Assay Detail
Binding
CHEMBL2443630
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant LSD1 (157 to 852 aa) expressed in Escherichia coli BL21(DE) using H3K4me2 as substrate by fluorescence assay
85
Total Activities
85
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
Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 85 | 4.48 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2334501 | — | — | 1 | 5.68 |
| CHEMBL2334497 | — | — | 1 | 5.10 |
| CHEMBL2334499 | — | — | 1 | 4.94 |
| CHEMBL2440574 | — | — | 1 | 4.82 |
| CHEMBL2440573 | — | — | 1 | 4.77 |
| CHEMBL2334505 | — | — | 1 | 4.76 |
| CHEMBL2334502 | — | — | 1 | 4.74 |
| CHEMBL2334504 | — | — | 1 | 4.72 |
| CHEMBL2334191 | — | — | 1 | 4.71 |
| CHEMBL2334498 | — | — | 1 | 4.67 |
| CHEMBL2334488 | — | — | 1 | 4.65 |
| CHEMBL2440577 | — | — | 1 | 4.60 |
| CHEMBL2440536 | — | — | 1 | 4.56 |
| CHEMBL2440565 | — | — | 1 | 4.56 |
| CHEMBL1255743 | TRANYLCYPROMINE HYDROCHLORIDE | — | 1 | 4.56 |
| CHEMBL2334190 | — | — | 1 | 4.54 |
| CHEMBL2334490 | — | — | 1 | 4.53 |
| CHEMBL2440575 | — | — | 1 | 4.52 |
| CHEMBL2334484 | — | — | 1 | 4.48 |
| CHEMBL2334489 | — | — | 1 | 4.46 |
| CHEMBL2440568 | — | — | 1 | 4.45 |
| CHEMBL2440566 | — | — | 1 | 4.40 |
| CHEMBL2440562 | — | — | 1 | 4.39 |
| CHEMBL2334491 | — | — | 1 | 4.36 |
| CHEMBL2440567 | — | — | 1 | 4.36 |
| CHEMBL2440532 | — | — | 1 | 4.36 |
| CHEMBL2440569 | — | — | 1 | 4.34 |
| CHEMBL2440576 | — | — | 1 | 4.33 |
| CHEMBL2334485 | — | — | 1 | 4.32 |
| CHEMBL2440542 | — | — | 1 | 4.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2334501 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2334497 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL2334499 | — | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL2440574 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2440573 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL2334505 | — | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL2334502 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL2334504 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2334191 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL2334498 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL2334488 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL2440577 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL2440565 | — | IC50 | = | 27600.0 | nM | 4.56 |
| CHEMBL1255743 | TRANYLCYPROMINE HYDROCHLORIDE | IC50 | = | 27800.0 | nM | 4.56 |
| CHEMBL2440536 | — | IC50 | = | 27500.0 | nM | 4.56 |
| CHEMBL2334190 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL2334490 | — | IC50 | = | 29500.0 | nM | 4.53 |
| CHEMBL2440575 | — | IC50 | = | 30200.0 | nM | 4.52 |
| CHEMBL2334484 | — | IC50 | = | 32800.0 | nM | 4.48 |
| CHEMBL2334489 | — | IC50 | = | 35100.0 | nM | 4.46 |
| CHEMBL2440568 | — | IC50 | = | 35700.0 | nM | 4.45 |
| CHEMBL2440566 | — | IC50 | = | 39800.0 | nM | 4.40 |
| CHEMBL2440562 | — | IC50 | = | 40300.0 | nM | 4.39 |
| CHEMBL2440532 | — | IC50 | = | 43300.0 | nM | 4.36 |
| CHEMBL2334491 | — | IC50 | = | 43500.0 | nM | 4.36 |
| CHEMBL2440567 | — | IC50 | = | 43900.0 | nM | 4.36 |
| CHEMBL2440569 | — | IC50 | = | 45700.0 | nM | 4.34 |
| CHEMBL2440576 | — | IC50 | = | 47100.0 | nM | 4.33 |
| CHEMBL2334485 | — | IC50 | = | 47600.0 | nM | 4.32 |
| CHEMBL2440542 | — | IC50 | = | 51200.0 | nM | 4.29 |
| CHEMBL2334486 | — | IC50 | = | 53200.0 | nM | 4.27 |
| CHEMBL2440570 | — | IC50 | = | 55100.0 | nM | 4.26 |
| CHEMBL2334500 | — | IC50 | = | 56500.0 | nM | 4.25 |
| CHEMBL2334187 | — | IC50 | = | 69300.0 | nM | 4.16 |
| CHEMBL2440538 | — | IC50 | = | 69200.0 | nM | 4.16 |
| CHEMBL2440537 | — | IC50 | = | 70700.0 | nM | 4.15 |
| CHEMBL2440540 | — | IC50 | = | 77100.0 | nM | 4.11 |
| CHEMBL2440541 | — | IC50 | = | 81300.0 | nM | 4.09 |
| CHEMBL2440559 | — | IC50 | = | 83400.0 | nM | 4.08 |
| CHEMBL2440571 | — | IC50 | = | 87400.0 | nM | 4.06 |
| CHEMBL2334503 | — | IC50 | = | 88900.0 | nM | 4.05 |
| CHEMBL2440534 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440527 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440522 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440539 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440526 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440535 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440530 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440533 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL2440528 | — | IC50 | > | 125000.0 | nM | - |