Assay Detail
Binding
CHEMBL3774221
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant PI3K alpha (unknown origin) using PIP2 as substrate by fluorescence polarization assay
19
Total Activities
19
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 9.16 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3770993 | — | — | 1 | 10.52 |
| CHEMBL3770306 | — | — | 1 | 10.00 |
| CHEMBL3770709 | — | — | 1 | 10.00 |
| CHEMBL3771364 | — | — | 1 | 9.70 |
| CHEMBL3770325 | — | — | 1 | 9.70 |
| CHEMBL3770140 | — | — | 1 | 9.52 |
| CHEMBL2387080 | TASELISIB | 3.0 | 1 | 9.52 |
| CHEMBL3770717 | — | — | 1 | 9.52 |
| CHEMBL3769854 | — | — | 1 | 9.30 |
| CHEMBL3769966 | — | — | 1 | 9.05 |
| CHEMBL3770824 | — | — | 1 | 9.00 |
| CHEMBL3770332 | — | — | 1 | 9.00 |
| CHEMBL3770630 | — | — | 1 | 8.92 |
| CHEMBL3770092 | — | — | 1 | 8.89 |
| CHEMBL3769972 | — | — | 1 | 8.51 |
| CHEMBL3769603 | — | — | 1 | 8.49 |
| CHEMBL3770644 | — | — | 1 | 8.44 |
| CHEMBL3770615 | — | — | 1 | 8.44 |
| CHEMBL3769857 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3770993 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3770306 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3770709 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3771364 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3770325 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3770140 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2387080 | TASELISIB | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3770717 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3769854 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3769966 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3770824 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3770332 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3770630 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3770092 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3769972 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3769603 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL3770644 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3770615 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL3769857 | — | Ki | = | 30.0 | nM | 7.52 |