Assay Detail
Binding
CHEMBL4222553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DCN1-mediated cullin neddylation assessed as reduction in transfer of fluorescein-5-maleimide-tagged NEDD8 from N-terminally acetylated human UBE2M to CUL2-CTD measured for 10 sec by pulse-chase 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
Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.42 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099097 | — | — | 1 | 7.10 |
| CHEMBL4072130 | — | — | 1 | 6.96 |
| CHEMBL4102019 | — | — | 1 | 6.85 |
| CHEMBL4063514 | — | — | 1 | 6.75 |
| CHEMBL4103922 | — | — | 1 | 6.43 |
| CHEMBL4078680 | — | — | 1 | 6.40 |
| CHEMBL4104419 | — | — | 1 | 6.31 |
| CHEMBL4096696 | — | — | 1 | 6.24 |
| CHEMBL4226502 | — | — | 1 | 5.77 |
| CHEMBL4086524 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099097 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4072130 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4102019 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4063514 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4103922 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4078680 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4104419 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4096696 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4226502 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4086524 | — | EC50 | = | 4200.0 | nM | 5.38 |