Assay Detail
Binding
CHEMBL4630174
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal His-tagged LSD1 (unknown origin) expressed in Escherichia coli expression system using ART-K(Me1)-QTARKSTGGKAPRKQLAGGK(Biotin) as substrate incubated for 60 mins by TR-FRET assay
30
Total Activities
30
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 and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.12 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4646795 | — | — | 1 | 8.59 |
| CHEMBL4644907 | — | — | 1 | 8.54 |
| CHEMBL4637451 | — | — | 1 | 8.52 |
| CHEMBL4636174 | — | — | 1 | 8.40 |
| CHEMBL4640768 | — | — | 1 | 8.38 |
| CHEMBL4647030 | — | — | 1 | 8.28 |
| CHEMBL4642534 | — | — | 1 | 8.14 |
| CHEMBL4641803 | — | — | 1 | 8.11 |
| CHEMBL4638408 | — | — | 1 | 8.06 |
| CHEMBL4645640 | — | — | 1 | 7.77 |
| CHEMBL4639957 | — | — | 1 | 7.70 |
| CHEMBL4644039 | — | — | 1 | 7.60 |
| CHEMBL4647263 | — | — | 1 | 7.55 |
| CHEMBL4649322 | — | — | 1 | 7.25 |
| CHEMBL4645912 | — | — | 1 | 6.70 |
| CHEMBL3786182 | GSK2879552 | 1.0 | 1 | 6.67 |
| CHEMBL4640829 | — | — | 1 | 6.38 |
| CHEMBL4632371 | — | — | 1 | 6.35 |
| CHEMBL4637228 | — | — | 1 | 6.10 |
| CHEMBL4646049 | — | — | 1 | 6.05 |
| CHEMBL4643691 | — | — | 1 | 5.37 |
| CHEMBL4639078 | — | — | 1 | 5.03 |
| CHEMBL4634330 | — | — | 1 | 4.69 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 4.64 |
| CHEMBL4646146 | — | — | 1 | - |
| CHEMBL4649041 | — | — | 1 | - |
| CHEMBL4646431 | — | — | 1 | - |
| CHEMBL4638015 | — | — | 1 | - |
| CHEMBL4637061 | — | — | 1 | - |
| CHEMBL4637906 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4646795 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4644907 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4637451 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4636174 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4640768 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4647030 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4642534 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4641803 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4638408 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4645640 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4639957 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4644039 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4647263 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4649322 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4645912 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3786182 | GSK2879552 | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL4640829 | — | IC50 | = | 412.0 | nM | 6.38 |
| CHEMBL4632371 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL4637228 | — | IC50 | = | 788.0 | nM | 6.10 |
| CHEMBL4646049 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL4643691 | — | IC50 | = | 4280.0 | nM | 5.37 |
| CHEMBL4639078 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4634330 | — | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL4646146 | — | IC50 | < | 2.8 | nM | - |
| CHEMBL4649041 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4646431 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4638015 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4637061 | — | IC50 | < | 2.6 | nM | - |
| CHEMBL4637906 | — | IC50 | < | 1.8 | nM | - |