Assay Detail
Binding
CHEMBL3706347
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: To test the efficacy of caspase-3 inhibitors at the cellular level, the ability of selected compounds to inhibit the proteolytic cleavage of PARP (poly ADP-ribose polymerase) was evaluated in live Hela cells.Briefly, in this assay Hela cells are seeded in 96 well plates and incubated for 4 hours with staurosporine, a well characterized inducer of apoptosis, alone or together with different concentrations of compound (50, 25, 10 and 3 uM). After formaldehyde-based fixation, the cells are stained with a fluorescein-labeled anti-cleaved PARP antibody (Cell signaling, Cat#: 9547) and counterstained with Hoechst33342 (Invitrogen, Cat#: H3570) to mark all nuclei.
26
Total Activities
26
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
Selective caspase inhibitors and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.22 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3673267 | — | — | 1 | 8.00 |
| CHEMBL3673263 | — | — | 1 | 8.00 |
| CHEMBL3673259 | — | — | 1 | 8.00 |
| CHEMBL3673265 | — | — | 1 | 7.70 |
| CHEMBL3673264 | — | — | 1 | 7.52 |
| CHEMBL3678066 | — | — | 1 | 7.52 |
| CHEMBL3678068 | — | — | 1 | 7.52 |
| CHEMBL3678069 | — | — | 1 | 7.40 |
| CHEMBL3673266 | — | — | 1 | 7.40 |
| CHEMBL3673262 | — | — | 1 | 7.22 |
| CHEMBL3678065 | — | — | 1 | 7.00 |
| CHEMBL3673270 | — | — | 1 | 7.00 |
| CHEMBL3673268 | — | — | 1 | 6.70 |
| CHEMBL3673269 | — | — | 1 | 6.70 |
| CHEMBL3678064 | — | — | 1 | 6.52 |
| CHEMBL3678067 | — | — | 1 | 6.52 |
| CHEMBL3673261 | — | — | 1 | 6.00 |
| CHEMBL3678072 | — | — | 1 | - |
| CHEMBL1242699 | — | — | 1 | - |
| CHEMBL3678071 | — | — | 1 | - |
| CHEMBL3673256 | — | — | 1 | - |
| CHEMBL3678070 | — | — | 1 | - |
| CHEMBL3673255 | — | — | 1 | - |
| CHEMBL3673258 | — | — | 1 | - |
| CHEMBL3673257 | — | — | 1 | - |
| CHEMBL3673260 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3673267 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673263 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673259 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3673265 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3673264 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678066 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678068 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678069 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3673266 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3673262 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3678065 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3673270 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3673268 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3673269 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3678064 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3678067 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3673261 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3678072 | — | IC50 | > | 3330.0 | nM | - |
| CHEMBL1242699 | — | IC50 | > | 3330.0 | nM | - |
| CHEMBL3678071 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3673256 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3678070 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3673255 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3673258 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3673257 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3673260 | — | IC50 | > | 3330.0 | nM | - |