Assay Detail
Binding
CHEMBL5167632
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 1 hr in presence of ATP by ADP-glo luminescence assay
30
Total Activities
30
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
Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.04 | 7.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3643413 | LENIOLISIB | 4.0 | 1 | 7.12 |
| CHEMBL5178373 | — | — | 1 | 6.81 |
| CHEMBL5192588 | — | — | 1 | 6.76 |
| CHEMBL5171306 | — | — | 1 | 6.62 |
| CHEMBL5204818 | — | — | 1 | 6.51 |
| CHEMBL5174889 | — | — | 1 | 6.49 |
| CHEMBL5175244 | — | — | 1 | 6.44 |
| CHEMBL5203775 | — | — | 1 | 6.41 |
| CHEMBL5205011 | — | — | 1 | 6.40 |
| CHEMBL5188347 | — | — | 1 | 6.39 |
| CHEMBL5177854 | — | — | 1 | 6.37 |
| CHEMBL5178942 | — | — | 1 | 6.32 |
| CHEMBL5179250 | — | — | 1 | 6.23 |
| CHEMBL5196839 | — | — | 1 | 6.14 |
| CHEMBL5185603 | — | — | 1 | 6.10 |
| CHEMBL5179550 | — | — | 1 | 5.92 |
| CHEMBL5208623 | — | — | 1 | 5.69 |
| CHEMBL5199087 | — | — | 1 | 5.59 |
| CHEMBL5188346 | — | — | 1 | 5.54 |
| CHEMBL5202530 | — | — | 1 | 5.51 |
| CHEMBL5182641 | — | — | 1 | 5.47 |
| CHEMBL5194806 | — | — | 1 | 5.39 |
| CHEMBL5184666 | — | — | 1 | 5.25 |
| CHEMBL5190613 | — | — | 1 | 5.20 |
| CHEMBL5208539 | — | — | 1 | 5.13 |
| CHEMBL5205397 | — | — | 1 | 5.11 |
| CHEMBL5202548 | — | — | 1 | - |
| CHEMBL5181233 | — | — | 1 | - |
| CHEMBL5206003 | — | — | 1 | - |
| CHEMBL5187872 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3643413 | LENIOLISIB | IC50 | = | 75.5 | nM | 7.12 |
| CHEMBL5178373 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL5192588 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL5171306 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL5204818 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5174889 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL5175244 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL5203775 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL5205011 | — | IC50 | = | 395.0 | nM | 6.40 |
| CHEMBL5188347 | — | IC50 | = | 411.0 | nM | 6.39 |
| CHEMBL5177854 | — | IC50 | = | 428.0 | nM | 6.37 |
| CHEMBL5178942 | — | IC50 | = | 483.0 | nM | 6.32 |
| CHEMBL5179250 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL5196839 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL5185603 | — | IC50 | = | 793.0 | nM | 6.10 |
| CHEMBL5179550 | — | IC50 | = | 1214.0 | nM | 5.92 |
| CHEMBL5208623 | — | IC50 | = | 2057.0 | nM | 5.69 |
| CHEMBL5199087 | — | IC50 | = | 2581.0 | nM | 5.59 |
| CHEMBL5188346 | — | IC50 | = | 2905.0 | nM | 5.54 |
| CHEMBL5202530 | — | IC50 | = | 3067.0 | nM | 5.51 |
| CHEMBL5182641 | — | IC50 | = | 3412.0 | nM | 5.47 |
| CHEMBL5194806 | — | IC50 | = | 4032.0 | nM | 5.39 |
| CHEMBL5184666 | — | IC50 | = | 5636.0 | nM | 5.25 |
| CHEMBL5190613 | — | IC50 | = | 6292.0 | nM | 5.20 |
| CHEMBL5208539 | — | IC50 | = | 7327.0 | nM | 5.13 |
| CHEMBL5205397 | — | IC50 | = | 7856.0 | nM | 5.11 |
| CHEMBL5202548 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5181233 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5206003 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5187872 | — | IC50 | > | 10000.0 | nM | - |