Assay Detail
Binding
CHEMBL5538337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-FLAG-tagged human recombinant HDAC2 (1 to 488 residues) expressed in Sf9 cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by plate reader analysis
2
Total Activities
2
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
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.91 | 7.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5592140 | — | — | 1 | 7.07 |
| CHEMBL5569425 | — | — | 1 | 6.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5592140 | — | IC50 | = | 84.5 | nM | 7.07 |
| CHEMBL5569425 | — | IC50 | = | 181.0 | nM | 6.74 |