Assay Detail
Binding
CHEMBL2072997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST-tagged PI3K p110alpha using [32P]ATP after 60 mins by scintillation proximity assay
18
Total Activities
18
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
Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.01 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2071338 | — | — | 1 | 8.30 |
| CHEMBL2071329 | — | — | 1 | 7.96 |
| CHEMBL2071337 | — | — | 1 | 7.70 |
| CHEMBL2071332 | — | — | 1 | 7.55 |
| CHEMBL2071333 | — | — | 1 | 7.52 |
| CHEMBL2071328 | — | — | 1 | 7.46 |
| CHEMBL2071331 | — | — | 1 | 7.35 |
| CHEMBL2071336 | — | — | 1 | 7.30 |
| CHEMBL2071340 | — | — | 1 | 6.96 |
| CHEMBL2071326 | — | — | 1 | 6.96 |
| CHEMBL2071330 | — | — | 1 | 6.91 |
| CHEMBL1986603 | — | — | 1 | 6.82 |
| CHEMBL2071335 | — | — | 1 | 6.73 |
| CHEMBL2071334 | — | — | 1 | 6.72 |
| CHEMBL2071327 | — | — | 1 | 6.70 |
| CHEMBL2071342 | — | — | 1 | 5.85 |
| CHEMBL2069328 | — | — | 1 | 5.72 |
| CHEMBL2071341 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2071338 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2071329 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2071337 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL2071332 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2071333 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2071328 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2071331 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2071336 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL2071340 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2071326 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2071330 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL1986603 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL2071335 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL2071334 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL2071327 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2071342 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL2069328 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL2071341 | — | Ki | = | 2130.0 | nM | 5.67 |