Assay Detail
Binding
CHEMBL4392572
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kgamma using PIP2 as substrate after 1 hr
5
Total Activities
5
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 of 1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-ones based novel, potent and PI3Kδ selective inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.40 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | 8.22 |
| CHEMBL4454741 | — | — | 1 | 7.42 |
| CHEMBL4550603 | — | — | 1 | 7.38 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 7.04 |
| CHEMBL4560054 | — | — | 1 | 6.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1879463 | DACTOLISIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4454741 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4550603 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4560054 | — | IC50 | = | 112.0 | nM | 6.95 |