Assay Detail
Binding
CHEMBL3855895
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kgamma (S144 to A1102 residues) expressed in mammalian expression system incubated for 60 mins by ADAPTA assay
21
Total Activities
21
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 Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.22 | 8.55 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3979343 | — | — | 1 | 8.55 |
| CHEMBL3039502 | DUVELISIB | 4.0 | 1 | 8.54 |
| CHEMBL3904942 | — | — | 1 | 8.37 |
| CHEMBL3959351 | — | — | 1 | 8.19 |
| CHEMBL3942643 | — | — | 1 | 7.96 |
| CHEMBL1673047 | — | — | 1 | 7.82 |
| CHEMBL3898901 | — | — | 1 | 7.82 |
| CHEMBL3950648 | — | — | 1 | 7.70 |
| CHEMBL3918001 | — | — | 1 | 7.31 |
| CHEMBL3922919 | — | — | 1 | 7.24 |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 7.19 |
| CHEMBL3909068 | — | — | 1 | 6.96 |
| CHEMBL3913941 | — | — | 1 | 6.96 |
| CHEMBL3889977 | — | — | 1 | 6.92 |
| CHEMBL3926951 | — | — | 1 | 6.51 |
| CHEMBL3907932 | — | — | 1 | 6.48 |
| CHEMBL3935895 | — | — | 1 | 6.47 |
| CHEMBL3986648 | — | — | 1 | 6.25 |
| CHEMBL3932938 | — | — | 1 | 5.62 |
| CHEMBL3948672 | — | — | 1 | 5.48 |
| CHEMBL3969370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3979343 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3039502 | DUVELISIB | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3904942 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3959351 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3942643 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1673047 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3898901 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3950648 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3918001 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3922919 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL2216870 | IDELALISIB | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3909068 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3913941 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3889977 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3926951 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3907932 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3935895 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3986648 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3932938 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL3948672 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3969370 | — | Inhibition | - | % | - |