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Assay Detail

CHEMBL1763373

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

Functional
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
23
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Macrophage
Confidence 1 — Organism
Curated By Autocuration

Publication

Tricyclic compounds containing nonenolizable cyano enones. A novel class of highly potent anti-inflammatory and cytoprotective agents.
Honda T, Yoshizawa H, Sundararajan C, David E, Lajoie MJ, Favaloro FG, Janosik T, Su X, Honda Y, Roebuck BD, Gribble GW.
J Med Chem (2011) 54 : 1762 -1778
PubMed 21361338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.76 10.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224752 1 10.25
CHEMBL1762621 BARDOXOLONE METHYL 3.0 1 9.70
CHEMBL1093059 BARDOXOLONE 2.0 2 9.30
CHEMBL1762616 1 8.89
CHEMBL356121 2 8.68
CHEMBL389621 HYDROCORTISONE 4.0 1 8.00
CHEMBL1762619 2 7.72
CHEMBL1762620 1 7.58
CHEMBL342544 1 7.28
CHEMBL1762614 1 7.24
CHEMBL142344 1 7.21
CHEMBL415458 2 7.21
CHEMBL146553 1 7.12
CHEMBL343629 1 7.04
CHEMBL145011 1 6.51
CHEMBL144916 1 6.32
CHEMBL343446 1 5.80
CHEMBL1762617 1 -
CHEMBL1762613 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224752 IC50 = 0.056 nM 10.25
CHEMBL1762621 BARDOXOLONE METHYL IC50 = 0.2 nM 9.70
CHEMBL1093059 BARDOXOLONE IC50 = 0.5 nM 9.30
CHEMBL1762616 IC50 = 1.3 nM 8.89
CHEMBL356121 IC50 = 2.1 nM 8.68
CHEMBL1093059 BARDOXOLONE IC50 = 4.3 nM 8.37
CHEMBL389621 HYDROCORTISONE IC50 = 10.0 nM 8.00
CHEMBL356121 IC50 = 14.0 nM 7.85
CHEMBL1762619 IC50 = 19.0 nM 7.72
CHEMBL1762619 IC50 = 19.0 nM 7.72
CHEMBL1762620 IC50 = 26.0 nM 7.58
CHEMBL342544 IC50 = 53.0 nM 7.28
CHEMBL1762614 IC50 = 58.0 nM 7.24
CHEMBL415458 IC50 = 61.0 nM 7.21
CHEMBL142344 IC50 = 61.0 nM 7.21
CHEMBL415458 IC50 = 64.0 nM 7.19
CHEMBL146553 IC50 = 75.0 nM 7.12
CHEMBL343629 IC50 = 91.0 nM 7.04
CHEMBL145011 IC50 = 310.0 nM 6.51
CHEMBL144916 IC50 = 480.0 nM 6.32
CHEMBL343446 IC50 = 1600.0 nM 5.80
CHEMBL1762613 IC50 > 600.0 nM -
CHEMBL1762617 IC50 > 60.0 nM -