Assay Detail
Binding
CHEMBL5032406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His6-tagged KDM2A (M1 to P517 residues) expressed in insect cells using H3K36(Me2) as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Alphascreen assay
13
Total Activities
13
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 |
Publication
First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 4.24 | 4.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5083418 | — | — | 1 | 4.62 |
| CHEMBL5081435 | — | — | 1 | 4.34 |
| CHEMBL5071002 | — | — | 1 | 4.30 |
| CHEMBL5084638 | — | — | 1 | 4.28 |
| CHEMBL5091848 | — | — | 1 | 4.23 |
| CHEMBL5071515 | — | — | 1 | 4.21 |
| CHEMBL5084143 | — | — | 1 | 4.20 |
| CHEMBL5089880 | — | — | 1 | 4.19 |
| CHEMBL5076580 | — | — | 1 | 4.17 |
| CHEMBL5070745 | — | — | 1 | 4.17 |
| CHEMBL5089117 | — | — | 1 | 4.16 |
| CHEMBL5072902 | — | — | 1 | 4.01 |
| CHEMBL5080728 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5083418 | — | IC50 | = | 24200.0 | nM | 4.62 |
| CHEMBL5081435 | — | IC50 | = | 45500.0 | nM | 4.34 |
| CHEMBL5071002 | — | IC50 | = | 49600.0 | nM | 4.30 |
| CHEMBL5084638 | — | IC50 | = | 52700.0 | nM | 4.28 |
| CHEMBL5091848 | — | IC50 | = | 58400.0 | nM | 4.23 |
| CHEMBL5071515 | — | IC50 | = | 61200.0 | nM | 4.21 |
| CHEMBL5084143 | — | IC50 | = | 63300.0 | nM | 4.20 |
| CHEMBL5089880 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL5076580 | — | IC50 | = | 67200.0 | nM | 4.17 |
| CHEMBL5070745 | — | IC50 | = | 68300.0 | nM | 4.17 |
| CHEMBL5089117 | — | IC50 | = | 69600.0 | nM | 4.16 |
| CHEMBL5072902 | — | IC50 | = | 97900.0 | nM | 4.01 |
| CHEMBL5080728 | — | IC50 | > | 100000.0 | nM | - |