Assay Detail
Binding
CHEMBL2379606
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Inhibition of mTOR (unknown origin)
23
Total Activities
23
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
Serine/threonine-protein kinase mTOR (CHEMBL2842) ↗| 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 |
|---|---|---|---|
| Ki | 23 | 7.91 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2375967 | — | — | 1 | 8.67 |
| CHEMBL2375964 | — | — | 1 | 8.60 |
| CHEMBL2376093 | — | — | 1 | 8.35 |
| CHEMBL2375962 | — | — | 1 | 8.35 |
| CHEMBL2375365 | — | — | 1 | 8.30 |
| CHEMBL2376092 | — | — | 1 | 8.12 |
| CHEMBL2375965 | — | — | 1 | 8.11 |
| CHEMBL2376096 | — | — | 1 | 8.06 |
| CHEMBL2375956 | — | — | 1 | 8.06 |
| CHEMBL2375953 | — | — | 1 | 8.04 |
| CHEMBL2375969 | — | — | 1 | 7.97 |
| CHEMBL2375957 | — | — | 1 | 7.96 |
| CHEMBL2375961 | — | — | 1 | 7.90 |
| CHEMBL2376095 | — | — | 1 | 7.89 |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | 7.80 |
| CHEMBL2375966 | — | — | 1 | 7.71 |
| CHEMBL2375968 | — | — | 1 | 7.61 |
| CHEMBL2375958 | — | — | 1 | 7.53 |
| CHEMBL2375963 | — | — | 1 | 7.34 |
| CHEMBL2375970 | — | — | 1 | 7.34 |
| CHEMBL2375959 | — | — | 1 | 7.32 |
| CHEMBL2375960 | — | — | 1 | 7.03 |
| CHEMBL2376094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2375967 | — | Ki | = | 2.15 | nM | 8.67 |
| CHEMBL2375964 | — | Ki | = | 2.54 | nM | 8.60 |
| CHEMBL2376093 | — | Ki | = | 4.46 | nM | 8.35 |
| CHEMBL2375962 | — | Ki | = | 4.52 | nM | 8.35 |
| CHEMBL2375365 | — | Ki | = | 5.05 | nM | 8.30 |
| CHEMBL2376092 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL2375965 | — | Ki | = | 7.82 | nM | 8.11 |
| CHEMBL2376096 | — | Ki | = | 8.63 | nM | 8.06 |
| CHEMBL2375956 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL2375953 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2375969 | — | Ki | = | 10.7 | nM | 7.97 |
| CHEMBL2375957 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL2375961 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL2376095 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL1234354 | PF-04691502 | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2375966 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL2375968 | — | Ki | = | 24.4 | nM | 7.61 |
| CHEMBL2375958 | — | Ki | = | 29.5 | nM | 7.53 |
| CHEMBL2375963 | — | Ki | = | 45.4 | nM | 7.34 |
| CHEMBL2375970 | — | Ki | = | 45.9 | nM | 7.34 |
| CHEMBL2375959 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL2375960 | — | Ki | = | 92.6 | nM | 7.03 |
| CHEMBL2376094 | — | Ki | - | — | - |