Assay Detail
Binding
CHEMBL5609908
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Inhibition of human recombinant HDAC1 using Boc-Lys (acetyl)-AMC as flurogenic substrate preincubated for 1 hr followed by substrate addition and measured after 2 hrs 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 activity evaluation of novel HDAC3 selective inhibitors for combination with Venetoclax against acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 6.93 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5613686 | — | — | 1 | 8.39 |
| CHEMBL4597954 | — | — | 1 | 8.36 |
| CHEMBL5613071 | — | — | 1 | 7.79 |
| CHEMBL5612659 | — | — | 1 | 7.59 |
| CHEMBL5613525 | — | — | 1 | 7.52 |
| CHEMBL5613673 | — | — | 1 | 7.33 |
| CHEMBL5614136 | — | — | 1 | 7.19 |
| CHEMBL5613340 | — | — | 1 | 7.06 |
| CHEMBL3621988 | TUCIDINOSTAT | 3.0 | 1 | 7.01 |
| CHEMBL5612404 | — | — | 1 | 7.01 |
| CHEMBL5612403 | — | — | 1 | 6.97 |
| CHEMBL5612950 | — | — | 1 | 6.94 |
| CHEMBL5612263 | — | — | 1 | 6.77 |
| CHEMBL5613057 | — | — | 1 | 6.56 |
| CHEMBL5613741 | — | — | 1 | 6.55 |
| CHEMBL5614363 | — | — | 1 | 6.53 |
| CHEMBL5613070 | — | — | 1 | 6.29 |
| CHEMBL5611904 | — | — | 1 | 6.24 |
| CHEMBL5612071 | — | — | 1 | 5.93 |
| CHEMBL5613949 | — | — | 1 | 5.92 |
| CHEMBL5612582 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5613686 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4597954 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5613071 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5612659 | — | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL5613525 | — | IC50 | = | 30.4 | nM | 7.52 |
| CHEMBL5613673 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL5614136 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL5613340 | — | IC50 | = | 86.5 | nM | 7.06 |
| CHEMBL3621988 | TUCIDINOSTAT | IC50 | = | 98.7 | nM | 7.01 |
| CHEMBL5612404 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5612403 | — | IC50 | = | 107.5 | nM | 6.97 |
| CHEMBL5612950 | — | IC50 | = | 114.8 | nM | 6.94 |
| CHEMBL5612263 | — | IC50 | = | 169.1 | nM | 6.77 |
| CHEMBL5613057 | — | IC50 | = | 277.4 | nM | 6.56 |
| CHEMBL5613741 | — | IC50 | = | 279.4 | nM | 6.55 |
| CHEMBL5614363 | — | IC50 | = | 298.2 | nM | 6.53 |
| CHEMBL5613070 | — | IC50 | = | 507.2 | nM | 6.29 |
| CHEMBL5611904 | — | IC50 | = | 578.3 | nM | 6.24 |
| CHEMBL5612071 | — | IC50 | = | 1181.0 | nM | 5.93 |
| CHEMBL5613949 | — | IC50 | = | 1196.0 | nM | 5.92 |
| CHEMBL5612582 | — | IC50 | = | 2244.0 | nM | 5.65 |