Assay Detail
Binding
CHEMBL2167522
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Inhibition of human KDM2A expressed in Escherichia coli using methyl lysine peptide substrate by AlphaScreen assay
10
Total Activities
10
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
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.77 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2164246 | — | — | 1 | 6.60 |
| CHEMBL2164245 | — | — | 1 | 6.43 |
| CHEMBL51979 | — | — | 1 | 6.37 |
| CHEMBL222824 | SUCCINYLACETONE | — | 1 | 6.24 |
| CHEMBL2164243 | — | — | 1 | 5.82 |
| CHEMBL2164247 | — | — | 1 | 5.43 |
| CHEMBL2164249 | — | — | 1 | 5.04 |
| CHEMBL2164244 | — | — | 1 | 4.20 |
| CHEMBL2164250 | — | — | 1 | - |
| CHEMBL2164248 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2164246 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2164245 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL51979 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL222824 | SUCCINYLACETONE | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL2164243 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2164247 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL2164249 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL2164244 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL2164250 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2164248 | — | IC50 | > | 100000.0 | nM | - |