Assay Detail
Binding
CHEMBL4233143
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr by Kinase-Glo luminescent assay
15
Total Activities
15
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
Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.98 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 7.52 |
| CHEMBL4238656 | — | — | 1 | 6.40 |
| CHEMBL4239712 | — | — | 1 | 5.89 |
| CHEMBL4239569 | — | — | 1 | 5.58 |
| CHEMBL4250280 | — | — | 1 | 5.52 |
| CHEMBL4239931 | — | — | 1 | 5.50 |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | 5.44 |
| CHEMBL4244147 | — | — | 1 | - |
| CHEMBL4246923 | — | — | 1 | - |
| CHEMBL4242668 | — | — | 1 | - |
| CHEMBL4248529 | — | — | 1 | - |
| CHEMBL4246481 | — | — | 1 | - |
| CHEMBL4240170 | — | — | 1 | - |
| CHEMBL4246121 | — | — | 1 | - |
| CHEMBL4251185 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4238656 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4239712 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4239569 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4250280 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4239931 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL1801204 | AZD-8055 | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4244147 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4246923 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4242668 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4248529 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4246481 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4240170 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4246121 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4251185 | — | IC50 | > | 10000.0 | nM | - |