Assay Detail
Binding
CHEMBL4424782
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human C-terminal FLAG-tagged KDM5A (1 to 1090 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
7
Total Activities
7
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 | 7 | 6.94 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4542928 | — | — | 1 | 8.36 |
| CHEMBL4536443 | — | — | 1 | 7.64 |
| CHEMBL4436444 | — | — | 1 | 7.18 |
| CHEMBL4446067 | — | — | 1 | 6.77 |
| CHEMBL4556977 | — | — | 1 | 6.75 |
| CHEMBL4454253 | — | — | 1 | 6.30 |
| CHEMBL3590426 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4542928 | — | IC50 | = | 4.37 | nM | 8.36 |
| CHEMBL4536443 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL4436444 | — | IC50 | = | 65.3 | nM | 7.18 |
| CHEMBL4446067 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4556977 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4454253 | — | IC50 | = | 506.0 | nM | 6.30 |
| CHEMBL3590426 | — | IC50 | = | 2700.0 | nM | 5.57 |