Assay Detail
Binding
CHEMBL4019282
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PI3Kdelta (R108 to Q1044 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 |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 7.79 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 8.48 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 8.48 |
| CHEMBL4102855 | — | — | 1 | 8.46 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 7.60 |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | 7.12 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL521851 | PICTILISIB | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL4102855 | — | Kd | = | 3.5 | nM | 8.46 |
| CHEMBL4084907 | BIMIRALISIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL592445 | GEDATOLISIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL2017974 | BUPARLISIB | Kd | = | 260.0 | nM | 6.58 |