Assay Detail
Binding
CHEMBL5039302
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Inhibition of HDAC6 (unknown origin) using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition by fluorescence assay
21
Total Activities
21
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
Design, synthesis, and biological evaluation of novel dual inhibitors targeting lysine specific demethylase 1 (LSD1) and histone deacetylases (HDAC) for treatment of gastric cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.13 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 8.04 |
| CHEMBL5087997 | — | — | 1 | 7.89 |
| CHEMBL5083395 | — | — | 1 | 7.85 |
| CHEMBL5093633 | — | — | 1 | 7.82 |
| CHEMBL5081674 | — | — | 1 | 7.72 |
| CHEMBL5081128 | — | — | 1 | 7.55 |
| CHEMBL5087466 | — | — | 1 | 7.47 |
| CHEMBL5075646 | — | — | 1 | 7.33 |
| CHEMBL5085680 | — | — | 1 | 7.27 |
| CHEMBL5081983 | — | — | 1 | 7.03 |
| CHEMBL5075694 | — | — | 1 | 6.96 |
| CHEMBL5094326 | — | — | 1 | 6.89 |
| CHEMBL5076948 | — | — | 1 | 6.89 |
| CHEMBL5081200 | — | — | 1 | 6.82 |
| CHEMBL5089538 | — | — | 1 | 6.82 |
| CHEMBL5087779 | — | — | 1 | 6.75 |
| CHEMBL5092482 | — | — | 1 | 6.70 |
| CHEMBL5087823 | — | — | 1 | 6.62 |
| CHEMBL5081459 | — | — | 1 | 6.50 |
| CHEMBL5070176 | — | — | 1 | 6.41 |
| CHEMBL5084881 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5087997 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5083395 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5093633 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5081674 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5081128 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5087466 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5075646 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5085680 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5081983 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5075694 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5094326 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5076948 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5081200 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5089538 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5087779 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5092482 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5087823 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5081459 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5070176 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5084881 | — | IC50 | = | 400.0 | nM | 6.40 |