Assay Detail
Binding
CHEMBL3744289
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Inhibition of HDAC6 in human HeLa cells assessed as inhibition of tubulin deacetylation incubated for overnight by cELISA
5
Total Activities
5
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
Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 6.39 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 8.28 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.66 |
| CHEMBL320497 | SUBEROHYDROXAMIC ACID | — | 1 | 5.96 |
| CHEMBL3739529 | — | — | 1 | 5.30 |
| CHEMBL3740591 | — | — | 1 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | EC50 | = | 5.2 | nM | 8.28 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 21.7 | nM | 7.66 |
| CHEMBL320497 | SUBEROHYDROXAMIC ACID | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3739529 | — | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3740591 | — | EC50 | = | 17700.0 | nM | 4.75 |