Assay Detail
Binding
CHEMBL1810296
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Inhibition of human PI3Kgamma expressed in SF9 insect cells after 2 hrs by fluorescence polarization assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.87 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1808983 | — | — | 1 | 8.40 |
| CHEMBL1808977 | — | — | 1 | 8.32 |
| CHEMBL1808990 | — | — | 1 | 8.22 |
| CHEMBL1808988 | — | — | 1 | 8.19 |
| CHEMBL1808979 | — | — | 1 | 8.15 |
| CHEMBL1808989 | — | — | 1 | 8.10 |
| CHEMBL589258 | — | — | 1 | 8.05 |
| CHEMBL1808984 | — | — | 1 | 8.02 |
| CHEMBL1808981 | — | — | 1 | 8.02 |
| CHEMBL1808980 | — | — | 1 | 7.98 |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | 7.96 |
| CHEMBL1808982 | — | — | 1 | 7.87 |
| CHEMBL1808991 | — | — | 1 | 7.84 |
| CHEMBL1808986 | — | — | 1 | 7.75 |
| CHEMBL1808978 | — | — | 1 | 7.69 |
| CHEMBL1808987 | — | — | 1 | 7.61 |
| CHEMBL1808985 | — | — | 1 | 7.30 |
| CHEMBL1808992 | — | — | 1 | 7.14 |
| CHEMBL1808993 | — | — | 1 | 7.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1808983 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1808977 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1808990 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1808988 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1808979 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1808989 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL589258 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1808984 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL1808981 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL1808980 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL592445 | GEDATOLISIB | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1808982 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL1808991 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL1808986 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1808978 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL1808987 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL1808985 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL1808992 | — | IC50 | = | 72.5 | nM | 7.14 |
| CHEMBL1808993 | — | IC50 | = | 96.5 | nM | 7.01 |