Assay Detail
Binding
CHEMBL896339
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Inhibition of recombinant CHK-mediated Cdc25C phosphorylation after 30 mins
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 8.20 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL232810 | — | — | 1 | 9.68 |
| CHEMBL234868 | — | — | 1 | 9.62 |
| CHEMBL428196 | — | — | 1 | 9.62 |
| CHEMBL232809 | — | — | 1 | 9.37 |
| CHEMBL393993 | — | — | 1 | 9.29 |
| CHEMBL232808 | — | — | 1 | 9.26 |
| CHEMBL234871 | — | — | 1 | 9.25 |
| CHEMBL234656 | — | — | 1 | 9.13 |
| CHEMBL234869 | — | — | 1 | 9.08 |
| CHEMBL234402 | — | — | 1 | 8.96 |
| CHEMBL234654 | — | — | 1 | 8.92 |
| CHEMBL392516 | — | — | 1 | 8.68 |
| CHEMBL444630 | — | — | 1 | 8.64 |
| CHEMBL232806 | — | — | 1 | 8.64 |
| CHEMBL391449 | — | — | 1 | 8.36 |
| CHEMBL232804 | — | — | 1 | 8.36 |
| CHEMBL232805 | — | — | 1 | 8.30 |
| CHEMBL234867 | — | — | 1 | 8.28 |
| CHEMBL232391 | — | — | 1 | 8.26 |
| CHEMBL234482 | — | — | 1 | 8.19 |
| CHEMBL393603 | — | — | 1 | 8.15 |
| CHEMBL232392 | — | — | 1 | 8.11 |
| CHEMBL391450 | — | — | 1 | 8.11 |
| CHEMBL234479 | — | — | 1 | 8.03 |
| CHEMBL234866 | — | — | 1 | 7.92 |
| CHEMBL233640 | — | — | 1 | 7.75 |
| CHEMBL399215 | — | — | 1 | 7.62 |
| CHEMBL233641 | — | — | 1 | 7.57 |
| CHEMBL233831 | — | — | 1 | 7.55 |
| CHEMBL234865 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL232810 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL234868 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL428196 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL232809 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL393993 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL232808 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL234871 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL234656 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL234869 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL234402 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL234654 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL392516 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL444630 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL232806 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL232804 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL391449 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL232805 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL234867 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL232391 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL234482 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL393603 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL232392 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL391450 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL234479 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL234866 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL233640 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL399215 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL233641 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL233831 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL234865 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL232807 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL392517 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL392555 | — | IC50 | = | 671.0 | nM | 6.17 |
| CHEMBL399012 | — | IC50 | = | 1373.0 | nM | 5.86 |
| CHEMBL233830 | — | IC50 | = | 9091.0 | nM | 5.04 |
| CHEMBL232803 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL393195 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL233832 | — | IC50 | > | 10000.0 | nM | - |