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Assay Detail

CHEMBL768682

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

Binding
Inhibition of Prostaglandin G/H synthase 2 was measured by the inhibition of PGE-2 produced by lipopolysaccharide-challenged HWB
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
Friesen RW, Brideau C, Chan CC, Charleson S, Deschênes D, Dubé D, Ethier D, Fortin R, Gauthier JY, Girard Y, Gordon R, Greig GM, Riendeau D, Savoie C, Wang Z, Wong E, Visco D, Xu LJ, Young RN.
Bioorg Med Chem Lett (1998) 8 : 2777 -2782
PubMed 9873621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.74 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42485 DUP-697 1 7.22
CHEMBL6 INDOMETHACIN 4.0 1 6.30
CHEMBL94938 1 6.05
CHEMBL416146 ETORICOXIB 4.0 1 5.96
CHEMBL96098 1 5.77
CHEMBL92759 1 5.75
CHEMBL95156 1 5.75
CHEMBL329120 1 5.68
CHEMBL420628 1 5.62
CHEMBL96950 1 5.58
CHEMBL92233 1 5.57
CHEMBL96947 1 5.42
CHEMBL94939 1 5.24
CHEMBL92793 1 5.16
CHEMBL96842 1 5.10
CHEMBL329419 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42485 DUP-697 IC50 = 60.0 nM 7.22
CHEMBL6 INDOMETHACIN IC50 = 500.0 nM 6.30
CHEMBL94938 IC50 = 900.0 nM 6.05
CHEMBL416146 ETORICOXIB IC50 = 1100.0 nM 5.96
CHEMBL96098 IC50 = 1700.0 nM 5.77
CHEMBL92759 IC50 = 1800.0 nM 5.75
CHEMBL95156 IC50 = 1800.0 nM 5.75
CHEMBL329120 IC50 = 2100.0 nM 5.68
CHEMBL420628 IC50 = 2400.0 nM 5.62
CHEMBL96950 IC50 = 2600.0 nM 5.58
CHEMBL92233 IC50 = 2700.0 nM 5.57
CHEMBL96947 IC50 = 3800.0 nM 5.42
CHEMBL94939 IC50 = 5800.0 nM 5.24
CHEMBL92793 IC50 = 7000.0 nM 5.16
CHEMBL96842 IC50 = 7900.0 nM 5.10
CHEMBL329419 IC50 > 33000.0 nM -