Assay Detail
Binding
CHEMBL5734704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: Briefly, bulk histones, histone peptides or nucleosomes are incubated with purified human recombinant KDM1A, in the histone demethylase activity (HDM) assay buffer 1 (50 mM Tris pH 8.5, 50 mM KCl, 5 mM MgCl, 0.5% BSA, and 5% glycerol) from 30 minutes to 4 hours at 37° C. A typical reaction is conducted in 100 microliters in which either 20 micrograms of purified bulk histones or 3 micrograms of modified histone peptides are used as substrates. Different amounts of KDM1A ranging from 1-20 micrograms are used in the reaction along with, as necessary, other co-factors such as FAD or CoREST, depending on the chosen substrate. The reaction mixture is analyzed by SDS-PAGE and Western blotting using histone methyl-specific antibodies or by formaldehyde formation assay to examine the removal and conversion of the methyl group to formaldehyde, or by mass spectrometry in the case of peptide substrates to identify the demethylated histone peptide.
501
Total Activities
165
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Lysine-specific histone demethylase 1A (CHEMBL6136) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
KDM1A inhibitors for the treatment of disease
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 167 | 4.92 | 6.10 |
| kon | 167 | - | - |
| k_off | 167 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5905859 | — | — | 3 | 6.10 |
| CHEMBL5880420 | — | — | 3 | 6.00 |
| CHEMBL5765675 | — | — | 3 | 5.70 |
| CHEMBL5742196 | — | — | 3 | 5.70 |
| CHEMBL6028916 | — | — | 3 | 5.70 |
| CHEMBL5778938 | — | — | 3 | 5.70 |
| CHEMBL6056865 | — | — | 3 | 5.52 |
| CHEMBL5981736 | — | — | 3 | 5.52 |
| CHEMBL5847512 | — | — | 3 | 5.52 |
| CHEMBL6014549 | — | — | 3 | 5.52 |
| CHEMBL5807766 | — | — | 3 | 5.52 |
| CHEMBL6045682 | — | — | 3 | 5.52 |
| CHEMBL5967558 | — | — | 3 | 5.52 |
| CHEMBL5812475 | — | — | 3 | 5.40 |
| CHEMBL5847735 | — | — | 3 | 5.40 |
| CHEMBL5908210 | — | — | 3 | 5.40 |
| CHEMBL5928525 | — | — | 3 | 5.40 |
| CHEMBL5787891 | — | — | 3 | 5.40 |
| CHEMBL5866999 | — | — | 3 | 5.40 |
| CHEMBL6032044 | — | — | 3 | 5.40 |
| CHEMBL5972560 | — | — | 3 | 5.40 |
| CHEMBL5933746 | — | — | 3 | 5.30 |
| CHEMBL5843903 | — | — | 3 | 5.30 |
| CHEMBL5793521 | — | — | 3 | 5.30 |
| CHEMBL5755146 | — | — | 3 | 5.30 |
| CHEMBL5861547 | — | — | 6 | 5.30 |
| CHEMBL5958240 | — | — | 3 | 5.30 |
| CHEMBL6016529 | — | — | 3 | 5.30 |
| CHEMBL5973342 | — | — | 3 | 5.30 |
| CHEMBL5873519 | — | — | 3 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5905859 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5880420 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5742196 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5765675 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5778938 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6028916 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL6014549 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5981736 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5967558 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5847512 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL6045682 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL6056865 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5807766 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5812475 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5928525 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5908210 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5972560 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5866999 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5787891 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL6032044 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5847735 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5755146 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5861547 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5808062 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5897078 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5843903 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL6016529 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5973342 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5873519 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5958240 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5933746 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5977278 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5793521 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL5993297 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5865418 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5812127 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5764138 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL6012498 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5789806 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5940519 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5856358 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL6015167 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5924410 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL6003294 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL5815096 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5937117 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5978958 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5782797 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5782825 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL5806907 | — | IC50 | = | 9000.0 | nM | 5.05 |