Assay Detail
Binding
CHEMBL4047447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal truncated LSD1 (151 to 852 residues) expressed in Escherichia coli using histone H3(1-21)K4(Me1) biotin peptide as substrate measured after 30 mins by TR-FRET assay
19
Total Activities
19
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 |
Target
Lysine-specific histone demethylase 1A (CHEMBL6136) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development and evaluation of 4-(pyrrolidin-3-yl)benzonitrile derivatives as inhibitors of lysine specific demethylase 1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.99 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3134377 | — | — | 1 | 7.39 |
| CHEMBL4071991 | — | — | 1 | 7.24 |
| CHEMBL4066130 | — | — | 1 | 6.68 |
| CHEMBL4092760 | — | — | 1 | 6.58 |
| CHEMBL4087724 | — | — | 1 | 6.24 |
| CHEMBL4100487 | — | — | 1 | 6.17 |
| CHEMBL4082476 | — | — | 1 | 6.09 |
| CHEMBL4105603 | — | — | 1 | 6.02 |
| CHEMBL4079770 | — | — | 1 | 5.92 |
| CHEMBL4074738 | — | — | 1 | 5.58 |
| CHEMBL4079847 | — | — | 1 | 5.52 |
| CHEMBL4097870 | — | — | 1 | 5.38 |
| CHEMBL4093703 | — | — | 1 | 5.36 |
| CHEMBL4101423 | — | — | 1 | 5.32 |
| CHEMBL4063365 | — | — | 1 | 5.24 |
| CHEMBL4085006 | — | — | 1 | 5.05 |
| CHEMBL4066293 | — | — | 1 | - |
| CHEMBL4104027 | — | — | 1 | - |
| CHEMBL4087649 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3134377 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4071991 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4066130 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4092760 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4087724 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4100487 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4082476 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4105603 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL4079770 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4074738 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4079847 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4097870 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4093703 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4101423 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4063365 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4085006 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4066293 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4104027 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4087649 | — | IC50 | > | 30000.0 | nM | - |