Assay Detail
Binding
CHEMBL4135161
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal His/GST-tagged LSD1 (172 to 852 residues) expressed in baculovirus infected insect cells using biotin-labeled H3K4me2 (1 to 24 residues) as substrate after 1 hr by TR-FRET assay
24
Total Activities
22
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
Tying up tranylcypromine: Novel selective histone lysine specific demethylase 1 (LSD1) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.09 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4170367 | — | — | 1 | 8.66 |
| CHEMBL4176756 | — | — | 1 | 8.19 |
| CHEMBL3906257 | — | — | 1 | 7.85 |
| CHEMBL4166129 | — | — | 1 | 7.77 |
| CHEMBL4170687 | — | — | 1 | 7.68 |
| CHEMBL4160042 | — | — | 1 | 7.12 |
| CHEMBL4162448 | — | — | 1 | 6.57 |
| CHEMBL4171896 | — | — | 1 | 6.31 |
| CHEMBL4166776 | — | — | 1 | 6.06 |
| CHEMBL4166524 | — | — | 1 | 5.96 |
| CHEMBL4174280 | — | — | 1 | 5.89 |
| CHEMBL4166366 | — | — | 1 | 5.73 |
| CHEMBL4171003 | — | — | 1 | 5.70 |
| CHEMBL4170181 | — | — | 1 | 5.39 |
| CHEMBL4166013 | — | — | 2 | 5.30 |
| CHEMBL4161508 | — | — | 2 | 5.25 |
| CHEMBL4174674 | — | — | 1 | 5.22 |
| CHEMBL4176623 | — | — | 1 | 5.14 |
| CHEMBL4163599 | — | — | 1 | 5.05 |
| CHEMBL313833 | — | — | 1 | 4.65 |
| CHEMBL4175342 | — | — | 1 | 4.60 |
| CHEMBL4164024 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4170367 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4176756 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3906257 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4166129 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4170687 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4160042 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4162448 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4171896 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4166776 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4166524 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4174280 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4166366 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL4171003 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL4170181 | — | IC50 | = | 4070.0 | nM | 5.39 |
| CHEMBL4166013 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4161508 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL4174674 | — | IC50 | = | 5950.0 | nM | 5.22 |
| CHEMBL4176623 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL4166013 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL4163599 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL4161508 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL313833 | — | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL4175342 | — | IC50 | = | 24900.0 | nM | 4.60 |
| CHEMBL4164024 | — | IC50 | > | 30000.0 | nM | - |