Assay Detail
Binding
CHEMBL5337140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TET3 catalytic domain (E824 to I1795 residues) expressed in mammalian cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 10 mins by Alphascreen assay
34
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 29 | 5.29 | 6.11 |
| pIC50 | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316034 | — | — | 1 | 6.11 |
| CHEMBL1398529 | — | — | 1 | 5.90 |
| CHEMBL1230640 | — | — | 1 | 5.57 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 2 | 5.42 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 5.26 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 2 | 5.16 |
| CHEMBL1982368 | — | — | 1 | 5.01 |
| CHEMBL1614745 | — | — | 2 | 4.02 |
| CHEMBL4475458 | — | — | 1 | - |
| CHEMBL3188597 | — | — | 2 | - |
| CHEMBL1615211 | — | — | 2 | - |
| 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 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316034 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL1398529 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL1230640 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 4677.35 | nM | 5.33 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1982368 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL1614745 | — | IC50 | = | 95499.26 | nM | 4.02 |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 118000.0 | nM | - |
| CHEMBL4475458 | — | pIC50 | - | — | - | |
| CHEMBL1614745 | — | IC50 | ~ | 100000.0 | nM | - |
| CHEMBL1615211 | — | IC50 | ~ | 100000.0 | nM | - |
| CHEMBL3188597 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4877741 | — | pIC50 | - | — | - | |
| CHEMBL597779 | — | pIC50 | - | — | - | |
| CHEMBL1234242 | — | pIC50 | - | — | - | |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 194984.46 | nM | - |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 245470.89 | nM | - |
| CHEMBL1615211 | — | IC50 | = | 104712.85 | nM | - |
| CHEMBL3188597 | — | pIC50 | - | — | - | |
| CHEMBL4078388 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4216044 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2338329 | ROXADUSTAT | IC50 | >= | 100000.0 | nM | - |
| CHEMBL2338329 | ROXADUSTAT | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4163812 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4163812 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL426560 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL426560 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL4454253 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 118000.0 | nM | - |