Assay Detail
Functional
CHEMBL891237
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Inhibition of recombinant CHK1 assessed as human Cdc25C phosphorylation
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.90 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL242325 | — | — | 1 | 8.70 |
| CHEMBL242754 | — | — | 1 | 8.44 |
| CHEMBL242535 | — | — | 1 | 8.41 |
| CHEMBL242537 | — | — | 1 | 8.40 |
| CHEMBL242521 | — | — | 1 | 8.22 |
| CHEMBL438485 | — | — | 1 | 8.21 |
| CHEMBL389378 | — | — | 1 | 8.18 |
| CHEMBL242536 | — | — | 1 | 8.13 |
| CHEMBL389780 | — | — | 1 | 8.10 |
| CHEMBL242523 | — | — | 1 | 7.92 |
| CHEMBL242738 | — | — | 1 | 7.92 |
| CHEMBL242753 | — | — | 1 | 7.89 |
| CHEMBL242522 | — | — | 1 | 7.82 |
| CHEMBL242949 | — | — | 1 | 7.82 |
| CHEMBL242737 | — | — | 1 | 7.70 |
| CHEMBL395752 | — | — | 1 | 7.66 |
| CHEMBL243188 | — | — | 1 | 7.54 |
| CHEMBL390626 | — | — | 1 | 7.16 |
| CHEMBL242736 | — | — | 1 | 6.91 |
| CHEMBL397233 | — | — | 1 | 6.34 |
| CHEMBL390024 | — | — | 1 | 6.32 |
| CHEMBL244231 | — | — | 1 | 6.30 |
| CHEMBL243398 | — | — | 1 | 6.27 |
| CHEMBL242735 | — | — | 1 | 6.22 |
| CHEMBL243817 | — | — | 1 | 6.10 |
| CHEMBL266664 | — | — | 1 | 6.09 |
| CHEMBL395307 | — | — | 1 | 6.01 |
| CHEMBL428392 | — | — | 1 | 5.99 |
| CHEMBL390222 | — | — | 1 | 5.98 |
| CHEMBL428398 | — | — | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL242325 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL242754 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL242535 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL242537 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL242521 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL438485 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL389378 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL242536 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL389780 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL242523 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL242738 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL242753 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL242522 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL242949 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL242737 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL395752 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL243188 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL390626 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL242736 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL397233 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL390024 | — | IC50 | = | 481.0 | nM | 6.32 |
| CHEMBL244231 | — | IC50 | = | 497.0 | nM | 6.30 |
| CHEMBL243398 | — | IC50 | = | 535.0 | nM | 6.27 |
| CHEMBL242735 | — | IC50 | = | 602.0 | nM | 6.22 |
| CHEMBL243817 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL266664 | — | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL395307 | — | IC50 | = | 966.0 | nM | 6.01 |
| CHEMBL428392 | — | IC50 | = | 1029.0 | nM | 5.99 |
| CHEMBL390222 | — | IC50 | = | 1042.0 | nM | 5.98 |
| CHEMBL428398 | — | IC50 | = | 1473.0 | nM | 5.83 |
| CHEMBL243818 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL242324 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL243819 | — | IC50 | = | 2044.0 | nM | 5.69 |
| CHEMBL396027 | — | IC50 | = | 3064.0 | nM | 5.51 |
| CHEMBL243399 | — | IC50 | = | 4825.0 | nM | 5.32 |
| CHEMBL396536 | — | IC50 | = | 5260.0 | nM | 5.28 |
| CHEMBL438329 | — | IC50 | = | 6472.0 | nM | 5.19 |
| CHEMBL390627 | — | IC50 | = | 8742.0 | nM | 5.06 |