Assay Detail
Binding
CHEMBL4832753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length LSD1 (unknown origin) transfected in Escherichia coli BL21 (DE) using H3K4me2 as substrate by flourescence based analysis
40
Total Activities
40
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
Discovery of quinazoline derivatives as a novel class of potent and in vivo efficacious LSD1 inhibitors by drug repurposing.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 4.95 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4868123 | — | — | 1 | 6.16 |
| CHEMBL4864525 | — | — | 1 | 6.09 |
| CHEMBL4877965 | — | — | 1 | 5.90 |
| CHEMBL4871961 | — | — | 1 | 5.72 |
| CHEMBL4850299 | — | — | 1 | 5.63 |
| CHEMBL4873342 | — | — | 1 | 5.32 |
| CHEMBL4859155 | — | — | 1 | 5.31 |
| CHEMBL4876782 | — | — | 1 | 5.07 |
| CHEMBL4852200 | — | — | 1 | 5.04 |
| CHEMBL4866073 | — | — | 1 | 4.91 |
| CHEMBL4868601 | — | — | 1 | 4.71 |
| CHEMBL4854838 | — | — | 1 | 4.70 |
| CHEMBL4851688 | — | — | 1 | 4.67 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 4.63 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 4.45 |
| CHEMBL4858111 | — | — | 1 | 4.42 |
| CHEMBL4849988 | — | — | 1 | 4.41 |
| CHEMBL2046727 | — | — | 1 | 4.38 |
| CHEMBL4864777 | — | — | 1 | 4.38 |
| CHEMBL4855229 | — | — | 1 | 4.37 |
| CHEMBL4848752 | — | — | 1 | 4.34 |
| CHEMBL4850384 | — | — | 1 | 4.33 |
| CHEMBL4852100 | — | — | 1 | - |
| CHEMBL4857994 | — | — | 1 | - |
| CHEMBL4876877 | — | — | 1 | - |
| CHEMBL4877380 | — | — | 1 | - |
| CHEMBL4876349 | — | — | 1 | - |
| CHEMBL4863139 | — | — | 1 | - |
| CHEMBL4871400 | — | — | 1 | - |
| CHEMBL4878172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4868123 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4864525 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4877965 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL4871961 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL4850299 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL4873342 | — | IC50 | = | 4810.0 | nM | 5.32 |
| CHEMBL4859155 | — | IC50 | = | 4880.0 | nM | 5.31 |
| CHEMBL4876782 | — | IC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL4852200 | — | IC50 | = | 9220.0 | nM | 5.04 |
| CHEMBL4866073 | — | IC50 | = | 12310.0 | nM | 4.91 |
| CHEMBL4868601 | — | IC50 | = | 19740.0 | nM | 4.71 |
| CHEMBL4854838 | — | IC50 | = | 20150.0 | nM | 4.70 |
| CHEMBL4851688 | — | IC50 | = | 21510.0 | nM | 4.67 |
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | = | 23650.0 | nM | 4.63 |
| CHEMBL553 | ERLOTINIB | IC50 | = | 35800.0 | nM | 4.45 |
| CHEMBL4858111 | — | IC50 | = | 38200.0 | nM | 4.42 |
| CHEMBL4849988 | — | IC50 | = | 39230.0 | nM | 4.41 |
| CHEMBL2046727 | — | IC50 | = | 41550.0 | nM | 4.38 |
| CHEMBL4864777 | — | IC50 | = | 41540.0 | nM | 4.38 |
| CHEMBL4855229 | — | IC50 | = | 43070.0 | nM | 4.37 |
| CHEMBL4848752 | — | IC50 | = | 45600.0 | nM | 4.34 |
| CHEMBL4850384 | — | IC50 | = | 46370.0 | nM | 4.33 |
| CHEMBL4862924 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4867831 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL304929 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4571565 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4862560 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4453876 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4851189 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4845815 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4877045 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4866743 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4878172 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4871400 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4863139 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4876349 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4877380 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4876877 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4857994 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4852100 | — | IC50 | > | 50000.0 | nM | - |