Assay Detail
Binding
CHEMBL5337146
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of N-terminal His-tagged recombinant human TET2 catalytic domain LCIdel mutant (D1129 to G1936 residues with Y1481 to N1843 replaced by a 3 x GGGGS linker) expressed in Escherichia coli BL21 (DE3) 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 |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 5.07 | 5.22 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1615211 | — | — | 1 | 5.22 |
| CHEMBL1614745 | — | — | 1 | 4.92 |
| CHEMBL1230640 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1615211 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL1614745 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL1230640 | — | Inhibition | - | % | - |