Assay Detail
Binding
CHEMBL5127903
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Inhibition of KDM1A (unknown origin)
8
Total Activities
8
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
Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.76 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4802155 | VAFIDEMSTAT | 2.0 | 1 | 9.85 |
| CHEMBL608561 | — | — | 1 | 8.41 |
| CHEMBL4596515 | — | — | 1 | 7.29 |
| CHEMBL5181906 | — | — | 1 | 6.53 |
| CHEMBL294199 | CAPSAICIN | 4.0 | 1 | 6.22 |
| CHEMBL81 | RALOXIFENE | 4.0 | 1 | 5.68 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.40 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | — | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4802155 | VAFIDEMSTAT | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL608561 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4596515 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL5181906 | — | IC50 | = | 296.0 | nM | 6.53 |
| CHEMBL294199 | CAPSAICIN | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL81 | RALOXIFENE | IC50 | = | 2080.0 | nM | 5.68 |
| CHEMBL3353410 | OSIMERTINIB | IC50 | = | 3980.0 | nM | 5.40 |
| CHEMBL257990 | (+)-TRANYLCYPROMINE | IC50 | = | 22000.0 | nM | 4.66 |