Assay Detail
Binding
CHEMBL3779256
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human HALO-tagged KDM5C1 expressed in human U2OS cells assessed as level of H3K9Me3 demethylation incubated overnight by Hoechst 33342/HaloTag/ Alexa Fluor 647 staining-based image analysis
4
Total Activities
4
Compounds Tested
1
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 | 4 | 4.40 | 4.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775889 | — | — | 1 | 4.60 |
| CHEMBL3775237 | — | — | 1 | 4.20 |
| CHEMBL3774615 | — | — | 1 | - |
| CHEMBL3774435 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775889 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3775237 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL3774615 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3774435 | — | IC50 | > | 100000.0 | nM | - |