Assay Detail
Functional
CHEMBL940955
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Inhibition of KSP-induced nucleolin phosphorylation in cell-based mitotic arrest assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.40 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL247044 | — | — | 1 | 8.49 |
| CHEMBL250125 | — | — | 1 | 8.30 |
| CHEMBL246604 | — | — | 1 | 8.03 |
| CHEMBL246603 | — | — | 1 | 7.96 |
| CHEMBL246422 | — | — | 1 | 7.82 |
| CHEMBL443490 | — | — | 1 | 7.57 |
| CHEMBL392599 | — | — | 1 | 7.42 |
| CHEMBL248244 | — | — | 1 | 7.40 |
| CHEMBL247414 | — | — | 1 | 7.34 |
| CHEMBL246001 | — | — | 1 | 7.28 |
| CHEMBL248400 | — | — | 1 | 7.11 |
| CHEMBL401006 | — | — | 1 | 6.86 |
| CHEMBL247594 | — | — | 1 | 6.68 |
| CHEMBL393647 | — | — | 1 | 6.43 |
| CHEMBL246000 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL247044 | — | EC50 | = | 3.2 | nM | 8.49 |
| CHEMBL250125 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL246604 | — | EC50 | = | 9.4 | nM | 8.03 |
| CHEMBL246603 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL246422 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL443490 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL392599 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL248244 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL247414 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL246001 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL248400 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL401006 | — | EC50 | = | 138.0 | nM | 6.86 |
| CHEMBL247594 | — | EC50 | = | 208.0 | nM | 6.68 |
| CHEMBL393647 | — | EC50 | = | 368.0 | nM | 6.43 |
| CHEMBL246000 | — | EC50 | = | 567.0 | nM | 6.25 |