Assay Detail
Binding
CHEMBL2020154
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Inhibition of PI3Kalpha using 1-alpha-phosphatidylinositol as substrate by ATP depletion assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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
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 |
|---|---|---|---|
| IC50 | 16 | 7.89 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2017970 | — | — | 1 | 8.66 |
| CHEMBL2017965 | — | — | 1 | 8.62 |
| CHEMBL2017968 | — | — | 1 | 8.59 |
| CHEMBL2017966 | — | — | 1 | 8.39 |
| CHEMBL2017969 | — | — | 1 | 8.13 |
| CHEMBL2016592 | — | — | 1 | 8.10 |
| CHEMBL2017977 | — | — | 1 | 7.85 |
| CHEMBL2017976 | — | — | 1 | 7.82 |
| CHEMBL2017971 | — | — | 1 | 7.74 |
| CHEMBL2017967 | — | — | 1 | 7.68 |
| CHEMBL2017975 | — | — | 1 | 7.64 |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | 7.52 |
| CHEMBL2017972 | — | — | 1 | 7.47 |
| CHEMBL2017973 | — | — | 1 | 7.17 |
| CHEMBL1672316 | — | — | 1 | 6.96 |
| CHEMBL1672323 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2017970 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL2017965 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2017968 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2017966 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL2017969 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2016592 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2017977 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2017976 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2017971 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL2017967 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2017975 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2017974 | BUPARLISIB | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2017972 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL2017973 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1672316 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1672323 | — | IC50 | < | 2.0 | nM | - |