Assay Detail
Functional
CHEMBL4733832
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Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI-H226 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Identification of methyl (5-(6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinopyrrolo[2,1-f][1,2,4]triazin-2-yl)-4-(trifluoromethyl)pyridin-2-yl)carbamate (CYH33) as an orally bioavailable, highly potent, PI3K alpha inhibitor for the treatment of advanced solid tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.06 | 6.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4756324 | — | — | 1 | 6.97 |
| CHEMBL4756074 | — | — | 1 | 5.97 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4756324 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4756074 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL521851 | PICTILISIB | IC50 | = | 5910.0 | nM | 5.23 |