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Assay Detail

CHEMBL5359835

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

Binding
Inhibition of NLRP3 inflammasome activation in mouse J774.A1 cells assessed as reduction in LPS-stimulated IL-1beta level pretreated for 1 hr followed by nigericin treatment for 1 hr by ELISA
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type J774.A1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

NACHT, LRR and PYD domains-containing protein 3 (CHEMBL3779755)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of a dual-acting inhibitor of interleukin-1β and STATs for the treatment of inflammatory bowel disease.
Cai H, Liu Z, Sun P, Zhou Y, Yan Y, Luo Y, Zhang X, Wu R, Liang X, Wu D, Hu W, Yang Z.
RSC Med Chem (2024) 15 : 193 -206
PubMed 38283225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.45 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5414924 1 6.89
CHEMBL5429161 1 5.97
CHEMBL5401581 1 5.96
CHEMBL5424691 1 5.80
CHEMBL5407779 1 5.52
CHEMBL5404529 1 5.52
CHEMBL5398679 1 5.47
CHEMBL4846605 1 5.43
CHEMBL5411280 1 5.42
CHEMBL5431684 1 5.40
CHEMBL5407010 1 5.31
CHEMBL5435953 1 5.28
CHEMBL5419637 1 5.22
CHEMBL5395385 1 5.22
CHEMBL5414723 1 5.22
CHEMBL5411854 1 5.08
CHEMBL5426512 1 4.84
CHEMBL5439313 1 4.57
CHEMBL5403247 1 -
CHEMBL5420505 1 -
CHEMBL5435228 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5414924 IC50 = 130.0 nM 6.89
CHEMBL5429161 IC50 = 1080.0 nM 5.97
CHEMBL5401581 IC50 = 1090.0 nM 5.96
CHEMBL5424691 IC50 = 1570.0 nM 5.80
CHEMBL5407779 IC50 = 3010.0 nM 5.52
CHEMBL5404529 IC50 = 3020.0 nM 5.52
CHEMBL5398679 IC50 = 3370.0 nM 5.47
CHEMBL4846605 IC50 = 3670.0 nM 5.43
CHEMBL5411280 IC50 = 3800.0 nM 5.42
CHEMBL5431684 IC50 = 3960.0 nM 5.40
CHEMBL5407010 IC50 = 4930.0 nM 5.31
CHEMBL5435953 IC50 = 5210.0 nM 5.28
CHEMBL5419637 IC50 = 5970.0 nM 5.22
CHEMBL5395385 IC50 = 5970.0 nM 5.22
CHEMBL5414723 IC50 = 5950.0 nM 5.22
CHEMBL5411854 IC50 = 8360.0 nM 5.08
CHEMBL5426512 IC50 = 14400.0 nM 4.84
CHEMBL5439313 IC50 = 27100.0 nM 4.57
CHEMBL5403247 IC50 > 50000.0 nM -
CHEMBL5420505 IC50 > 50000.0 nM -
CHEMBL5435228 IC50 > 50000.0 nM -