Assay Detail
Binding
CHEMBL4813265
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NLRP3 inflammasome in LPS-primed mouse J774.A1 cells assessed as reduction in IL-1beta secretion preincubated with compound for 1 hr followed by nigericin stimulation for 1 hr by ELISA
39
Total Activities
38
Compounds Tested
2
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 dronedarone and its analogues as NLRP3 inflammasome inhibitors with potent anti-inflammation activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 4.69 | 5.42 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874900 | — | — | 2 | 5.42 |
| CHEMBL4878576 | — | — | 1 | 5.24 |
| CHEMBL184412 | DRONEDARONE | 4.0 | 1 | 5.17 |
| CHEMBL4847862 | — | — | 1 | 5.17 |
| CHEMBL4855368 | — | — | 1 | 5.12 |
| CHEMBL4862936 | — | — | 1 | 5.04 |
| CHEMBL4868879 | — | — | 1 | 4.97 |
| CHEMBL4858664 | — | — | 1 | 4.94 |
| CHEMBL4875931 | — | — | 1 | 4.90 |
| CHEMBL4877661 | — | — | 1 | 4.88 |
| CHEMBL4854858 | — | — | 1 | 4.88 |
| CHEMBL4857996 | — | — | 1 | 4.87 |
| CHEMBL4872710 | — | — | 1 | 4.79 |
| CHEMBL4874861 | — | — | 1 | 4.73 |
| CHEMBL4856299 | — | — | 1 | 4.72 |
| CHEMBL4872730 | — | — | 1 | 4.72 |
| CHEMBL4869743 | — | — | 1 | 4.65 |
| CHEMBL4863841 | — | — | 1 | 4.61 |
| CHEMBL4856687 | — | — | 1 | 4.60 |
| CHEMBL4856358 | — | — | 1 | 4.60 |
| CHEMBL4857471 | — | — | 1 | 4.60 |
| CHEMBL4851771 | — | — | 1 | 4.60 |
| CHEMBL4865010 | — | — | 1 | 4.57 |
| CHEMBL4866972 | — | — | 1 | 4.57 |
| CHEMBL4862125 | — | — | 1 | 4.55 |
| CHEMBL4860713 | — | — | 1 | 4.48 |
| CHEMBL4849767 | — | — | 1 | 4.37 |
| CHEMBL4870808 | — | — | 1 | 4.34 |
| CHEMBL4872444 | — | — | 1 | 4.21 |
| CHEMBL4877243 | — | — | 1 | 4.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874900 | — | IC50 | = | 3850.0 | nM | 5.42 |
| CHEMBL4878576 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL4847862 | — | IC50 | = | 6770.0 | nM | 5.17 |
| CHEMBL184412 | DRONEDARONE | IC50 | = | 6840.0 | nM | 5.17 |
| CHEMBL4855368 | — | IC50 | = | 7650.0 | nM | 5.12 |
| CHEMBL4862936 | — | IC50 | = | 9030.0 | nM | 5.04 |
| CHEMBL4868879 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL4858664 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4875931 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4877661 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4854858 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4857996 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL4872710 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL4874861 | — | IC50 | = | 18500.0 | nM | 4.73 |
| CHEMBL4872730 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4856299 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4869743 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL4863841 | — | IC50 | = | 24500.0 | nM | 4.61 |
| CHEMBL4851771 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL4856358 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4856687 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4857471 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4865010 | — | IC50 | = | 26700.0 | nM | 4.57 |
| CHEMBL4866972 | — | IC50 | = | 26700.0 | nM | 4.57 |
| CHEMBL4862125 | — | IC50 | = | 27900.0 | nM | 4.55 |
| CHEMBL4860713 | — | IC50 | = | 33400.0 | nM | 4.48 |
| CHEMBL4849767 | — | IC50 | = | 42500.0 | nM | 4.37 |
| CHEMBL4870808 | — | IC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL4872444 | — | IC50 | = | 61100.0 | nM | 4.21 |
| CHEMBL4877243 | — | IC50 | = | 71200.0 | nM | 4.15 |
| CHEMBL4863110 | — | IC50 | = | 74800.0 | nM | 4.13 |
| CHEMBL4867288 | — | IC50 | = | 81600.0 | nM | 4.09 |
| CHEMBL4858149 | — | IC50 | = | 83800.0 | nM | 4.08 |
| CHEMBL4862788 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4851542 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4850237 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4877298 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4874900 | — | Inhibition | - | % | - | |
| CHEMBL4857490 | — | IC50 | > | 100000.0 | nM | - |