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Assay Detail

CHEMBL3861640

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

Binding
Inhibition of mPGES-1 in mouse RAW264.7 cells assessed as reduction in LPS-induced PGE2 production after 24 hrs
8
Total Activities
8
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 E synthase (CHEMBL2046261)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis, structure determination, and biological evaluation of phenylsulfonyl hydrazide derivatives as potential anti-inflammatory agents.
Park EB, Kim KJ, Jeong HR, Lee JK, Kim HJ, Lee HH, Lim JW, Shin JS, Koeberle A, Werz O, Lee KT, Lee JY.
Bioorg Med Chem Lett (2016) 26 : 5193 -5197
PubMed 27720548 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.78 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7162 NS-398 1 8.15
CHEMBL3747473 1 7.22
CHEMBL3922351 1 6.26
CHEMBL3747171 1 6.16
CHEMBL3921251 1 6.10
CHEMBL3961576 1 -
CHEMBL3949085 1 -
CHEMBL3928687 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7162 NS-398 IC50 = 7.0 nM 8.15
CHEMBL3747473 IC50 = 60.0 nM 7.22
CHEMBL3922351 IC50 = 550.0 nM 6.26
CHEMBL3747171 IC50 = 690.0 nM 6.16
CHEMBL3921251 IC50 = 790.0 nM 6.10
CHEMBL3961576 IC50 > 10000.0 nM -
CHEMBL3949085 IC50 - -
CHEMBL3928687 IC50 - -