Assay Detail
Binding
CHEMBL5046925
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Inhibition of human PI3Kdelta 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 delta isoform (CHEMBL3130) ↗| 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 | 7.59 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4125884 | — | — | 1 | 8.54 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 8.41 |
| CHEMBL5094393 | — | — | 1 | 8.09 |
| CHEMBL5093356 | — | — | 1 | 8.07 |
| CHEMBL5078681 | — | — | 1 | 8.05 |
| CHEMBL5086257 | — | — | 1 | 8.02 |
| CHEMBL5087654 | — | — | 1 | 8.00 |
| CHEMBL5082167 | — | — | 1 | 7.93 |
| CHEMBL5077891 | — | — | 1 | 7.90 |
| CHEMBL5086251 | — | — | 1 | 7.77 |
| CHEMBL5092014 | — | — | 1 | 7.58 |
| CHEMBL5088136 | — | — | 1 | 7.33 |
| CHEMBL5075977 | — | — | 1 | 7.22 |
| CHEMBL5085424 | — | — | 1 | 6.87 |
| CHEMBL5089694 | — | — | 1 | 6.86 |
| CHEMBL3400288 | — | — | 1 | 6.85 |
| CHEMBL5084156 | — | — | 1 | 6.63 |
| CHEMBL5080466 | — | — | 1 | 6.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4125884 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5094393 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5093356 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5078681 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5086257 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL5087654 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5082167 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5077891 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5086251 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5092014 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5088136 | — | IC50 | = | 46.7 | nM | 7.33 |
| CHEMBL5075977 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5085424 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5089694 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL3400288 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5084156 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL5080466 | — | IC50 | = | 291.0 | nM | 6.54 |