Assay Detail
Binding
CHEMBL5046924
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Inhibition of human PI3Kgamma 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 gamma isoform (CHEMBL3267) ↗| 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 | 6.83 | 7.84 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087654 | — | — | 1 | 7.84 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 7.68 |
| CHEMBL4125884 | — | — | 1 | 7.68 |
| CHEMBL5075977 | — | — | 1 | 7.65 |
| CHEMBL5078681 | — | — | 1 | 7.51 |
| CHEMBL5094393 | — | — | 1 | 7.27 |
| CHEMBL5086257 | — | — | 1 | 7.27 |
| CHEMBL5082167 | — | — | 1 | 7.26 |
| CHEMBL5086251 | — | — | 1 | 7.19 |
| CHEMBL5092014 | — | — | 1 | 7.17 |
| CHEMBL5093356 | — | — | 1 | 6.86 |
| CHEMBL5077891 | — | — | 1 | 6.30 |
| CHEMBL5085424 | — | — | 1 | 6.17 |
| CHEMBL5080466 | — | — | 1 | 6.11 |
| CHEMBL5088136 | — | — | 1 | 6.06 |
| CHEMBL3400288 | — | — | 1 | 5.73 |
| CHEMBL5089694 | — | — | 1 | 5.59 |
| CHEMBL5084156 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087654 | — | IC50 | = | 14.6 | nM | 7.84 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL4125884 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5075977 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL5078681 | — | IC50 | = | 30.7 | nM | 7.51 |
| CHEMBL5094393 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5086257 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5082167 | — | IC50 | = | 55.2 | nM | 7.26 |
| CHEMBL5086251 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL5092014 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5093356 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5077891 | — | IC50 | = | 502.0 | nM | 6.30 |
| CHEMBL5085424 | — | IC50 | = | 681.0 | nM | 6.17 |
| CHEMBL5080466 | — | IC50 | = | 771.0 | nM | 6.11 |
| CHEMBL5088136 | — | IC50 | = | 869.0 | nM | 6.06 |
| CHEMBL3400288 | — | IC50 | = | 1873.0 | nM | 5.73 |
| CHEMBL5089694 | — | IC50 | = | 2567.0 | nM | 5.59 |
| CHEMBL5084156 | — | IC50 | = | 2745.0 | nM | 5.56 |