Assay Detail
Binding
CHEMBL3112129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma (unknown origin) after 1 hr by TR-FRET assay
32
Total Activities
32
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
Design, synthesis, and biological activity of pyridopyrimidine scaffolds as novel PI3K/mTOR dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.12 | 7.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3109142 | — | — | 1 | 7.58 |
| CHEMBL3109116 | — | — | 1 | 7.51 |
| CHEMBL3109141 | — | — | 1 | 7.21 |
| CHEMBL3109146 | — | — | 1 | 7.10 |
| CHEMBL3109134 | — | — | 1 | 7.09 |
| CHEMBL3109133 | — | — | 1 | 7.06 |
| CHEMBL3109145 | — | — | 1 | 6.82 |
| CHEMBL3109126 | — | — | 1 | 6.74 |
| CHEMBL3109140 | — | — | 1 | 6.64 |
| CHEMBL3109144 | — | — | 1 | 6.58 |
| CHEMBL3109143 | — | — | 1 | 6.45 |
| CHEMBL3109121 | — | — | 1 | 6.24 |
| CHEMBL3109137 | — | — | 1 | 6.13 |
| CHEMBL3109132 | — | — | 1 | 5.47 |
| CHEMBL3109139 | — | — | 1 | 5.33 |
| CHEMBL3109128 | — | — | 1 | 5.20 |
| CHEMBL3109123 | — | — | 1 | 5.19 |
| CHEMBL3109131 | — | — | 1 | 5.10 |
| CHEMBL3109122 | — | — | 1 | 5.03 |
| CHEMBL3109135 | — | — | 1 | 4.91 |
| CHEMBL3109147 | — | — | 1 | 4.66 |
| CHEMBL3109127 | — | — | 1 | 4.51 |
| CHEMBL3109125 | — | — | 1 | - |
| CHEMBL3109124 | — | — | 1 | - |
| CHEMBL3109129 | — | — | 1 | - |
| CHEMBL3109130 | — | — | 1 | - |
| CHEMBL3109136 | — | — | 1 | - |
| CHEMBL3109120 | — | — | 1 | - |
| CHEMBL3109119 | — | — | 1 | - |
| CHEMBL3109118 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3109142 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3109116 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3109141 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3109146 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3109134 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3109133 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3109145 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL3109126 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3109140 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL3109144 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL3109143 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL3109121 | — | IC50 | = | 574.0 | nM | 6.24 |
| CHEMBL3109137 | — | IC50 | = | 741.0 | nM | 6.13 |
| CHEMBL3109132 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3109139 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3109128 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3109123 | — | IC50 | = | 6390.0 | nM | 5.19 |
| CHEMBL3109131 | — | IC50 | = | 7880.0 | nM | 5.10 |
| CHEMBL3109122 | — | IC50 | = | 9360.0 | nM | 5.03 |
| CHEMBL3109135 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL3109147 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3109127 | — | IC50 | = | 30700.0 | nM | 4.51 |
| CHEMBL3109125 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109124 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109129 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109130 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109136 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109120 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109119 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109118 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109117 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL3109138 | — | IC50 | > | 50000.0 | nM | - |