Assay Detail
Binding
CHEMBL5337138
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 3xFlag-tagged human TET1 catalytic domain (E1418 to V2136 residues) expressed in Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by DNA-cofactor addition and measured after 30 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 | 5.30 | 6.08 |
| pIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230640 | — | — | 1 | 6.08 |
| CHEMBL1398529 | — | — | 1 | 5.89 |
| CHEMBL316034 | — | — | 1 | 5.77 |
| CHEMBL4475458 | — | — | 1 | 5.42 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 2 | 5.38 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 5.20 |
| CHEMBL1982368 | — | — | 1 | 5.13 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 2 | 4.89 |
| CHEMBL3646117 | — | — | 2 | 4.77 |
| CHEMBL1615211 | — | — | 2 | - |
| CHEMBL1614745 | — | — | 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 | - |
| CHEMBL3188597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230640 | — | IC50 | = | 831.76 | nM | 6.08 |
| CHEMBL1398529 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL316034 | — | IC50 | = | 1698.24 | nM | 5.77 |
| CHEMBL4475458 | — | IC50 | = | 3801.89 | nM | 5.42 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL1982368 | — | IC50 | = | 7413.1 | nM | 5.13 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL3646117 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3646117 | — | IC50 | = | 17378.01 | nM | 4.76 |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 117489.76 | nM | - |
| CHEMBL1234242 | — | pIC50 | - | — | - | |
| CHEMBL597779 | — | pIC50 | - | — | - | |
| CHEMBL4877741 | — | pIC50 | - | — | - | |
| CHEMBL1614745 | — | IC50 | = | 676082.98 | nM | - |
| CHEMBL1615211 | — | IC50 | = | 1047128.55 | nM | - |
| CHEMBL1615211 | — | IC50 | ~ | 800000.0 | nM | - |
| CHEMBL1614745 | — | IC50 | ~ | 800000.0 | nM | - |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 118000.0 | nM | - |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 118000.0 | nM | - |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 190546.07 | nM | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL426560 | — | IC50 | >= | 100000.0 | nM | - |
| 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 | - |
| CHEMBL3186774 | — | IC50 | >= | 100000.0 | nM | - |