Assay Detail
Binding
CHEMBL2427609
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Inhibition of KDM4A (unknown origin) using H3K9me3 peptide and 2-oxoglutarate as substrate after 1 hr by FDH-coupled assay
12
Total Activities
12
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
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.62 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1229308 | — | — | 1 | 6.10 |
| CHEMBL316034 | — | — | 1 | 5.38 |
| CHEMBL2424816 | — | — | 1 | 4.19 |
| CHEMBL2424809 | — | — | 1 | 4.04 |
| CHEMBL2424815 | — | — | 1 | 4.00 |
| CHEMBL2424811 | — | — | 1 | 4.00 |
| CHEMBL2424814 | — | — | 1 | - |
| CHEMBL2424813 | — | — | 1 | - |
| CHEMBL2424812 | — | — | 1 | - |
| CHEMBL2424810 | — | — | 1 | - |
| CHEMBL2164243 | — | — | 1 | - |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1229308 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL316034 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL2424816 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL2424809 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL2424815 | — | IC50 | = | 99000.0 | nM | 4.00 |
| CHEMBL2424811 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL2424814 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL2424813 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL2424812 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL2424810 | — | IC50 | > | 120000.0 | nM | - |
| CHEMBL2164243 | — | IC50 | > | 3300000.0 | nM | - |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 250000.0 | nM | - |