Assay Detail
Binding
CHEMBL4428709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.16 | 6.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449366 | — | — | 1 | 6.35 |
| CHEMBL4570159 | — | — | 1 | 6.15 |
| CHEMBL4449576 | — | — | 1 | 6.02 |
| CHEMBL4442808 | — | — | 1 | 5.24 |
| CHEMBL4555334 | — | — | 1 | 5.24 |
| CHEMBL4464055 | — | — | 1 | 5.21 |
| CHEMBL3403678 | — | — | 1 | 5.10 |
| CHEMBL4594095 | — | — | 1 | 4.96 |
| CHEMBL4461539 | — | — | 1 | 4.90 |
| CHEMBL4516601 | — | — | 1 | 4.90 |
| CHEMBL4443843 | — | — | 1 | 4.85 |
| CHEMBL4572863 | — | — | 1 | 4.78 |
| CHEMBL4470291 | — | — | 1 | 4.75 |
| CHEMBL4525494 | — | — | 1 | 4.54 |
| CHEMBL4303596 | AMG-319 | 2.0 | 1 | 4.48 |
| CHEMBL4542785 | — | — | 1 | - |
| CHEMBL4438514 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449366 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL4570159 | — | IC50 | = | 703.0 | nM | 6.15 |
| CHEMBL4449576 | — | IC50 | = | 949.0 | nM | 6.02 |
| CHEMBL4442808 | — | IC50 | = | 5750.0 | nM | 5.24 |
| CHEMBL4555334 | — | IC50 | = | 5760.0 | nM | 5.24 |
| CHEMBL4464055 | — | IC50 | = | 6230.0 | nM | 5.21 |
| CHEMBL3403678 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4594095 | — | IC50 | = | 10900.0 | nM | 4.96 |
| CHEMBL4461539 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4516601 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4443843 | — | IC50 | = | 14180.0 | nM | 4.85 |
| CHEMBL4572863 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL4470291 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL4525494 | — | IC50 | = | 29200.0 | nM | 4.54 |
| CHEMBL4303596 | AMG-319 | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4542785 | — | IC50 | - | — | - | |
| CHEMBL4438514 | — | IC50 | - | — | - |