Assay Detail
Binding
CHEMBL5356226
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase-Glo plus luminescent 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
Function-oriented synthesis of Imidazo[1,2-a]pyrazine and Imidazo[1,2-b]pyridazine derivatives as potent PI3K/mTOR dual inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 8.97 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5395998 | — | — | 1 | 10.22 |
| CHEMBL5422635 | — | — | 1 | 10.10 |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | 9.96 |
| CHEMBL5400439 | — | — | 1 | 9.96 |
| CHEMBL5401298 | — | — | 1 | 9.80 |
| CHEMBL5413309 | — | — | 1 | 9.80 |
| CHEMBL5415726 | — | — | 1 | 9.77 |
| CHEMBL4440406 | — | — | 1 | 9.70 |
| CHEMBL5431325 | — | — | 1 | 9.62 |
| CHEMBL5409142 | — | — | 1 | 9.62 |
| CHEMBL4213353 | — | — | 1 | 9.51 |
| CHEMBL5428160 | — | — | 1 | 9.34 |
| CHEMBL5440536 | — | — | 1 | 9.19 |
| CHEMBL5415865 | — | — | 1 | 9.00 |
| CHEMBL5432324 | — | — | 1 | 8.96 |
| CHEMBL5428411 | — | — | 1 | 8.94 |
| CHEMBL5417402 | — | — | 1 | 8.88 |
| CHEMBL5431132 | — | — | 1 | 8.44 |
| CHEMBL5398514 | — | — | 1 | 8.28 |
| CHEMBL5402186 | — | — | 1 | 8.18 |
| CHEMBL5403717 | — | — | 1 | 8.14 |
| CHEMBL5407573 | — | — | 1 | 8.13 |
| CHEMBL5429174 | — | — | 1 | 8.12 |
| CHEMBL5401801 | — | — | 1 | 8.04 |
| CHEMBL5421477 | — | — | 1 | 7.98 |
| CHEMBL5394535 | — | — | 1 | 7.95 |
| CHEMBL5405706 | — | — | 1 | 7.95 |
| CHEMBL5405623 | — | — | 1 | 7.44 |
| CHEMBL5418523 | — | — | 1 | - |
| CHEMBL1765463 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5395998 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL5422635 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3218576 | COPANLISIB | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL5400439 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL5401298 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5413309 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5415726 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL4440406 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5431325 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL5409142 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL4213353 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL5428160 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL5440536 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5415865 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL5432324 | — | IC50 | = | 1.09 | nM | 8.96 |
| CHEMBL5428411 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL5417402 | — | IC50 | = | 1.33 | nM | 8.88 |
| CHEMBL5431132 | — | IC50 | = | 3.62 | nM | 8.44 |
| CHEMBL5398514 | — | IC50 | = | 5.21 | nM | 8.28 |
| CHEMBL5402186 | — | IC50 | = | 6.63 | nM | 8.18 |
| CHEMBL5403717 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5407573 | — | IC50 | = | 7.46 | nM | 8.13 |
| CHEMBL5429174 | — | IC50 | = | 7.53 | nM | 8.12 |
| CHEMBL5401801 | — | IC50 | = | 9.01 | nM | 8.04 |
| CHEMBL5421477 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL5394535 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL5405706 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5405623 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL5418523 | — | IC50 | > | 5.0 | nM | - |
| CHEMBL1765463 | — | IC50 | > | 5.0 | nM | - |