Assay Detail
Binding
CHEMBL5374760
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NLRP3 inflammasome activation in LPS-induced human THP-1 cells expressing GFP-tagged ASC assessed as disruption of ASC speck formation pretreated for 2 hrs with LPS followed by compound addition for 30 mins and further incubated with zVAD-FMK and nigericin for 1 hr by Hoechst 33342 staining based analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
NACHT, LRR and PYD domains-containing protein 3 (CHEMBL1741208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.90 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5409389 | NT-0796 | 1.0 | 1 | 8.68 |
| CHEMBL3183703 | — | — | 1 | 7.55 |
| CHEMBL4780624 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5409389 | NT-0796 | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3183703 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4780624 | — | IC50 | = | 33.0 | nM | 7.48 |