Assay Detail
Binding
CHEMBL3134677
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Inhibition of recombinant human caspase-3 expressed in Escherichia coli using Ac-DEVD-AMC as substrate preincubated for 30 mins before substrate addition measured after 2 hrs
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.90 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3133146 | — | — | 1 | 8.51 |
| CHEMBL3133149 | — | — | 1 | 8.36 |
| CHEMBL213759 | — | — | 1 | 8.21 |
| CHEMBL3133253 | — | — | 1 | 8.21 |
| CHEMBL3133148 | — | — | 1 | 8.20 |
| CHEMBL3133254 | — | — | 1 | 8.15 |
| CHEMBL3133258 | — | — | 1 | 8.09 |
| CHEMBL215480 | — | — | 1 | 8.08 |
| CHEMBL3133256 | — | — | 1 | 8.02 |
| CHEMBL3133257 | — | — | 1 | 7.94 |
| CHEMBL3133147 | — | — | 1 | 7.89 |
| CHEMBL3133259 | — | — | 1 | 7.86 |
| CHEMBL3133252 | — | — | 1 | 7.86 |
| CHEMBL3133255 | — | — | 1 | 7.82 |
| CHEMBL217777 | — | — | 1 | 7.75 |
| CHEMBL3133251 | — | — | 1 | 7.72 |
| CHEMBL3133150 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3133146 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3133149 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL213759 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3133253 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3133148 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL3133254 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3133258 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL215480 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3133256 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL3133257 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL3133147 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL3133259 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL3133252 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL3133255 | — | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL217777 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL3133251 | — | IC50 | = | 19.2 | nM | 7.72 |
| CHEMBL3133150 | — | IC50 | = | 2209.0 | nM | 5.66 |