Assay Detail
Binding
CHEMBL2175141
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Inhibition of human recombinant HDAC8 using fluor de Lys as substrate preincubated for 5 mins followed by substrate addition measured after 25 mins by microplate reader analysis
16
Total Activities
16
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
Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.34 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2170177 | — | — | 1 | 8.00 |
| CHEMBL1914708 | — | — | 1 | 7.77 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 6.41 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.36 |
| CHEMBL1914702 | — | — | 1 | 6.19 |
| CHEMBL585164 | — | — | 1 | 5.13 |
| CHEMBL2170174 | — | — | 1 | 4.55 |
| CHEMBL2170175 | — | — | 1 | 4.44 |
| CHEMBL2170167 | — | — | 1 | 4.43 |
| CHEMBL2170168 | — | — | 1 | 4.37 |
| CHEMBL2170176 | — | — | 1 | 4.33 |
| CHEMBL2170171 | — | — | 1 | 4.32 |
| CHEMBL2170172 | — | — | 1 | 4.27 |
| CHEMBL2170173 | — | — | 1 | 4.17 |
| CHEMBL2170170 | — | — | 1 | - |
| CHEMBL2170169 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2170177 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1914708 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1914702 | — | IC50 | = | 651.0 | nM | 6.19 |
| CHEMBL585164 | — | IC50 | = | 7340.0 | nM | 5.13 |
| CHEMBL2170174 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL2170175 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL2170167 | — | IC50 | = | 37400.0 | nM | 4.43 |
| CHEMBL2170168 | — | IC50 | = | 42600.0 | nM | 4.37 |
| CHEMBL2170176 | — | IC50 | = | 47100.0 | nM | 4.33 |
| CHEMBL2170171 | — | IC50 | = | 47800.0 | nM | 4.32 |
| CHEMBL2170172 | — | IC50 | = | 53200.0 | nM | 4.27 |
| CHEMBL2170173 | — | IC50 | = | 67500.0 | nM | 4.17 |
| CHEMBL2170170 | — | IC50 | - | — | - | |
| CHEMBL2170169 | — | IC50 | - | — | - |