Assay Detail
Binding
CHEMBL3377638
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant caspase 3 using Ac-DEVD-AMC substrate assessed as accumulation of cleaved fluorogenic product
30
Total Activities
29
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.43 | 8.62 |
| Ki | 2 | 7.52 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216819 | — | — | 1 | 8.62 |
| CHEMBL3359197 | — | — | 1 | 8.59 |
| CHEMBL3359202 | — | — | 1 | 8.54 |
| CHEMBL3359200 | — | — | 1 | 8.32 |
| CHEMBL493926 | — | — | 1 | 8.28 |
| CHEMBL293034 | — | — | 1 | 7.82 |
| CHEMBL3359186 | — | — | 1 | 7.76 |
| CHEMBL3359187 | — | — | 1 | 7.70 |
| CHEMBL3359193 | — | — | 1 | 7.58 |
| CHEMBL521840 | — | — | 1 | 7.54 |
| CHEMBL3359196 | — | — | 1 | 7.50 |
| CHEMBL3359189 | — | — | 1 | 7.48 |
| CHEMBL3359203 | — | — | 1 | 7.39 |
| CHEMBL494140 | — | — | 1 | 7.39 |
| CHEMBL3359194 | — | — | 1 | 7.33 |
| CHEMBL3359188 | — | — | 1 | 7.29 |
| CHEMBL3359199 | — | — | 1 | 7.24 |
| CHEMBL60190 | — | — | 2 | 7.22 |
| CHEMBL3359195 | — | — | 1 | 7.09 |
| CHEMBL3359185 | — | — | 1 | 6.91 |
| CHEMBL3359192 | — | — | 1 | 6.88 |
| CHEMBL521839 | — | — | 1 | 6.74 |
| CHEMBL3359184 | — | — | 1 | 6.68 |
| CHEMBL3359191 | — | — | 1 | 6.45 |
| CHEMBL3359183 | — | — | 1 | 5.92 |
| CHEMBL3359190 | — | — | 1 | - |
| CHEMBL3359182 | — | — | 1 | - |
| CHEMBL3359198 | — | — | 1 | - |
| CHEMBL3359201 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216819 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3359197 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3359202 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3359200 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL493926 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL293034 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3359186 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL3359187 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL3359193 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL521840 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3359196 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL3359189 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL3359203 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL494140 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3359194 | — | IC50 | = | 46.9 | nM | 7.33 |
| CHEMBL3359188 | — | IC50 | = | 50.7 | nM | 7.29 |
| CHEMBL3359199 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL60190 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL3359195 | — | IC50 | = | 81.4 | nM | 7.09 |
| CHEMBL60190 | — | IC50 | = | 84.9 | nM | 7.07 |
| CHEMBL3359185 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3359192 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL521839 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3359184 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3359191 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL3359183 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL3359190 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3359198 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3359201 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3359182 | — | IC50 | = | 500000.0 | nM | - |