Assay Detail
Binding
CHEMBL4733839
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kgamma R459Q mutant using PIP2 as substrate in presence of ATP measured after 40 mins by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 2 | 6.22 | 6.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | 2.0 | 1 | 6.65 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 5.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | IC50 | = | 224.8 | nM | 6.65 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 1673.0 | nM | 5.78 |