Assay Detail
Binding
CHEMBL4024549
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Inhibition of biotin-labeled DCN1 (unknown origin) assessed as reduction in protein interaction with Ac-UBE2M12-AlexaFluor488 after 1 hr by TR-FRET assay
53
Total Activities
53
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
Discovery of an Orally Bioavailable Inhibitor of Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 6.24 | 7.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4067795 | — | — | 1 | 7.75 |
| CHEMBL4074213 | — | — | 1 | 7.35 |
| CHEMBL4099097 | — | — | 1 | 7.30 |
| CHEMBL4077431 | — | — | 1 | 7.27 |
| CHEMBL4077759 | — | — | 1 | 7.24 |
| CHEMBL4094517 | — | — | 1 | 7.17 |
| CHEMBL4078685 | — | — | 1 | 7.11 |
| CHEMBL4103209 | — | — | 1 | 7.09 |
| CHEMBL4086099 | — | — | 1 | 6.95 |
| CHEMBL4065355 | — | — | 1 | 6.62 |
| CHEMBL4079749 | — | — | 1 | 6.59 |
| CHEMBL4105639 | — | — | 1 | 6.58 |
| CHEMBL4087755 | — | — | 1 | 6.54 |
| CHEMBL4077301 | — | — | 1 | 6.52 |
| CHEMBL4064579 | — | — | 1 | 6.50 |
| CHEMBL4103413 | — | — | 1 | 6.49 |
| CHEMBL4093655 | — | — | 1 | 6.45 |
| CHEMBL4093853 | — | — | 1 | 6.45 |
| CHEMBL4102261 | — | — | 1 | 6.45 |
| CHEMBL4102027 | — | — | 1 | 6.32 |
| CHEMBL4065590 | — | — | 1 | 6.23 |
| CHEMBL4085483 | — | — | 1 | 6.21 |
| CHEMBL4096706 | — | — | 1 | 6.20 |
| CHEMBL4084296 | — | — | 1 | 6.18 |
| CHEMBL4086785 | — | — | 1 | 6.09 |
| CHEMBL4089008 | — | — | 1 | 6.00 |
| CHEMBL4075257 | — | — | 1 | 5.96 |
| CHEMBL4062267 | — | — | 1 | 5.89 |
| CHEMBL4101581 | — | — | 1 | 5.77 |
| CHEMBL4078934 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4067795 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4074213 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4099097 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4077431 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4077759 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4094517 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4078685 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4103209 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4086099 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4065355 | — | IC50 | = | 241.0 | nM | 6.62 |
| CHEMBL4079749 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL4105639 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4087755 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4077301 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL4064579 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL4103413 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL4093655 | — | IC50 | = | 358.0 | nM | 6.45 |
| CHEMBL4093853 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL4102261 | — | IC50 | = | 356.0 | nM | 6.45 |
| CHEMBL4102027 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL4065590 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL4085483 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL4096706 | — | IC50 | = | 626.0 | nM | 6.20 |
| CHEMBL4084296 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL4086785 | — | IC50 | = | 817.0 | nM | 6.09 |
| CHEMBL4089008 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4075257 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4062267 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4101581 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL4078934 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL4066268 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL4090274 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL4087623 | — | IC50 | = | 3210.0 | nM | 5.49 |
| CHEMBL4066082 | — | IC50 | = | 3570.0 | nM | 5.45 |
| CHEMBL4069860 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL4100965 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL4084962 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL4103074 | — | IC50 | = | 4490.0 | nM | 5.35 |
| CHEMBL4066771 | — | IC50 | = | 7440.0 | nM | 5.13 |
| CHEMBL4104429 | — | IC50 | = | 9430.0 | nM | 5.03 |
| CHEMBL4086530 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL4085911 | — | IC50 | > | 21000.0 | nM | - |
| CHEMBL4094295 | — | IC50 | > | 34000.0 | nM | - |
| CHEMBL4104015 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4103836 | — | IC50 | > | 22000.0 | nM | - |
| CHEMBL4063310 | — | IC50 | > | 24000.0 | nM | - |
| CHEMBL4079682 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4074690 | — | IC50 | > | 28000.0 | nM | - |
| CHEMBL4065214 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4092876 | — | IC50 | > | 28000.0 | nM | - |