Assay Detail
Binding
CHEMBL5337150
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'-ACCAC5mCGGTGGT-3' as DNA substrate preincubated for 10 mins followed by DNA substrate addition and measured after 10 mins by SPE-MS analysis
23
Total Activities
19
Compounds Tested
3
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 | 16 | 5.29 | 6.30 |
| deltapIC50 | 4 | - | - |
| pIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL90852 | N-OXALYLGLYCINE | — | 2 | 6.30 |
| CHEMBL1614745 | — | — | 1 | 5.93 |
| CHEMBL1615211 | — | — | 1 | 5.87 |
| CHEMBL316034 | — | — | 1 | 5.82 |
| CHEMBL1230640 | — | — | 2 | 5.77 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 5.69 |
| CHEMBL426560 | — | — | 1 | 5.29 |
| CHEMBL4475458 | — | — | 1 | 5.25 |
| CHEMBL503160 | FUMARIC ACID | 3.0 | 1 | 5.03 |
| CHEMBL576 | SUCCINIC ACID | 3.0 | 1 | 4.83 |
| CHEMBL3186774 | — | — | 1 | 4.78 |
| CHEMBL1398529 | — | — | 2 | 4.74 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 2 | 4.62 |
| CHEMBL3646117 | — | — | 1 | 4.52 |
| CHEMBL4163812 | — | — | 1 | 4.38 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | - |
| CHEMBL3188597 | — | — | 1 | - |
| CHEMBL4877741 | — | — | 1 | - |
| CHEMBL1982368 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL1614745 | — | IC50 | = | 1174.9 | nM | 5.93 |
| CHEMBL1615211 | — | IC50 | = | 1348.96 | nM | 5.87 |
| CHEMBL316034 | — | IC50 | = | 1513.56 | nM | 5.82 |
| CHEMBL1230640 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL1230640 | — | IC50 | = | 1737.8 | nM | 5.76 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 2041.74 | nM | 5.69 |
| CHEMBL426560 | — | IC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL4475458 | — | IC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL503160 | FUMARIC ACID | IC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL576 | SUCCINIC ACID | IC50 | = | 14791.08 | nM | 4.83 |
| CHEMBL3186774 | — | IC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL1398529 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL483254 | PANOBINOSTAT | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL3646117 | — | IC50 | = | 30199.52 | nM | 4.52 |
| CHEMBL4163812 | — | IC50 | = | 41686.94 | nM | 4.38 |
| CHEMBL1398529 | — | deltapIC50 | = | -1.35 | — | - |
| CHEMBL1982368 | — | deltapIC50 | = | -1.43 | — | - |
| CHEMBL483254 | PANOBINOSTAT | deltapIC50 | = | -1.06 | — | - |
| CHEMBL90852 | N-OXALYLGLYCINE | deltapIC50 | = | 1.18 | — | - |
| CHEMBL4877741 | — | pIC50 | - | — | - | |
| CHEMBL3188597 | — | pIC50 | - | — | - | |
| CHEMBL2338329 | ROXADUSTAT | pIC50 | - | — | - |