Assay Detail
Binding
CHEMBL1937672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha by luminescent kinase assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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
Discovery and bioactivity of 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl) morpholine derivatives as novel PI3K inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.93 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573339 | PI-103 | — | 1 | 7.78 |
| CHEMBL1934300 | — | — | 1 | 7.47 |
| CHEMBL1934305 | — | — | 1 | 7.32 |
| CHEMBL1934301 | — | — | 1 | 7.30 |
| CHEMBL1934304 | — | — | 1 | 7.22 |
| CHEMBL1934307 | — | — | 1 | 6.38 |
| CHEMBL1934306 | — | — | 1 | 6.37 |
| CHEMBL1934303 | — | — | 1 | 6.29 |
| CHEMBL1934302 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573339 | PI-103 | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL1934300 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL1934305 | — | IC50 | = | 47.8 | nM | 7.32 |
| CHEMBL1934301 | — | IC50 | = | 49.7 | nM | 7.30 |
| CHEMBL1934304 | — | IC50 | = | 60.7 | nM | 7.22 |
| CHEMBL1934307 | — | IC50 | = | 421.3 | nM | 6.38 |
| CHEMBL1934306 | — | IC50 | = | 424.7 | nM | 6.37 |
| CHEMBL1934303 | — | IC50 | = | 510.5 | nM | 6.29 |
| CHEMBL1934302 | — | IC50 | = | 544.0 | nM | 6.26 |