Assay Detail
Binding
CHEMBL4707178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kdelta incubated for 1 hr by ADP-Glo kinase assay
10
Total Activities
8
Compounds Tested
2
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 delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.24 | 8.20 |
| Kd | 2 | 7.01 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | 2.0 | 1 | 8.20 |
| CHEMBL573339 | PI-103 | — | 1 | 7.96 |
| CHEMBL4749655 | — | — | 2 | 7.43 |
| CHEMBL4744689 | — | — | 2 | 7.20 |
| CHEMBL4787267 | — | — | 1 | 6.88 |
| CHEMBL4785064 | — | — | 1 | 6.52 |
| CHEMBL4799530 | — | — | 1 | 6.48 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622533 | FIMEPINOSTAT | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL573339 | PI-103 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4749655 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4749655 | — | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL4744689 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4787267 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4744689 | — | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL4785064 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4799530 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL521851 | PICTILISIB | IC50 | - | — | - |