Assay Detail
Binding
CHEMBL5337147
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Competitive 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 in presence of 2-OG and measured after 10 mins by Alphascreen assay
3
Total Activities
3
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 |
|---|---|---|---|
| Ki | 2 | 4.68 | 4.72 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1615211 | — | — | 1 | 4.72 |
| CHEMBL1614745 | — | — | 1 | 4.64 |
| CHEMBL1230640 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1615211 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL1614745 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL1230640 | — | Inhibition | - | % | - |