Assay Detail
Binding
CHEMBL4724043
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PI3Kbeta in human 786-O cells assessed as reduction in phosphorylation of AKT at 473 measured after 1 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 | 786-0 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (CHEMBL3145) ↗| 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 | 6.80 | 7.32 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | 7.32 |
| CHEMBL4463183 | — | — | 1 | 7.11 |
| CHEMBL4787659 | — | — | 1 | 6.87 |
| CHEMBL4749877 | — | — | 1 | 6.72 |
| CHEMBL4756563 | — | — | 2 | 6.68 |
| CHEMBL4794328 | — | — | 1 | 6.62 |
| CHEMBL4782337 | — | — | 1 | 6.29 |
| CHEMBL4742693 | — | — | 1 | - |
| CHEMBL4751779 | — | — | 1 | - |
| CHEMBL4748043 | — | — | 1 | - |
| CHEMBL4792005 | — | — | 1 | - |
| CHEMBL4777036 | — | — | 1 | - |
| CHEMBL4749578 | — | — | 1 | - |
| CHEMBL4755417 | — | — | 1 | - |
| CHEMBL4797361 | — | — | 1 | - |
| CHEMBL4748330 | — | — | 1 | - |
| CHEMBL4778687 | — | — | 1 | - |
| CHEMBL4791717 | — | — | 1 | - |
| CHEMBL4752055 | — | — | 1 | - |
| CHEMBL4750109 | — | — | 1 | - |
| CHEMBL4784696 | — | — | 1 | - |
| CHEMBL4754291 | — | — | 1 | - |
| CHEMBL4787382 | — | — | 1 | - |
| CHEMBL4747142 | — | — | 1 | - |
| CHEMBL4746288 | — | — | 1 | - |
| CHEMBL4742973 | — | — | 1 | - |
| CHEMBL4755607 | — | — | 1 | - |
| CHEMBL4783353 | — | — | 1 | - |
| CHEMBL4750875 | — | — | 1 | - |
| CHEMBL4777399 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3188551 | GSK-2636771 | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4463183 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4787659 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4749877 | — | IC50 | = | 191.0 | nM | 6.72 |
| CHEMBL4756563 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL4794328 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4782337 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL4792005 | — | IC50 | - | — | - | |
| CHEMBL4784743 | — | IC50 | - | — | - | |
| CHEMBL4777036 | — | IC50 | - | — | - | |
| CHEMBL4749578 | — | IC50 | - | — | - | |
| CHEMBL4755417 | — | IC50 | - | — | - | |
| CHEMBL4797361 | — | IC50 | - | — | - | |
| CHEMBL4748330 | — | IC50 | - | — | - | |
| CHEMBL4778687 | — | IC50 | - | — | - | |
| CHEMBL4791717 | — | IC50 | - | — | - | |
| CHEMBL4751779 | — | IC50 | - | — | - | |
| CHEMBL4749521 | — | IC50 | - | — | - | |
| CHEMBL4750646 | — | IC50 | - | — | - | |
| CHEMBL4795389 | — | IC50 | - | — | - | |
| CHEMBL4756563 | — | IC90 | = | 8050.0 | nM | - |
| CHEMBL4748043 | — | IC50 | - | — | - | |
| CHEMBL4742693 | — | IC50 | - | — | - | |
| CHEMBL4752055 | — | IC50 | - | — | - | |
| CHEMBL4750109 | — | IC50 | - | — | - | |
| CHEMBL4784696 | — | IC50 | - | — | - | |
| CHEMBL4754291 | — | IC50 | - | — | - | |
| CHEMBL4787382 | — | IC50 | - | — | - | |
| CHEMBL4747142 | — | IC50 | - | — | - | |
| CHEMBL4746288 | — | IC50 | - | — | - | |
| CHEMBL4742973 | — | IC50 | - | — | - | |
| CHEMBL4755607 | — | IC50 | - | — | - | |
| CHEMBL4783353 | — | IC50 | - | — | - | |
| CHEMBL4750875 | — | IC50 | - | — | - | |
| CHEMBL4777399 | — | IC50 | - | — | - |