Assay Detail
Binding
CHEMBL4312246
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PI3Kalpha using PIP2 as substrate incubated for 1 hr by kinase-glo assay
37
Total Activities
37
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, Synthesis, and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.70 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445101 | — | — | 1 | 9.22 |
| CHEMBL4581165 | — | — | 1 | 9.20 |
| CHEMBL4527487 | — | — | 1 | 9.18 |
| CHEMBL4435527 | — | — | 1 | 9.16 |
| CHEMBL4465475 | — | — | 1 | 9.05 |
| CHEMBL4471718 | — | — | 1 | 8.96 |
| CHEMBL4588404 | — | — | 1 | 8.89 |
| CHEMBL4444204 | — | — | 1 | 8.74 |
| CHEMBL4456391 | — | — | 1 | 8.64 |
| CHEMBL4535819 | — | — | 1 | 8.41 |
| CHEMBL4458497 | — | — | 1 | 8.40 |
| CHEMBL4434897 | — | — | 1 | 8.29 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.70 |
| CHEMBL4465851 | — | — | 1 | 7.52 |
| CHEMBL4474627 | — | — | 1 | 7.39 |
| CHEMBL4536105 | — | — | 1 | 7.38 |
| CHEMBL4452585 | — | — | 1 | 7.37 |
| CHEMBL4459720 | — | — | 1 | 7.37 |
| CHEMBL4464542 | — | — | 1 | 7.37 |
| CHEMBL4568675 | — | — | 1 | 7.32 |
| CHEMBL4580600 | — | — | 1 | 7.29 |
| CHEMBL4437190 | — | — | 1 | 7.27 |
| CHEMBL4593985 | — | — | 1 | 7.24 |
| CHEMBL4470989 | — | — | 1 | 7.17 |
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 7.16 |
| CHEMBL4462934 | — | — | 1 | 7.14 |
| CHEMBL4474676 | — | — | 1 | 7.14 |
| CHEMBL4580727 | — | — | 1 | 7.14 |
| CHEMBL4521497 | — | — | 1 | 7.09 |
| CHEMBL4457009 | — | — | 1 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445101 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4581165 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4527487 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4435527 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL4465475 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4471718 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4588404 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4444204 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4456391 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4535819 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4458497 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4434897 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4465851 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4474627 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4536105 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4464542 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4452585 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4459720 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4568675 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4580600 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4437190 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4593985 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4470989 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL3622533 | FIMEPINOSTAT | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4580727 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4474676 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4462934 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4521497 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4457009 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4561458 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4440596 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4442688 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4448002 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL4588397 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4524198 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4462577 | — | IC50 | = | 226.0 | nM | 6.65 |