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Assay Detail

CHEMBL5377737

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

Binding
Inhibition of NLRP3 inflammasome in mouse JJ74.A1 cells assessed as inhibition of LPS/ATP-induced IL-1 beta release stimulated with LPS for 4.5 hs followed by incubation with compound for 30 mins and ATP addition for 30 mins by ELISA
ChEMBL ↗
65
Total Activities
65
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 Novel 2,3-Dihydro-1<i>H</i>-indene-5-sulfonamide NLRP3 Inflammasome Inhibitors Targeting Colon as a Potential Therapy for Colitis.
Sun S, Li Z, Huang C, Liu J, Yu Q, Jiang X, Yue K, Zhao J, Xu T, Liu Y, Li X, Qin C, Jiang Y.
J Med Chem (2023) 66 : 16141 -16167
PubMed 38029358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.86 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3183703 — — 1 7.89
CHEMBL5413950 — — 1 6.89
CHEMBL5411875 — — 1 6.85
CHEMBL5433038 — — 1 6.77
CHEMBL5438536 — — 1 6.72
CHEMBL5426773 — — 1 6.70
CHEMBL5399147 — — 1 6.68
CHEMBL5425129 — — 1 6.58
CHEMBL5425258 — — 1 6.42
CHEMBL5397003 — — 1 6.42
CHEMBL5405822 — — 1 6.42
CHEMBL4559751 — — 1 6.38
CHEMBL5404781 — — 1 6.33
CHEMBL5404399 — — 1 6.30
CHEMBL5427235 — — 1 6.29
CHEMBL5399241 — — 1 6.16
CHEMBL5421434 — — 1 6.16
CHEMBL5402443 — — 1 6.14
CHEMBL5440329 — — 1 6.14
CHEMBL5402042 — — 1 6.12
CHEMBL5427405 — — 1 6.10
CHEMBL5401024 — — 1 6.02
CHEMBL5436086 — — 1 6.00
CHEMBL5394338 — — 1 6.00
CHEMBL5406986 — — 1 5.97
CHEMBL5439915 — — 1 5.97
CHEMBL5434103 — — 1 5.97
CHEMBL5419504 — — 1 5.96
CHEMBL5410048 — — 1 5.90
CHEMBL5415250 — — 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3183703 — IC50 = 13.0 nM 7.89
CHEMBL5413950 — IC50 = 130.0 nM 6.89
CHEMBL5411875 — IC50 = 140.0 nM 6.85
CHEMBL5433038 — IC50 = 170.0 nM 6.77
CHEMBL5438536 — IC50 = 190.0 nM 6.72
CHEMBL5426773 — IC50 = 200.0 nM 6.70
CHEMBL5399147 — IC50 = 210.0 nM 6.68
CHEMBL5425129 — IC50 = 260.0 nM 6.58
CHEMBL5425258 — IC50 = 380.0 nM 6.42
CHEMBL5397003 — IC50 = 380.0 nM 6.42
CHEMBL5405822 — IC50 = 380.0 nM 6.42
CHEMBL4559751 — IC50 = 420.0 nM 6.38
CHEMBL5404781 — IC50 = 470.0 nM 6.33
CHEMBL5404399 — IC50 = 500.0 nM 6.30
CHEMBL5427235 — IC50 = 510.0 nM 6.29
CHEMBL5399241 — IC50 = 690.0 nM 6.16
CHEMBL5421434 — IC50 = 700.0 nM 6.16
CHEMBL5402443 — IC50 = 730.0 nM 6.14
CHEMBL5440329 — IC50 = 720.0 nM 6.14
CHEMBL5402042 — IC50 = 760.0 nM 6.12
CHEMBL5427405 — IC50 = 790.0 nM 6.10
CHEMBL5401024 — IC50 = 960.0 nM 6.02
CHEMBL5436086 — IC50 = 1010.0 nM 6.00
CHEMBL5394338 — IC50 = 990.0 nM 6.00
CHEMBL5434103 — IC50 = 1070.0 nM 5.97
CHEMBL5439915 — IC50 = 1070.0 nM 5.97
CHEMBL5406986 — IC50 = 1080.0 nM 5.97
CHEMBL5419504 — IC50 = 1110.0 nM 5.96
CHEMBL5410048 — IC50 = 1270.0 nM 5.90
CHEMBL5415250 — IC50 = 1310.0 nM 5.88
CHEMBL5406839 — IC50 = 1330.0 nM 5.88
CHEMBL5401682 — IC50 = 1510.0 nM 5.82
CHEMBL5396903 — IC50 = 1510.0 nM 5.82
CHEMBL5406412 — IC50 = 1650.0 nM 5.78
CHEMBL5409764 — IC50 = 1660.0 nM 5.78
CHEMBL5432596 — IC50 = 1700.0 nM 5.77
CHEMBL5416194 — IC50 = 1740.0 nM 5.76
CHEMBL5413576 — IC50 = 1750.0 nM 5.76
CHEMBL5398101 — IC50 = 1820.0 nM 5.74
CHEMBL5431788 — IC50 = 1840.0 nM 5.74
CHEMBL5424191 — IC50 = 1870.0 nM 5.73
CHEMBL5408858 — IC50 = 1950.0 nM 5.71
CHEMBL5411186 — IC50 = 1970.0 nM 5.71
CHEMBL5431010 — IC50 = 1990.0 nM 5.70
CHEMBL5434931 — IC50 = 2090.0 nM 5.68
CHEMBL5438386 — IC50 = 2110.0 nM 5.68
CHEMBL5423673 — IC50 = 2090.0 nM 5.68
CHEMBL5397566 — IC50 = 2820.0 nM 5.55
CHEMBL5432085 — IC50 = 3130.0 nM 5.50
CHEMBL4277456 — IC50 = 3210.0 nM 5.49