Assay Detail
Binding
CHEMBL5537720
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Inhibition of human recombinant HDAC6 using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 90 mins by fluorescence based microplate reader analysis
12
Total Activities
12
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
5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.95 | 5.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5563683 | — | — | 1 | 5.69 |
| CHEMBL5571522 | — | — | 1 | 5.25 |
| CHEMBL3692688 | — | — | 1 | 5.24 |
| CHEMBL5571546 | — | — | 1 | 4.94 |
| CHEMBL5570082 | — | — | 1 | 4.77 |
| CHEMBL5575926 | — | — | 1 | 4.74 |
| CHEMBL5571764 | — | — | 1 | 4.71 |
| CHEMBL3692573 | — | — | 1 | 4.26 |
| CHEMBL5572569 | — | — | 1 | - |
| CHEMBL5571685 | — | — | 1 | - |
| CHEMBL5579748 | — | — | 1 | - |
| CHEMBL5572470 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5563683 | — | IC50 | = | 2030.0 | nM | 5.69 |
| CHEMBL5571522 | — | IC50 | = | 5610.0 | nM | 5.25 |
| CHEMBL3692688 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL5571546 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL5570082 | — | IC50 | = | 16900.0 | nM | 4.77 |
| CHEMBL5575926 | — | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL5571764 | — | IC50 | = | 19600.0 | nM | 4.71 |
| CHEMBL3692573 | — | IC50 | = | 55400.0 | nM | 4.26 |
| CHEMBL5572569 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5571685 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5579748 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5572470 | — | IC50 | > | 100000.0 | nM | - |