Assay Detail
Functional
CHEMBL941014
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Mitotic arrest in human A2780 cells assessed as G2/M block after 16 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | A2780 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 8.20 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250127 | — | — | 1 | 8.60 |
| CHEMBL398478 | — | — | 1 | 8.36 |
| CHEMBL251142 | — | — | 1 | 8.32 |
| CHEMBL429553 | — | — | 1 | 8.32 |
| CHEMBL401476 | — | — | 1 | 8.30 |
| CHEMBL250125 | — | — | 1 | 8.30 |
| CHEMBL250532 | — | — | 1 | 8.19 |
| CHEMBL438876 | — | — | 1 | 8.16 |
| CHEMBL250328 | — | — | 1 | 8.13 |
| CHEMBL250126 | — | — | 1 | 8.05 |
| CHEMBL250743 | — | — | 1 | 7.96 |
| CHEMBL399378 | — | — | 1 | 7.96 |
| CHEMBL250533 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250127 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL398478 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL251142 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL429553 | — | EC50 | = | 4.8 | nM | 8.32 |
| CHEMBL401476 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL250125 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL250532 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL438876 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL250328 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL250126 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL250743 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL399378 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL250533 | — | EC50 | = | 13.0 | nM | 7.89 |