Assay Detail
Binding
CHEMBL5649049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to N-terminal His6-tagged TEV protease fused wild-type AKT1 (2 to 446 residues) (unknown origin) expressed in Sf9 cells assessed as inhibition constant
6
Total Activities
6
Compounds Tested
1
Activity Types
4
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
Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.80 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| EFO_ID | EFO_ID | - | — | MONDO:0004992 |
| EFO_ID | EFO_ID | - | — | EFO:0000400 |
| EFO_TERM | EFO_TERM | - | — | cancer |
| EFO_TERM | EFO_TERM | - | — | diabetes mellitus |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4795065 | Borussertib | — | 1 | 8.52 |
| CHEMBL5282715 | — | — | 1 | 7.23 |
| CHEMBL5267341 | — | — | 1 | 7.15 |
| CHEMBL5649156 | — | — | 1 | 6.12 |
| CHEMBL5649160 | — | — | 1 | 5.91 |
| CHEMBL5649162 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4795065 | Borussertib | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5282715 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL5267341 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL5649156 | — | Ki | = | 755.0 | nM | 6.12 |
| CHEMBL5649160 | — | Ki | = | 1243.0 | nM | 5.91 |
| CHEMBL5649162 | — | Ki | = | 1432.0 | nM | 5.84 |