Assay Detail
Binding
CHEMBL3865232
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human PI3Kalpha (108 to 1068 residues) expressed in mammalian expression system by KINOMEscan assay
16
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 alpha isoform (CHEMBL4005) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Imidazopyridazine Inhibitors of PI3Kβ.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 16 | 5.55 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3986383 | — | — | 1 | 6.21 |
| CHEMBL3983623 | — | — | 1 | 6.18 |
| CHEMBL3946307 | — | — | 1 | 6.04 |
| CHEMBL3970860 | — | — | 1 | 5.87 |
| CHEMBL3974658 | — | — | 1 | 5.80 |
| CHEMBL3956037 | — | — | 1 | 5.37 |
| CHEMBL3975628 | — | — | 1 | 5.29 |
| CHEMBL3955003 | — | — | 1 | 5.24 |
| CHEMBL3928423 | — | — | 2 | 5.18 |
| CHEMBL3916621 | — | — | 1 | 5.09 |
| CHEMBL3897548 | — | — | 1 | 4.78 |
| CHEMBL3903747 | — | — | 1 | - |
| CHEMBL3966155 | — | — | 1 | - |
| CHEMBL3894812 | — | — | 1 | - |
| CHEMBL3941289 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3986383 | — | Kd | = | 617.0 | nM | 6.21 |
| CHEMBL3983623 | — | Kd | = | 661.0 | nM | 6.18 |
| CHEMBL3946307 | — | Kd | = | 912.0 | nM | 6.04 |
| CHEMBL3970860 | — | Kd | = | 1349.0 | nM | 5.87 |
| CHEMBL3974658 | — | Kd | = | 1585.0 | nM | 5.80 |
| CHEMBL3956037 | — | Kd | = | 4266.0 | nM | 5.37 |
| CHEMBL3975628 | — | Kd | = | 5130.0 | nM | 5.29 |
| CHEMBL3955003 | — | Kd | = | 5754.0 | nM | 5.24 |
| CHEMBL3928423 | — | Kd | = | 6607.0 | nM | 5.18 |
| CHEMBL3916621 | — | Kd | = | 8128.0 | nM | 5.09 |
| CHEMBL3897548 | — | Kd | = | 16596.0 | nM | 4.78 |
| CHEMBL3928423 | — | Kd | > | 30200.0 | nM | - |
| CHEMBL3903747 | — | Kd | > | 30200.0 | nM | - |
| CHEMBL3966155 | — | Kd | - | — | - | |
| CHEMBL3894812 | — | Kd | > | 30200.0 | nM | - |
| CHEMBL3941289 | — | Kd | > | 30200.0 | nM | - |