Assay Detail
Binding
CHEMBL4353689
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG as cosubstrate pre-incubated for 10 mins before substrate addition followed by centrifugation for 1 min and measured after 20 mins by AlphaScreen assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 |
|---|---|---|---|
| IC50 | 33 | 7.15 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438830 | — | — | 1 | 8.10 |
| CHEMBL4440395 | — | — | 1 | 7.82 |
| CHEMBL4466130 | — | — | 1 | 7.75 |
| CHEMBL4592908 | — | — | 1 | 7.72 |
| CHEMBL4585876 | — | — | 1 | 7.70 |
| CHEMBL4590283 | — | — | 1 | 7.70 |
| CHEMBL4559561 | — | — | 1 | 7.62 |
| CHEMBL4567766 | — | — | 1 | 7.57 |
| CHEMBL4573390 | — | — | 1 | 7.54 |
| CHEMBL4447515 | — | — | 1 | 7.50 |
| CHEMBL4438034 | — | — | 1 | 7.50 |
| CHEMBL4561958 | — | — | 1 | 7.48 |
| CHEMBL4516101 | — | — | 1 | 7.48 |
| CHEMBL4449500 | — | — | 1 | 7.37 |
| CHEMBL4435185 | — | — | 1 | 7.35 |
| CHEMBL4558689 | — | — | 1 | 7.33 |
| CHEMBL4520178 | — | — | 1 | 7.31 |
| CHEMBL4464471 | — | — | 1 | 7.24 |
| CHEMBL4549505 | — | — | 1 | 7.20 |
| CHEMBL4538741 | — | — | 1 | 7.17 |
| CHEMBL4522584 | — | — | 1 | 7.10 |
| CHEMBL4476629 | — | — | 1 | 7.00 |
| CHEMBL4553540 | — | — | 1 | 6.99 |
| CHEMBL4473678 | — | — | 1 | 6.84 |
| CHEMBL4572027 | — | — | 1 | 6.82 |
| CHEMBL4525269 | — | — | 1 | 6.61 |
| CHEMBL4529932 | — | — | 1 | 6.52 |
| CHEMBL4532069 | — | — | 1 | 6.43 |
| CHEMBL4560811 | — | — | 1 | 6.34 |
| CHEMBL4445652 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438830 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4440395 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4466130 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4592908 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4585876 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4590283 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4559561 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4567766 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4573390 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4447515 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4438034 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4561958 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4516101 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4449500 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4435185 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4558689 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4520178 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4464471 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4549505 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4538741 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4522584 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4476629 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4553540 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4473678 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4572027 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4525269 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4529932 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4532069 | — | IC50 | = | 372.0 | nM | 6.43 |
| CHEMBL4560811 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4445652 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL4455283 | — | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL4483792 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL4483780 | — | IC50 | = | 820.0 | nM | 6.09 |