Assay Detail
Binding
CHEMBL3776332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDM5A (1 to 797 residues) (unknown origin) expressed in insect sf21 cells using ARTK(Me3)QTARKSTGGKAPRK peptide/ 100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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 | 6 | 4.46 | 6.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316034 | — | — | 1 | 6.12 |
| CHEMBL3775867 | — | — | 1 | 4.64 |
| CHEMBL3775262 | — | — | 1 | 4.35 |
| CHEMBL3775272 | — | — | 1 | 4.28 |
| CHEMBL3775380 | — | — | 1 | 3.75 |
| CHEMBL3774598 | — | — | 1 | 3.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316034 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3775867 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3775262 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL3775272 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL3775380 | — | IC50 | = | 180000.0 | nM | 3.75 |
| CHEMBL3774598 | — | IC50 | = | 240000.0 | nM | 3.62 |