Assay Detail
ADMET
CHEMBL4134212
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human myristoylated PI3Kalpha catalytic domain expressed in Rat1 cells assessed as reduction in Akt phosphorylation at Ser47 residue after 1 hr by alpha screen Surefire assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Rat1 |
| 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 CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.42 | 5.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3643413 | LENIOLISIB | 4.0 | 1 | 5.78 |
| CHEMBL3947814 | — | — | 1 | 5.67 |
| CHEMBL3643414 | — | — | 1 | 5.67 |
| CHEMBL3643409 | — | — | 1 | 5.58 |
| CHEMBL3977066 | — | — | 1 | 5.46 |
| CHEMBL3643407 | — | — | 1 | 5.45 |
| CHEMBL3643429 | — | — | 1 | 5.21 |
| CHEMBL3643349 | — | — | 1 | 5.19 |
| CHEMBL3643427 | — | — | 1 | 5.13 |
| CHEMBL4163245 | — | — | 1 | 5.04 |
| CHEMBL4164149 | — | — | 1 | - |
| CHEMBL4171158 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3643413 | LENIOLISIB | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL3947814 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL3643414 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL3643409 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3977066 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL3643407 | — | IC50 | = | 3550.0 | nM | 5.45 |
| CHEMBL3643429 | — | IC50 | = | 6190.0 | nM | 5.21 |
| CHEMBL3643349 | — | IC50 | = | 6490.0 | nM | 5.19 |
| CHEMBL3643427 | — | IC50 | = | 7410.0 | nM | 5.13 |
| CHEMBL4163245 | — | IC50 | = | 9030.0 | nM | 5.04 |
| CHEMBL4164149 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4171158 | — | IC50 | > | 10000.0 | nM | - |