Assay Detail
Binding
CHEMBL4019300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His6-tagged PI3K p110alpha/p85alpha expressed in baculovirus expression system after 1 hr using AlexaFluor647-labeled kinase tracer 314 by TR-FRET assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.71 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102855 | — | — | 1 | 8.09 |
| CHEMBL4081904 | — | — | 1 | 8.01 |
| CHEMBL4092165 | — | — | 1 | 7.89 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 7.77 |
| CHEMBL4097282 | — | — | 1 | 7.34 |
| CHEMBL4071150 | — | — | 1 | 7.21 |
| CHEMBL4068426 | — | — | 1 | 6.91 |
| CHEMBL4074098 | — | — | 1 | 6.16 |
| CHEMBL4079258 | — | — | 1 | 6.04 |
| CHEMBL4098203 | — | — | 1 | 5.92 |
| CHEMBL4089567 | — | — | 1 | 5.82 |
| CHEMBL4099904 | — | — | 1 | 5.64 |
| CHEMBL4100862 | — | — | 1 | 4.48 |
| CHEMBL4062723 | — | — | 1 | - |
| CHEMBL4071370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102855 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL4081904 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL4092165 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4084907 | BIMIRALISIB | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4097282 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL4071150 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4068426 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL4074098 | — | Ki | = | 689.0 | nM | 6.16 |
| CHEMBL4079258 | — | Ki | = | 911.0 | nM | 6.04 |
| CHEMBL4098203 | — | Ki | = | 1205.0 | nM | 5.92 |
| CHEMBL4089567 | — | Ki | = | 1513.0 | nM | 5.82 |
| CHEMBL4099904 | — | Ki | = | 2299.0 | nM | 5.64 |
| CHEMBL4100862 | — | Ki | = | 32833.0 | nM | 4.48 |
| CHEMBL4062723 | — | Ki | - | — | - | |
| CHEMBL4071370 | — | Ki | = | 4300000.0 | nM | - |