Assay Detail
Binding
CHEMBL5730429
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Several TP Scaffold compounds were tested for inhibition activity against isoforms of PI3K (alpha, beta, gamma, and delta isoforms) and the bromodomain protein BRD4 at regions 1 (BRD4-1) and 2 (BRD4-2).
18
Total Activities
6
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thienopyranones as kinase and epigenetic inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.91 | 6.67 |
| kon | 6 | - | - |
| k_off | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2322228 | — | — | 3 | 6.67 |
| CHEMBL2322239 | — | — | 3 | 6.42 |
| CHEMBL98350 | LY-294002 | -1.0 | 3 | 6.13 |
| CHEMBL2326952 | — | — | 3 | 5.76 |
| CHEMBL2326953 | — | — | 3 | 5.44 |
| CHEMBL2322246 | — | — | 3 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2322228 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL2322239 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL98350 | LY-294002 | IC50 | = | 736.0 | nM | 6.13 |
| CHEMBL2326952 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL2326953 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2322246 | — | IC50 | = | 9247.0 | nM | 5.03 |
| CHEMBL98350 | LY-294002 | kon | = | - | — | - |
| CHEMBL98350 | LY-294002 | k_off | = | - | s-1 | - |
| CHEMBL2322228 | — | kon | = | - | — | - |
| CHEMBL2322228 | — | k_off | = | - | s-1 | - |
| CHEMBL2326953 | — | kon | = | - | — | - |
| CHEMBL2326953 | — | k_off | = | - | s-1 | - |
| CHEMBL2326952 | — | kon | = | - | — | - |
| CHEMBL2326952 | — | k_off | = | - | s-1 | - |
| CHEMBL2322246 | — | kon | = | - | — | - |
| CHEMBL2322246 | — | k_off | = | - | s-1 | - |
| CHEMBL2322239 | — | kon | = | - | — | - |
| CHEMBL2322239 | — | k_off | = | - | s-1 | - |