Assay Detail
Binding
CHEMBL4042261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human LSD1 (157 to 852 residues) expressed in Escherichia coli BL21(DE3) using H3K4me2 as substrate preincubated for 1 hr followed by substrate addition by fluorescence assay
31
Total Activities
31
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
Design, synthesis and biological evaluation of [1,2,4]triazolo[1,5-a]pyrimidines as potent lysine specific demethylase 1 (LSD1/KDM1A) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.65 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786182 | GSK2879552 | 1.0 | 1 | 7.62 |
| CHEMBL4098092 | — | — | 1 | 6.81 |
| CHEMBL4089024 | — | — | 1 | 6.25 |
| CHEMBL4099019 | — | — | 1 | 5.92 |
| CHEMBL4072052 | — | — | 1 | - |
| CHEMBL4094062 | — | — | 1 | - |
| CHEMBL2177862 | — | — | 1 | - |
| CHEMBL4080060 | — | — | 1 | - |
| CHEMBL4090367 | — | — | 1 | - |
| CHEMBL4069335 | — | — | 1 | - |
| CHEMBL4101839 | — | — | 1 | - |
| CHEMBL4060712 | — | — | 1 | - |
| CHEMBL4087815 | — | — | 1 | - |
| CHEMBL4065645 | — | — | 1 | - |
| CHEMBL4064818 | — | — | 1 | - |
| CHEMBL334644 | — | — | 1 | - |
| CHEMBL4073417 | — | — | 1 | - |
| CHEMBL4060656 | — | — | 1 | - |
| CHEMBL4082527 | — | — | 1 | - |
| CHEMBL4099054 | — | — | 1 | - |
| CHEMBL4101488 | — | — | 1 | - |
| CHEMBL4099168 | — | — | 1 | - |
| CHEMBL4081141 | — | — | 1 | - |
| CHEMBL4060820 | — | — | 1 | - |
| CHEMBL4083660 | — | — | 1 | - |
| CHEMBL4061895 | — | — | 1 | - |
| CHEMBL4091439 | — | — | 1 | - |
| CHEMBL4070519 | — | — | 1 | - |
| CHEMBL4082098 | — | — | 1 | - |
| CHEMBL4067124 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786182 | GSK2879552 | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4098092 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4089024 | — | IC50 | = | 557.0 | nM | 6.25 |
| CHEMBL4099019 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL2177862 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4083797 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4080060 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4090367 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4069335 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4101839 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4060712 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4087815 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4065645 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4064818 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL334644 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4073417 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4094062 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4072052 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4060656 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4082527 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4099054 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4101488 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4099168 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4081141 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4060820 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4083660 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4061895 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4091439 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4070519 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4082098 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4067124 | — | IC50 | > | 10000.0 | nM | - |