Assay Detail
Binding
CHEMBL5337156
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of tetracyclin/Dox-inducible N-terminal 3xFLAG tagged human TET2 catalytic domain (1129 to 2002 residues) expressed in human U2OS cells assessed as reduction in 5-hydroxymethylcytosine level incubated for 24 hrs by immunofluorescence analysis
7
Total Activities
4
Compounds Tested
1
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 | 7 | 5.06 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230640 | — | — | 2 | 5.16 |
| CHEMBL92309 | — | — | 2 | 4.96 |
| CHEMBL5436751 | — | — | 1 | - |
| CHEMBL5415330 | — | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230640 | — | EC50 | = | 6918.31 | nM | 5.16 |
| CHEMBL1230640 | — | EC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL92309 | — | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL92309 | — | EC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL5436751 | — | EC50 | > | 3162277.66 | nM | - |
| CHEMBL5415330 | — | EC50 | = | 131825.67 | nM | - |
| CHEMBL5415330 | — | EC50 | = | 131000.0 | nM | - |