Assay Detail
Binding
CHEMBL5151019
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Inhibition of NAE (unknown origin) mediated neddylation assessed as decrease in NEDD8-Ubcl2 adduct formation incubated for 2 hrs in presence of L-glutathione and ATP by HTRF assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Development of Potent NEDD8-Activating Enzyme Inhibitors Bearing a Pyrimidotriazole Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.96 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5170838 | — | — | 1 | 10.70 |
| CHEMBL5182746 | — | — | 1 | 9.68 |
| CHEMBL1231160 | PEVONEDISTAT | 3.0 | 1 | 9.59 |
| CHEMBL5177755 | — | — | 1 | 9.26 |
| CHEMBL5206652 | — | — | 1 | 9.24 |
| CHEMBL5173723 | — | — | 1 | 8.65 |
| CHEMBL5192493 | — | — | 1 | 8.64 |
| CHEMBL5197178 | — | — | 1 | 8.45 |
| CHEMBL5209054 | — | — | 1 | 8.38 |
| CHEMBL5188530 | — | — | 1 | 8.24 |
| CHEMBL5193236 | — | — | 1 | 8.22 |
| CHEMBL5177700 | — | — | 1 | 8.21 |
| CHEMBL5178136 | — | — | 1 | 8.01 |
| CHEMBL5192527 | — | — | 1 | 8.00 |
| CHEMBL5169743 | — | — | 1 | 7.80 |
| CHEMBL5170141 | — | — | 1 | 7.68 |
| CHEMBL5179467 | — | — | 1 | 7.68 |
| CHEMBL5207989 | — | — | 1 | 7.51 |
| CHEMBL5201960 | — | — | 1 | 7.17 |
| CHEMBL5206633 | — | — | 1 | 7.09 |
| CHEMBL5206263 | — | — | 1 | 7.09 |
| CHEMBL5190183 | — | — | 1 | 6.97 |
| CHEMBL5188300 | — | — | 1 | 6.92 |
| CHEMBL5200375 | — | — | 1 | 6.83 |
| CHEMBL5173277 | — | — | 1 | 6.77 |
| CHEMBL5188093 | — | — | 1 | 6.73 |
| CHEMBL5189807 | — | — | 1 | 6.68 |
| CHEMBL5197934 | — | — | 1 | 6.66 |
| CHEMBL5187203 | — | — | 1 | - |
| CHEMBL5197609 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5170838 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5182746 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL1231160 | PEVONEDISTAT | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL5177755 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL5206652 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5173723 | — | IC50 | = | 2.23 | nM | 8.65 |
| CHEMBL5192493 | — | IC50 | = | 2.28 | nM | 8.64 |
| CHEMBL5197178 | — | IC50 | = | 3.56 | nM | 8.45 |
| CHEMBL5209054 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5188530 | — | IC50 | = | 5.77 | nM | 8.24 |
| CHEMBL5193236 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5177700 | — | IC50 | = | 6.11 | nM | 8.21 |
| CHEMBL5178136 | — | IC50 | = | 9.76 | nM | 8.01 |
| CHEMBL5192527 | — | IC50 | = | 9.98 | nM | 8.00 |
| CHEMBL5169743 | — | IC50 | = | 15.9 | nM | 7.80 |
| CHEMBL5170141 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL5179467 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL5207989 | — | IC50 | = | 30.6 | nM | 7.51 |
| CHEMBL5201960 | — | IC50 | = | 66.9 | nM | 7.17 |
| CHEMBL5206633 | — | IC50 | = | 81.8 | nM | 7.09 |
| CHEMBL5206263 | — | IC50 | = | 80.9 | nM | 7.09 |
| CHEMBL5190183 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5188300 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5200375 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL5173277 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5188093 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL5189807 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5197934 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL5187203 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5197609 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5183530 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5173798 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5199010 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5201980 | — | IC50 | > | 10000.0 | nM | - |