Assay Detail
Binding
CHEMBL5337139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His10-FLAG tagged human TET2 catalytic domain (Q969 to I2002 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay
35
Total Activities
24
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 5.15 | 5.81 |
| pIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1398529 | — | — | 1 | 5.81 |
| CHEMBL1982368 | — | — | 1 | 5.52 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 2 | 5.42 |
| CHEMBL1230640 | — | — | 1 | 5.31 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 5.30 |
| CHEMBL316034 | — | — | 1 | 5.29 |
| CHEMBL4475458 | — | — | 1 | 5.26 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 2 | 5.05 |
| CHEMBL1615211 | — | — | 2 | 4.89 |
| CHEMBL1614745 | — | — | 2 | 4.89 |
| CHEMBL3646117 | — | — | 2 | 4.73 |
| CHEMBL576 | SUCCINIC ACID | 3.0 | 2 | - |
| CHEMBL503160 | FUMARIC ACID | 3.0 | 2 | - |
| CHEMBL1234242 | — | — | 1 | - |
| CHEMBL597779 | — | — | 1 | - |
| CHEMBL4877741 | — | — | 1 | - |
| CHEMBL3186774 | — | — | 2 | - |
| CHEMBL426560 | — | — | 2 | - |
| CHEMBL4163812 | — | — | 2 | - |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 2 | - |
| CHEMBL4216044 | — | — | 1 | - |
| CHEMBL4078388 | — | — | 1 | - |
| CHEMBL4454253 | — | — | 1 | - |
| CHEMBL3188597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1398529 | — | IC50 | = | 1548.82 | nM | 5.81 |
| CHEMBL1982368 | — | IC50 | = | 3019.95 | nM | 5.52 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1230640 | — | IC50 | = | 4897.79 | nM | 5.31 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL316034 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL4475458 | — | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1615211 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1614745 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1615211 | — | IC50 | = | 12882.5 | nM | 4.89 |
| CHEMBL1614745 | — | IC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL3646117 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL3646117 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL597779 | — | pIC50 | - | — | - | |
| CHEMBL1234242 | — | pIC50 | - | — | - | |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 204173.79 | nM | - |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 138038.43 | nM | - |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 118000.0 | nM | - |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 118000.0 | nM | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4877741 | — | pIC50 | - | — | - | |
| CHEMBL426560 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4163812 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4163812 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL2338329 | ROXADUSTAT | IC50 | >= | 100000.0 | nM | - |
| CHEMBL2338329 | ROXADUSTAT | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4216044 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4078388 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4454253 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3188597 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL426560 | — | IC50 | >= | 100000.0 | nM | - |