Assay Detail
Binding
CHEMBL4673080
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Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in anti-IgM-induced AKT phosphorylation at Ser473 residue preincubated for 20 mins followed by anti-IgM stimulation for 30 mins
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| 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
Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.93 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4792586 | — | — | 1 | 7.64 |
| CHEMBL4795757 | — | — | 1 | 7.58 |
| CHEMBL4754014 | — | — | 1 | 7.52 |
| CHEMBL4787672 | — | — | 1 | 7.50 |
| CHEMBL4452905 | — | — | 1 | 7.32 |
| CHEMBL4757468 | — | — | 1 | 7.26 |
| CHEMBL4753205 | — | — | 1 | 7.16 |
| CHEMBL4776201 | — | — | 1 | 7.15 |
| CHEMBL4743715 | — | — | 1 | 7.14 |
| CHEMBL4762936 | — | — | 1 | 7.07 |
| CHEMBL4781592 | — | — | 1 | 7.00 |
| CHEMBL4748947 | — | — | 1 | 6.96 |
| CHEMBL4761378 | — | — | 1 | 6.96 |
| CHEMBL4744546 | — | — | 1 | 6.92 |
| CHEMBL4779781 | — | — | 1 | 6.89 |
| CHEMBL4745502 | — | — | 1 | 6.75 |
| CHEMBL4745624 | — | — | 1 | 6.72 |
| CHEMBL4778656 | — | — | 1 | 6.72 |
| CHEMBL4743750 | — | — | 1 | 6.70 |
| CHEMBL4750385 | — | — | 1 | 6.70 |
| CHEMBL4745746 | — | — | 1 | 6.70 |
| CHEMBL4750236 | — | — | 1 | 6.64 |
| CHEMBL4791004 | — | — | 1 | 6.60 |
| CHEMBL4800086 | — | — | 1 | 6.50 |
| CHEMBL4781485 | — | — | 1 | 6.36 |
| CHEMBL4800583 | — | — | 1 | 6.35 |
| CHEMBL4744508 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4792586 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4795757 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4754014 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4787672 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4452905 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4757468 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4753205 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4776201 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4743715 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4762936 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4781592 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4748947 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4761378 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4744546 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4779781 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4745502 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4745624 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4778656 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4743750 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4750385 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4745746 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4750236 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4791004 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4800086 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4781485 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4800583 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4744508 | — | IC50 | = | 570.0 | nM | 6.24 |