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Assay Detail

CHEMBL4416609

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

Binding
Inhibition of NLRP3 in mouse peritoneal macrophages assessed as inhibition of LPS and ATP-induced IL-1beta production pre-stimulated with LPS for 4.5 hrs before compound addition with ATP for 30 mins by ELISA
5
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
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 Second-Generation NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization.
Jiang Y, He L, Green J, Blevins H, Guo C, Patel SH, Halquist MS, McRae M, Venitz J, Wang XY, Zhang S.
J Med Chem (2019) 62 : 9718 -9731
PubMed 31626545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 3 - -
IC50 2 6.60 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3183703 2 7.40
CHEMBL4559751 2 5.80
CHEMBL4455922 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3183703 IC50 = 40.0 nM 7.40
CHEMBL4559751 IC50 = 1590.0 nM 5.80
CHEMBL4455922 Inhibition - % -
CHEMBL4559751 Inhibition - % -
CHEMBL3183703 Inhibition - % -