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Assay Detail

CHEMBL664079

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

Binding
Inhibition of PGE-2 production in CHO cells expressing human COX-2.
21
Total Activities
21
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 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, Gauthier JY, Gordon R, Guay J, Kargman S, Li CS, Prasit P, Riendeau D, Thérien M, Visco DM, Xu L.
Bioorg Med Chem Lett (1999) 9 : 3187 -3192
PubMed 10576685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.05 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118 CELECOXIB 4.0 1 8.70
CHEMBL322703 1 7.70
CHEMBL320585 1 7.70
CHEMBL108512 1 7.70
CHEMBL122 ROFECOXIB 4.0 1 7.70
CHEMBL6 INDOMETHACIN 4.0 1 7.58
CHEMBL322276 1 7.52
CHEMBL108917 1 7.52
CHEMBL107706 1 7.40
CHEMBL110824 1 7.40
CHEMBL322807 1 7.05
CHEMBL110822 1 6.92
CHEMBL320111 1 6.82
CHEMBL110514 1 6.58
CHEMBL106255 1 6.57
CHEMBL321597 1 6.48
CHEMBL108857 1 6.46
CHEMBL320273 1 6.26
CHEMBL326254 1 6.21
CHEMBL323267 1 6.17
CHEMBL319446 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118 CELECOXIB IC50 = 2.0 nM 8.70
CHEMBL322703 IC50 = 20.0 nM 7.70
CHEMBL320585 IC50 = 20.0 nM 7.70
CHEMBL108512 IC50 = 20.0 nM 7.70
CHEMBL122 ROFECOXIB IC50 = 20.0 nM 7.70
CHEMBL6 INDOMETHACIN IC50 = 26.0 nM 7.58
CHEMBL322276 IC50 = 30.0 nM 7.52
CHEMBL108917 IC50 = 30.0 nM 7.52
CHEMBL107706 IC50 = 40.0 nM 7.40
CHEMBL110824 IC50 = 40.0 nM 7.40
CHEMBL322807 IC50 = 90.0 nM 7.05
CHEMBL110822 IC50 = 120.0 nM 6.92
CHEMBL320111 IC50 = 150.0 nM 6.82
CHEMBL110514 IC50 = 260.0 nM 6.58
CHEMBL106255 IC50 = 270.0 nM 6.57
CHEMBL321597 IC50 = 330.0 nM 6.48
CHEMBL108857 IC50 = 350.0 nM 6.46
CHEMBL320273 IC50 = 550.0 nM 6.26
CHEMBL326254 IC50 = 620.0 nM 6.21
CHEMBL323267 IC50 = 670.0 nM 6.17
CHEMBL319446 IC50 = 2900.0 nM 5.54