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Assay Detail

CHEMBL2066802

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

Functional
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type RAW264.7
Confidence 1 — Organism
Curated By Autocuration

Target

RAW264.7 (CHEMBL612557)
Type CELL-LINE
Organism Mus musculus

Publication

Synthesis, chemical reactivity as Michael acceptors, and biological potency of monocyclic cyanoenones, novel and highly potent anti-inflammatory and cytoprotective agents.
Zheng S, Santosh Laxmi YR, David E, Dinkova-Kostova AT, Shiavoni KH, Ren Y, Zheng Y, Trevino I, Bumeister R, Ojima I, Wigley WC, Bliska JB, Mierke DF, Honda T.
J Med Chem (2012) 55 : 4837 -4846
PubMed 22533790 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.10 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064456 1 8.24
CHEMBL2064457 1 8.14
CHEMBL1093059 BARDOXOLONE 2.0 1 7.78
CHEMBL2064461 1 7.24
CHEMBL2064462 1 6.82
CHEMBL2064458 1 6.77
CHEMBL2064460 1 6.66
CHEMBL2064459 1 6.52
CHEMBL2064463 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064456 IC50 = 5.8 nM 8.24
CHEMBL2064457 IC50 = 7.3 nM 8.14
CHEMBL1093059 BARDOXOLONE IC50 = 16.5 nM 7.78
CHEMBL2064461 IC50 = 58.0 nM 7.24
CHEMBL2064462 IC50 = 151.9 nM 6.82
CHEMBL2064458 IC50 = 169.9 nM 6.77
CHEMBL2064460 IC50 = 219.4 nM 6.66
CHEMBL2064459 IC50 = 304.8 nM 6.52
CHEMBL2064463 IC50 = 1901.4 nM 5.72