Assay Detail
Functional
CHEMBL856403
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inhibition of histone-H3 phosphorylation following 24 hr incubation in SW620 tumor cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | SW-620 |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.00 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214637 | — | — | 1 | 8.70 |
| CHEMBL215022 | — | — | 1 | 8.30 |
| CHEMBL201307 | — | — | 1 | 8.30 |
| CHEMBL215495 | — | — | 1 | 8.15 |
| CHEMBL215322 | — | — | 1 | 8.15 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.77 |
| CHEMBL214849 | — | — | 1 | 7.75 |
| CHEMBL215203 | — | — | 1 | 7.62 |
| CHEMBL385049 | — | — | 1 | 7.38 |
| CHEMBL214848 | — | — | 1 | 7.35 |
| CHEMBL214940 | — | — | 1 | 7.35 |
| CHEMBL386310 | — | — | 1 | 7.15 |
| CHEMBL214842 | — | — | 1 | 7.11 |
| CHEMBL214601 | — | — | 1 | 6.92 |
| CHEMBL384054 | — | — | 1 | 6.89 |
| CHEMBL215275 | — | — | 1 | 6.57 |
| CHEMBL217804 | — | — | 1 | 6.54 |
| CHEMBL424899 | — | — | 1 | 6.48 |
| CHEMBL262434 | — | — | 1 | 6.43 |
| CHEMBL263067 | — | — | 1 | 6.27 |
| CHEMBL386253 | — | — | 1 | 6.20 |
| CHEMBL216769 | — | — | 1 | 6.17 |
| CHEMBL215636 | — | — | 1 | 5.92 |
| CHEMBL405120 | — | — | 1 | 5.75 |
| CHEMBL216388 | — | — | 1 | 5.58 |
| CHEMBL385597 | — | — | 1 | 5.26 |
| CHEMBL216053 | — | — | 1 | - |
| CHEMBL214648 | — | — | 1 | - |
| CHEMBL268345 | — | — | 1 | - |
| CHEMBL217037 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214637 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL215022 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL201307 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL215495 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL215322 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL215152 | DEFOSBARASERTIB | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL214849 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL215203 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL385049 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL214848 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL214940 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL386310 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL214842 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL214601 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL384054 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL215275 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL217804 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL424899 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL262434 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL263067 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL386253 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL216769 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL215636 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL405120 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL216388 | — | Ki | = | 2600.0 | nM | 5.58 |
| CHEMBL385597 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL216053 | — | Ki | < | 1.0 | nM | - |
| CHEMBL214648 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL268345 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL217037 | — | Ki | > | 10000.0 | nM | - |