Assay Detail
Binding
CHEMBL4671767
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Inhibition of NLRP3 in human THP1 cells assessed as inhibition of IL-1beta production
26
Total Activities
26
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
Identification of a novel orally bioavailable NLRP3 inflammasome inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.82 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3183703 | — | — | 1 | 8.10 |
| CHEMBL4752523 | — | — | 1 | 7.46 |
| CHEMBL4758640 | — | — | 1 | 7.16 |
| CHEMBL4759516 | — | — | 1 | 7.12 |
| CHEMBL4791679 | — | — | 1 | 7.10 |
| CHEMBL4745667 | — | — | 1 | 7.03 |
| CHEMBL4756798 | — | — | 1 | 7.02 |
| CHEMBL4756693 | — | — | 1 | 6.90 |
| CHEMBL4742825 | — | — | 1 | 6.85 |
| CHEMBL4778322 | — | — | 1 | 6.79 |
| CHEMBL4792478 | — | — | 1 | 6.68 |
| CHEMBL4778164 | — | — | 1 | 6.61 |
| CHEMBL4751187 | — | — | 1 | 6.53 |
| CHEMBL4753623 | — | — | 1 | 6.51 |
| CHEMBL4758006 | — | — | 1 | 6.46 |
| CHEMBL4795321 | — | — | 1 | 6.43 |
| CHEMBL4744515 | — | — | 1 | 6.00 |
| CHEMBL4760079 | — | — | 1 | 5.97 |
| CHEMBL4763529 | — | — | 1 | - |
| CHEMBL4755384 | — | — | 1 | - |
| CHEMBL4753197 | — | — | 1 | - |
| CHEMBL4745706 | — | — | 1 | - |
| CHEMBL4797652 | — | — | 1 | - |
| CHEMBL4777050 | — | — | 1 | - |
| CHEMBL4748040 | — | — | 1 | - |
| CHEMBL4782757 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3183703 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4752523 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4758640 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4759516 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4791679 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4745667 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4756798 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4756693 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4742825 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4778322 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL4792478 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL4778164 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL4751187 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL4753623 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4758006 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL4795321 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL4744515 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4760079 | — | IC50 | = | 1061.0 | nM | 5.97 |
| CHEMBL4763529 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4755384 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4753197 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4745706 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4797652 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4777050 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4748040 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4782757 | — | IC50 | > | 1000.0 | nM | - |