Assay Detail
Binding
CHEMBL902509
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Inhibition of PI3Kgamma assessed as inhibition of 32P-PIP3 formation
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (CHEMBL3267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinasegamma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 8.00 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL393121 | — | — | 1 | 8.72 |
| CHEMBL246440 | — | — | 1 | 8.63 |
| CHEMBL241710 | — | — | 1 | 8.62 |
| CHEMBL392349 | — | — | 1 | 8.59 |
| CHEMBL394234 | — | — | 1 | 8.58 |
| CHEMBL246859 | — | — | 1 | 8.57 |
| CHEMBL394235 | — | — | 1 | 8.55 |
| CHEMBL246647 | — | — | 1 | 8.37 |
| CHEMBL246441 | — | — | 1 | 8.37 |
| CHEMBL392914 | — | — | 1 | 8.36 |
| CHEMBL241718 | — | — | 1 | 8.32 |
| CHEMBL429657 | — | — | 1 | 8.31 |
| CHEMBL246857 | — | — | 1 | 8.30 |
| CHEMBL398988 | — | — | 1 | 8.18 |
| CHEMBL393276 | — | — | 1 | 8.14 |
| CHEMBL239374 | — | — | 1 | 8.05 |
| CHEMBL428496 | WORTMANNIN | — | 1 | 7.72 |
| CHEMBL391998 | — | — | 1 | 7.64 |
| CHEMBL240623 | — | — | 1 | 7.61 |
| CHEMBL240620 | — | — | 1 | 7.56 |
| CHEMBL241708 | — | — | 1 | 7.53 |
| CHEMBL246645 | — | — | 1 | 7.48 |
| CHEMBL241713 | — | — | 1 | 7.44 |
| CHEMBL240621 | — | — | 1 | 7.36 |
| CHEMBL438133 | — | — | 1 | 7.11 |
| CHEMBL98350 | LY-294002 | -1.0 | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL393121 | — | IC50 | = | 1.92 | nM | 8.72 |
| CHEMBL246440 | — | IC50 | = | 2.34 | nM | 8.63 |
| CHEMBL241710 | — | IC50 | = | 2.42 | nM | 8.62 |
| CHEMBL392349 | — | IC50 | = | 2.59 | nM | 8.59 |
| CHEMBL394234 | — | IC50 | = | 2.65 | nM | 8.58 |
| CHEMBL246859 | — | IC50 | = | 2.66 | nM | 8.57 |
| CHEMBL394235 | — | IC50 | = | 2.79 | nM | 8.55 |
| CHEMBL246647 | — | IC50 | = | 4.28 | nM | 8.37 |
| CHEMBL246441 | — | IC50 | = | 4.27 | nM | 8.37 |
| CHEMBL392914 | — | IC50 | = | 4.36 | nM | 8.36 |
| CHEMBL241718 | — | IC50 | = | 4.76 | nM | 8.32 |
| CHEMBL429657 | — | IC50 | = | 4.84 | nM | 8.31 |
| CHEMBL246857 | — | IC50 | = | 4.96 | nM | 8.30 |
| CHEMBL398988 | — | IC50 | = | 6.57 | nM | 8.18 |
| CHEMBL393276 | — | IC50 | = | 7.16 | nM | 8.14 |
| CHEMBL239374 | — | IC50 | = | 8.83 | nM | 8.05 |
| CHEMBL428496 | WORTMANNIN | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL391998 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL240623 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL240620 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL241708 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL246645 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL241713 | — | IC50 | = | 36.1 | nM | 7.44 |
| CHEMBL240621 | — | IC50 | = | 43.7 | nM | 7.36 |
| CHEMBL438133 | — | IC50 | = | 77.7 | nM | 7.11 |
| CHEMBL98350 | LY-294002 | IC50 | = | 1720.0 | nM | 5.76 |