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Assay Detail

CHEMBL768746

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

Binding
In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells
88
Total Activities
88
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type U-937
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Prostaglandin G/H synthase 1 (CHEMBL221)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
Almansa C, Alfón J, de Arriba AF, Cavalcanti FL, Escamilla I, Gómez LA, Miralles A, Soliva R, Bartrolí J, Carceller E, Merlos M, García-Rafanell J.
J Med Chem (2003) 46 : 3463 -3475
PubMed 12877584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 88 5.63 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6 INDOMETHACIN 4.0 1 8.70
CHEMBL325894 1 6.96
CHEMBL117528 1 6.96
CHEMBL419407 1 6.22
CHEMBL115410 1 6.05
CHEMBL115979 1 5.92
CHEMBL333651 1 5.89
CHEMBL324048 1 5.72
CHEMBL324312 1 5.66
CHEMBL332251 1 5.57
CHEMBL326270 1 5.51
CHEMBL435381 CIMICOXIB 2.0 1 5.48
CHEMBL326291 1 5.40
CHEMBL118 CELECOXIB 4.0 1 5.29
CHEMBL118064 1 5.29
CHEMBL324826 1 5.05
CHEMBL118962 1 4.97
CHEMBL117917 1 4.81
CHEMBL115752 1 4.62
CHEMBL117947 1 4.12
CHEMBL117650 1 4.00
CHEMBL324042 1 -
CHEMBL118067 1 -
CHEMBL115905 1 -
CHEMBL117306 1 -
CHEMBL118936 1 -
CHEMBL333755 1 -
CHEMBL119076 1 -
CHEMBL324472 1 -
CHEMBL114783 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6 INDOMETHACIN IC50 = 2.0 nM 8.70
CHEMBL325894 IC50 = 110.0 nM 6.96
CHEMBL117528 IC50 = 110.0 nM 6.96
CHEMBL419407 IC50 = 600.0 nM 6.22
CHEMBL115410 IC50 = 900.0 nM 6.05
CHEMBL115979 IC50 = 1200.0 nM 5.92
CHEMBL333651 IC50 = 1300.0 nM 5.89
CHEMBL324048 IC50 = 1900.0 nM 5.72
CHEMBL324312 IC50 = 2200.0 nM 5.66
CHEMBL332251 IC50 = 2700.0 nM 5.57
CHEMBL326270 IC50 = 3100.0 nM 5.51
CHEMBL435381 CIMICOXIB IC50 = 3300.0 nM 5.48
CHEMBL326291 IC50 = 4000.0 nM 5.40
CHEMBL118 CELECOXIB IC50 = 5100.0 nM 5.29
CHEMBL118064 IC50 = 5100.0 nM 5.29
CHEMBL324826 IC50 = 9000.0 nM 5.05
CHEMBL118962 IC50 = 10800.0 nM 4.97
CHEMBL117917 IC50 = 15500.0 nM 4.81
CHEMBL115752 IC50 = 23800.0 nM 4.62
CHEMBL117947 IC50 = 76000.0 nM 4.12
CHEMBL117650 IC50 = 100000.0 nM 4.00
CHEMBL117547 IC50 > 10000.0 nM -
CHEMBL116016 IC50 > 10000.0 nM -
CHEMBL116253 IC50 > 100000.0 nM -
CHEMBL331135 IC50 > 10000.0 nM -
CHEMBL116498 IC50 > 10000.0 nM -
CHEMBL117946 IC50 > 10000.0 nM -
CHEMBL119089 IC50 > 10000.0 nM -
CHEMBL117855 IC50 > 10000.0 nM -
CHEMBL325492 IC50 > 10000.0 nM -
CHEMBL116848 IC50 > 10000.0 nM -
CHEMBL333505 IC50 > 10000.0 nM -
CHEMBL326335 IC50 > 10000.0 nM -
CHEMBL324957 IC50 > 10000.0 nM -
CHEMBL116683 IC50 > 1000.0 nM -
CHEMBL119853 IC50 > 10000.0 nM -
CHEMBL324923 IC50 > 10000.0 nM -
CHEMBL117862 IC50 > 10000.0 nM -
CHEMBL324825 IC50 > 10000.0 nM -
CHEMBL116933 IC50 > 10000.0 nM -
CHEMBL325297 IC50 > 10000.0 nM -
CHEMBL114783 IC50 > 10000.0 nM -
CHEMBL324472 IC50 > 10000.0 nM -
CHEMBL119076 IC50 > 10000.0 nM -
CHEMBL333755 IC50 > 10000.0 nM -
CHEMBL118936 IC50 > 10000.0 nM -
CHEMBL117306 IC50 > 10000.0 nM -
CHEMBL115905 IC50 > 1000.0 nM -
CHEMBL118067 IC50 > 10000.0 nM -
CHEMBL324042 IC50 > 10000.0 nM -