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Assay Detail

CHEMBL2321397

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

Binding
Inhibition of human recombinant mPGES-1 using PGH2 as substrate incubated 20 mins prior to substrate addition measured after 30 secs by EIA
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E synthase (CHEMBL5658)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel benzoxazole inhibitors of mPGES-1.
Kablaoui N, Patel S, Shao J, Demian D, Hoffmaster K, Berlioz F, Vazquez ML, Moore WM, Nugent RA.
Bioorg Med Chem Lett (2013) 23 : 907 -911
PubMed 23266122 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.47 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL412099 1 9.00
CHEMBL182032 1 8.52
CHEMBL2315853 1 7.75
CHEMBL2315856 1 7.47
CHEMBL2315854 1 7.40
CHEMBL2315857 1 7.37
CHEMBL2315855 1 7.09
CHEMBL2315862 1 6.75
CHEMBL2315867 1 6.62
CHEMBL2315866 1 6.54
CHEMBL2315861 1 6.42
CHEMBL2315859 1 6.11
CHEMBL2315868 1 6.09
CHEMBL2315864 1 6.08
CHEMBL2315877 1 6.07
CHEMBL2315876 1 5.92
CHEMBL29097 1 5.80
CHEMBL2315870 1 5.78
CHEMBL2315869 1 5.52
CHEMBL2315858 1 5.50
CHEMBL2315865 1 5.14
CHEMBL2315863 1 5.09
CHEMBL2315872 1 4.89
CHEMBL2315871 1 -
CHEMBL2315874 1 -
CHEMBL2315873 1 -
CHEMBL2315875 1 -
CHEMBL2315860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL412099 IC50 = 1.0 nM 9.00
CHEMBL182032 IC50 = 3.0 nM 8.52
CHEMBL2315853 IC50 = 18.0 nM 7.75
CHEMBL2315856 IC50 = 34.0 nM 7.47
CHEMBL2315854 IC50 = 40.0 nM 7.40
CHEMBL2315857 IC50 = 43.1 nM 7.37
CHEMBL2315855 IC50 = 82.0 nM 7.09
CHEMBL2315862 IC50 = 176.0 nM 6.75
CHEMBL2315867 IC50 = 242.0 nM 6.62
CHEMBL2315866 IC50 = 291.0 nM 6.54
CHEMBL2315861 IC50 = 383.0 nM 6.42
CHEMBL2315859 IC50 = 785.0 nM 6.11
CHEMBL2315868 IC50 = 821.0 nM 6.09
CHEMBL2315864 IC50 = 826.0 nM 6.08
CHEMBL2315877 IC50 = 853.0 nM 6.07
CHEMBL2315876 IC50 = 1200.0 nM 5.92
CHEMBL29097 IC50 = 1600.0 nM 5.80
CHEMBL2315870 IC50 = 1680.0 nM 5.78
CHEMBL2315869 IC50 = 3010.0 nM 5.52
CHEMBL2315858 IC50 = 3200.0 nM 5.50
CHEMBL2315865 IC50 = 7180.0 nM 5.14
CHEMBL2315863 IC50 = 8150.0 nM 5.09
CHEMBL2315872 IC50 = 12900.0 nM 4.89
CHEMBL2315871 IC50 > 30000.0 nM -
CHEMBL2315874 IC50 > 10000.0 nM -
CHEMBL2315873 IC50 > 10000.0 nM -
CHEMBL2315875 IC50 > 10000.0 nM -
CHEMBL2315860 IC50 > 19100.0 nM -