Assay Detail
Binding
CHEMBL5374759
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NLRP3 inflammasome activation in human whole blood assessed as inhibition of LPS/ATP induced IL-1beta secretion preincubated with LPS for 3 hrs followed by compound addition for 30 mins and further stimulated with ATP for 60 mins by ELISA
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 36 | 6.23 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5408007 | — | — | 1 | 8.30 |
| CHEMBL5403928 | — | — | 1 | 8.22 |
| CHEMBL5409389 | NT-0796 | 1.0 | 1 | 8.15 |
| CHEMBL5423228 | — | — | 1 | 7.89 |
| CHEMBL5438164 | — | — | 1 | 7.89 |
| CHEMBL5423220 | — | — | 1 | 7.70 |
| CHEMBL5411537 | — | — | 1 | 7.64 |
| CHEMBL5427865 | — | — | 1 | 7.48 |
| CHEMBL5408252 | — | — | 1 | 7.38 |
| CHEMBL5399814 | — | — | 1 | 6.85 |
| CHEMBL4780624 | — | — | 1 | 6.80 |
| CHEMBL5407505 | — | — | 1 | 6.00 |
| CHEMBL5420080 | — | — | 1 | 5.96 |
| CHEMBL5427193 | — | — | 1 | 5.89 |
| CHEMBL5440114 | — | — | 1 | 5.85 |
| CHEMBL5432079 | — | — | 1 | 5.77 |
| CHEMBL5436264 | — | — | 1 | 5.62 |
| CHEMBL5404989 | — | — | 1 | 5.54 |
| CHEMBL3183703 | — | — | 1 | 5.54 |
| CHEMBL5417052 | — | — | 1 | 5.41 |
| CHEMBL5423530 | — | — | 1 | 5.33 |
| CHEMBL5426519 | — | — | 1 | 5.26 |
| CHEMBL5424149 | — | — | 1 | 5.17 |
| CHEMBL5432654 | — | — | 1 | 5.04 |
| CHEMBL5406685 | — | — | 1 | 5.03 |
| CHEMBL5402869 | — | — | 1 | 4.89 |
| CHEMBL5433230 | — | — | 1 | 4.72 |
| CHEMBL5409945 | — | — | 1 | 4.72 |
| CHEMBL4795130 | — | — | 1 | 4.54 |
| CHEMBL5422068 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408007 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5403928 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5409389 | NT-0796 | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5423228 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5438164 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5423220 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5411537 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5427865 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5408252 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5399814 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4780624 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5407505 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5420080 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5427193 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5440114 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5432079 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5436264 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3183703 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5404989 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5417052 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5423530 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5426519 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5424149 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL5432654 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL5406685 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL5402869 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL5409945 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL5433230 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4795130 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL5422068 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5416016 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5433625 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5420131 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5408441 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL5397039 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5408846 | — | IC50 | > | 40000.0 | nM | - |