Assay Detail
Binding
CHEMBL3868300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of myristoylated PI3K-delta (unknown origin) overexpressed in Rat1 cells assessed as inhibition of Akt phosphorylation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Rat1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗| 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 | 7.00 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3947814 | — | — | 1 | 7.55 |
| CHEMBL3896413 | — | — | 1 | 7.55 |
| CHEMBL3944013 | — | — | 1 | 7.41 |
| CHEMBL3930000 | — | — | 1 | 7.36 |
| CHEMBL3977066 | — | — | 1 | 7.31 |
| CHEMBL3966263 | — | — | 1 | 7.14 |
| CHEMBL3960012 | — | — | 1 | 7.10 |
| CHEMBL3969716 | — | — | 1 | 7.09 |
| CHEMBL3905342 | — | — | 1 | 6.79 |
| CHEMBL3977135 | — | — | 1 | 6.19 |
| CHEMBL3933360 | — | — | 1 | 5.55 |
| CHEMBL3939028 | — | — | 1 | - |
| CHEMBL3910692 | — | — | 1 | - |
| CHEMBL3921081 | — | — | 1 | - |
| CHEMBL3948901 | — | — | 1 | - |
| CHEMBL3914282 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3947814 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3896413 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3944013 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3930000 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3977066 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3966263 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3960012 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3969716 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3905342 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL3977135 | — | IC50 | = | 646.0 | nM | 6.19 |
| CHEMBL3933360 | — | IC50 | = | 2840.0 | nM | 5.55 |
| CHEMBL3939028 | — | IC50 | - | — | - | |
| CHEMBL3910692 | — | IC50 | - | — | - | |
| CHEMBL3921081 | — | IC50 | - | — | - | |
| CHEMBL3948901 | — | IC50 | - | — | - | |
| CHEMBL3914282 | — | IC50 | - | — | - |