Assay Detail
Binding
CHEMBL4733831
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Inhibition of human PI3Kalpha using PIP2 as substrate in presence of ATP measured after 30 mins by HTRF assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 15 | 7.44 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | 2.0 | 1 | 8.23 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | 7.75 |
| CHEMBL4783228 | — | — | 1 | 7.75 |
| CHEMBL4740055 | — | — | 1 | 7.70 |
| CHEMBL4779801 | — | — | 1 | 7.68 |
| CHEMBL4784118 | — | — | 1 | 7.63 |
| CHEMBL4742751 | — | — | 1 | 7.40 |
| CHEMBL4756324 | — | — | 1 | 7.39 |
| CHEMBL4781518 | — | — | 1 | 7.38 |
| CHEMBL4760391 | — | — | 1 | 7.35 |
| CHEMBL4791280 | — | — | 1 | 7.30 |
| CHEMBL4761702 | — | — | 1 | 7.26 |
| CHEMBL4800181 | — | — | 1 | 7.17 |
| CHEMBL4756074 | — | — | 1 | 6.98 |
| CHEMBL4799728 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4800252 | RISOVALISIB | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL2396661 | ALPELISIB | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL4783228 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL4740055 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL4779801 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4784118 | — | IC50 | = | 23.6 | nM | 7.63 |
| CHEMBL4742751 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL4756324 | — | IC50 | = | 41.1 | nM | 7.39 |
| CHEMBL4781518 | — | IC50 | = | 41.7 | nM | 7.38 |
| CHEMBL4760391 | — | IC50 | = | 44.4 | nM | 7.35 |
| CHEMBL4791280 | — | IC50 | = | 50.5 | nM | 7.30 |
| CHEMBL4761702 | — | IC50 | = | 55.4 | nM | 7.26 |
| CHEMBL4800181 | — | IC50 | = | 67.5 | nM | 7.17 |
| CHEMBL4756074 | — | IC50 | = | 105.3 | nM | 6.98 |
| CHEMBL4799728 | — | IC50 | = | 243.8 | nM | 6.61 |