Assay Detail
Binding
CHEMBL5711926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Covalent-allosteric inhibition of full length N-terminal his6-tagged AKT (2 to 446 residues) (unknown origin) expressed in Spodoptera frugiperda Sf9 cells by HTRF analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
2
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 and chemical insights into the covalent-allosteric inhibition of the protein kinase Akt.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.00 | 9.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0007254 |
| EFO_TERM | EFO_TERM | - | — | breast cancer |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4795065 | Borussertib | — | 1 | 9.10 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 9.05 |
| CHEMBL5712063 | — | — | 1 | 8.92 |
| CHEMBL5712048 | — | — | 1 | 8.52 |
| CHEMBL2177390 | IPATASERTIB | 3.0 | 1 | 8.46 |
| CHEMBL5712042 | — | — | 1 | 8.44 |
| CHEMBL5712046 | — | — | 1 | 8.43 |
| CHEMBL5712049 | — | — | 1 | 8.04 |
| CHEMBL1079175 | MK-2206 | 2.0 | 1 | 8.00 |
| CHEMBL5712045 | — | — | 1 | 7.97 |
| CHEMBL5712066 | — | — | 1 | 7.85 |
| CHEMBL5712061 | — | — | 1 | 7.74 |
| CHEMBL5712044 | — | — | 1 | 7.28 |
| CHEMBL5712058 | — | — | 1 | 6.90 |
| CHEMBL5712059 | — | — | 1 | 6.72 |
| CHEMBL5712055 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4795065 | Borussertib | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2325741 | CAPIVASERTIB | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5712063 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5712048 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2177390 | IPATASERTIB | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5712042 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5712046 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5712049 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL1079175 | MK-2206 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5712045 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5712066 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5712061 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL5712044 | — | IC50 | = | 52.8 | nM | 7.28 |
| CHEMBL5712058 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5712059 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5712055 | — | IC50 | = | 285.0 | nM | 6.54 |