Assay Detail
Binding
CHEMBL2020156
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Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.83 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1672323 | — | — | 1 | 7.38 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.26 |
| CHEMBL2017977 | — | — | 1 | 7.16 |
| CHEMBL2017976 | — | — | 1 | 7.14 |
| CHEMBL2017975 | — | — | 1 | 7.10 |
| CHEMBL2016592 | — | — | 1 | 7.05 |
| CHEMBL2017971 | — | — | 1 | 7.00 |
| CHEMBL2017973 | — | — | 1 | 7.00 |
| CHEMBL2017972 | — | — | 1 | 6.96 |
| CHEMBL2017968 | — | — | 1 | 6.75 |
| CHEMBL2017965 | — | — | 1 | 6.54 |
| CHEMBL1672316 | — | — | 1 | 6.51 |
| CHEMBL2017970 | — | — | 1 | 6.37 |
| CHEMBL2017967 | — | — | 1 | 6.35 |
| CHEMBL2017966 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1672323 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2017974 | BUPARLISIB | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2017977 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2017976 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2017975 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2016592 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2017971 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2017973 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2017972 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2017968 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2017965 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1672316 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2017970 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2017967 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL2017966 | — | EC50 | = | 1300.0 | nM | 5.89 |