Assay Detail
Binding
CHEMBL5046923
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Inhibition of human PI3Kbeta by TR-FRET based Adapta assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (CHEMBL3145) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.41 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4125884 | — | — | 1 | 7.84 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.82 |
| CHEMBL5094393 | — | — | 1 | 7.15 |
| CHEMBL5087654 | — | — | 1 | 7.13 |
| CHEMBL5078681 | — | — | 1 | 6.87 |
| CHEMBL5086257 | — | — | 1 | 6.70 |
| CHEMBL5086251 | — | — | 1 | 6.68 |
| CHEMBL5082167 | — | — | 1 | 6.39 |
| CHEMBL5092014 | — | — | 1 | 6.37 |
| CHEMBL5088136 | — | — | 1 | 6.20 |
| CHEMBL5075977 | — | — | 1 | 6.10 |
| CHEMBL5093356 | — | — | 1 | 5.96 |
| CHEMBL3400288 | — | — | 1 | 5.96 |
| CHEMBL5084156 | — | — | 1 | 5.81 |
| CHEMBL5077891 | — | — | 1 | 5.73 |
| CHEMBL5080466 | — | — | 1 | 5.67 |
| CHEMBL5085424 | — | — | 1 | 5.54 |
| CHEMBL5089694 | — | — | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4125884 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 15.2 | nM | 7.82 |
| CHEMBL5094393 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL5087654 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5078681 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5086257 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL5086251 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL5082167 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL5092014 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL5088136 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL5075977 | — | IC50 | = | 787.0 | nM | 6.10 |
| CHEMBL5093356 | — | IC50 | = | 1085.0 | nM | 5.96 |
| CHEMBL3400288 | — | IC50 | = | 1093.0 | nM | 5.96 |
| CHEMBL5084156 | — | IC50 | = | 1537.0 | nM | 5.81 |
| CHEMBL5077891 | — | IC50 | = | 1867.0 | nM | 5.73 |
| CHEMBL5080466 | — | IC50 | = | 2117.0 | nM | 5.67 |
| CHEMBL5085424 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5089694 | — | IC50 | = | 3880.0 | nM | 5.41 |