Assay Detail
Binding
CHEMBL4733837
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3K p110alpha H1047R mutant/p85alpha using PIP2 as substrate incubated for 40 mins in presence of ATP 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 | 8.02 | 8.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | 2.0 | 1 | 8.08 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 10.9 | nM | 7.96 |