Assay Detail
Binding
CHEMBL5524259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human TET3 catalytic domain (E824 to I1795 residues) expressed in baculovirus infected Sf9 cells using 5-methylcytosine as substrate preincubated for 10 mins followed by substrate and DNA-cofactor addition measured after 10 mins by Alphascreen assay
37
Total Activities
35
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 36 | 5.28 | 6.74 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5527999 | — | — | 2 | 6.74 |
| CHEMBL5561920 | — | — | 1 | 6.30 |
| CHEMBL5561497 | — | — | 1 | 6.20 |
| CHEMBL5562105 | — | — | 1 | 6.16 |
| CHEMBL1230640 | — | — | 1 | 6.01 |
| CHEMBL5532540 | — | — | 1 | 5.99 |
| CHEMBL5557587 | — | — | 1 | 5.86 |
| CHEMBL5557793 | — | — | 1 | 5.62 |
| CHEMBL5557957 | — | — | 1 | 5.62 |
| CHEMBL5549844 | — | — | 1 | 5.57 |
| CHEMBL5567655 | — | — | 1 | 5.56 |
| CHEMBL5559263 | — | — | 1 | 5.51 |
| CHEMBL5564944 | — | — | 1 | 5.45 |
| CHEMBL5566835 | — | — | 1 | 5.28 |
| CHEMBL5557372 | — | — | 1 | 5.23 |
| CHEMBL5563232 | — | — | 1 | 5.22 |
| CHEMBL5556063 | — | — | 1 | 5.20 |
| CHEMBL5564005 | — | — | 1 | 4.96 |
| CHEMBL5563922 | — | — | 1 | 4.86 |
| CHEMBL5560439 | — | — | 1 | 4.82 |
| CHEMBL5557758 | — | — | 1 | 4.81 |
| CHEMBL5542479 | — | — | 1 | 4.80 |
| CHEMBL5558323 | — | — | 1 | 4.79 |
| CHEMBL5561894 | — | — | 1 | 4.74 |
| CHEMBL5563415 | — | — | 1 | 4.69 |
| CHEMBL5562605 | — | — | 1 | 4.63 |
| CHEMBL5542589 | — | — | 1 | 4.51 |
| CHEMBL5564980 | — | — | 1 | 4.50 |
| CHEMBL5560200 | — | — | 1 | 4.33 |
| CHEMBL5549950 | — | — | 1 | 4.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5527999 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL5561920 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL5561497 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5562105 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL1230640 | — | IC50 | = | 977.24 | nM | 6.01 |
| CHEMBL5532540 | — | IC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL5557587 | — | IC50 | = | 1380.38 | nM | 5.86 |
| CHEMBL5557957 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL5557793 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL5549844 | — | IC50 | = | 2691.53 | nM | 5.57 |
| CHEMBL5567655 | — | IC50 | = | 2754.23 | nM | 5.56 |
| CHEMBL5559263 | — | IC50 | = | 3090.3 | nM | 5.51 |
| CHEMBL5564944 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL5566835 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL5557372 | — | IC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL5563232 | — | IC50 | = | 6025.6 | nM | 5.22 |
| CHEMBL5556063 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL5564005 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL5563922 | — | IC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL5560439 | — | IC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL5557758 | — | IC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL5542479 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL5558323 | — | IC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL5561894 | — | IC50 | = | 18197.01 | nM | 4.74 |
| CHEMBL5563415 | — | IC50 | = | 20417.38 | nM | 4.69 |
| CHEMBL5562605 | — | IC50 | = | 23442.29 | nM | 4.63 |
| CHEMBL5542589 | — | IC50 | = | 30902.95 | nM | 4.51 |
| CHEMBL5564980 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL5560200 | — | IC50 | = | 46773.51 | nM | 4.33 |
| CHEMBL5549950 | — | IC50 | = | 48977.88 | nM | 4.31 |
| CHEMBL5527999 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5565375 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5561450 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5565375 | — | pIC50 | - | — | - | |
| CHEMBL5565962 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4203498 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3785455 | — | IC50 | > | 100000.0 | nM | - |