Assay Detail
Binding
CHEMBL4119810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length His-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system coexpressing PIK3R1 by TR-FRET assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.49 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 8.30 |
| CHEMBL4125884 | — | — | 1 | 8.09 |
| CHEMBL4127267 | — | — | 1 | 7.94 |
| CHEMBL4127114 | — | — | 1 | 7.16 |
| CHEMBL3400288 | — | — | 1 | 6.75 |
| CHEMBL3819302 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL586702 | ZSTK-474 | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4125884 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4127267 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL4127114 | — | IC50 | = | 69.2 | nM | 7.16 |
| CHEMBL3400288 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3819302 | — | IC50 | = | 191.0 | nM | 6.72 |