Assay Detail
Binding
CHEMBL4822200
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GST-tagged TET2 (1099 to 1936 residues) expressed in Escherichia coli BL21 (DE3)pLysS assessed as reduction in 5hmc level incubated for 2 hrs by ELISA
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.79 | 5.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4851104 | — | — | 1 | 5.03 |
| CHEMBL4860506 | — | — | 1 | 4.98 |
| CHEMBL4872110 | — | — | 1 | 4.96 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 1 | 4.71 |
| CHEMBL4855677 | — | — | 1 | 4.26 |
| CHEMBL4870693 | — | — | 1 | - |
| CHEMBL4859276 | — | — | 1 | - |
| CHEMBL4847806 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4851104 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4860506 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL4872110 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL4855677 | — | IC50 | = | 54800.0 | nM | 4.26 |
| CHEMBL4870693 | — | IC50 | = | 261500.0 | nM | - |
| CHEMBL4859276 | — | IC50 | = | 108300.0 | nM | - |
| CHEMBL4847806 | — | IC50 | = | 106600.0 | nM | - |