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Assay Detail

CHEMBL3240510

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

Binding
Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type RAW264.7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin G/H synthase 2 (CHEMBL4321)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis, biological evaluation, and docking analysis of a novel family of 1-methyl-1H-pyrrole-2,5-diones as highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.
Kim KJ, Choi MJ, Shin JS, Kim M, Choi HE, Kang SM, Jin JH, Lee KT, Lee JY.
Bioorg Med Chem Lett (2014) 24 : 1958 -1962
PubMed 24656662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.17 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233601 1 8.51
CHEMBL7162 NS-398 1 8.15
CHEMBL3233600 1 8.11
CHEMBL3233602 1 8.06
CHEMBL118 CELECOXIB 4.0 1 8.06
CHEMBL3233599 1 7.96
CHEMBL3233597 1 6.35
CHEMBL595838 1 6.21
CHEMBL521 IBUPROFEN 4.0 1 6.07
CHEMBL3233596 1 6.06
CHEMBL3233598 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233601 IC50 = 3.1 nM 8.51
CHEMBL7162 NS-398 IC50 = 7.0 nM 8.15
CHEMBL3233600 IC50 = 7.8 nM 8.11
CHEMBL3233602 IC50 = 8.7 nM 8.06
CHEMBL118 CELECOXIB IC50 = 8.7 nM 8.06
CHEMBL3233599 IC50 = 11.0 nM 7.96
CHEMBL3233597 IC50 = 450.0 nM 6.35
CHEMBL595838 IC50 = 610.0 nM 6.21
CHEMBL521 IBUPROFEN IC50 = 860.0 nM 6.07
CHEMBL3233596 IC50 = 870.0 nM 6.06
CHEMBL3233598 IC50 = 4700.0 nM 5.33