Assay Detail
Binding
CHEMBL5649045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged TEV protease fused wild-type AKT2 (2 to 447 residues) (unknown origin) expressed in Sf9 cells by HTRF KinEASE assay
15
Total Activities
15
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-beta serine/threonine-protein kinase (CHEMBL2431) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.23 | 8.30 |
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 |
|---|---|---|---|---|
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 8.30 |
| CHEMBL4795065 | Borussertib | — | 1 | 7.25 |
| CHEMBL5649162 | — | — | 1 | 6.92 |
| CHEMBL1079175 | MK-2206 | 2.0 | 1 | 6.80 |
| CHEMBL5649163 | — | — | 1 | 5.91 |
| CHEMBL5267341 | — | — | 1 | 5.80 |
| CHEMBL5649156 | — | — | 1 | 5.30 |
| CHEMBL5649157 | — | — | 1 | 4.94 |
| CHEMBL5282715 | — | — | 1 | 4.88 |
| CHEMBL5649159 | — | — | 1 | - |
| CHEMBL5649161 | — | — | 1 | - |
| CHEMBL5649160 | — | — | 1 | - |
| CHEMBL5649164 | — | — | 1 | - |
| CHEMBL5649154 | — | — | 1 | - |
| CHEMBL5649155 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2325741 | CAPIVASERTIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4795065 | Borussertib | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5649162 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL1079175 | MK-2206 | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL5649163 | — | IC50 | = | 1237.0 | nM | 5.91 |
| CHEMBL5267341 | — | IC50 | = | 1569.0 | nM | 5.80 |
| CHEMBL5649156 | — | IC50 | = | 5033.0 | nM | 5.30 |
| CHEMBL5649157 | — | IC50 | = | 11541.0 | nM | 4.94 |
| CHEMBL5282715 | — | IC50 | = | 13030.0 | nM | 4.88 |
| CHEMBL5649159 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5649161 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5649160 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5649164 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5649154 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5649155 | — | IC50 | > | 20000.0 | nM | - |