Assay Detail
Binding
CHEMBL5609910
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Inhibition of human recombinant HDAC3 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 | 7.69 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4597954 | — | — | 1 | 9.52 |
| CHEMBL5613686 | — | — | 1 | 9.30 |
| CHEMBL5613071 | — | — | 1 | 8.62 |
| CHEMBL5613673 | — | — | 1 | 8.62 |
| CHEMBL5614136 | — | — | 1 | 8.51 |
| CHEMBL5614363 | — | — | 1 | 8.38 |
| CHEMBL5612659 | — | — | 1 | 8.34 |
| CHEMBL5613525 | — | — | 1 | 8.05 |
| CHEMBL5612950 | — | — | 1 | 7.95 |
| CHEMBL5613340 | — | — | 1 | 7.69 |
| CHEMBL5611904 | — | — | 1 | 7.49 |
| CHEMBL5612403 | — | — | 1 | 7.40 |
| CHEMBL3621988 | TUCIDINOSTAT | 3.0 | 1 | 7.20 |
| CHEMBL5613070 | — | — | 1 | 7.09 |
| CHEMBL5612071 | — | — | 1 | 6.97 |
| CHEMBL5612582 | — | — | 1 | 6.91 |
| CHEMBL5613949 | — | — | 1 | 6.87 |
| CHEMBL5613741 | — | — | 1 | 6.77 |
| CHEMBL5612263 | — | — | 1 | 6.76 |
| CHEMBL5613057 | — | — | 1 | 6.57 |
| CHEMBL5612404 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4597954 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5613686 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL5613071 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5613673 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5614136 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5614363 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5612659 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5613525 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5612950 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5613340 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL5611904 | — | IC50 | = | 32.3 | nM | 7.49 |
| CHEMBL5612403 | — | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL3621988 | TUCIDINOSTAT | IC50 | = | 63.3 | nM | 7.20 |
| CHEMBL5613070 | — | IC50 | = | 80.4 | nM | 7.09 |
| CHEMBL5612071 | — | IC50 | = | 106.8 | nM | 6.97 |
| CHEMBL5612582 | — | IC50 | = | 124.3 | nM | 6.91 |
| CHEMBL5613949 | — | IC50 | = | 135.6 | nM | 6.87 |
| CHEMBL5613741 | — | IC50 | = | 169.6 | nM | 6.77 |
| CHEMBL5612263 | — | IC50 | = | 171.6 | nM | 6.76 |
| CHEMBL5613057 | — | IC50 | = | 268.2 | nM | 6.57 |
| CHEMBL5612404 | — | IC50 | = | 362.5 | nM | 6.44 |