Assay Detail
Binding
CHEMBL5737706
Review assay metadata, readout intent, target linkage, and publication context from the same page.
IL-1 Secretion Assa: Monocytic THP-1 cells (ATCC: TIB-202) were maintained according to providers' instructions in RPMI media (RPMI/Hepes+10% fetal bovine serum+Sodium Pyruvate+0.05 mM Beta-mercaptoethanol (1000× stock)+Pen-Strep). Cells were differentiated in bulk with 0.5 μM phorbol 12-myristate 13-acetate (PMA; Sigma #P8139) for 3 hours, media was exchanged, and cells were plated at 50,000 cells per well in a 384-well flat-bottom cell culture plates (Greiner, #781986), and allowed to differentiate overnight. Compound in a 1:3.16 serial dilution series in DMSO was added 1:100 to the cells and incubated for 1 hour. The NLRP3 inflammasome was activated with the addition of 15 μM (final concentration) Nigericin (Enzo Life Sciences, #BML-CA421-0005), and cells were incubated for 3 hours. 10 μL supernatant was removed, and IL-1p levels were monitored using an HTRF assay (CisBio, #621L1PEC) according to manufacturers' instructions. Viability and pyroptosis was monitored with the addition of PrestoBlue cell viability reagent (Life Technologies, #A13261) directly to the cell culture plate.
351
Total Activities
114
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
NLRP3 inflammasome inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 117 | 7.51 | 9.40 |
| kon | 117 | - | - |
| k_off | 117 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5414596 | — | — | 3 | 9.40 |
| CHEMBL5426651 | — | — | 3 | 9.40 |
| CHEMBL5992744 | — | — | 3 | 9.22 |
| CHEMBL5774519 | — | — | 3 | 9.15 |
| CHEMBL5433380 | — | — | 3 | 9.10 |
| CHEMBL5991941 | — | — | 3 | 9.10 |
| CHEMBL5906571 | — | — | 3 | 9.10 |
| CHEMBL5797061 | — | — | 3 | 9.10 |
| CHEMBL5910216 | — | — | 3 | 9.10 |
| CHEMBL5881090 | — | — | 3 | 9.05 |
| CHEMBL6036597 | — | — | 3 | 8.92 |
| CHEMBL5970809 | — | — | 3 | 8.89 |
| CHEMBL5752218 | — | — | 6 | 8.89 |
| CHEMBL5808276 | — | — | 3 | 8.80 |
| CHEMBL5763108 | — | — | 3 | 8.80 |
| CHEMBL5782617 | — | — | 6 | 8.74 |
| CHEMBL5928082 | — | — | 3 | 8.72 |
| CHEMBL5971979 | — | — | 3 | 8.72 |
| CHEMBL6011033 | — | — | 3 | 8.64 |
| CHEMBL6029082 | — | — | 3 | 8.59 |
| CHEMBL5812129 | — | — | 3 | 8.59 |
| CHEMBL5852308 | — | — | 6 | 8.52 |
| CHEMBL5960754 | — | — | 3 | 8.52 |
| CHEMBL5761984 | — | — | 3 | 8.49 |
| CHEMBL5801636 | — | — | 3 | 8.49 |
| CHEMBL6049792 | — | — | 3 | 8.48 |
| CHEMBL6015148 | — | — | 3 | 8.46 |
| CHEMBL5758980 | — | — | 3 | 8.44 |
| CHEMBL6001622 | — | — | 3 | 8.33 |
| CHEMBL5782662 | — | — | 3 | 8.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5414596 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5426651 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5992744 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5774519 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5797061 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5910216 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5433380 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5991941 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5906571 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5881090 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL6036597 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5970809 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5752218 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5808276 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5763108 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5782617 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5971979 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5928082 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6011033 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL6029082 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5812129 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5852308 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5960754 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5761984 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5801636 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL6049792 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL6015148 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5758980 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL6001622 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5782662 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL5840970 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5847930 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL5973713 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5834410 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5963394 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5763742 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5882443 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5790303 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5984350 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL5874946 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5808248 | — | IC50 | = | 18.3 | nM | 7.74 |
| CHEMBL5836561 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL6015125 | — | IC50 | = | 24.1 | nM | 7.62 |
| CHEMBL6035509 | — | IC50 | = | 25.3 | nM | 7.60 |
| CHEMBL6009102 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL5843429 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL6023173 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL5912010 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL5745086 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL5801025 | — | IC50 | = | 40.1 | nM | 7.40 |