Assay Detail
Binding
CHEMBL3778170
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Inhibition of KDM4E (unknown origin) using H3K9Me3 peptide as substrate assessed as demethylation of substrate by Rapidfire mass spectrometric analysis
5
Total Activities
5
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
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 7.37 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775237 | — | — | 1 | 7.40 |
| CHEMBL3775612 | — | — | 1 | 7.40 |
| CHEMBL3775889 | — | — | 1 | 7.30 |
| CHEMBL3774615 | — | — | 1 | - |
| CHEMBL3774435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775237 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3775612 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3775889 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL3774615 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3774435 | — | IC50 | > | 100000.0 | nM | - |