Assay Detail
Binding
CHEMBL4723564
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Inhibition of mTOR2 in human A2058 cells assessed as reduction in PKB/Akt phosphorylation at Ser473 incubated for 1 hr by Western blot analysis
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2058 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
4-(Difluoromethyl)-5-(4-((3R,5S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.42 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4749352 | — | — | 1 | 7.02 |
| CHEMBL4287799 | — | — | 1 | 6.83 |
| CHEMBL4758329 | — | — | 1 | 6.76 |
| CHEMBL4741511 | — | — | 1 | 6.72 |
| CHEMBL4777159 | — | — | 1 | 6.70 |
| CHEMBL4749250 | — | — | 1 | 6.64 |
| CHEMBL4757223 | — | — | 1 | 6.61 |
| CHEMBL4792469 | — | — | 1 | 6.57 |
| CHEMBL4290128 | — | — | 1 | 6.36 |
| CHEMBL4779306 | — | — | 1 | 6.30 |
| CHEMBL4746047 | — | — | 1 | 6.28 |
| CHEMBL4764200 | — | — | 1 | 6.02 |
| CHEMBL4753323 | — | — | 1 | 5.87 |
| CHEMBL4783277 | — | — | 1 | 5.83 |
| CHEMBL4752162 | — | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4749352 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4287799 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL4758329 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL4741511 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4777159 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4749250 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4757223 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4792469 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL4290128 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL4779306 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL4746047 | — | IC50 | = | 524.0 | nM | 6.28 |
| CHEMBL4764200 | — | IC50 | = | 956.0 | nM | 6.02 |
| CHEMBL4753323 | — | IC50 | = | 1338.0 | nM | 5.87 |
| CHEMBL4783277 | — | IC50 | = | 1483.0 | nM | 5.83 |
| CHEMBL4752162 | — | IC50 | = | 1561.0 | nM | 5.81 |