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Assay Detail

CHEMBL1763374

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 IFN-gamma induced NO production after 24 hrs by Griess reaction
43
Total Activities
41
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

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 43 7.54 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224752 2 9.00
CHEMBL1762757 1 9.00
CHEMBL1720855 1 9.00
CHEMBL1762758 1 8.70
CHEMBL222861 2 8.52
CHEMBL1762609 1 8.52
CHEMBL376599 1 8.40
CHEMBL221714 1 8.30
CHEMBL223760 1 8.00
CHEMBL225333 1 8.00
CHEMBL1762761 1 8.00
CHEMBL1093059 BARDOXOLONE 2.0 1 7.77
CHEMBL384467 DEXAMETHASONE 4.0 1 7.70
CHEMBL1762762 1 7.70
CHEMBL1760027 1 7.70
CHEMBL222528 1 7.70
CHEMBL356121 1 7.64
CHEMBL1762759 1 7.46
CHEMBL1762751 1 7.40
CHEMBL1762763 1 7.30
CHEMBL1762619 1 7.24
CHEMBL389621 HYDROCORTISONE 4.0 1 7.21
CHEMBL1762612 1 7.19
CHEMBL1762615 1 7.19
CHEMBL1762611 1 7.10
CHEMBL1762754 1 7.10
CHEMBL1762610 1 7.08
CHEMBL1762749 1 7.08
CHEMBL1762755 1 7.08
CHEMBL1762618 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224752 IC50 = 1.0 nM 9.00
CHEMBL1720855 IC50 = 1.0 nM 9.00
CHEMBL1762757 IC50 = 1.0 nM 9.00
CHEMBL1762758 IC50 = 2.0 nM 8.70
CHEMBL1762609 IC50 = 3.0 nM 8.52
CHEMBL224752 IC50 = 3.0 nM 8.52
CHEMBL222861 IC50 = 3.0 nM 8.52
CHEMBL222861 IC50 = 3.0 nM 8.52
CHEMBL376599 IC50 = 4.0 nM 8.40
CHEMBL221714 IC50 = 5.0 nM 8.30
CHEMBL1762761 IC50 = 10.0 nM 8.00
CHEMBL225333 IC50 = 10.0 nM 8.00
CHEMBL223760 IC50 = 10.0 nM 8.00
CHEMBL1093059 BARDOXOLONE IC50 = 17.0 nM 7.77
CHEMBL222528 IC50 = 20.0 nM 7.70
CHEMBL1760027 IC50 = 20.0 nM 7.70
CHEMBL1762762 IC50 = 20.0 nM 7.70
CHEMBL384467 DEXAMETHASONE IC50 = 20.0 nM 7.70
CHEMBL356121 IC50 = 23.0 nM 7.64
CHEMBL1762759 IC50 = 35.0 nM 7.46
CHEMBL1762751 IC50 = 40.0 nM 7.40
CHEMBL1762763 IC50 = 50.0 nM 7.30
CHEMBL1762619 IC50 = 57.0 nM 7.24
CHEMBL389621 HYDROCORTISONE IC50 = 61.0 nM 7.21
CHEMBL1762612 IC50 = 64.0 nM 7.19
CHEMBL1762615 IC50 = 64.0 nM 7.19
CHEMBL1762611 IC50 = 80.0 nM 7.10
CHEMBL1762754 IC50 = 80.0 nM 7.10
CHEMBL1762610 IC50 = 83.0 nM 7.08
CHEMBL1762749 IC50 = 83.0 nM 7.08
CHEMBL1762755 IC50 = 83.0 nM 7.08
CHEMBL1762618 IC50 = 85.0 nM 7.07
CHEMBL415458 IC50 = 87.0 nM 7.06
CHEMBL1762608 IC50 = 100.0 nM 7.00
CHEMBL1762756 IC50 = 115.0 nM 6.94
CHEMBL1762623 IC50 = 150.0 nM 6.82
CHEMBL1762753 IC50 = 240.0 nM 6.62
CHEMBL1762622 IC50 = 290.0 nM 6.54
CHEMBL1762606 IC50 = 350.0 nM 6.46
CHEMBL1762752 IC50 = 360.0 nM 6.44
CHEMBL1762760 IC50 = 400.0 nM 6.40
CHEMBL1762607 IC50 = 480.0 nM 6.32
CHEMBL1762750 IC50 > 10000.0 nM -