Assay Detail
Binding
CHEMBL2379607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse PI3Kalpha
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL2499) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 |
|---|---|---|---|
| Ki | 25 | 8.48 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2375957 | — | — | 1 | 9.51 |
| CHEMBL2376096 | — | — | 1 | 9.46 |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | 9.24 |
| CHEMBL2375968 | — | — | 1 | 9.18 |
| CHEMBL2375963 | — | — | 1 | 9.15 |
| CHEMBL2375365 | — | — | 1 | 9.00 |
| CHEMBL2376094 | — | — | 1 | 8.93 |
| CHEMBL2375964 | — | — | 1 | 8.78 |
| CHEMBL2375956 | — | — | 1 | 8.74 |
| CHEMBL2375961 | — | — | 1 | 8.74 |
| CHEMBL2375958 | — | — | 1 | 8.72 |
| CHEMBL2376093 | — | — | 1 | 8.62 |
| CHEMBL2375967 | — | — | 1 | 8.46 |
| CHEMBL2376095 | — | — | 1 | 8.35 |
| CHEMBL2375953 | — | — | 1 | 8.24 |
| CHEMBL2375955 | — | — | 1 | 8.21 |
| CHEMBL2375962 | — | — | 1 | 8.16 |
| CHEMBL2375959 | — | — | 1 | 8.13 |
| CHEMBL2375965 | — | — | 1 | 8.10 |
| CHEMBL2375966 | — | — | 1 | 8.00 |
| CHEMBL2376092 | — | — | 1 | 7.87 |
| CHEMBL2375954 | — | — | 1 | 7.66 |
| CHEMBL2375969 | — | — | 1 | 7.62 |
| CHEMBL2375960 | — | — | 1 | 7.61 |
| CHEMBL2375970 | — | — | 1 | 7.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2375957 | — | Ki | = | 0.312 | nM | 9.51 |
| CHEMBL2376096 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL1234354 | PF-04691502 | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL2375968 | — | Ki | = | 0.654 | nM | 9.18 |
| CHEMBL2375963 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2375365 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2376094 | — | Ki | = | 1.18 | nM | 8.93 |
| CHEMBL2375964 | — | Ki | = | 1.67 | nM | 8.78 |
| CHEMBL2375956 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL2375961 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL2375958 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL2376093 | — | Ki | = | 2.41 | nM | 8.62 |
| CHEMBL2375967 | — | Ki | = | 3.44 | nM | 8.46 |
| CHEMBL2376095 | — | Ki | = | 4.51 | nM | 8.35 |
| CHEMBL2375953 | — | Ki | = | 5.74 | nM | 8.24 |
| CHEMBL2375955 | — | Ki | = | 6.16 | nM | 8.21 |
| CHEMBL2375962 | — | Ki | = | 6.89 | nM | 8.16 |
| CHEMBL2375959 | — | Ki | = | 7.41 | nM | 8.13 |
| CHEMBL2375965 | — | Ki | = | 8.01 | nM | 8.10 |
| CHEMBL2375966 | — | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL2376092 | — | Ki | = | 13.5 | nM | 7.87 |
| CHEMBL2375954 | — | Ki | = | 21.8 | nM | 7.66 |
| CHEMBL2375969 | — | Ki | = | 24.1 | nM | 7.62 |
| CHEMBL2375960 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL2375970 | — | Ki | = | 26.4 | nM | 7.58 |