Assay Detail
Binding
CHEMBL5735388
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PI3K-delta Selective Assay: A compound's ability in selectively inhibiting PI3K-δ can be assessed using RAJI cells, i.e., B lymphocyte cells derived from lymphoma patients. Briefly, serum-starved RAJI cells are stimulated with anti-human IgM, thereby causing signaling through the B-cell receptors, as described in, for example, He et al., Leukemia Research (2009) 33: 798-802. B-cell receptor signaling is important for the activation, differentiation, and survival of B cells and certain B-cell derived cancers. Reduction of phospho-AKT is indicative of compounds that may inhibit B-cell proliferation and function in certain diseases. By monitoring the reduction of phospho-AKT in stimulated RAJI cells (using for example, phospho-AKT antibodies), a compound's potential efficacy in selectively inhibiting PI3Kδ can be assessed.
258
Total Activities
86
Compounds Tested
3
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 delta isoform (CHEMBL3130) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Heterocyclic compounds and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 86 | 5.40 | 5.40 |
| kon | 86 | - | - |
| k_off | 86 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6051763 | — | — | 3 | 5.40 |
| CHEMBL5796536 | — | — | 3 | 5.40 |
| CHEMBL5791000 | — | — | 3 | 5.40 |
| CHEMBL5750806 | — | — | 3 | 5.40 |
| CHEMBL5851176 | — | — | 3 | 5.40 |
| CHEMBL5936480 | — | — | 3 | 5.40 |
| CHEMBL5764062 | — | — | 3 | 5.40 |
| CHEMBL5866941 | — | — | 3 | 5.40 |
| CHEMBL5929894 | — | — | 3 | 5.40 |
| CHEMBL5913203 | — | — | 3 | 5.40 |
| CHEMBL5861424 | — | — | 3 | 5.40 |
| CHEMBL5880726 | — | — | 3 | 5.40 |
| CHEMBL5740069 | — | — | 3 | 5.40 |
| CHEMBL5899739 | — | — | 3 | 5.40 |
| CHEMBL5941496 | — | — | 3 | 5.40 |
| CHEMBL6032645 | — | — | 3 | 5.40 |
| CHEMBL5807905 | — | — | 3 | 5.40 |
| CHEMBL3923629 | — | — | 3 | 5.40 |
| CHEMBL5973275 | — | — | 3 | 5.40 |
| CHEMBL6021741 | — | — | 3 | 5.40 |
| CHEMBL5762937 | — | — | 3 | 5.40 |
| CHEMBL5796587 | — | — | 3 | 5.40 |
| CHEMBL3895629 | — | — | 3 | 5.40 |
| CHEMBL5935134 | — | — | 3 | 5.40 |
| CHEMBL5838632 | — | — | 3 | 5.40 |
| CHEMBL5909018 | — | — | 3 | 5.40 |
| CHEMBL5863742 | — | — | 3 | 5.40 |
| CHEMBL5991752 | — | — | 3 | 5.40 |
| CHEMBL5743380 | — | — | 3 | 5.40 |
| CHEMBL5979518 | — | — | 3 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5898042 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6041044 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3955769 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6063648 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5741547 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5829946 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5965024 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5935134 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6059381 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5740488 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5889102 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5923197 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5867332 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5838632 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5922586 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6015850 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5992887 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3895629 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6013589 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5913203 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5953253 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5929894 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3928146 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5790749 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5798011 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5900678 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5991752 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5971164 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5974586 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5743380 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6011851 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6053354 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5860579 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5979518 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5863742 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5789934 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6021741 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3893430 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5900338 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5935368 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5933124 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5909018 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3914602 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6007856 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3946030 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5910358 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6050868 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5745833 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3921445 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5900412 | — | IC50 | = | 4000.0 | nM | 5.40 |