Assay Detail
Binding
CHEMBL3776326
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged KDM4C (1 to 352 residues) (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using biotinylated histone H3 (1 to 21 residues) lysine 9 trimethylated peptide/50 uM alpha-ketoglutarate as substrate/cofactor measured after 45 mins by TR-FRET assay
15
Total Activities
15
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
Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 5.24 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3775272 | — | — | 1 | 5.82 |
| CHEMBL3775262 | — | — | 1 | 5.58 |
| CHEMBL3775162 | — | — | 1 | 5.47 |
| CHEMBL3775563 | — | — | 1 | 5.43 |
| CHEMBL3775867 | — | — | 1 | 5.30 |
| CHEMBL3775380 | — | — | 1 | 5.13 |
| CHEMBL3774814 | — | — | 1 | 4.77 |
| CHEMBL3774598 | — | — | 1 | 4.40 |
| CHEMBL3775869 | — | — | 1 | - |
| CHEMBL3774480 | — | — | 1 | - |
| CHEMBL3775495 | — | — | 1 | - |
| CHEMBL3774513 | — | — | 1 | - |
| CHEMBL3774611 | — | — | 1 | - |
| CHEMBL3775759 | — | — | 1 | - |
| CHEMBL3774693 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3775272 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3775262 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3775162 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3775563 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3775867 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3775380 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3774814 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL3774598 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL3775869 | — | IC50 | - | — | - | |
| CHEMBL3774480 | — | IC50 | - | — | - | |
| CHEMBL3775495 | — | IC50 | - | — | - | |
| CHEMBL3774513 | — | IC50 | - | — | - | |
| CHEMBL3774611 | — | IC50 | - | — | - | |
| CHEMBL3775759 | — | IC50 | - | — | - | |
| CHEMBL3774693 | — | IC50 | - | — | - |