Assay Detail
Binding
CHEMBL3757620
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Inhibition of JMJD3 (unknown origin) using biotinylated H3K27me3 peptide as substrate after 1 hr by AlphaLISA assay
30
Total Activities
30
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
Design and discovery of new pyrimidine coupled nitrogen aromatic rings as chelating groups of JMJD3 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.00 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3753391 | — | — | 1 | 6.82 |
| CHEMBL3188597 | — | — | 1 | 6.82 |
| CHEMBL3752893 | — | — | 1 | 6.70 |
| CHEMBL3752179 | — | — | 1 | 6.68 |
| CHEMBL3753740 | — | — | 1 | 6.57 |
| CHEMBL3752769 | — | — | 1 | 6.31 |
| CHEMBL3752835 | — | — | 1 | 6.26 |
| CHEMBL3752143 | — | — | 1 | 6.22 |
| CHEMBL3752551 | — | — | 1 | 6.13 |
| CHEMBL3753449 | — | — | 1 | 6.12 |
| CHEMBL3752294 | — | — | 1 | 6.05 |
| CHEMBL3752343 | — | — | 1 | 6.03 |
| CHEMBL3753199 | — | — | 1 | 6.00 |
| CHEMBL3753326 | — | — | 1 | 6.00 |
| CHEMBL3753893 | — | — | 1 | 5.92 |
| CHEMBL3754078 | — | — | 1 | 5.92 |
| CHEMBL3752967 | — | — | 1 | 5.89 |
| CHEMBL3752156 | — | — | 1 | 5.85 |
| CHEMBL3753356 | — | — | 1 | 5.85 |
| CHEMBL3753787 | — | — | 1 | 5.82 |
| CHEMBL3752995 | — | — | 1 | 5.68 |
| CHEMBL3752006 | — | — | 1 | 5.68 |
| CHEMBL3754555 | — | — | 1 | 5.66 |
| CHEMBL3753303 | — | — | 1 | 5.58 |
| CHEMBL3754777 | — | — | 1 | 5.24 |
| CHEMBL3754383 | — | — | 1 | 5.21 |
| CHEMBL3754052 | — | — | 1 | 5.00 |
| CHEMBL3753122 | — | — | 1 | - |
| CHEMBL3752327 | — | — | 1 | - |
| CHEMBL3752471 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3753391 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3188597 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3752893 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3752179 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3753740 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3752769 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3752835 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3752143 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3752551 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3753449 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3752294 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3752343 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL3753199 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL3753326 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3753893 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3754078 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL3752967 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3752156 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3753356 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3753787 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3752995 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3752006 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3754555 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3753303 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3754777 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3754383 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL3754052 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL3753122 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3752327 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3752471 | — | IC50 | > | 100000.0 | nM | - |