Assay Detail
Binding
CHEMBL4121779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKT1 in human U87MG cells assessed as reduction in GSK3beta Ser9 phosphorylation incubated for 1 hr by alpha screen Surefire assay
4
Total Activities
4
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
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of chiral dihydropyridopyrimidinones as potent, selective and orally bioavailable inhibitors of AKT.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.68 | 7.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4128457 | — | — | 1 | 7.41 |
| CHEMBL4129379 | — | — | 1 | 7.04 |
| CHEMBL4126067 | — | — | 1 | 6.64 |
| CHEMBL4129817 | — | — | 1 | 5.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4128457 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4129379 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4126067 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4129817 | — | IC50 | = | 2460.0 | nM | 5.61 |