Assay Detail
Binding
CHEMBL3624698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDM2A (unknown origin) using Biotin-H3(28-48)K36Me2 and H3(28-48)K36Me2 substrates incubated for 30 mins by alpha screen assay
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.34 | 7.20 |
| pIC50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3621881 | — | — | 1 | 7.20 |
| CHEMBL3621878 | — | — | 1 | 6.90 |
| CHEMBL3621872 | — | — | 1 | 6.40 |
| CHEMBL3621880 | — | — | 1 | 6.20 |
| CHEMBL3621873 | — | — | 1 | 6.00 |
| CHEMBL3621879 | — | — | 1 | 5.70 |
| CHEMBL3621864 | — | — | 1 | 5.60 |
| CHEMBL3621882 | — | — | 1 | 5.50 |
| CHEMBL3621863 | — | — | 1 | 5.40 |
| CHEMBL3621852 | — | — | 1 | 5.40 |
| CHEMBL3621877 | — | — | 1 | 5.30 |
| CHEMBL3621851 | — | — | 1 | 5.30 |
| CHEMBL3621868 | — | — | 1 | 5.30 |
| CHEMBL3621858 | — | — | 1 | 5.20 |
| CHEMBL3621860 | — | — | 1 | 5.20 |
| CHEMBL3621855 | — | — | 1 | 5.20 |
| CHEMBL3621869 | — | — | 1 | 5.20 |
| CHEMBL3621876 | — | — | 1 | 5.10 |
| CHEMBL3621857 | — | — | 1 | 5.10 |
| CHEMBL3621859 | — | — | 1 | 5.10 |
| CHEMBL3621861 | — | — | 1 | 5.10 |
| CHEMBL3621862 | — | — | 1 | 5.10 |
| CHEMBL3621870 | — | — | 1 | 5.00 |
| CHEMBL3621856 | — | — | 1 | 5.00 |
| CHEMBL3621853 | — | — | 1 | 4.90 |
| CHEMBL3621875 | — | — | 1 | 4.90 |
| CHEMBL3621871 | — | — | 1 | 4.90 |
| CHEMBL3621854 | — | — | 1 | 4.50 |
| CHEMBL3621867 | — | — | 1 | 4.30 |
| CHEMBL3621866 | — | — | 1 | 4.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3621881 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3621878 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3621872 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3621880 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3621873 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3621879 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3621864 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL3621882 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL3621863 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3621852 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3621877 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3621851 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3621868 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3621860 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3621858 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3621869 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3621855 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3621876 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3621857 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3621859 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3621861 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3621862 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL3621856 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3621870 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3621853 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3621875 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3621871 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL3621854 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL3621867 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL3621866 | — | IC50 | = | 79432.82 | nM | 4.10 |
| CHEMBL3621865 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3621874 | — | pIC50 | - | — | - |