Assay Detail
Binding
CHEMBL4035840
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal FLAG-tagged KDM4C expressed in baculovirus infected Sf9 insect cells using H3K9me3 peptide as substrate after 30 to 45 mins by TR-FRET assay
4
Total Activities
2
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
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.14 | 5.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4088737 | — | — | 1 | 5.39 |
| CHEMBL4083572 | — | — | 3 | 4.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4088737 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4083572 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4083572 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4083572 | — | IC50 | - | — | - |