Assay Detail
Binding
CHEMBL4353690
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDM5B (unknown origin) assessed as decrease in demethylation of substrate using peptide (H3(1-21)K4-Me3-GGKBiotin) as substrate and 2OG as cosubstrate pre-incubated for 15 mins before substrate addition followed by centrifugation for 15 secs 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 |
| 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 | 7.28 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438830 | — | — | 1 | 8.22 |
| CHEMBL4585876 | — | — | 1 | 7.92 |
| CHEMBL4592908 | — | — | 1 | 7.92 |
| CHEMBL4440395 | — | — | 1 | 7.92 |
| CHEMBL4573390 | — | — | 1 | 7.85 |
| CHEMBL4516101 | — | — | 1 | 7.77 |
| CHEMBL4567766 | — | — | 1 | 7.77 |
| CHEMBL4558689 | — | — | 1 | 7.68 |
| CHEMBL4538741 | — | — | 1 | 7.64 |
| CHEMBL4520178 | — | — | 1 | 7.60 |
| CHEMBL4466130 | — | — | 1 | 7.58 |
| CHEMBL4447515 | — | — | 1 | 7.54 |
| CHEMBL4553540 | — | — | 1 | 7.50 |
| CHEMBL4449500 | — | — | 1 | 7.42 |
| CHEMBL4590283 | — | — | 1 | 7.39 |
| CHEMBL4561958 | — | — | 1 | 7.38 |
| CHEMBL4549505 | — | — | 1 | 7.32 |
| CHEMBL4476629 | — | — | 1 | 7.29 |
| CHEMBL4473678 | — | — | 1 | 7.18 |
| CHEMBL4529932 | — | — | 1 | 7.17 |
| CHEMBL4559561 | — | — | 1 | 7.10 |
| CHEMBL4522584 | — | — | 1 | 7.09 |
| CHEMBL4435185 | — | — | 1 | 6.94 |
| CHEMBL4464471 | — | — | 1 | 6.91 |
| CHEMBL4438034 | — | — | 1 | 6.90 |
| CHEMBL4483792 | — | — | 1 | 6.88 |
| CHEMBL4525269 | — | — | 1 | 6.87 |
| CHEMBL4572027 | — | — | 1 | 6.84 |
| CHEMBL4560811 | — | — | 1 | 6.83 |
| CHEMBL4483780 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438830 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4585876 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4440395 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4592908 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4573390 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4516101 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4567766 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4558689 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4538741 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4520178 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4466130 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4447515 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4553540 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4449500 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4590283 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4561958 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4549505 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4476629 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4473678 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4529932 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4559561 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4522584 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4435185 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4464471 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4438034 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4483792 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL4525269 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4572027 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4560811 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4483780 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4455283 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL4532069 | — | IC50 | = | 447.0 | nM | 6.35 |
| CHEMBL4445652 | — | IC50 | = | 601.0 | nM | 6.22 |