Assay Detail
Binding
CHEMBL5370463
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant LSD1 expressed in Escherichia coli using H3K4me2 peptide as substrate incubated for 60 mins by AlphaLISA assay
43
Total Activities
43
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 Pyrrolo[2,3-<i>c</i>]pyridines as Potent and Reversible LSD1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 7.54 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5410439 | — | — | 1 | 8.89 |
| CHEMBL5410299 | — | — | 1 | 8.85 |
| CHEMBL5436614 | — | — | 1 | 8.51 |
| CHEMBL5421505 | — | — | 1 | 8.46 |
| CHEMBL5433666 | — | — | 1 | 8.43 |
| CHEMBL5436979 | — | — | 1 | 8.41 |
| CHEMBL5408486 | — | — | 1 | 8.37 |
| CHEMBL5405014 | — | — | 1 | 8.37 |
| CHEMBL5422998 | — | — | 1 | 8.34 |
| CHEMBL5402939 | — | — | 1 | 8.29 |
| CHEMBL5405592 | — | — | 1 | 8.19 |
| CHEMBL5400044 | — | — | 1 | 8.03 |
| CHEMBL5425081 | — | — | 1 | 7.91 |
| CHEMBL5407627 | — | — | 1 | 7.89 |
| CHEMBL5405687 | — | — | 1 | 7.81 |
| CHEMBL5399283 | — | — | 1 | 7.78 |
| CHEMBL5402736 | — | — | 1 | 7.76 |
| CHEMBL5418795 | — | — | 1 | 7.69 |
| CHEMBL5405194 | — | — | 1 | 7.68 |
| CHEMBL5421980 | — | — | 1 | 7.61 |
| CHEMBL4297641 | SECLIDEMSTAT | 2.0 | 1 | 7.58 |
| CHEMBL5440467 | — | — | 1 | 7.55 |
| CHEMBL5405326 | — | — | 1 | 7.46 |
| CHEMBL5415382 | — | — | 1 | 7.37 |
| CHEMBL5396712 | — | — | 1 | 7.34 |
| CHEMBL5430791 | — | — | 1 | 7.32 |
| CHEMBL5403000 | — | — | 1 | 7.27 |
| CHEMBL5406073 | — | — | 1 | 7.23 |
| CHEMBL5427183 | — | — | 1 | 7.16 |
| CHEMBL5439191 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5410439 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5410299 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5436614 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5421505 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5433666 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL5436979 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5408486 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5405014 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5422998 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5402939 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5405592 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5400044 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5425081 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5407627 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL5405687 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL5399283 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5402736 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL5418795 | — | IC50 | = | 20.5 | nM | 7.69 |
| CHEMBL5405194 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL5421980 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL4297641 | SECLIDEMSTAT | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL5440467 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL5405326 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL5415382 | — | IC50 | = | 42.8 | nM | 7.37 |
| CHEMBL5396712 | — | IC50 | = | 46.1 | nM | 7.34 |
| CHEMBL5430791 | — | IC50 | = | 47.9 | nM | 7.32 |
| CHEMBL5403000 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL5406073 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL5427183 | — | IC50 | = | 69.8 | nM | 7.16 |
| CHEMBL5439191 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5417291 | — | IC50 | = | 94.3 | nM | 7.03 |
| CHEMBL5400159 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL3134377 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5407075 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5402233 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5437054 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL5422216 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL5418187 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL5433815 | — | IC50 | = | 3713.0 | nM | 5.43 |
| CHEMBL5399271 | — | IC50 | = | 6250.0 | nM | 5.20 |
| CHEMBL5440108 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5422472 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406978 | — | IC50 | > | 1000.0 | nM | - |