Assay Detail
Binding
CHEMBL4723567
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of alexa fluor 647-labeled kinase tracer 314 binding to recombinant human N-terminal GST-tagged mTOR (1360 to 2549 residues) expressed in baculovirus expression system measured after 60 mins by TR-FRET based LanthaScreen Eu kinase binding assay
15
Total Activities
15
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
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 |
|---|---|---|---|
| Ki | 15 | 7.76 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4749352 | — | — | 1 | 8.44 |
| CHEMBL4741511 | — | — | 1 | 8.33 |
| CHEMBL4777159 | — | — | 1 | 8.19 |
| CHEMBL4287799 | — | — | 1 | 8.10 |
| CHEMBL4792469 | — | — | 1 | 7.96 |
| CHEMBL4758329 | — | — | 1 | 7.96 |
| CHEMBL4290128 | — | — | 1 | 7.85 |
| CHEMBL4749250 | — | — | 1 | 7.75 |
| CHEMBL4764200 | — | — | 1 | 7.64 |
| CHEMBL4779306 | — | — | 1 | 7.60 |
| CHEMBL4746047 | — | — | 1 | 7.55 |
| CHEMBL4753323 | — | — | 1 | 7.38 |
| CHEMBL4783277 | — | — | 1 | 7.30 |
| CHEMBL4757223 | — | — | 1 | 7.17 |
| CHEMBL4752162 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4749352 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4741511 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL4777159 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL4287799 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4792469 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4758329 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4290128 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4749250 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4764200 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4779306 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4746047 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4753323 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL4783277 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL4757223 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL4752162 | — | Ki | = | 73.0 | nM | 7.14 |