Assay Detail
Binding
CHEMBL2379605
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of AKT phosphorylation at Ser 473 in human BT20 cells
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | BT-20 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
RAC-alpha serine/threonine-protein kinase (CHEMBL4282) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.25 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2375968 | — | — | 1 | 8.28 |
| CHEMBL2375957 | — | — | 1 | 8.23 |
| CHEMBL2375963 | — | — | 1 | 8.09 |
| CHEMBL2376092 | — | — | 1 | 7.95 |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | 7.89 |
| CHEMBL2375958 | — | — | 1 | 7.71 |
| CHEMBL2376095 | — | — | 1 | 7.67 |
| CHEMBL2375365 | — | — | 1 | 7.66 |
| CHEMBL2375964 | — | — | 1 | 7.63 |
| CHEMBL2375965 | — | — | 1 | 7.62 |
| CHEMBL2375967 | — | — | 1 | 7.59 |
| CHEMBL2376093 | — | — | 1 | 7.53 |
| CHEMBL2375956 | — | — | 1 | 7.29 |
| CHEMBL2375953 | — | — | 1 | 7.25 |
| CHEMBL2375961 | — | — | 1 | 7.08 |
| CHEMBL2375969 | — | — | 1 | 6.98 |
| CHEMBL2375959 | — | — | 1 | 6.94 |
| CHEMBL2375962 | — | — | 1 | 6.83 |
| CHEMBL2375955 | — | — | 1 | 6.59 |
| CHEMBL2375966 | — | — | 1 | 6.54 |
| CHEMBL2375970 | — | — | 1 | 6.51 |
| CHEMBL2375954 | — | — | 1 | 6.42 |
| CHEMBL2375960 | — | — | 1 | 6.00 |
| CHEMBL2376096 | — | — | 1 | 5.68 |
| CHEMBL2376094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2375968 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL2375957 | — | IC50 | = | 5.82 | nM | 8.23 |
| CHEMBL2375963 | — | IC50 | = | 8.22 | nM | 8.09 |
| CHEMBL2376092 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL1234354 | PF-04691502 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2375958 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL2376095 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL2375365 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2375964 | — | IC50 | = | 23.3 | nM | 7.63 |
| CHEMBL2375965 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL2375967 | — | IC50 | = | 25.9 | nM | 7.59 |
| CHEMBL2376093 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL2375956 | — | IC50 | = | 51.9 | nM | 7.29 |
| CHEMBL2375953 | — | IC50 | = | 56.8 | nM | 7.25 |
| CHEMBL2375961 | — | IC50 | = | 82.9 | nM | 7.08 |
| CHEMBL2375969 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL2375959 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL2375962 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL2375955 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL2375966 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL2375970 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2375954 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL2375960 | — | IC50 | = | 988.0 | nM | 6.00 |
| CHEMBL2376096 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL2376094 | — | IC50 | - | — | - |