Assay Detail
Binding
CHEMBL4376727
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Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay
12
Total Activities
12
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
Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.62 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 8.18 |
| CHEMBL4563224 | — | — | 1 | 6.88 |
| CHEMBL4452620 | — | — | 1 | 6.73 |
| CHEMBL4565392 | — | — | 1 | 6.67 |
| CHEMBL4437895 | — | — | 1 | 6.67 |
| CHEMBL4565296 | — | — | 1 | 6.56 |
| CHEMBL4560533 | — | — | 1 | 6.43 |
| CHEMBL4559559 | — | — | 1 | 6.43 |
| CHEMBL4576056 | — | — | 1 | 6.31 |
| CHEMBL4472310 | — | — | 1 | 6.30 |
| CHEMBL4520400 | — | — | 1 | 6.18 |
| CHEMBL4464527 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | IC50 | = | 6.57 | nM | 8.18 |
| CHEMBL4563224 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4452620 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4565392 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4437895 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4565296 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL4560533 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4559559 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL4576056 | — | IC50 | = | 492.0 | nM | 6.31 |
| CHEMBL4472310 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL4520400 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL4464527 | — | IC50 | = | 708.0 | nM | 6.15 |