Assay Detail
Binding
CHEMBL4723565
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Inhibition of mTORC1 in human A2058 cells assessed as reduction in RPS6 phosphorylation at S235/236 residue incubated for 1 hrs 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 | 6.66 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741511 | — | — | 1 | 7.21 |
| CHEMBL4749352 | — | — | 1 | 7.15 |
| CHEMBL4777159 | — | — | 1 | 6.87 |
| CHEMBL4758329 | — | — | 1 | 6.86 |
| CHEMBL4287799 | — | — | 1 | 6.86 |
| CHEMBL4792469 | — | — | 1 | 6.72 |
| CHEMBL4757223 | — | — | 1 | 6.62 |
| CHEMBL4749250 | — | — | 1 | 6.62 |
| CHEMBL4290128 | — | — | 1 | 6.58 |
| CHEMBL4779306 | — | — | 1 | 6.41 |
| CHEMBL4752162 | — | — | 1 | 6.39 |
| CHEMBL4764200 | — | — | 1 | 6.37 |
| CHEMBL4746047 | — | — | 1 | 6.33 |
| CHEMBL4753323 | — | — | 1 | 6.25 |
| CHEMBL4783277 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741511 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4749352 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4777159 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4758329 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4287799 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4792469 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4757223 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4749250 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL4290128 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL4779306 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL4752162 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4764200 | — | IC50 | = | 426.0 | nM | 6.37 |
| CHEMBL4746047 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL4753323 | — | IC50 | = | 561.0 | nM | 6.25 |
| CHEMBL4783277 | — | IC50 | > | 1000.0 | nM | - |