Assay Detail
Binding
CHEMBL4192490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKT1 (unknown origin) using biotinylated-STK as substrate after 45 mins by HTRF assay
16
Total Activities
16
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
Structural optimization elaborates novel potent Akt inhibitors with promising anticancer activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.16 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4207231 | — | — | 1 | 8.82 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 8.77 |
| CHEMBL4202879 | — | — | 1 | 8.74 |
| CHEMBL4204854 | — | — | 1 | 8.72 |
| CHEMBL4213657 | — | — | 1 | 8.54 |
| CHEMBL4207643 | — | — | 1 | 8.37 |
| CHEMBL4217723 | — | — | 1 | 8.25 |
| CHEMBL4212000 | — | — | 1 | 8.12 |
| CHEMBL4216977 | — | — | 1 | 7.85 |
| CHEMBL4214539 | — | — | 1 | 7.75 |
| CHEMBL4217841 | — | — | 1 | 7.69 |
| CHEMBL4212569 | — | — | 1 | 7.58 |
| CHEMBL4211584 | — | — | 1 | 7.57 |
| CHEMBL4217489 | — | — | 1 | 7.45 |
| CHEMBL4208194 | — | — | 1 | - |
| CHEMBL4206698 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4207231 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL494089 | GSK-690693 | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4202879 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4204854 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4213657 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4207643 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4217723 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4212000 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4216977 | — | IC50 | = | 14.1 | nM | 7.85 |
| CHEMBL4214539 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4217841 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL4212569 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL4211584 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL4217489 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL4208194 | — | IC50 | > | 40.0 | nM | - |
| CHEMBL4206698 | — | IC50 | > | 40.0 | nM | - |