Assay Detail
Binding
CHEMBL4276433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kgamma (144 to 1102 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 gamma isoform (CHEMBL3267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 5.91 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | 2.0 | 1 | 8.43 |
| CHEMBL1241674 | — | — | 1 | 7.38 |
| CHEMBL3586404 | ONATASERTIB | 2.0 | 1 | 5.15 |
| CHEMBL2336325 | VISTUSERTIB | 2.0 | 1 | 5.08 |
| CHEMBL4286698 | — | — | 1 | 4.75 |
| CHEMBL4279703 | — | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545097 | SAPANISERTIB | Kd | = | 3.7 | nM | 8.43 |
| CHEMBL1241674 | — | Kd | = | 42.0 | nM | 7.38 |
| CHEMBL3586404 | ONATASERTIB | Kd | = | 7100.0 | nM | 5.15 |
| CHEMBL2336325 | VISTUSERTIB | Kd | = | 8400.0 | nM | 5.08 |
| CHEMBL4286698 | — | Kd | = | 18000.0 | nM | 4.75 |
| CHEMBL4279703 | — | Kd | = | 22000.0 | nM | 4.66 |