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Assay Detail

CHEMBL763092

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

Binding
Inhibition of Prostaglandin G/H synthase 2 in human whole blood (HWB) assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.
Dubé D, Brideau C, Deschênes D, Fortin R, Friesen RW, Gordon R, Girard Y, Riendeau D, Savoie C, Chan CC.
Bioorg Med Chem Lett (1999) 9 : 1715 -1720
PubMed 10397507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.22 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42485 DUP-697 1 7.22
CHEMBL296370 1 6.85
CHEMBL47294 1 6.34
CHEMBL6 INDOMETHACIN 4.0 1 6.30
CHEMBL49918 1 6.30
CHEMBL48671 1 6.30
CHEMBL300710 1 6.16
CHEMBL49394 1 6.10
CHEMBL49319 1 6.00
CHEMBL47540 1 5.85
CHEMBL45583 1 5.85
CHEMBL48073 1 5.33
CHEMBL46171 1 -
CHEMBL296220 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42485 DUP-697 IC50 = 60.0 nM 7.22
CHEMBL296370 IC50 = 140.0 nM 6.85
CHEMBL47294 IC50 = 460.0 nM 6.34
CHEMBL6 INDOMETHACIN IC50 = 500.0 nM 6.30
CHEMBL49918 IC50 = 500.0 nM 6.30
CHEMBL48671 IC50 = 500.0 nM 6.30
CHEMBL300710 IC50 = 700.0 nM 6.16
CHEMBL49394 IC50 = 800.0 nM 6.10
CHEMBL49319 IC50 = 1000.0 nM 6.00
CHEMBL47540 IC50 = 1400.0 nM 5.85
CHEMBL45583 IC50 = 1400.0 nM 5.85
CHEMBL48073 IC50 = 4700.0 nM 5.33
CHEMBL46171 IC50 > 33000.0 nM -
CHEMBL296220 IC50 < 400.0 nM -