Assay Detail
Binding
CHEMBL2215896
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Inhibition of PI3Kdelta assessed as change in pIC50 by kinobeads assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.10 | 5.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2064571 | — | — | 1 | 5.10 |
| CHEMBL2205764 | — | — | 1 | - |
| CHEMBL2205763 | — | — | 1 | - |
| CHEMBL2205767 | — | — | 1 | - |
| CHEMBL2205771 | — | — | 1 | - |
| CHEMBL2205770 | — | — | 1 | - |
| CHEMBL2205769 | — | — | 1 | - |
| CHEMBL2205774 | — | — | 1 | - |
| CHEMBL2205772 | — | — | 1 | - |
| CHEMBL2205768 | — | — | 1 | - |
| CHEMBL2205765 | — | — | 1 | - |
| CHEMBL2205773 | — | — | 1 | - |
| CHEMBL2203312 | — | — | 1 | - |
| CHEMBL2205766 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2064571 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL2205764 | — | IC50 | < | 19952623.15 | nM | - |
| CHEMBL2205763 | — | IC50 | = | 7943282.35 | nM | - |
| CHEMBL2205767 | — | IC50 | = | 7943282.35 | nM | - |
| CHEMBL2205771 | — | IC50 | = | 12589254.12 | nM | - |
| CHEMBL2205770 | — | IC50 | = | 19952623.15 | nM | - |
| CHEMBL2205769 | — | IC50 | = | 25118864.32 | nM | - |
| CHEMBL2205774 | — | IC50 | = | 25118864.32 | nM | - |
| CHEMBL2205772 | — | IC50 | = | 31622776.6 | nM | - |
| CHEMBL2205768 | — | IC50 | = | 31622776.6 | nM | - |
| CHEMBL2205765 | — | IC50 | = | 31622776.6 | nM | - |
| CHEMBL2205773 | — | IC50 | = | 31622776.6 | nM | - |
| CHEMBL2203312 | — | IC50 | = | 39810717.06 | nM | - |
| CHEMBL2205766 | — | IC50 | = | 50118723.36 | nM | - |