Assay Detail
Binding
CHEMBL4424784
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Inhibition of human N-terminal FLAG/His-tagged KDM5B (2 to 751 residues) expressed in baculovirus infected Sf9 insect cells using H3(1-21)K4(Me3)-GGK(Biotin)/2-OG as substrate measured after 1 hr by Alphalisa assay
4
Total Activities
4
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
Identification of novel lysine demethylase 5-selective inhibitors by inhibitor-based fragment merging strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.92 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4542928 | — | — | 1 | 8.87 |
| CHEMBL4536443 | — | — | 1 | 7.29 |
| CHEMBL4454253 | — | — | 1 | 6.47 |
| CHEMBL3590426 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4542928 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL4536443 | — | IC50 | = | 51.1 | nM | 7.29 |
| CHEMBL4454253 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL3590426 | — | IC50 | = | 9240.0 | nM | 5.03 |