Assay Detail
Binding
CHEMBL995909
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Inhibition of PI3Kalpha by luminescent kinase glo assay
27
Total Activities
27
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 4.65 | 6.70 |
| Inhibition | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 6.70 |
| CHEMBL469796 | — | — | 1 | 5.30 |
| CHEMBL469565 | — | — | 1 | 5.16 |
| CHEMBL512309 | — | — | 1 | 4.70 |
| CHEMBL511807 | — | — | 1 | 4.54 |
| CHEMBL449172 | — | — | 1 | 4.44 |
| CHEMBL450243 | — | — | 1 | 4.29 |
| CHEMBL470639 | — | — | 1 | 4.00 |
| CHEMBL469806 | — | — | 1 | 4.00 |
| CHEMBL470852 | — | — | 1 | 4.00 |
| CHEMBL512311 | — | — | 1 | 4.00 |
| CHEMBL472084 | — | — | 1 | - |
| CHEMBL472085 | — | — | 1 | - |
| CHEMBL469564 | — | — | 1 | - |
| CHEMBL449816 | — | — | 1 | - |
| CHEMBL469797 | — | — | 1 | - |
| CHEMBL470001 | — | — | 1 | - |
| CHEMBL471045 | — | — | 1 | - |
| CHEMBL471046 | — | — | 1 | - |
| CHEMBL469981 | — | — | 1 | - |
| CHEMBL469807 | — | — | 1 | - |
| CHEMBL470638 | — | — | 1 | - |
| CHEMBL470853 | — | — | 1 | - |
| CHEMBL502174 | — | — | 1 | - |
| CHEMBL470855 | — | — | 1 | - |
| CHEMBL512487 | — | — | 1 | - |
| CHEMBL471057 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98350 | LY-294002 | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL469796 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL469565 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL512309 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL511807 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL449172 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL450243 | — | IC50 | = | 51000.0 | nM | 4.29 |
| CHEMBL470639 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL469806 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL470852 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL512311 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL472084 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL472085 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL469564 | — | Inhibition | < | 10.0 | % | - |
| CHEMBL449816 | — | Inhibition | < | 10.0 | % | - |
| CHEMBL469797 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL470001 | — | Inhibition | < | 10.0 | % | - |
| CHEMBL471045 | — | Inhibition | < | 10.0 | % | - |
| CHEMBL471046 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL469981 | — | IC50 | >= | 50000.0 | nM | - |
| CHEMBL469807 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL470638 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL470853 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL502174 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL470855 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL512487 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL471057 | — | IC50 | > | 100000.0 | nM | - |