Assay Detail
Binding
CHEMBL4370795
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PI3Kalpha using phosphatidyl inositol as substrate after 3 hrs by Kinase-Glo Plus reagent-based luminescence assay
11
Total Activities
11
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of 5,6,7,8-tetrahydropyrido[4,3-d]pyrimidines to generate a highly selective PI3Kδ inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.31 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4518787 | — | — | 1 | 5.85 |
| CHEMBL4569467 | — | — | 1 | 5.58 |
| CHEMBL4528263 | — | — | 1 | 5.34 |
| CHEMBL4475876 | — | — | 1 | 5.31 |
| CHEMBL4554894 | — | — | 1 | 5.24 |
| CHEMBL4582553 | — | — | 1 | 5.21 |
| CHEMBL4581474 | — | — | 1 | 5.14 |
| CHEMBL4467692 | — | — | 1 | 5.12 |
| CHEMBL4530810 | — | — | 1 | 5.01 |
| CHEMBL4453747 | — | — | 1 | - |
| CHEMBL4514389 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4518787 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4569467 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4528263 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4475876 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4554894 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4582553 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4581474 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4467692 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL4530810 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4453747 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4514389 | — | IC50 | > | 10000.0 | nM | - |