Assay Detail
Functional
CHEMBL967870
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.61 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL493290 | — | — | 1 | 7.16 |
| CHEMBL493289 | — | — | 1 | 6.96 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.85 |
| CHEMBL523379 | — | — | 1 | 6.80 |
| CHEMBL522031 | — | — | 1 | 6.72 |
| CHEMBL510164 | — | — | 1 | 6.57 |
| CHEMBL493083 | — | — | 1 | 6.55 |
| CHEMBL494921 | — | — | 1 | 6.00 |
| CHEMBL493090 | — | — | 1 | 5.85 |
| CHEMBL493296 | — | — | 1 | - |
| CHEMBL493084 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL493290 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL493289 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL523379 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL522031 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL510164 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL493083 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL494921 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL493090 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL493296 | — | IC50 | - | — | - | |
| CHEMBL493084 | — | IC50 | - | — | - |