Assay Detail
Binding
CHEMBL5524258
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 3 x GGGGS linker) expressed in Escherichia coli BL21 (DE3) using 5-methylcytosine as substrate preincubated for 10 mins followed by substrate and DNA-cofactor addition measured after 12 mins by SPE-MS analysis
18
Total Activities
18
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.44 | 6.26 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230640 | — | — | 1 | 6.26 |
| CHEMBL5560200 | — | — | 1 | 5.66 |
| CHEMBL5557957 | — | — | 1 | 5.61 |
| CHEMBL5549950 | — | — | 1 | 5.60 |
| CHEMBL5561920 | — | — | 1 | 5.55 |
| CHEMBL5561497 | — | — | 1 | 5.54 |
| CHEMBL5532540 | — | — | 1 | 5.52 |
| CHEMBL5549844 | — | — | 1 | 5.51 |
| CHEMBL5563232 | — | — | 1 | 5.50 |
| CHEMBL5557587 | — | — | 1 | 5.47 |
| CHEMBL5564980 | — | — | 1 | 5.44 |
| CHEMBL5562105 | — | — | 1 | 5.40 |
| CHEMBL5557372 | — | — | 1 | 5.27 |
| CHEMBL5557793 | — | — | 1 | 5.19 |
| CHEMBL5561894 | — | — | 1 | 4.85 |
| CHEMBL5564944 | — | — | 1 | 4.62 |
| CHEMBL5542589 | — | — | 1 | - |
| CHEMBL5567655 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230640 | — | IC50 | = | 549.54 | nM | 6.26 |
| CHEMBL5560200 | — | IC50 | = | 2187.76 | nM | 5.66 |
| CHEMBL5557957 | — | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL5549950 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL5561920 | — | IC50 | = | 2818.38 | nM | 5.55 |
| CHEMBL5561497 | — | IC50 | = | 2884.03 | nM | 5.54 |
| CHEMBL5532540 | — | IC50 | = | 3019.95 | nM | 5.52 |
| CHEMBL5549844 | — | IC50 | = | 3090.3 | nM | 5.51 |
| CHEMBL5563232 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5557587 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL5564980 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL5562105 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL5557372 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL5557793 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL5561894 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL5564944 | — | IC50 | = | 23988.33 | nM | 4.62 |
| CHEMBL5542589 | — | pIC50 | - | — | - | |
| CHEMBL5567655 | — | IC50 | ~ | 10000.0 | nM | - |