Assay Detail
Binding
CHEMBL3779254
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Inhibition of full length human HALO-tagged KDM4C expressed in human U2OS cells assessed as level of H3K9Me3 demethylation incubated overnight by Hoechst 33342/HaloTag/ Alexa Fluor 647 staining-based image analysis
24
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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 | 22 | 4.79 | 5.30 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774834 | — | — | 1 | 5.30 |
| CHEMBL3774408 | — | — | 1 | 5.20 |
| CHEMBL3775889 | — | — | 1 | 5.20 |
| CHEMBL3775175 | — | — | 1 | 5.20 |
| CHEMBL3774859 | — | — | 1 | 5.20 |
| CHEMBL3774552 | — | — | 1 | 5.20 |
| CHEMBL3775834 | — | — | 1 | 5.10 |
| CHEMBL3775237 | — | — | 1 | 5.10 |
| CHEMBL3775522 | — | — | 1 | 4.80 |
| CHEMBL3774545 | — | — | 1 | 4.70 |
| CHEMBL3775957 | — | — | 1 | 4.50 |
| CHEMBL3775276 | — | — | 1 | 4.50 |
| CHEMBL3775439 | — | — | 1 | 4.50 |
| CHEMBL3775612 | — | — | 2 | 4.40 |
| CHEMBL3775498 | — | — | 1 | 4.40 |
| CHEMBL3774487 | — | — | 1 | 4.30 |
| CHEMBL3775110 | — | — | 1 | 4.20 |
| CHEMBL3775716 | — | — | 1 | - |
| CHEMBL3775151 | — | — | 1 | - |
| CHEMBL3775056 | — | — | 1 | - |
| CHEMBL3774863 | — | — | 1 | - |
| CHEMBL3774615 | — | — | 1 | - |
| CHEMBL3774435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774834 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3774408 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3775175 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3774859 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3774552 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3775889 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3775237 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3775834 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3775522 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3774545 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL3775439 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3775957 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3775276 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3775612 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3775612 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3775498 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL3774487 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3775110 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL3775716 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3775056 | — | pIC50 | - | — | - | |
| CHEMBL3774863 | — | pIC50 | - | — | - | |
| CHEMBL3774615 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3774435 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3775151 | — | IC50 | > | 100000.0 | nM | - |