Assay Detail
Binding
CHEMBL3855726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo luminescence assay
26
Total Activities
26
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
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.80 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3975359 | — | — | 1 | 7.85 |
| CHEMBL3984425 | EGANELISIB | 2.0 | 1 | 7.80 |
| CHEMBL3937119 | — | — | 1 | 7.60 |
| CHEMBL3963736 | — | — | 1 | 7.40 |
| CHEMBL3976330 | — | — | 1 | 7.30 |
| CHEMBL3911278 | — | — | 1 | 7.22 |
| CHEMBL3923629 | — | — | 1 | 7.12 |
| CHEMBL3914602 | — | — | 1 | 7.00 |
| CHEMBL3928146 | — | — | 1 | 6.96 |
| CHEMBL3921445 | — | — | 1 | 6.96 |
| CHEMBL3947903 | — | — | 1 | 6.96 |
| CHEMBL3959293 | — | — | 1 | 6.82 |
| CHEMBL3893430 | — | — | 1 | 6.77 |
| CHEMBL3944056 | — | — | 1 | 6.62 |
| CHEMBL3966879 | — | — | 1 | 6.55 |
| CHEMBL3917188 | — | — | 1 | 6.52 |
| CHEMBL3946030 | — | — | 1 | 6.48 |
| CHEMBL3955769 | — | — | 1 | 6.46 |
| CHEMBL3895629 | — | — | 1 | 6.44 |
| CHEMBL3908224 | — | — | 1 | 6.40 |
| CHEMBL3916095 | — | — | 1 | 6.00 |
| CHEMBL3978650 | — | — | 1 | 6.00 |
| CHEMBL3983349 | — | — | 1 | 5.96 |
| CHEMBL3954718 | — | — | 1 | 5.96 |
| CHEMBL3890228 | — | — | 1 | - |
| CHEMBL3986947 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3975359 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3984425 | EGANELISIB | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3937119 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3963736 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3976330 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3911278 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3923629 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3914602 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3928146 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3921445 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3947903 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3959293 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3893430 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3944056 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3966879 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3917188 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3946030 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3955769 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3895629 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3908224 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3916095 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3978650 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3983349 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3954718 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3890228 | — | IC50 | > | 7000.0 | nM | - |
| CHEMBL3986947 | — | IC50 | > | 10000.0 | nM | - |