Assay Detail
Binding
CHEMBL4199833
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Inhibition of PI3K in human PC3 cells assessed as reduction in AKT phosphorylation at Ser473 measured after 2 hrs by fluorescence assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 6.30 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4211402 | — | — | 1 | 6.92 |
| CHEMBL4218707 | — | — | 1 | 6.74 |
| CHEMBL4211915 | — | — | 1 | 6.71 |
| CHEMBL4207037 | — | — | 1 | 6.67 |
| CHEMBL4214713 | — | — | 1 | 6.61 |
| CHEMBL4215235 | — | — | 1 | 6.52 |
| CHEMBL4203109 | — | — | 1 | 6.51 |
| CHEMBL4218171 | — | — | 1 | 6.51 |
| CHEMBL4215969 | — | — | 1 | 6.50 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 6.44 |
| CHEMBL4203634 | — | — | 1 | 6.43 |
| CHEMBL4208505 | — | — | 1 | 6.43 |
| CHEMBL4206215 | — | — | 1 | 6.42 |
| CHEMBL4210822 | — | — | 1 | 6.37 |
| CHEMBL4206442 | — | — | 1 | 6.26 |
| CHEMBL4204166 | — | — | 1 | 6.22 |
| CHEMBL4213772 | — | — | 1 | 6.17 |
| CHEMBL4207389 | — | — | 1 | 6.17 |
| CHEMBL4205959 | — | — | 1 | 6.07 |
| CHEMBL4210301 | — | — | 1 | 6.02 |
| CHEMBL4205938 | — | — | 1 | 5.93 |
| CHEMBL4215841 | — | — | 1 | 5.89 |
| CHEMBL4202499 | — | — | 1 | 5.81 |
| CHEMBL4213112 | — | — | 1 | 5.61 |
| CHEMBL4210320 | — | — | 1 | 5.52 |
| CHEMBL4210843 | — | — | 1 | - |
| CHEMBL4211255 | — | — | 1 | - |
| CHEMBL4216218 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4211402 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4218707 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL4211915 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL4207037 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4214713 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4215235 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4203109 | — | IC50 | = | 312.0 | nM | 6.51 |
| CHEMBL4218171 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4215969 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL4203634 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL4208505 | — | IC50 | = | 369.0 | nM | 6.43 |
| CHEMBL4206215 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL4210822 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4206442 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL4204166 | — | IC50 | = | 606.0 | nM | 6.22 |
| CHEMBL4213772 | — | IC50 | = | 674.0 | nM | 6.17 |
| CHEMBL4207389 | — | IC50 | = | 668.0 | nM | 6.17 |
| CHEMBL4205959 | — | IC50 | = | 846.0 | nM | 6.07 |
| CHEMBL4210301 | — | IC50 | = | 947.0 | nM | 6.02 |
| CHEMBL4205938 | — | IC50 | = | 1178.0 | nM | 5.93 |
| CHEMBL4215841 | — | IC50 | = | 1275.0 | nM | 5.89 |
| CHEMBL4202499 | — | IC50 | = | 1548.0 | nM | 5.81 |
| CHEMBL4213112 | — | IC50 | = | 2446.0 | nM | 5.61 |
| CHEMBL4210320 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL4210843 | — | IC50 | - | — | - | |
| CHEMBL4211255 | — | IC50 | - | — | - | |
| CHEMBL4216218 | — | IC50 | - | — | - |