Assay Detail
Functional
CHEMBL1925477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human MCF7.1 cells expressing HER2 gene after overnight incubation by CellTiter-Glo luminescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | MCF7.1 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.58 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1083192 | — | — | 1 | 6.89 |
| CHEMBL1091978 | — | — | 1 | 6.84 |
| CHEMBL1922095 | — | — | 1 | 6.79 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 6.59 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.54 |
| CHEMBL1922092 | — | — | 1 | 6.54 |
| CHEMBL1922093 | — | — | 1 | 6.54 |
| CHEMBL1921986 | — | — | 1 | 6.45 |
| CHEMBL1922091 | — | — | 1 | 6.33 |
| CHEMBL1922090 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1083192 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1091978 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL1922095 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL1922094 | APITOLISIB | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1922092 | — | IC50 | = | 289.0 | nM | 6.54 |
| CHEMBL1922093 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL1921986 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL1922091 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL1922090 | — | IC50 | = | 518.0 | nM | 6.29 |