Assay Detail
Binding
CHEMBL4427798
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CENP-E motor domain assessed as ADP levels preincubated with protein motor domain/microtubule for 60 mins followed by ATP addition measured after 20 mins by ADPglo assay
8
Total Activities
8
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 synthesis of fused bicyclic inhibitors targeting the L5 loop site of centromere-associated protein E.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.35 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4470356 | — | — | 1 | 8.82 |
| CHEMBL4579540 | — | — | 1 | 8.80 |
| CHEMBL4549646 | — | — | 1 | 8.77 |
| CHEMBL4468555 | — | — | 1 | 8.66 |
| CHEMBL4515745 | — | — | 1 | 8.57 |
| CHEMBL4579162 | — | — | 1 | 7.85 |
| CHEMBL4466617 | — | — | 1 | 7.72 |
| CHEMBL4483703 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4470356 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4579540 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4549646 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4468555 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4515745 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4579162 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4466617 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4483703 | — | IC50 | = | 24.0 | nM | 7.62 |