Assay Detail
Functional
CHEMBL1809665
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Antiproliferative activity in human A2780 cells after 72 hrs by CellTiter-Glo assay
17
Total Activities
17
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
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.53 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1807301 | — | — | 1 | 7.14 |
| CHEMBL1807303 | — | — | 1 | 7.08 |
| CHEMBL1808343 | — | — | 1 | 7.08 |
| CHEMBL1808341 | — | — | 1 | 7.00 |
| CHEMBL1808338 | — | — | 1 | 6.87 |
| CHEMBL1808340 | — | — | 1 | 6.82 |
| CHEMBL1807306 | — | — | 1 | 6.61 |
| CHEMBL1808339 | — | — | 1 | 6.53 |
| CHEMBL1807302 | — | — | 1 | 6.39 |
| CHEMBL1807300 | — | — | 1 | 6.38 |
| CHEMBL1807304 | — | — | 1 | 6.31 |
| CHEMBL559845 | — | — | 1 | 6.30 |
| CHEMBL1808336 | — | — | 1 | 6.27 |
| CHEMBL1808342 | — | — | 1 | 6.11 |
| CHEMBL1236095 | — | — | 1 | 6.00 |
| CHEMBL1808337 | — | — | 1 | 5.54 |
| CHEMBL1807305 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1807301 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1807303 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1808343 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1808341 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL1808338 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL1808340 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL1807306 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL1808339 | — | IC50 | = | 298.0 | nM | 6.53 |
| CHEMBL1807302 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL1807300 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL1807304 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL559845 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1808336 | — | IC50 | = | 541.0 | nM | 6.27 |
| CHEMBL1808342 | — | IC50 | = | 771.0 | nM | 6.11 |
| CHEMBL1236095 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1808337 | — | IC50 | = | 2858.0 | nM | 5.54 |
| CHEMBL1807305 | — | IC50 | < | 16.0 | nM | - |