 DUP-697 1 8.68
CHEMBL92443 1 8.66
CHEMBL420987 1 8.55
CHEMBL91832 1 8.30
CHEMBL90988 1 7.92
CHEMBL6 INDOMETHACIN 4.0 1 7.31
CHEMBL330516 1 7.21
CHEMBL92485 1 7.02
CHEMBL328003 1 6.96
CHEMBL328521 1 6.28
CHEMBL93803 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92154 IC50 = 1.1 nM 8.96
CHEMBL91118 IC50 = 1.2 nM 8.92
CHEMBL42485 DUP-697 IC50 = 2.1 nM 8.68
CHEMBL92443 IC50 = 2.2 nM 8.66
CHEMBL420987 IC50 = 2.8 nM 8.55
CHEMBL91832 IC50 = 5.0 nM 8.30
CHEMBL90988 IC50 = 12.0 nM 7.92
CHEMBL6 INDOMETHACIN IC50 = 49.0 nM 7.31
CHEMBL330516 IC50 = 61.0 nM 7.21
CHEMBL92485 IC50 = 96.0 nM 7.02
CHEMBL328003 IC50 = 110.0 nM 6.96
CHEMBL328521 IC50 = 530.0 nM 6.28
CHEMBL93803 IC50 > 5000.0 nM -