Assay Detail
Binding
CHEMBL5367104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3K alpha (unknown origin)
11
Total Activities
11
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
Discovery of (S)-N<sup>1</sup>-(thiazol-2-yl) pyrrolidine-1,2-dicarboxamide derivatives targeting PI3Ka/HDAC6 for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.70 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439214 | — | — | 1 | 8.54 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 8.30 |
| CHEMBL5422044 | — | — | 1 | 8.09 |
| CHEMBL5420057 | — | — | 1 | 7.89 |
| CHEMBL5406498 | — | — | 1 | 7.89 |
| CHEMBL5438456 | — | — | 1 | 7.82 |
| CHEMBL5418257 | — | — | 1 | 7.41 |
| CHEMBL5410758 | — | — | 1 | 7.38 |
| CHEMBL5400641 | — | — | 1 | 7.32 |
| CHEMBL5435973 | — | — | 1 | 7.25 |
| CHEMBL5410409 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439214 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5422044 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5420057 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5406498 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5438456 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5418257 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5410758 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5400641 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5435973 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5410409 | — | IC50 | = | 140.0 | nM | 6.85 |