Assay Detail
Binding
CHEMBL4019286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PI4KCbeta (M1 to M828 residues) expressed in mammalian expression system by Kinomescan assay
6
Total Activities
6
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 |
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 |
|---|---|---|---|
| Kd | 6 | 4.44 | 4.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102855 | — | — | 1 | 4.57 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 4.40 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 4.40 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 4.40 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102855 | — | Kd | = | 27000.0 | nM | 4.57 |
| CHEMBL521851 | PICTILISIB | Kd | = | 40000.0 | nM | 4.40 |
| CHEMBL2017974 | BUPARLISIB | Kd | = | 40000.0 | nM | 4.40 |
| CHEMBL4084907 | BIMIRALISIB | Kd | = | 40000.0 | nM | 4.40 |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |