Assay Detail
Binding
CHEMBL4831258
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human AKT1 expressed in baculovirus expression system using TC-AHA-GRPRTSSFAEG-NH2 as substrate incubated for 90 mins by mobility shift assay
18
Total Activities
18
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
Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.67 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871106 | RUPITASERTIB | 2.0 | 1 | 8.40 |
| CHEMBL4860970 | — | — | 1 | 8.40 |
| CHEMBL3685329 | — | — | 1 | 8.40 |
| CHEMBL4876446 | — | — | 1 | 8.22 |
| CHEMBL4846712 | — | — | 1 | 8.22 |
| CHEMBL4856439 | — | — | 1 | 8.00 |
| CHEMBL4855657 | — | — | 1 | 7.85 |
| CHEMBL3675415 | — | — | 1 | 7.82 |
| CHEMBL4871853 | — | — | 1 | 7.77 |
| CHEMBL4851020 | — | — | 1 | 7.66 |
| CHEMBL4875416 | — | — | 1 | 7.64 |
| CHEMBL4854144 | — | — | 1 | 7.36 |
| CHEMBL4869229 | — | — | 1 | 6.67 |
| CHEMBL4853030 | — | — | 1 | 6.40 |
| CHEMBL4857965 | — | — | 1 | 6.25 |
| CHEMBL4853114 | — | — | 1 | - |
| CHEMBL3675367 | — | — | 1 | - |
| CHEMBL3675353 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871106 | RUPITASERTIB | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4860970 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3685329 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4876446 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4846712 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4856439 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4855657 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3675415 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4871853 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4851020 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4875416 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4854144 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4869229 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4853030 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4857965 | — | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL4853114 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3675367 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3675353 | — | IC50 | > | 10000.0 | nM | - |