Assay Detail
Binding
CHEMBL3377240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3KCalpha by non-radiometric ADP-Glo assay
6
Total Activities
6
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
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.60 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354566 | — | — | 1 | 8.15 |
| CHEMBL573339 | PI-103 | — | 1 | 8.10 |
| CHEMBL1241857 | — | — | 1 | 7.96 |
| CHEMBL3218571 | — | — | 1 | 7.64 |
| CHEMBL3218581 | — | — | 1 | 7.50 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354566 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL573339 | PI-103 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1241857 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3218571 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3218581 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL98350 | LY-294002 | IC50 | = | 600.0 | nM | 6.22 |