Assay Detail
Binding
CHEMBL4823880
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Inhibition of full length recombinant human HDAC1 expressed in baculovirus infected Sf9 insect cells using RHKKAc fluorogenic peptide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 2 hrs by fluorescence assay
14
Total Activities
14
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
Tetrahydroquinoline-Capped Histone Deacetylase 6 Inhibitor SW-101 Ameliorates Pathological Phenotypes in a Charcot-Marie-Tooth Type 2A Mouse Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.68 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 8.82 |
| CHEMBL4536605 | — | — | 1 | 8.54 |
| CHEMBL4865650 | — | — | 1 | 8.47 |
| CHEMBL4852645 | — | — | 1 | 8.44 |
| CHEMBL4846263 | — | — | 1 | 8.32 |
| CHEMBL4852043 | — | — | 1 | 8.29 |
| CHEMBL2179618 | NEXTURASTAT A | — | 1 | 8.29 |
| CHEMBL4849440 | — | — | 1 | 7.91 |
| CHEMBL4873780 | — | — | 1 | 7.42 |
| CHEMBL4871991 | — | — | 1 | 7.35 |
| CHEMBL4856805 | — | — | 1 | 6.79 |
| CHEMBL4871846 | — | — | 1 | 6.48 |
| CHEMBL4856047 | — | — | 1 | 6.42 |
| CHEMBL4846892 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4536605 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4865650 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4852645 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4846263 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4852043 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2179618 | NEXTURASTAT A | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4849440 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL4873780 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL4871991 | — | IC50 | = | 45.1 | nM | 7.35 |
| CHEMBL4856805 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL4871846 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL4856047 | — | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL4846892 | — | IC50 | = | 961.0 | nM | 6.02 |