Assay Detail
Binding
CHEMBL4122979
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Displacement of C-terminally biotinylated-H3K4me3 (1 to 21 residues) peptide from KDM7A (PHD-JmjC) (unknown origin) preincubated for 15 mins followed by peptide addition measured after 1 hr by luminescence-based AlphaScreen assay
6
Total Activities
6
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
Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.55 | 5.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126406 | — | — | 1 | 5.25 |
| CHEMBL4129540 | — | — | 1 | 4.80 |
| CHEMBL633 | AMIODARONE | 4.0 | 1 | 4.10 |
| CHEMBL4128152 | — | — | 1 | 4.06 |
| CHEMBL4126951 | — | — | 1 | - |
| CHEMBL4130224 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126406 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4129540 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL633 | AMIODARONE | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL4128152 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL4126951 | — | IC50 | = | 295000.0 | nM | - |
| CHEMBL4130224 | — | IC50 | = | 149000.0 | nM | - |