Assay Detail
Binding
CHEMBL3377640
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant caspase 7 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 | 7.00 | 8.48 |
| Ki | 2 | 7.05 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3359194 | — | — | 1 | 8.48 |
| CHEMBL3359196 | — | — | 1 | 8.22 |
| CHEMBL521840 | — | — | 1 | 8.09 |
| CHEMBL3359202 | — | — | 1 | 8.01 |
| CHEMBL3359195 | — | — | 1 | 7.70 |
| CHEMBL3359184 | — | — | 1 | 7.70 |
| CHEMBL3359197 | — | — | 1 | 7.64 |
| CHEMBL494140 | — | — | 1 | 7.55 |
| CHEMBL3359203 | — | — | 1 | 7.41 |
| CHEMBL3359185 | — | — | 1 | 7.37 |
| CHEMBL293034 | — | — | 1 | 7.33 |
| CHEMBL3359200 | — | — | 1 | 7.25 |
| CHEMBL493926 | — | — | 1 | 7.24 |
| CHEMBL3359188 | — | — | 1 | 7.17 |
| CHEMBL3359187 | — | — | 1 | 6.91 |
| CHEMBL3359192 | — | — | 1 | 6.87 |
| CHEMBL3359193 | — | — | 1 | 6.80 |
| CHEMBL60190 | — | — | 2 | 6.77 |
| CHEMBL3359199 | — | — | 1 | 6.58 |
| CHEMBL3359189 | — | — | 1 | 6.55 |
| CHEMBL216819 | — | — | 1 | 6.52 |
| CHEMBL521839 | — | — | 1 | 6.50 |
| CHEMBL3359191 | — | — | 1 | 6.26 |
| CHEMBL3359186 | — | — | 1 | 6.04 |
| CHEMBL3359201 | — | — | 1 | 5.18 |
| CHEMBL3359183 | — | — | 1 | 4.98 |
| CHEMBL3359190 | — | — | 1 | - |
| CHEMBL3359198 | — | — | 1 | - |
| CHEMBL3359182 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3359194 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3359196 | — | IC50 | = | 5.95 | nM | 8.22 |
| CHEMBL521840 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL3359202 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3359184 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL3359195 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL3359197 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL494140 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3359203 | — | IC50 | = | 39.3 | nM | 7.41 |
| CHEMBL3359185 | — | IC50 | = | 42.4 | nM | 7.37 |
| CHEMBL293034 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL3359200 | — | IC50 | = | 55.7 | nM | 7.25 |
| CHEMBL493926 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3359188 | — | IC50 | = | 68.1 | nM | 7.17 |
| CHEMBL3359187 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3359192 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3359193 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL60190 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL3359199 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL3359189 | — | IC50 | = | 279.0 | nM | 6.55 |
| CHEMBL216819 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL521839 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL3359191 | — | IC50 | = | 553.0 | nM | 6.26 |
| CHEMBL3359186 | — | IC50 | = | 907.0 | nM | 6.04 |
| CHEMBL60190 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL3359201 | — | IC50 | = | 6620.0 | nM | 5.18 |
| CHEMBL3359183 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3359198 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3359190 | — | IC50 | = | 500000.0 | nM | - |
| CHEMBL3359182 | — | IC50 | = | 500000.0 | nM | - |