Assay Detail
Binding
CHEMBL3591913
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged bovine p110alpha expressed in Sf9/Baculovirus system using [gamma-33P]ATP by scintillation proximity assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL2498) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Kα inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.78 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3589372 | — | — | 1 | 10.00 |
| CHEMBL3589370 | — | — | 1 | 9.52 |
| CHEMBL3589371 | — | — | 1 | 9.30 |
| CHEMBL3589324 | — | — | 1 | 9.10 |
| CHEMBL3589377 | — | — | 1 | 8.92 |
| CHEMBL3589379 | — | — | 1 | 8.72 |
| CHEMBL3589376 | — | — | 1 | 8.42 |
| CHEMBL3589378 | — | — | 1 | 8.42 |
| CHEMBL3589375 | — | — | 1 | 8.11 |
| CHEMBL3589320 | — | — | 1 | 6.63 |
| CHEMBL3589321 | — | — | 1 | 6.41 |
| CHEMBL3589323 | — | — | 1 | 6.17 |
| CHEMBL3589322 | — | — | 1 | 6.16 |
| CHEMBL3589373 | — | — | 1 | 5.63 |
| CHEMBL3589374 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3589372 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3589370 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3589371 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3589324 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3589377 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3589379 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3589376 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3589378 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3589375 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3589320 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL3589321 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL3589323 | — | IC50 | = | 678.0 | nM | 6.17 |
| CHEMBL3589322 | — | IC50 | = | 695.0 | nM | 6.16 |
| CHEMBL3589373 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL3589374 | — | IC50 | = | 5490.0 | nM | 5.26 |