Assay Detail
Binding
CHEMBL5538330
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by ADP-Glo assay
38
Total Activities
38
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 |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 38 | 7.78 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5569757 | — | — | 1 | 9.70 |
| CHEMBL5569920 | — | — | 1 | 9.68 |
| CHEMBL5569425 | — | — | 1 | 9.64 |
| CHEMBL5569507 | — | — | 1 | 9.64 |
| CHEMBL5590999 | — | — | 1 | 9.60 |
| CHEMBL5592140 | — | — | 1 | 9.59 |
| CHEMBL5574871 | — | — | 1 | 9.55 |
| CHEMBL5569221 | — | — | 1 | 9.41 |
| CHEMBL5573240 | — | — | 1 | 9.41 |
| CHEMBL5568791 | — | — | 1 | 9.40 |
| CHEMBL5571753 | — | — | 1 | 9.34 |
| CHEMBL5570737 | — | — | 1 | 9.24 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.21 |
| CHEMBL5591487 | — | — | 1 | 7.55 |
| CHEMBL5569303 | — | — | 1 | 7.50 |
| CHEMBL4536105 | — | — | 1 | 7.38 |
| CHEMBL5572117 | — | — | 1 | 7.32 |
| CHEMBL5574499 | — | — | 1 | 7.28 |
| CHEMBL5569630 | — | — | 1 | 7.25 |
| CHEMBL5595751 | — | — | 1 | 7.24 |
| CHEMBL5571617 | — | — | 1 | 7.17 |
| CHEMBL5564987 | — | — | 1 | 7.14 |
| CHEMBL5575122 | — | — | 1 | 7.12 |
| CHEMBL5562535 | — | — | 1 | 7.04 |
| CHEMBL5570427 | — | — | 1 | 6.97 |
| CHEMBL5572268 | — | — | 1 | 6.94 |
| CHEMBL5570265 | — | — | 1 | 6.90 |
| CHEMBL5570626 | — | — | 1 | 6.84 |
| CHEMBL5571499 | — | — | 1 | 6.83 |
| CHEMBL5572480 | — | — | 1 | 6.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5569757 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5569920 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL5569507 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5569425 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5590999 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL5592140 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5574871 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5569221 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5573240 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL5568791 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5571753 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL5570737 | — | IC50 | = | 0.58 | nM | 9.24 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5591487 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5569303 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4536105 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5572117 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL5574499 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5569630 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5595751 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5571617 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5564987 | — | IC50 | = | 72.5 | nM | 7.14 |
| CHEMBL5575122 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL5562535 | — | IC50 | = | 90.5 | nM | 7.04 |
| CHEMBL5570427 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL5572268 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5570265 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5570626 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL5571499 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5572480 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5589731 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL5574185 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL5563440 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL5572633 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL5571672 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL5572364 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL5583643 | — | IC50 | = | 603.0 | nM | 6.22 |
| CHEMBL5563957 | — | IC50 | = | 705.0 | nM | 6.15 |