Assay Detail
Binding
CHEMBL4605569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NLRP3 inflammasome activation in LPS-primed human THP1 cells assessed as reduction in IL-1beta level preincubated for 1 hr followed by addition of ATP and nigericin further incubated for 1 hrs and measured post ATP addition 1 hr by ELISA method
30
Total Activities
30
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 <i>N</i>-Cyano-sulfoximineurea Derivatives as Potent and Orally Bioavailable NLRP3 Inflammasome Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.72 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4644835 | — | — | 1 | 8.28 |
| CHEMBL4647321 | — | — | 1 | 8.17 |
| CHEMBL3183703 | — | — | 1 | 8.10 |
| CHEMBL4641961 | — | — | 1 | 7.93 |
| CHEMBL4642066 | — | — | 1 | 7.82 |
| CHEMBL4647621 | — | — | 1 | 7.68 |
| CHEMBL4649141 | — | — | 1 | 7.64 |
| CHEMBL4643205 | — | — | 1 | 7.47 |
| CHEMBL4640151 | — | — | 1 | 7.46 |
| CHEMBL4636825 | — | — | 1 | 7.44 |
| CHEMBL4646271 | — | — | 1 | 6.96 |
| CHEMBL4649621 | — | — | 1 | - |
| CHEMBL4641660 | — | — | 1 | - |
| CHEMBL4649881 | — | — | 1 | - |
| CHEMBL4636808 | — | — | 1 | - |
| CHEMBL4643011 | — | — | 1 | - |
| CHEMBL4640804 | — | — | 1 | - |
| CHEMBL4633769 | — | — | 1 | - |
| CHEMBL4634682 | — | — | 1 | - |
| CHEMBL4644865 | — | — | 1 | - |
| CHEMBL4643208 | — | — | 1 | - |
| CHEMBL4646037 | — | — | 1 | - |
| CHEMBL4643062 | — | — | 1 | - |
| CHEMBL4637610 | — | — | 1 | - |
| CHEMBL4644503 | — | — | 1 | - |
| CHEMBL4635816 | — | — | 1 | - |
| CHEMBL4633580 | — | — | 1 | - |
| CHEMBL4634472 | — | — | 1 | - |
| CHEMBL4640644 | — | — | 1 | - |
| CHEMBL4649429 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4644835 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4647321 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3183703 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4641961 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4642066 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4647621 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4649141 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4643205 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4640151 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4636825 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL4646271 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4649621 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4641660 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4649881 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4636808 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4643011 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4640804 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4633769 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4634682 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4644865 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4643208 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4646037 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4643062 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4637610 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4644503 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4635816 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4633580 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4634472 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4640644 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4649429 | — | IC50 | > | 1000.0 | nM | - |