Assay Detail
Binding
CHEMBL1764806
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of staurosporine induced activation of caspase 3 activation in human Hela cells assessed as hydrolysis of Z-DEVD-R110 substrate by microplate fluorescence assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 27 | 5.82 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1762363 | — | — | 1 | 6.46 |
| CHEMBL1762349 | — | — | 1 | 6.42 |
| CHEMBL1762353 | — | — | 1 | 6.41 |
| CHEMBL1762362 | — | — | 1 | 6.38 |
| CHEMBL372322 | — | — | 1 | 6.35 |
| CHEMBL1762350 | — | — | 1 | 6.35 |
| CHEMBL197549 | — | — | 1 | 6.19 |
| CHEMBL456799 | — | — | 1 | 6.17 |
| CHEMBL1762361 | — | — | 1 | 6.10 |
| CHEMBL456798 | — | — | 1 | 6.03 |
| CHEMBL1762366 | — | — | 1 | 5.97 |
| CHEMBL1762352 | — | — | 1 | 5.89 |
| CHEMBL1762364 | — | — | 1 | 5.86 |
| CHEMBL1762351 | — | — | 1 | 5.77 |
| CHEMBL371879 | — | — | 1 | 5.75 |
| CHEMBL197535 | — | — | 1 | 5.74 |
| CHEMBL1762346 | — | — | 1 | 5.70 |
| CHEMBL1762347 | — | — | 1 | 5.67 |
| CHEMBL1762365 | — | — | 1 | 5.60 |
| CHEMBL200785 | — | — | 1 | 5.55 |
| CHEMBL200813 | — | — | 1 | 5.51 |
| CHEMBL371709 | — | — | 1 | 5.49 |
| CHEMBL439753 | — | — | 1 | 5.43 |
| CHEMBL213759 | — | — | 1 | 5.35 |
| CHEMBL293034 | — | — | 1 | 5.12 |
| CHEMBL200767 | — | — | 1 | 5.02 |
| CHEMBL62993 | — | — | 1 | 4.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1762363 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1762349 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL1762353 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1762362 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL372322 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1762350 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL197549 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL456799 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1762361 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL456798 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL1762366 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL1762352 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1762364 | — | EC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL1762351 | — | EC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL371879 | — | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL197535 | — | EC50 | = | 1830.0 | nM | 5.74 |
| CHEMBL1762346 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1762347 | — | EC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL1762365 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL200785 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL200813 | — | EC50 | = | 3070.0 | nM | 5.51 |
| CHEMBL371709 | — | EC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL439753 | — | EC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL213759 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL293034 | — | EC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL200767 | — | EC50 | = | 9570.0 | nM | 5.02 |
| CHEMBL62993 | — | EC50 | = | 11500.0 | nM | 4.94 |