Assay Detail
Binding
CHEMBL5347349
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Inhibition of P13Kalpha (unknown origin)
10
Total Activities
10
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
Recent advances in PI3K/PKB/mTOR inhibitors as new anticancer agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 8.32 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 9.40 |
| CHEMBL5278435 | — | — | 1 | 9.34 |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | 9.30 |
| CHEMBL3813842 | PAXALISIB | 2.0 | 1 | 8.70 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.30 |
| CHEMBL1684984 | IZORLISIB | 2.0 | 1 | 7.85 |
| CHEMBL4071083 | — | — | 1 | 7.82 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.80 |
| CHEMBL3545366 | VOXTALISIB | 2.0 | 1 | 7.41 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5278435 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL3218576 | COPANLISIB | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3813842 | PAXALISIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1684984 | IZORLISIB | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4071083 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3545366 | VOXTALISIB | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 52.0 | nM | 7.28 |