Assay Detail
Binding
CHEMBL4430042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kgamma (unknown origin) assessed as reduction in ADP formation using phosphatidyl inositol as substrate after 30 to 60 mins by TR-FRET assay
16
Total Activities
16
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
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.59 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3944013 | — | — | 1 | 6.66 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 6.50 |
| CHEMBL4588314 | — | — | 1 | 6.13 |
| CHEMBL4521888 | — | — | 1 | 5.85 |
| CHEMBL4475622 | — | — | 1 | 5.58 |
| CHEMBL3947814 | — | — | 1 | 5.57 |
| CHEMBL4454454 | — | — | 1 | 5.35 |
| CHEMBL3977066 | — | — | 1 | 5.33 |
| CHEMBL4521863 | — | — | 1 | 5.25 |
| CHEMBL4469006 | — | — | 1 | 5.25 |
| CHEMBL4581278 | — | — | 1 | 5.10 |
| CHEMBL4467868 | — | — | 1 | 5.04 |
| CHEMBL4453497 | — | — | 1 | 5.03 |
| CHEMBL4450615 | — | — | 1 | - |
| CHEMBL4437791 | — | — | 1 | - |
| CHEMBL4460621 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3944013 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL4588314 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4521888 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4475622 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3947814 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4454454 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3977066 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL4521863 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4469006 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4581278 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4467868 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL4453497 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL4450615 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4437791 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4460621 | — | IC50 | > | 10000.0 | nM | - |