Assay Detail
Binding
CHEMBL5519919
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Inhibition of PI3Kbeta (unknown origin) using biotin-PIP3 as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence polarization assay
4
Total Activities
4
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 beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Advancements in dual-target inhibitors of PI3K for tumor therapy: Clinical progress, development strategies, prospects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.72 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 9.22 |
| CHEMBL573339 | PI-103 | — | 1 | 8.52 |
| CHEMBL3545366 | VOXTALISIB | 2.0 | 1 | 6.96 |
| CHEMBL4084907 | BIMIRALISIB | 2.0 | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL573339 | PI-103 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3545366 | VOXTALISIB | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4084907 | BIMIRALISIB | IC50 | = | 661.0 | nM | 6.18 |