Assay Detail
Binding
CHEMBL4727730
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NLRP3 inflammasome in mouse J774.A1 cells assessed as reduction in LPS-induced IL-1beta release
7
Total Activities
7
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
Synthesis and biological evaluation of parthenolide derivatives with reduced toxicity as potential inhibitors of the NLRP3 inflammasome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.15 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4740148 | — | — | 1 | 6.52 |
| CHEMBL4756259 | — | — | 1 | 6.40 |
| CHEMBL4798966 | — | — | 1 | 6.31 |
| CHEMBL4781662 | — | — | 1 | 6.30 |
| CHEMBL299112 | — | — | 1 | 6.03 |
| CHEMBL4781244 | — | — | 1 | 5.85 |
| CHEMBL449579 | MICHELIOLIDE | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4740148 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4756259 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4798966 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4781662 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL299112 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL4781244 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL449579 | MICHELIOLIDE | IC50 | = | 2300.0 | nM | 5.64 |