Assay Detail
Binding
CHEMBL4236606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal truncated recombinant human LSD1 (151 to 852 residues) expressed in Escherichia coli using histone H3 (1 to 21 residues) K4me2 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by peroxidase-coupled assay
17
Total Activities
17
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
Optimization of 5-arylidene barbiturates as potent, selective, reversible LSD1 inhibitors for the treatment of acute promyelocytic leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.78 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3651585 | — | — | 1 | 8.10 |
| CHEMBL4248408 | — | — | 1 | 6.52 |
| CHEMBL4240336 | — | — | 1 | 6.39 |
| CHEMBL4241311 | — | — | 1 | 6.26 |
| CHEMBL4245069 | — | — | 1 | 6.06 |
| CHEMBL4240782 | — | — | 1 | 5.96 |
| CHEMBL4244605 | — | — | 1 | 5.92 |
| CHEMBL4239151 | — | — | 1 | 5.55 |
| CHEMBL4238393 | — | — | 1 | 5.51 |
| CHEMBL4244132 | — | — | 1 | 5.44 |
| CHEMBL4251434 | — | — | 1 | 5.44 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | — | 1 | 5.44 |
| CHEMBL4237686 | — | — | 1 | 5.36 |
| CHEMBL4237521 | — | — | 1 | 5.19 |
| CHEMBL4248955 | — | — | 1 | 4.74 |
| CHEMBL4248864 | — | — | 1 | 4.64 |
| CHEMBL4250459 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3651585 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4248408 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4240336 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4241311 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4245069 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4240782 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4244605 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4239151 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4238393 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4244132 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4251434 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4237686 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4237521 | — | IC50 | = | 6420.0 | nM | 5.19 |
| CHEMBL4248955 | — | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL4248864 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4250459 | — | IC50 | > | 75000.0 | nM | - |