Assay Detail
Binding
CHEMBL3868294
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K-alpha (unknown origin) by KinaseGlo assay
16
Total Activities
16
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 pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.33 | 6.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3969716 | — | — | 1 | 6.90 |
| CHEMBL3944013 | — | — | 1 | 6.90 |
| CHEMBL3930000 | — | — | 1 | 6.83 |
| CHEMBL3896413 | — | — | 1 | 6.66 |
| CHEMBL3905342 | — | — | 1 | 6.66 |
| CHEMBL3977066 | — | — | 1 | 6.58 |
| CHEMBL3960012 | — | — | 1 | 6.41 |
| CHEMBL3947814 | — | — | 1 | 6.38 |
| CHEMBL3977135 | — | — | 1 | 6.37 |
| CHEMBL3966263 | — | — | 1 | 6.31 |
| CHEMBL3914282 | — | — | 1 | 6.17 |
| CHEMBL3910692 | — | — | 1 | 6.16 |
| CHEMBL3948901 | — | — | 1 | 6.08 |
| CHEMBL3921081 | — | — | 1 | 6.05 |
| CHEMBL3939028 | — | — | 1 | 5.49 |
| CHEMBL3933360 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3969716 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3944013 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3930000 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL3896413 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL3905342 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3977066 | — | IC50 | = | 262.0 | nM | 6.58 |
| CHEMBL3960012 | — | IC50 | = | 386.0 | nM | 6.41 |
| CHEMBL3947814 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL3977135 | — | IC50 | = | 424.0 | nM | 6.37 |
| CHEMBL3966263 | — | IC50 | = | 491.0 | nM | 6.31 |
| CHEMBL3914282 | — | IC50 | = | 676.0 | nM | 6.17 |
| CHEMBL3910692 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL3948901 | — | IC50 | = | 842.0 | nM | 6.08 |
| CHEMBL3921081 | — | IC50 | = | 888.0 | nM | 6.05 |
| CHEMBL3939028 | — | IC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL3933360 | — | IC50 | = | 5080.0 | nM | 5.29 |