Assay Detail
Binding
CHEMBL4355674
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST-tagged human HDAC6 (1 to 1215 residues) expressed in baculovirus infected sf9 insect cells using p53 (379 to 382 residues) derived fluorogenic peptide RHKKAc as substrate preincubated for 5 to 10 mins followed by substrate addition and further incubated for 2 hrs by fluorescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a New Isoxazole-3-hydroxamate-Based Histone Deacetylase 6 Inhibitor SS-208 with Antitumor Activity in Syngeneic Melanoma Mouse Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.29 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126811 | — | — | 1 | 9.48 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 8.70 |
| CHEMBL4536605 | — | — | 1 | 8.64 |
| CHEMBL2179618 | NEXTURASTAT A | — | 1 | 8.30 |
| CHEMBL4554511 | — | — | 1 | 8.22 |
| CHEMBL4556111 | — | — | 1 | 8.00 |
| CHEMBL511749 | — | — | 1 | 7.86 |
| CHEMBL4483795 | — | — | 1 | 7.62 |
| CHEMBL4447715 | — | — | 1 | 7.55 |
| CHEMBL4520424 | — | — | 1 | 7.51 |
| CHEMBL4469488 | — | — | 1 | 7.12 |
| CHEMBL4584312 | — | — | 1 | 6.72 |
| CHEMBL4470946 | — | — | 1 | 6.70 |
| CHEMBL4551620 | — | — | 1 | 6.16 |
| CHEMBL4526191 | — | — | 1 | 5.87 |
| CHEMBL4589770 | — | — | 1 | 5.70 |
| CHEMBL4473037 | — | — | 1 | 5.70 |
| CHEMBL4561802 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126811 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4536605 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL2179618 | NEXTURASTAT A | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4554511 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4556111 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL511749 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4483795 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4447715 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4520424 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4469488 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4584312 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4470946 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4551620 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4526191 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4589770 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4473037 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL4561802 | — | IC50 | = | 4360.0 | nM | 5.36 |