Assay Detail
Binding
CHEMBL1058639
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Inhibition of PI3Kalpha expressed in Escherichia coli by microtiter plate-based fluorescence polarization assay
24
Total Activities
24
Compounds Tested
1
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
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.81 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL558955 | — | — | 1 | 8.22 |
| CHEMBL550972 | — | — | 1 | 7.85 |
| CHEMBL556947 | — | — | 1 | 7.82 |
| CHEMBL557963 | — | — | 1 | 7.75 |
| CHEMBL551442 | — | — | 1 | 7.64 |
| CHEMBL538378 | — | — | 1 | 7.46 |
| CHEMBL551440 | — | — | 1 | 7.39 |
| CHEMBL550286 | — | — | 1 | 7.33 |
| CHEMBL563985 | — | — | 1 | 7.00 |
| CHEMBL558288 | — | — | 1 | 6.83 |
| CHEMBL562439 | — | — | 1 | 6.68 |
| CHEMBL564099 | — | — | 1 | 6.68 |
| CHEMBL562365 | — | — | 1 | 6.65 |
| CHEMBL552532 | — | — | 1 | 6.55 |
| CHEMBL561844 | — | — | 1 | 6.39 |
| CHEMBL558486 | — | — | 1 | 6.31 |
| CHEMBL561907 | — | — | 1 | 6.30 |
| CHEMBL540695 | — | — | 1 | 6.26 |
| CHEMBL562165 | — | — | 1 | 6.20 |
| CHEMBL562999 | — | — | 1 | 6.18 |
| CHEMBL564404 | — | — | 1 | 6.17 |
| CHEMBL561103 | — | — | 1 | 6.10 |
| CHEMBL561708 | — | — | 1 | 5.99 |
| CHEMBL557895 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL558955 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL550972 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL556947 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL557963 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL551442 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL538378 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL551440 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL550286 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL563985 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL558288 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL562439 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL564099 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL562365 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL552532 | — | IC50 | = | 284.0 | nM | 6.55 |
| CHEMBL561844 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL558486 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL561907 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL540695 | — | IC50 | = | 548.0 | nM | 6.26 |
| CHEMBL562165 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL562999 | — | IC50 | = | 661.0 | nM | 6.18 |
| CHEMBL564404 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL561103 | — | IC50 | = | 801.0 | nM | 6.10 |
| CHEMBL561708 | — | IC50 | = | 1026.0 | nM | 5.99 |
| CHEMBL557895 | — | IC50 | = | 2005.0 | nM | 5.70 |