Assay Detail
Binding
CHEMBL4380269
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 ADP-glo plus luminescence assay
19
Total Activities
19
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
Discovery of Novel Dual Poly(ADP-ribose)polymerase and Phosphoinositide 3-Kinase Inhibitors as a Promising Strategy for Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.81 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438741 | — | — | 1 | 8.32 |
| CHEMBL4470724 | — | — | 1 | 8.25 |
| CHEMBL4551630 | — | — | 1 | 7.52 |
| CHEMBL4593274 | — | — | 1 | 7.36 |
| CHEMBL4531016 | — | — | 1 | 7.35 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.28 |
| CHEMBL4461382 | — | — | 1 | 7.04 |
| CHEMBL4551779 | — | — | 1 | 6.88 |
| CHEMBL4541731 | — | — | 1 | 6.77 |
| CHEMBL4465869 | — | — | 1 | 6.49 |
| CHEMBL4438927 | — | — | 1 | 6.48 |
| CHEMBL4461392 | — | — | 1 | 6.46 |
| CHEMBL4571423 | — | — | 1 | 6.25 |
| CHEMBL4437593 | — | — | 1 | 6.20 |
| CHEMBL4525998 | — | — | 1 | 6.16 |
| CHEMBL4436980 | — | — | 1 | 6.15 |
| CHEMBL4446789 | — | — | 1 | 5.92 |
| CHEMBL4436366 | — | — | 1 | 5.64 |
| CHEMBL4549595 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438741 | — | IC50 | = | 4.786 | nM | 8.32 |
| CHEMBL4470724 | — | IC50 | = | 5.623 | nM | 8.25 |
| CHEMBL4551630 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4593274 | — | IC50 | = | 43.65 | nM | 7.36 |
| CHEMBL4531016 | — | IC50 | = | 44.67 | nM | 7.35 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 52.48 | nM | 7.28 |
| CHEMBL4461382 | — | IC50 | = | 91.2 | nM | 7.04 |
| CHEMBL4551779 | — | IC50 | = | 131.83 | nM | 6.88 |
| CHEMBL4541731 | — | IC50 | = | 169.82 | nM | 6.77 |
| CHEMBL4465869 | — | IC50 | = | 323.59 | nM | 6.49 |
| CHEMBL4438927 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL4461392 | — | IC50 | = | 346.74 | nM | 6.46 |
| CHEMBL4571423 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL4437593 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4525998 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4436980 | — | IC50 | = | 707.95 | nM | 6.15 |
| CHEMBL4446789 | — | IC50 | = | 1202.26 | nM | 5.92 |
| CHEMBL4436366 | — | IC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL4549595 | — | IC50 | > | 10000.0 | nM | - |