Assay Detail
Binding
CHEMBL4818405
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Inhibition of NLRP3 in mouse J774A.1 cells infected with FLA-ST assessed as inhibition of LPS- induced IL-1beta production by ELISA
43
Total Activities
43
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
Discovery of chalcone analogues as novel NLRP3 inflammasome inhibitors with potent anti-inflammation activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 5.01 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3989943 | DAPANSUTRILE | 2.0 | 1 | 7.00 |
| CHEMBL4862238 | — | — | 1 | 5.89 |
| CHEMBL4877267 | — | — | 1 | 5.80 |
| CHEMBL4846605 | — | — | 1 | 5.68 |
| CHEMBL964 | DISULFIRAM | 4.0 | 1 | 5.52 |
| CHEMBL4863235 | — | — | 1 | 5.47 |
| CHEMBL4853965 | — | — | 1 | 5.46 |
| CHEMBL4866055 | — | — | 1 | 5.41 |
| CHEMBL4879208 | — | — | 1 | 5.30 |
| CHEMBL4867413 | — | — | 1 | 5.28 |
| CHEMBL4873993 | — | — | 1 | 5.24 |
| CHEMBL4583133 | — | — | 1 | 5.08 |
| CHEMBL4868303 | — | — | 1 | 5.06 |
| CHEMBL4877752 | — | — | 1 | 5.02 |
| CHEMBL4863875 | — | — | 1 | 5.01 |
| CHEMBL4876251 | — | — | 1 | 5.00 |
| CHEMBL4866717 | — | — | 1 | 4.97 |
| CHEMBL4868373 | — | — | 1 | 4.97 |
| CHEMBL4864667 | — | — | 1 | 4.93 |
| CHEMBL58929 | — | — | 1 | 4.91 |
| CHEMBL4857526 | — | — | 1 | 4.90 |
| CHEMBL4860415 | — | — | 1 | 4.90 |
| CHEMBL4855126 | — | — | 1 | 4.89 |
| CHEMBL4871463 | — | — | 1 | 4.84 |
| CHEMBL4879333 | — | — | 1 | 4.66 |
| CHEMBL4850742 | — | — | 1 | 4.65 |
| CHEMBL4875256 | — | — | 1 | 4.63 |
| CHEMBL4869751 | — | — | 1 | 4.62 |
| CHEMBL4876549 | — | — | 1 | 4.59 |
| CHEMBL4863996 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3989943 | DAPANSUTRILE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4862238 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4877267 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4846605 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL964 | DISULFIRAM | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4863235 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL4853965 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4866055 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL4879208 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4867413 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4873993 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4583133 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4868303 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4877752 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL4863875 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4876251 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4866717 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4868373 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL4864667 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL58929 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL4860415 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4857526 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4855126 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL4871463 | — | IC50 | = | 14600.0 | nM | 4.84 |
| CHEMBL4879333 | — | IC50 | = | 21900.0 | nM | 4.66 |
| CHEMBL4850742 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL4875256 | — | IC50 | = | 23500.0 | nM | 4.63 |
| CHEMBL4869751 | — | IC50 | = | 24200.0 | nM | 4.62 |
| CHEMBL4876549 | — | IC50 | = | 25900.0 | nM | 4.59 |
| CHEMBL4863996 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL4867279 | — | IC50 | = | 28600.0 | nM | 4.54 |
| CHEMBL4848015 | — | IC50 | = | 29400.0 | nM | 4.53 |
| CHEMBL4872428 | — | IC50 | = | 31700.0 | nM | 4.50 |
| CHEMBL4869764 | — | IC50 | = | 33200.0 | nM | 4.48 |
| CHEMBL4859254 | — | IC50 | = | 38700.0 | nM | 4.41 |
| CHEMBL3707395 | ELAFIBRANOR | IC50 | = | 39600.0 | nM | 4.40 |
| CHEMBL4861777 | — | IC50 | = | 49500.0 | nM | 4.30 |
| CHEMBL4854642 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4853113 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4865676 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4867318 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4851731 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL4862784 | — | IC50 | > | 40000.0 | nM | - |