Assay Detail
Binding
CHEMBL4253672
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged LSD1 (2 to 852 residues) (unknown origin) expressed in baculovirus infected sf9 cells preincubated for 15 mins followed by H3K4me2 substrate addition measured after 60 mins by amplex red reagent based HRP enzyme coupled fluorescence assay
48
Total Activities
46
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
Structure-activity studies on N-Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 6.86 | 7.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4285212 | — | — | 1 | 7.45 |
| CHEMBL4281778 | — | — | 2 | 7.29 |
| CHEMBL4292597 | — | — | 1 | 7.22 |
| CHEMBL4277281 | — | — | 1 | 7.19 |
| CHEMBL4290752 | — | — | 1 | 7.18 |
| CHEMBL4285166 | — | — | 1 | 7.18 |
| CHEMBL4287709 | — | — | 1 | 7.18 |
| CHEMBL4292825 | — | — | 1 | 7.16 |
| CHEMBL4289408 | — | — | 2 | 7.11 |
| CHEMBL4278920 | — | — | 1 | 7.10 |
| CHEMBL4284179 | — | — | 1 | 7.09 |
| CHEMBL4279808 | — | — | 1 | 7.08 |
| CHEMBL4282845 | — | — | 1 | 7.04 |
| CHEMBL4287563 | — | — | 1 | 7.04 |
| CHEMBL4285989 | — | — | 1 | 7.02 |
| CHEMBL4294148 | — | — | 1 | 7.02 |
| CHEMBL4285786 | — | — | 1 | 7.00 |
| CHEMBL4288523 | — | — | 1 | 7.00 |
| CHEMBL4278738 | — | — | 1 | 6.98 |
| CHEMBL4285695 | — | — | 1 | 6.96 |
| CHEMBL4294062 | — | — | 1 | 6.96 |
| CHEMBL4284077 | — | — | 1 | 6.95 |
| CHEMBL4289655 | — | — | 1 | 6.95 |
| CHEMBL4277841 | — | — | 1 | 6.94 |
| CHEMBL4282381 | — | — | 1 | 6.93 |
| CHEMBL4286163 | — | — | 1 | 6.93 |
| CHEMBL4284708 | — | — | 1 | 6.92 |
| CHEMBL4282608 | — | — | 1 | 6.91 |
| CHEMBL4280740 | — | — | 1 | 6.83 |
| CHEMBL4282324 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4285212 | — | IC50 | = | 35.3 | nM | 7.45 |
| CHEMBL4281778 | — | IC50 | = | 51.8 | nM | 7.29 |
| CHEMBL4292597 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4277281 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL4290752 | — | IC50 | = | 65.5 | nM | 7.18 |
| CHEMBL4285166 | — | IC50 | = | 66.1 | nM | 7.18 |
| CHEMBL4287709 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL4292825 | — | IC50 | = | 69.1 | nM | 7.16 |
| CHEMBL4289408 | — | IC50 | = | 77.5 | nM | 7.11 |
| CHEMBL4278920 | — | IC50 | = | 79.7 | nM | 7.10 |
| CHEMBL4284179 | — | IC50 | = | 80.7 | nM | 7.09 |
| CHEMBL4279808 | — | IC50 | = | 82.6 | nM | 7.08 |
| CHEMBL4287563 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4282845 | — | IC50 | = | 91.1 | nM | 7.04 |
| CHEMBL4294148 | — | IC50 | = | 95.9 | nM | 7.02 |
| CHEMBL4285989 | — | IC50 | = | 94.9 | nM | 7.02 |
| CHEMBL4289408 | — | IC50 | = | 95.6 | nM | 7.02 |
| CHEMBL4288523 | — | IC50 | = | 100.2 | nM | 7.00 |
| CHEMBL4281778 | — | IC50 | = | 99.5 | nM | 7.00 |
| CHEMBL4285786 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4278738 | — | IC50 | = | 103.9 | nM | 6.98 |
| CHEMBL4294062 | — | IC50 | = | 108.5 | nM | 6.96 |
| CHEMBL4285695 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4284077 | — | IC50 | = | 112.1 | nM | 6.95 |
| CHEMBL4289655 | — | IC50 | = | 111.7 | nM | 6.95 |
| CHEMBL4277841 | — | IC50 | = | 114.1 | nM | 6.94 |
| CHEMBL4282381 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4286163 | — | IC50 | = | 117.5 | nM | 6.93 |
| CHEMBL4284708 | — | IC50 | = | 119.9 | nM | 6.92 |
| CHEMBL4282608 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4280740 | — | IC50 | = | 146.5 | nM | 6.83 |
| CHEMBL4282324 | — | IC50 | = | 154.5 | nM | 6.81 |
| CHEMBL4292976 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4277206 | — | IC50 | = | 157.9 | nM | 6.80 |
| CHEMBL4288999 | — | IC50 | = | 187.3 | nM | 6.73 |
| CHEMBL4294740 | — | IC50 | = | 194.6 | nM | 6.71 |
| CHEMBL4292356 | — | IC50 | = | 202.4 | nM | 6.69 |
| CHEMBL4290483 | — | IC50 | = | 202.8 | nM | 6.69 |
| CHEMBL4287919 | — | IC50 | = | 276.5 | nM | 6.56 |
| CHEMBL4289595 | — | IC50 | = | 294.5 | nM | 6.53 |
| CHEMBL492697 | — | IC50 | = | 321.1 | nM | 6.49 |
| CHEMBL4282210 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL4292813 | — | IC50 | = | 417.5 | nM | 6.38 |
| CHEMBL4278320 | — | IC50 | = | 643.5 | nM | 6.19 |
| CHEMBL4284789 | — | IC50 | = | 817.1 | nM | 6.09 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4284358 | — | IC50 | - | — | - | |
| CHEMBL4283975 | — | IC50 | - | — | - |