Assay Detail
Binding
CHEMBL4430043
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kalpha expressed in rat-1 fibroblasts assessed as reduction in Akt phosphorylation at Ser 473 after 1 hr by alphascreen assay
12
Total Activities
12
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 and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.84 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4453497 | — | — | 1 | 6.40 |
| CHEMBL4521888 | — | — | 1 | 6.16 |
| CHEMBL4588314 | — | — | 1 | 5.96 |
| CHEMBL4437791 | — | — | 1 | 5.94 |
| CHEMBL3944013 | — | — | 1 | 5.88 |
| CHEMBL4467868 | — | — | 1 | 5.81 |
| CHEMBL4581278 | — | — | 1 | 5.81 |
| CHEMBL4454454 | — | — | 1 | 5.74 |
| CHEMBL4469006 | — | — | 1 | 5.68 |
| CHEMBL3947814 | — | — | 1 | 5.67 |
| CHEMBL4460621 | — | — | 1 | 5.60 |
| CHEMBL3977066 | — | — | 1 | 5.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4453497 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4521888 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4588314 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4437791 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL3944013 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4467868 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL4581278 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL4454454 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL4469006 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3947814 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL4460621 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL3977066 | — | IC50 | = | 3440.0 | nM | 5.46 |