Assay Detail
Functional
CHEMBL5588209
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IL-1beta release in PMA-differentiated/ LPS and nigericin stimulated human THP-1 cells pretreated with LPS for 3 hrs followed by incubation with compound for 40 mins and later stimulated with nigericin for 40 mins by ELISA
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of Potent, Specific, and Orally Available NLRP3 Inflammasome Inhibitors Based on Pyridazine Scaffolds for the Treatment of Septic Shock and Peritonitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.77 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598432 | — | — | 1 | 9.00 |
| CHEMBL5598150 | — | — | 1 | 9.00 |
| CHEMBL5596458 | — | — | 1 | 8.70 |
| CHEMBL5597392 | — | — | 1 | 8.52 |
| CHEMBL5598123 | — | — | 1 | 8.40 |
| CHEMBL5598398 | — | — | 1 | 8.40 |
| CHEMBL5598499 | — | — | 1 | 8.30 |
| CHEMBL5596435 | — | — | 1 | 8.22 |
| CHEMBL5596299 | — | — | 1 | 8.22 |
| CHEMBL3183703 | — | — | 1 | 8.10 |
| CHEMBL5597995 | — | — | 1 | 8.05 |
| CHEMBL5421303 | — | — | 1 | 7.92 |
| CHEMBL5596672 | — | — | 1 | 7.60 |
| CHEMBL5597861 | — | — | 1 | 7.58 |
| CHEMBL5598059 | — | — | 1 | 7.57 |
| CHEMBL5596680 | — | — | 1 | 7.57 |
| CHEMBL5596102 | — | — | 1 | 7.42 |
| CHEMBL5596711 | — | — | 1 | 7.42 |
| CHEMBL5596079 | — | — | 1 | 7.38 |
| CHEMBL5598073 | — | — | 1 | 7.31 |
| CHEMBL5590476 | — | — | 1 | 7.31 |
| CHEMBL5589750 | — | — | 1 | 7.28 |
| CHEMBL5597990 | — | — | 1 | 7.24 |
| CHEMBL5596222 | — | — | 1 | 7.12 |
| CHEMBL5597002 | — | — | 1 | 7.10 |
| CHEMBL5597552 | — | — | 1 | 7.06 |
| CHEMBL5598058 | — | — | 1 | 6.99 |
| CHEMBL5598247 | — | — | 1 | 6.91 |
| CHEMBL5597787 | — | — | 1 | - |
| CHEMBL5598226 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598432 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5598150 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5596458 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5597392 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5598123 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5598398 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5598499 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5596435 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5596299 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3183703 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5597995 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5421303 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5596672 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5597861 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5596680 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5598059 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5596102 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5596711 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5596079 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5598073 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5590476 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5589750 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5597990 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5596222 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5597002 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL5597552 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5598058 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5598247 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5590559 | — | IC50 | - | — | - | |
| CHEMBL5596078 | — | IC50 | - | — | - | |
| CHEMBL5590424 | — | IC50 | - | — | - | |
| CHEMBL5598145 | — | IC50 | - | — | - | |
| CHEMBL5596749 | — | IC50 | - | — | - | |
| CHEMBL5597510 | — | IC50 | - | — | - | |
| CHEMBL5597133 | — | IC50 | - | — | - | |
| CHEMBL5598062 | — | IC50 | - | — | - | |
| CHEMBL5597600 | — | IC50 | - | — | - | |
| CHEMBL5596994 | — | IC50 | - | — | - | |
| CHEMBL5596628 | — | IC50 | - | — | - | |
| CHEMBL5596492 | — | IC50 | - | — | - | |
| CHEMBL5598226 | — | IC50 | - | — | - | |
| CHEMBL5597787 | — | IC50 | - | — | - |