Assay Detail
Binding
CHEMBL4428725
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in human whole blood assessed as inhibition of Anti-IgD antibody-induced AKT Ser473 phosphorylation pre-incubated for 60 mins before Anti-IgD antibody stimulation
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗| 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 | 3 | 7.69 | 7.96 |
| fIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4303596 | AMG-319 | 2.0 | 2 | 7.96 |
| CHEMBL4443843 | — | — | 2 | 7.73 |
| CHEMBL4470291 | — | — | 2 | 7.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4303596 | AMG-319 | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4443843 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL4470291 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4303596 | AMG-319 | fIC50 | = | 1.7 | nM | - |
| CHEMBL4470291 | — | fIC50 | = | 4.6 | nM | - |
| CHEMBL4443843 | — | fIC50 | = | 7.7 | nM | - |