Assay Detail
Binding
CHEMBL4274857
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of SHIP2 (unknown origin) assessed as decrease in PIP2 production using PtdIns(3,4,5)P3 as substrate preincubated for 20 mins followed by substrate addition measured for 50 mins by malachite green staining based assay
51
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase 2 (CHEMBL2331064) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of crizotinib derivatives as potent SHIP2 inhibitors for the treatment of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 4.99 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4287228 | — | — | 2 | 5.70 |
| CHEMBL4282693 | — | — | 1 | 5.70 |
| CHEMBL4285629 | — | — | 1 | 5.50 |
| CHEMBL4286681 | — | — | 1 | 5.43 |
| CHEMBL4286790 | — | — | 1 | 5.43 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.26 |
| CHEMBL4285693 | — | — | 1 | 5.23 |
| CHEMBL4277817 | — | — | 1 | 5.07 |
| CHEMBL4286383 | — | — | 1 | 5.03 |
| CHEMBL4279295 | — | — | 2 | 4.92 |
| CHEMBL4283903 | — | — | 1 | 4.92 |
| CHEMBL4291073 | — | — | 1 | 4.92 |
| CHEMBL4286747 | — | — | 1 | 4.92 |
| CHEMBL4290198 | — | — | 1 | 4.92 |
| CHEMBL4282526 | — | — | 1 | 4.89 |
| CHEMBL4292049 | — | — | 1 | 4.84 |
| CHEMBL4293128 | — | — | 1 | 4.80 |
| CHEMBL4289152 | — | — | 2 | 4.77 |
| CHEMBL4284852 | — | — | 1 | 4.73 |
| CHEMBL4278517 | — | — | 1 | 4.70 |
| CHEMBL4281770 | — | — | 1 | 4.66 |
| CHEMBL4294032 | — | — | 2 | 4.52 |
| CHEMBL4292124 | — | — | 2 | 4.41 |
| CHEMBL4294694 | — | — | 1 | - |
| CHEMBL4292732 | — | — | 1 | - |
| CHEMBL4288660 | — | — | 1 | - |
| CHEMBL4287404 | — | — | 1 | - |
| CHEMBL4279492 | — | — | 1 | - |
| CHEMBL4281849 | — | — | 1 | - |
| CHEMBL4279891 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4287228 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4282693 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4287228 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4285629 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4286681 | — | IC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL4286790 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL601719 | CRIZOTINIB | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4285693 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4277817 | — | IC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL4286383 | — | IC50 | = | 9280.0 | nM | 5.03 |
| CHEMBL4283903 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4279295 | — | IC50 | = | 11939.99 | nM | 4.92 |
| CHEMBL4279295 | — | IC50 | = | 11940.0 | nM | 4.92 |
| CHEMBL4291073 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4286747 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4290198 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4282526 | — | IC50 | = | 12800.0 | nM | 4.89 |
| CHEMBL4292049 | — | IC50 | = | 14500.0 | nM | 4.84 |
| CHEMBL4293128 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL4289152 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4289152 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL4284852 | — | IC50 | = | 18800.0 | nM | 4.73 |
| CHEMBL4278517 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4281770 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL4294032 | — | IC50 | = | 30240.01 | nM | 4.52 |
| CHEMBL4294032 | — | IC50 | = | 30240.0 | nM | 4.52 |
| CHEMBL4292124 | — | IC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL4292124 | — | IC50 | = | 38900.04 | nM | 4.41 |
| CHEMBL4279541 | — | IC50 | - | — | - | |
| CHEMBL4291287 | — | IC50 | - | — | - | |
| CHEMBL4283441 | — | IC50 | - | — | - | |
| CHEMBL4287100 | — | IC50 | - | — | - | |
| CHEMBL4293975 | — | IC50 | - | — | - | |
| CHEMBL4293596 | — | IC50 | - | — | - | |
| CHEMBL4279866 | — | IC50 | - | — | - | |
| CHEMBL4293925 | — | IC50 | - | — | - | |
| CHEMBL4283330 | — | IC50 | - | — | - | |
| CHEMBL4278773 | — | IC50 | - | — | - | |
| CHEMBL4283016 | — | IC50 | - | — | - | |
| CHEMBL4285911 | — | IC50 | - | — | - | |
| CHEMBL4290206 | — | IC50 | - | — | - | |
| CHEMBL4294481 | — | IC50 | - | — | - | |
| CHEMBL4278466 | — | IC50 | - | — | - | |
| CHEMBL4280444 | — | IC50 | - | — | - | |
| CHEMBL4292732 | — | IC50 | - | — | - | |
| CHEMBL4288660 | — | IC50 | - | — | - | |
| CHEMBL4287404 | — | IC50 | - | — | - | |
| CHEMBL4279492 | — | IC50 | - | — | - | |
| CHEMBL4281849 | — | IC50 | - | — | - | |
| CHEMBL4279891 | — | IC50 | - | — | - |