Assay Detail
Binding
CHEMBL2215893
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Inhibition of PI3Kgamma 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 gamma isoform (CHEMBL3267) ↗| 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 | 7.59 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2205771 | — | — | 1 | 8.10 |
| CHEMBL2205766 | — | — | 1 | 7.90 |
| CHEMBL2205763 | — | — | 1 | 7.80 |
| CHEMBL2205768 | — | — | 1 | 7.70 |
| CHEMBL2205767 | — | — | 1 | 7.70 |
| CHEMBL2205773 | — | — | 1 | 7.70 |
| CHEMBL2064571 | — | — | 1 | 7.60 |
| CHEMBL2205772 | — | — | 1 | 7.60 |
| CHEMBL2205765 | — | — | 1 | 7.60 |
| CHEMBL2205774 | — | — | 1 | 7.60 |
| CHEMBL2205764 | — | — | 1 | 7.50 |
| CHEMBL2205769 | — | — | 1 | 7.40 |
| CHEMBL2203312 | — | — | 1 | 7.10 |
| CHEMBL2205770 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2205771 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL2205766 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL2205763 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2205768 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2205767 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2205773 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2064571 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2205772 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2205765 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2205774 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL2205764 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2205769 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL2203312 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL2205770 | — | IC50 | = | 100.0 | nM | 7.00 |