Assay Detail
Binding
CHEMBL4724045
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kdelta in human Raji cells assessed as reduction in phosphorylation of AKT at 473 measured after 2 hr by alpha screen assay
35
Total Activities
34
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Raji |
| 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 of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 8.13 | 9.05 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787382 | — | — | 1 | 9.05 |
| CHEMBL3805348 | — | — | 1 | 8.92 |
| CHEMBL4754291 | — | — | 1 | 8.89 |
| CHEMBL4794328 | — | — | 1 | 8.83 |
| CHEMBL4787659 | — | — | 1 | 8.77 |
| CHEMBL4783353 | — | — | 1 | 8.64 |
| CHEMBL4778687 | — | — | 1 | 8.47 |
| CHEMBL4752055 | — | — | 1 | 8.47 |
| CHEMBL4782337 | — | — | 1 | 8.44 |
| CHEMBL4750109 | — | — | 1 | 8.30 |
| CHEMBL4791717 | — | — | 1 | 8.25 |
| CHEMBL4751779 | — | — | 1 | 8.23 |
| CHEMBL4742973 | — | — | 1 | 8.15 |
| CHEMBL4750646 | — | — | 1 | 8.12 |
| CHEMBL4755417 | — | — | 1 | 8.03 |
| CHEMBL4756563 | — | — | 2 | 8.02 |
| CHEMBL4749877 | — | — | 1 | 8.01 |
| CHEMBL4749521 | — | — | 1 | 7.85 |
| CHEMBL4463183 | — | — | 1 | 7.85 |
| CHEMBL4748330 | — | — | 1 | 7.80 |
| CHEMBL4792005 | — | — | 1 | 7.77 |
| CHEMBL4795389 | — | — | 1 | 7.77 |
| CHEMBL4749578 | — | — | 1 | 7.72 |
| CHEMBL4748043 | — | — | 1 | 7.58 |
| CHEMBL4742693 | — | — | 1 | 7.50 |
| CHEMBL4784743 | — | — | 1 | 7.27 |
| CHEMBL4797361 | — | — | 1 | 6.94 |
| CHEMBL4746288 | — | — | 1 | - |
| CHEMBL4747142 | — | — | 1 | - |
| CHEMBL4784696 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787382 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL3805348 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4754291 | — | IC50 | = | 1.28 | nM | 8.89 |
| CHEMBL4794328 | — | IC50 | = | 1.49 | nM | 8.83 |
| CHEMBL4787659 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4783353 | — | IC50 | = | 2.28 | nM | 8.64 |
| CHEMBL4778687 | — | IC50 | = | 3.39 | nM | 8.47 |
| CHEMBL4752055 | — | IC50 | = | 3.36 | nM | 8.47 |
| CHEMBL4782337 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4750109 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4791717 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4751779 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4742973 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4750646 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4755417 | — | IC50 | = | 9.42 | nM | 8.03 |
| CHEMBL4756563 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4749877 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4463183 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4749521 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4748330 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4795389 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4792005 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4749578 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4748043 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4742693 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4784743 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4797361 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4747142 | — | IC50 | - | — | - | |
| CHEMBL4746288 | — | IC50 | - | — | - | |
| CHEMBL4784696 | — | IC50 | - | — | - | |
| CHEMBL4777036 | — | IC50 | - | — | - | |
| CHEMBL4750875 | — | IC50 | - | — | - | |
| CHEMBL4777399 | — | IC50 | - | — | - | |
| CHEMBL4756563 | — | IC90 | = | 37.6 | nM | - |
| CHEMBL4755607 | — | IC50 | - | — | - |