Assay Detail
Binding
CHEMBL4353733
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to recombinant human N-terminal KDM4B (1 to 348 residues) fused upstream with E31G-R71G-K105E/ePL-tagged C-terminal transfected in HEK293T cells measured after 30 mins by chemiluminescence based cellular target engagement assay
8
Total Activities
8
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
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 | 8 | 5.65 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774537 | — | — | 1 | 6.00 |
| CHEMBL4449500 | — | — | 1 | 5.89 |
| CHEMBL4567766 | — | — | 1 | 5.85 |
| CHEMBL4573390 | — | — | 1 | 5.77 |
| CHEMBL4447515 | — | — | 1 | 5.70 |
| CHEMBL4438830 | — | — | 1 | 5.52 |
| CHEMBL4585876 | — | — | 1 | 5.46 |
| CHEMBL4525269 | — | — | 1 | 5.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774537 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4449500 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4567766 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4573390 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4447515 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4438830 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4585876 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4525269 | — | EC50 | = | 9100.0 | nM | 5.04 |