Assay Detail
Binding
CHEMBL1914070
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3K p110alpha helical domain E545K mutant after 2 hrs by HTRF assay
5
Total Activities
5
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
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.53 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1910998 | — | — | 1 | 9.92 |
| CHEMBL1911117 | — | — | 1 | 9.00 |
| CHEMBL1911002 | — | — | 1 | 8.52 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.92 |
| CHEMBL1911114 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1910998 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL1911117 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1911002 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1911114 | — | IC50 | = | 49.0 | nM | 7.31 |