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Assay Detail

CHEMBL1014420

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

Binding
Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase.
Koeberle A, Zettl H, Greiner C, Wurglics M, Schubert-Zsilavecz M, Werz O.
J Med Chem (2008) 51 : 8068 -8076
PubMed 19053751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.62 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462523 1 5.89
CHEMBL460616 1 5.80
CHEMBL457204 1 5.80
CHEMBL456792 1 5.77
CHEMBL463776 1 5.68
CHEMBL29097 1 5.68
CHEMBL456800 1 5.68
CHEMBL457000 1 5.58
CHEMBL518038 1 5.41
CHEMBL455936 1 5.29
CHEMBL459722 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462523 IC50 = 1300.0 nM 5.89
CHEMBL460616 IC50 = 1600.0 nM 5.80
CHEMBL457204 IC50 = 1600.0 nM 5.80
CHEMBL456792 IC50 = 1700.0 nM 5.77
CHEMBL463776 IC50 = 2100.0 nM 5.68
CHEMBL29097 IC50 = 2100.0 nM 5.68
CHEMBL456800 IC50 = 2100.0 nM 5.68
CHEMBL457000 IC50 = 2600.0 nM 5.58
CHEMBL518038 IC50 = 3900.0 nM 5.41
CHEMBL455936 IC50 = 5100.0 nM 5.29
CHEMBL459722 IC50 = 5600.0 nM 5.25