Assay Detail
Binding
CHEMBL5337152
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis
35
Total Activities
25
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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 |
|---|---|---|---|
| EC50 | 31 | 4.91 | 6.36 |
| pEC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1982368 | — | — | 2 | 6.36 |
| CHEMBL1230640 | — | — | 2 | 5.00 |
| CHEMBL3183531 | — | — | 2 | 4.80 |
| CHEMBL4475458 | — | — | 2 | 4.62 |
| CHEMBL1398529 | — | — | 1 | 4.28 |
| CHEMBL3646117 | — | — | 2 | 4.10 |
| CHEMBL3186774 | — | — | 1 | - |
| CHEMBL426560 | — | — | 1 | - |
| CHEMBL4163812 | — | — | 1 | - |
| CHEMBL3646118 | MOLIDUSTAT | 2.0 | 2 | - |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | - |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | - |
| CHEMBL1601133 | — | — | 1 | - |
| CHEMBL4078388 | — | — | 1 | - |
| CHEMBL4454253 | — | — | 1 | - |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | - |
| CHEMBL1234242 | — | — | 1 | - |
| CHEMBL597779 | — | — | 1 | - |
| CHEMBL92309 | — | — | 2 | - |
| CHEMBL5415330 | — | — | 1 | - |
| CHEMBL4877741 | — | — | 2 | - |
| CHEMBL1215657 | — | — | 1 | - |
| CHEMBL556489 | DIMETHYL SUCCINATE | — | 2 | - |
| CHEMBL2107333 | DIMETHYL FUMARATE | 4.0 | 2 | - |
| CHEMBL4216044 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1982368 | — | EC50 | = | 436.52 | nM | 6.36 |
| CHEMBL1982368 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1230640 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1230640 | — | EC50 | = | 10232.93 | nM | 4.99 |
| CHEMBL3183531 | — | EC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3183531 | — | EC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4475458 | — | EC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL4475458 | — | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL1398529 | — | EC50 | = | 52480.75 | nM | 4.28 |
| CHEMBL3646117 | — | EC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL3646117 | — | EC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL1234242 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL483254 | PANOBINOSTAT | EC50 | > | 1000000.0 | nM | - |
| CHEMBL4454253 | — | pEC50 | - | — | - | |
| CHEMBL4078388 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL4216044 | — | pEC50 | - | — | - | |
| CHEMBL1601133 | — | pEC50 | - | — | - | |
| CHEMBL3646221 | VADADUSTAT | EC50 | > | 1000000.0 | nM | - |
| CHEMBL2338329 | ROXADUSTAT | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3646118 | MOLIDUSTAT | EC50 | ~ | 100000.0 | nM | - |
| CHEMBL4163812 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL426560 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3186774 | — | EC50 | >= | 1000000.0 | nM | - |
| CHEMBL92309 | — | EC50 | = | 109647.82 | nM | - |
| CHEMBL5415330 | — | EC50 | = | 1479108.39 | nM | - |
| CHEMBL4877741 | — | EC50 | = | 6760829.75 | nM | - |
| CHEMBL2107333 | DIMETHYL FUMARATE | EC50 | = | 316000.0 | nM | - |
| CHEMBL556489 | DIMETHYL SUCCINATE | EC50 | ~ | 3500000.0 | nM | - |
| CHEMBL4877741 | — | EC50 | ~ | 6700000.0 | nM | - |
| CHEMBL92309 | — | EC50 | = | 110000.0 | nM | - |
| CHEMBL3646118 | MOLIDUSTAT | EC50 | ~ | 100000.0 | nM | - |
| CHEMBL2107333 | DIMETHYL FUMARATE | EC50 | = | 316227.77 | nM | - |
| CHEMBL556489 | DIMETHYL SUCCINATE | EC50 | = | 3467368.5 | nM | - |
| CHEMBL597779 | — | pEC50 | - | — | - | |
| CHEMBL1215657 | — | EC50 | > | 1000000.0 | nM | - |