Assay Detail
Binding
CHEMBL4231676
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Inhibition of PI3Kdelta (unknown origin) using Biotin-S11S12 as substrate after 120 mins in presence of ATP by ADPGlo luminescence assay
15
Total Activities
15
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 delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.42 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | 8.80 |
| CHEMBL4249477 | — | — | 1 | 8.08 |
| CHEMBL4245221 | — | — | 1 | 8.07 |
| CHEMBL4250311 | — | — | 1 | 7.80 |
| CHEMBL4249850 | — | — | 1 | 7.58 |
| CHEMBL4241373 | — | — | 1 | 7.51 |
| CHEMBL4243529 | — | — | 1 | 7.39 |
| CHEMBL4250842 | — | — | 1 | 7.09 |
| CHEMBL4238027 | — | — | 1 | 7.08 |
| CHEMBL4246053 | — | — | 1 | 7.07 |
| CHEMBL4239740 | — | — | 1 | 6.97 |
| CHEMBL4251492 | — | — | 1 | 6.64 |
| CHEMBL4243064 | — | — | 1 | 6.38 |
| CHEMBL4239308 | — | — | 1 | - |
| CHEMBL4248031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2216870 | IDELALISIB | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4249477 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4245221 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4250311 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4249850 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4241373 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4243529 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4250842 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4238027 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4246053 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4239740 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4251492 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4243064 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL4239308 | — | IC50 | - | — | - | |
| CHEMBL4248031 | — | IC50 | - | — | - |