Assay Detail
Binding
CHEMBL4193871
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length His-tagged human PI3K p110gamma expressed in baculovirus expression system using PIP2/PS as substrate after 1 hr by ADP-Glo luminescence assay
26
Total Activities
26
Compounds Tested
2
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
Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.01 | 9.30 |
| Inhibition | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217725 | — | — | 1 | 9.30 |
| CHEMBL4213317 | — | — | 1 | 9.15 |
| CHEMBL4208385 | — | — | 1 | 9.15 |
| CHEMBL4212775 | — | — | 1 | 8.15 |
| CHEMBL4204586 | — | — | 1 | 7.82 |
| CHEMBL4216255 | — | — | 1 | 7.77 |
| CHEMBL4204119 | — | — | 1 | 7.43 |
| CHEMBL4208997 | — | — | 1 | 7.20 |
| CHEMBL4208746 | — | — | 1 | 7.17 |
| CHEMBL4214320 | — | — | 1 | 7.01 |
| CHEMBL4208922 | — | — | 1 | 6.81 |
| CHEMBL4204046 | — | — | 1 | 6.57 |
| CHEMBL4209923 | — | — | 1 | 6.43 |
| CHEMBL4205049 | — | — | 1 | 6.42 |
| CHEMBL4217733 | — | — | 1 | 6.38 |
| CHEMBL4205510 | — | — | 1 | 6.35 |
| CHEMBL4217268 | — | — | 1 | 5.83 |
| CHEMBL4205985 | — | — | 1 | 5.80 |
| CHEMBL4208476 | — | — | 1 | 5.69 |
| CHEMBL4213409 | — | — | 1 | 5.53 |
| CHEMBL4209424 | — | — | 1 | 5.32 |
| CHEMBL3360203 | PILARALISIB | 2.0 | 1 | - |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | - |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | - |
| CHEMBL2017974 | BUPARLISIB | 3.0 | 1 | - |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217725 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4213317 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4208385 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4212775 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4204586 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4216255 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4204119 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4208997 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4208746 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4214320 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4208922 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4204046 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL4209923 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL4205049 | — | IC50 | = | 381.0 | nM | 6.42 |
| CHEMBL4217733 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4205510 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL4217268 | — | IC50 | = | 1491.0 | nM | 5.83 |
| CHEMBL4205985 | — | IC50 | = | 1593.0 | nM | 5.80 |
| CHEMBL4208476 | — | IC50 | = | 2062.0 | nM | 5.69 |
| CHEMBL4213409 | — | IC50 | = | 2966.0 | nM | 5.53 |
| CHEMBL4209424 | — | IC50 | = | 4752.0 | nM | 5.32 |
| CHEMBL3360203 | PILARALISIB | Inhibition | - | % | - | |
| CHEMBL1922094 | APITOLISIB | Inhibition | - | % | - | |
| CHEMBL1879463 | DACTOLISIB | Inhibition | - | % | - | |
| CHEMBL2017974 | BUPARLISIB | Inhibition | - | % | - | |
| CHEMBL521851 | PICTILISIB | Inhibition | - | % | - |