Assay Detail
Binding
CHEMBL4817610
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Inhibition of recombinant human His-tagged DCN1 (58 to 259 residues) expressed in Escherichia coli BL21 (DE3) using MIKLFSLKQQKKEEESAGGTK-biotin as substrate incubated for 30 mins by HTRF assay
41
Total Activities
40
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
Development of phenyltriazole thiol-based derivatives as highly potent inhibitors of DCN1-UBC12 interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.53 | 7.58 |
| Ki | 1 | 7.64 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4865016 | — | — | 2 | 7.64 |
| CHEMBL4440896 | — | — | 1 | 7.22 |
| CHEMBL4878599 | — | — | 1 | 7.13 |
| CHEMBL4869654 | — | — | 1 | 7.11 |
| CHEMBL4847848 | — | — | 1 | 7.08 |
| CHEMBL4874768 | — | — | 1 | 6.97 |
| CHEMBL4854235 | — | — | 1 | 6.94 |
| CHEMBL4851610 | — | — | 1 | 6.92 |
| CHEMBL1334768 | — | — | 1 | 6.90 |
| CHEMBL4860176 | — | — | 1 | 6.87 |
| CHEMBL4868697 | — | — | 1 | 6.84 |
| CHEMBL4871768 | — | — | 1 | 6.84 |
| CHEMBL4846458 | — | — | 1 | 6.81 |
| CHEMBL4847553 | — | — | 1 | 6.72 |
| CHEMBL4866253 | — | — | 1 | 6.49 |
| CHEMBL4860279 | — | — | 1 | 6.42 |
| CHEMBL4856019 | — | — | 1 | 6.30 |
| CHEMBL4849618 | — | — | 1 | 6.30 |
| CHEMBL1447470 | — | — | 1 | 6.30 |
| CHEMBL1448063 | — | — | 1 | 6.30 |
| CHEMBL85091 | — | — | 1 | 6.30 |
| CHEMBL4869738 | — | — | 1 | 6.15 |
| CHEMBL4875837 | — | — | 1 | 6.15 |
| CHEMBL4866516 | — | — | 1 | 6.02 |
| CHEMBL1990098 | — | — | 1 | 5.99 |
| CHEMBL225662 | — | — | 1 | 5.49 |
| CHEMBL4855199 | — | — | 1 | 5.38 |
| CHEMBL4857539 | — | — | 1 | 5.31 |
| CHEMBL4850533 | — | — | 1 | - |
| CHEMBL1370907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4865016 | — | Ki | = | 22.92 | nM | 7.64 |
| CHEMBL4865016 | — | IC50 | = | 26.36 | nM | 7.58 |
| CHEMBL4440896 | — | IC50 | = | 60.28 | nM | 7.22 |
| CHEMBL4878599 | — | IC50 | = | 74.69 | nM | 7.13 |
| CHEMBL4869654 | — | IC50 | = | 77.55 | nM | 7.11 |
| CHEMBL4847848 | — | IC50 | = | 83.91 | nM | 7.08 |
| CHEMBL4874768 | — | IC50 | = | 107.56 | nM | 6.97 |
| CHEMBL4854235 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4851610 | — | IC50 | = | 121.21 | nM | 6.92 |
| CHEMBL1334768 | — | IC50 | = | 126.99 | nM | 6.90 |
| CHEMBL4860176 | — | IC50 | = | 136.1 | nM | 6.87 |
| CHEMBL4868697 | — | IC50 | = | 144.74 | nM | 6.84 |
| CHEMBL4871768 | — | IC50 | = | 145.99 | nM | 6.84 |
| CHEMBL4846458 | — | IC50 | = | 155.8 | nM | 6.81 |
| CHEMBL4847553 | — | IC50 | = | 188.53 | nM | 6.72 |
| CHEMBL4866253 | — | IC50 | = | 326.46 | nM | 6.49 |
| CHEMBL4860279 | — | IC50 | = | 377.57 | nM | 6.42 |
| CHEMBL85091 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1448063 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4849618 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4856019 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1447470 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4869738 | — | IC50 | = | 706.88 | nM | 6.15 |
| CHEMBL4875837 | — | IC50 | = | 710.78 | nM | 6.15 |
| CHEMBL4866516 | — | IC50 | = | 957.11 | nM | 6.02 |
| CHEMBL1990098 | — | IC50 | = | 1023.29 | nM | 5.99 |
| CHEMBL225662 | — | IC50 | = | 3262.67 | nM | 5.49 |
| CHEMBL4855199 | — | IC50 | = | 4195.78 | nM | 5.38 |
| CHEMBL4857539 | — | IC50 | = | 4871.55 | nM | 5.31 |
| CHEMBL4867481 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4879214 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4865774 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL22794 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1334528 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4859802 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1461372 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4872319 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3809713 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1322981 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1370907 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4850533 | — | IC50 | > | 10000.0 | nM | - |