Assay Detail
Binding
CHEMBL4199836
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Inhibition of recombinant human full-length N-terminal His6-tagged p110beta/recombinant human full length p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polarization assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 6.53 | 6.63 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 6.63 |
| CHEMBL4206442 | — | — | 1 | 6.58 |
| CHEMBL4215969 | — | — | 1 | 6.50 |
| CHEMBL4211915 | — | — | 1 | 6.42 |
| CHEMBL4210320 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4206442 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL4215969 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL4211915 | — | IC50 | = | 376.0 | nM | 6.42 |
| CHEMBL4210320 | — | IC50 | - | — | - |