Assay Detail
Binding
CHEMBL5337141
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 and measured after 10 mins by Alphascreen assay
18
Total Activities
16
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 |
|---|---|---|---|
| IC50 | 15 | 5.31 | 6.09 |
| pIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1398529 | — | — | 1 | 6.09 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 1 | 5.68 |
| CHEMBL1230640 | — | — | 1 | 5.59 |
| CHEMBL1982368 | — | — | 1 | 5.45 |
| CHEMBL4475458 | — | — | 1 | 5.33 |
| CHEMBL1615211 | — | — | 2 | 5.22 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 5.21 |
| CHEMBL1614745 | — | — | 2 | 5.14 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 1 | 5.12 |
| CHEMBL316034 | — | — | 1 | 5.01 |
| CHEMBL3646117 | — | — | 1 | 4.80 |
| CHEMBL576 | SUCCINIC ACID | 3.0 | 1 | - |
| CHEMBL503160 | FUMARIC ACID | 3.0 | 1 | - |
| CHEMBL1234242 | — | — | 1 | - |
| CHEMBL597779 | — | — | 1 | - |
| CHEMBL4877741 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1398529 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL1230640 | — | IC50 | = | 2570.4 | nM | 5.59 |
| CHEMBL1982368 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL4475458 | — | IC50 | = | 4677.35 | nM | 5.33 |
| CHEMBL1615211 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 6165.95 | nM | 5.21 |
| CHEMBL1615211 | — | IC50 | = | 6165.95 | nM | 5.21 |
| CHEMBL1614745 | — | IC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL1614745 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 7585.78 | nM | 5.12 |
| CHEMBL316034 | — | IC50 | = | 9772.37 | nM | 5.01 |
| CHEMBL3646117 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 104712.85 | nM | - |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 158489.32 | nM | - |
| CHEMBL1234242 | — | pIC50 | - | — | - | |
| CHEMBL597779 | — | pIC50 | - | — | - | |
| CHEMBL4877741 | — | pIC50 | - | — | - |