Assay Detail
Binding
CHEMBL3376669
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Inhibition of human PI3KC2alpha by non-radiometric ADP-Glo assay
12
Total Activities
12
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-phosphate 3-kinase C2 domain-containing subunit alpha (CHEMBL1075102) ↗| 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 | 12 | 6.17 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354566 | — | — | 1 | 7.47 |
| CHEMBL1241857 | — | — | 1 | 7.33 |
| CHEMBL3218571 | — | — | 1 | 6.85 |
| CHEMBL573339 | PI-103 | — | 1 | 6.00 |
| CHEMBL1229535 | — | — | 1 | 4.80 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 4.57 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | - |
| CHEMBL3218581 | — | — | 1 | - |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | - |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | - |
| CHEMBL3354565 | — | — | 1 | - |
| CHEMBL3354564 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354566 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1241857 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3218571 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL573339 | PI-103 | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1229535 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL98350 | LY-294002 | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2216870 | IDELALISIB | IC50 | - | — | - | |
| CHEMBL3218581 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | IC50 | > | 100000.0 | nM | - |
| CHEMBL586702 | ZSTK-474 | IC50 | > | 100000.0 | nM | - |
| CHEMBL3354565 | — | IC50 | - | — | - | |
| CHEMBL3354564 | — | IC50 | - | — | - |