Assay Detail
Binding
CHEMBL4370538
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human LSD1 (172 to 852 residues) using biotin-labelled H3K4me2 (1 to 24 residues) after 1 hr by TR-FRET assay
18
Total Activities
18
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
Tranylcypromine and 6-trifluoroethyl thienopyrimidine hybrid as LSD1 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.58 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4569986 | — | — | 1 | 7.21 |
| CHEMBL4533143 | — | — | 1 | 7.18 |
| CHEMBL4580675 | — | — | 1 | 7.07 |
| CHEMBL4520948 | — | — | 1 | 6.96 |
| CHEMBL4437554 | — | — | 1 | 6.91 |
| CHEMBL4589914 | — | — | 1 | 6.83 |
| CHEMBL4550942 | — | — | 1 | 6.74 |
| CHEMBL4447074 | — | — | 1 | 6.73 |
| CHEMBL4442317 | — | — | 1 | 6.67 |
| CHEMBL4440500 | — | — | 1 | 6.62 |
| CHEMBL4530202 | — | — | 1 | 6.62 |
| CHEMBL4593261 | — | — | 1 | 6.60 |
| CHEMBL4474185 | — | — | 1 | 6.52 |
| CHEMBL4558443 | — | — | 1 | 6.44 |
| CHEMBL4526830 | — | — | 1 | 6.16 |
| CHEMBL3786182 | GSK2879552 | 1.0 | 1 | 5.92 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 4.66 |
| CHEMBL3586090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4569986 | — | IC50 | = | 61.04 | nM | 7.21 |
| CHEMBL4533143 | — | IC50 | = | 66.13 | nM | 7.18 |
| CHEMBL4580675 | — | IC50 | = | 84.38 | nM | 7.07 |
| CHEMBL4520948 | — | IC50 | = | 109.35 | nM | 6.96 |
| CHEMBL4437554 | — | IC50 | = | 124.05 | nM | 6.91 |
| CHEMBL4589914 | — | IC50 | = | 146.35 | nM | 6.83 |
| CHEMBL4550942 | — | IC50 | = | 184.15 | nM | 6.74 |
| CHEMBL4447074 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4442317 | — | IC50 | = | 211.35 | nM | 6.67 |
| CHEMBL4440500 | — | IC50 | = | 240.5 | nM | 6.62 |
| CHEMBL4530202 | — | IC50 | = | 241.95 | nM | 6.62 |
| CHEMBL4593261 | — | IC50 | = | 252.33 | nM | 6.60 |
| CHEMBL4474185 | — | IC50 | = | 303.35 | nM | 6.52 |
| CHEMBL4558443 | — | IC50 | = | 359.7 | nM | 6.44 |
| CHEMBL4526830 | — | IC50 | = | 692.15 | nM | 6.16 |
| CHEMBL3786182 | GSK2879552 | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | = | 21850.0 | nM | 4.66 |
| CHEMBL3586090 | — | IC50 | - | — | - |