Assay Detail
Binding
CHEMBL829508
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Inhibitory concentration against recombinant human caspase-1 in neuronal precursor (NT2) cells
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 6.60 | 8.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367356 | — | — | 1 | 8.06 |
| CHEMBL360788 | — | — | 1 | 7.89 |
| CHEMBL178514 | — | — | 1 | 7.60 |
| CHEMBL369290 | — | — | 1 | 7.60 |
| CHEMBL359598 | — | — | 1 | 7.55 |
| CHEMBL179551 | — | — | 1 | 7.51 |
| CHEMBL441118 | — | — | 1 | 7.33 |
| CHEMBL181623 | — | — | 1 | 7.32 |
| CHEMBL366927 | — | — | 1 | 7.30 |
| CHEMBL264344 | — | — | 1 | 7.25 |
| CHEMBL178116 | — | — | 1 | 7.22 |
| CHEMBL180646 | — | — | 1 | 7.20 |
| CHEMBL361613 | — | — | 1 | 7.19 |
| CHEMBL181274 | — | — | 1 | 7.19 |
| CHEMBL361825 | — | — | 1 | 7.17 |
| CHEMBL362213 | — | — | 1 | 7.06 |
| CHEMBL180669 | — | — | 1 | 6.96 |
| CHEMBL362074 | — | — | 1 | 6.96 |
| CHEMBL179503 | — | — | 1 | 6.96 |
| CHEMBL181768 | — | — | 1 | 6.89 |
| CHEMBL360355 | — | — | 1 | 6.82 |
| CHEMBL180273 | — | — | 1 | 6.72 |
| CHEMBL181775 | — | — | 1 | 6.66 |
| CHEMBL433771 | — | — | 1 | 6.66 |
| CHEMBL180763 | — | — | 1 | 6.64 |
| CHEMBL424789 | — | — | 1 | 6.54 |
| CHEMBL443565 | — | — | 1 | 6.51 |
| CHEMBL362191 | — | — | 1 | 6.40 |
| CHEMBL179066 | — | — | 1 | 6.34 |
| CHEMBL181763 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367356 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL360788 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL369290 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL178514 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL359598 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL179551 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL441118 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL181623 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL366927 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL264344 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL178116 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL180646 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL361613 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL181274 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL361825 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL362213 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL180669 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL362074 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL179503 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL181768 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL360355 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL180273 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL181775 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL433771 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL180763 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL424789 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL443565 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL362191 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL179066 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL181763 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL434147 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL360956 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL178775 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL178674 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL181027 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL360915 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL359643 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL220238 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL447233 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL178280 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL359542 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL181396 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL178339 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL425699 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL361983 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL181295 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL360020 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL182103 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL181948 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL180623 | — | IC50 | = | 5130.0 | nM | 5.29 |