Assay Detail
Binding
CHEMBL4353735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 5.03 | 5.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4449500 | — | — | 1 | 5.33 |
| CHEMBL4573390 | — | — | 1 | 5.23 |
| CHEMBL3774537 | — | — | 1 | 5.07 |
| CHEMBL4567766 | — | — | 1 | 4.98 |
| CHEMBL4438830 | — | — | 1 | 4.52 |
| CHEMBL4447515 | — | — | 1 | - |
| CHEMBL4585876 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4449500 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4573390 | — | EC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3774537 | — | EC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4567766 | — | EC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL4438830 | — | EC50 | = | 30300.0 | nM | 4.52 |
| CHEMBL4447515 | — | EC50 | - | — | - | |
| CHEMBL4585876 | — | EC50 | - | — | - |