Assay Detail
Binding
CHEMBL1914129
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Inhibition of mouse recombinant PI3K p110alpha expressed in Sf21 insect cells using phosphatidylinositol as substrate after 1 hr by phosphoimaging
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (CHEMBL2499) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
Synthesis and biological evaluation of novel analogues of the pan class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole (ZSTK474).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.34 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1911117 | — | — | 1 | 9.66 |
| CHEMBL1910998 | — | — | 1 | 9.05 |
| CHEMBL1911122 | — | — | 1 | 8.82 |
| CHEMBL1911118 | — | — | 1 | 8.70 |
| CHEMBL1911000 | — | — | 1 | 8.57 |
| CHEMBL1910999 | — | — | 1 | 8.57 |
| CHEMBL1911125 | — | — | 1 | 8.40 |
| CHEMBL1911005 | — | — | 1 | 8.32 |
| CHEMBL1911123 | — | — | 1 | 8.29 |
| CHEMBL1911119 | — | — | 1 | 8.10 |
| CHEMBL586702 | ZSTK-474 | 2.0 | 1 | 8.07 |
| CHEMBL1911009 | — | — | 1 | 8.03 |
| CHEMBL1909655 | — | — | 1 | 7.80 |
| CHEMBL1911002 | — | — | 1 | 7.58 |
| CHEMBL1911008 | — | — | 1 | 7.57 |
| CHEMBL1911001 | — | — | 1 | 7.55 |
| CHEMBL1911121 | — | — | 1 | 7.52 |
| CHEMBL1911115 | — | — | 1 | 7.50 |
| CHEMBL1910990 | — | — | 1 | 7.47 |
| CHEMBL1911114 | — | — | 1 | 7.43 |
| CHEMBL1911116 | — | — | 1 | 7.24 |
| CHEMBL1911013 | — | — | 1 | 7.21 |
| CHEMBL1911124 | — | — | 1 | 7.06 |
| CHEMBL1910989 | — | — | 1 | 6.84 |
| CHEMBL1910993 | — | — | 1 | 6.77 |
| CHEMBL1910991 | — | — | 1 | 6.70 |
| CHEMBL1910997 | — | — | 1 | 6.69 |
| CHEMBL1911006 | — | — | 1 | 6.68 |
| CHEMBL1910988 | — | — | 1 | 6.58 |
| CHEMBL1911011 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1911117 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL1910998 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1911122 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1911118 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1911000 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1910999 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1911125 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1911005 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1911123 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1911119 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL586702 | ZSTK-474 | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL1911009 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1909655 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1911002 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1911008 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1911001 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1911121 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1911115 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1910990 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1911114 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL1911116 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL1911013 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL1911124 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL1910989 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL1910993 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1910991 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL1910997 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL1911006 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1910988 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL1911011 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL1911004 | — | IC50 | = | 294.0 | nM | 6.53 |
| CHEMBL1911015 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL1911003 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL1910995 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1911014 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1910994 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1911120 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL1910996 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1911007 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL1911012 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1911010 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1910992 | — | IC50 | > | 1000.0 | nM | - |