Assay Detail
Binding
CHEMBL4199832
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by Alexa633 Tracer-based fluorescence polarization assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 28 | 7.53 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4218707 | — | — | 1 | 8.22 |
| CHEMBL4218171 | — | — | 1 | 8.22 |
| CHEMBL4203634 | — | — | 1 | 8.15 |
| CHEMBL4202499 | — | — | 1 | 8.05 |
| CHEMBL4206442 | — | — | 1 | 8.05 |
| CHEMBL4211915 | — | — | 1 | 8.00 |
| CHEMBL4203109 | — | — | 1 | 7.89 |
| CHEMBL4215969 | — | — | 1 | 7.89 |
| CHEMBL4215235 | — | — | 1 | 7.89 |
| CHEMBL4204166 | — | — | 1 | 7.85 |
| CHEMBL4214713 | — | — | 1 | 7.82 |
| CHEMBL4211402 | — | — | 1 | 7.70 |
| CHEMBL4213772 | — | — | 1 | 7.66 |
| CHEMBL4205959 | — | — | 1 | 7.60 |
| CHEMBL4207389 | — | — | 1 | 7.58 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.40 |
| CHEMBL4210301 | — | — | 1 | 7.40 |
| CHEMBL4208505 | — | — | 1 | 7.39 |
| CHEMBL4206215 | — | — | 1 | 7.38 |
| CHEMBL4213112 | — | — | 1 | 7.25 |
| CHEMBL4210822 | — | — | 1 | 7.24 |
| CHEMBL4215841 | — | — | 1 | 7.24 |
| CHEMBL4205938 | — | — | 1 | 7.19 |
| CHEMBL4207037 | — | — | 1 | 7.18 |
| CHEMBL4210320 | — | — | 1 | 6.72 |
| CHEMBL4210843 | — | — | 1 | 6.66 |
| CHEMBL4216218 | — | — | 1 | 6.65 |
| CHEMBL4211255 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4218707 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4218171 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4203634 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4202499 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4206442 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4211915 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4203109 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4215969 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4215235 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4204166 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4214713 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4211402 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4213772 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4205959 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4207389 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4210301 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4208505 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4206215 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4213112 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4210822 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4215841 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4205938 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4207037 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4210320 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4210843 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL4216218 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL4211255 | — | IC50 | = | 321.0 | nM | 6.49 |