Assay Detail
Binding
CHEMBL895119
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Chk1 expressed in Sf9 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological activities of new checkpoint kinase 1 inhibitors structurally related to granulatimide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.70 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388648 | BIS-IMIDE A | — | 1 | 7.70 |
| CHEMBL397022 | — | — | 1 | 7.64 |
| CHEMBL243931 | — | — | 1 | 7.57 |
| CHEMBL395016 | — | — | 1 | 7.37 |
| CHEMBL240747 | GRANULATIMIDE | — | 1 | 7.09 |
| CHEMBL388037 | — | — | 1 | 6.97 |
| CHEMBL244141 | — | — | 1 | 6.79 |
| CHEMBL243930 | — | — | 1 | 6.57 |
| CHEMBL244140 | — | — | 1 | 6.51 |
| CHEMBL413188 | ISOGRANULATIMIDE | — | 1 | 6.36 |
| CHEMBL394608 | — | — | 1 | 6.05 |
| CHEMBL388434 | — | — | 1 | 6.04 |
| CHEMBL244353 | — | — | 1 | 5.75 |
| CHEMBL244142 | — | — | 1 | 5.43 |
| CHEMBL230868 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388648 | BIS-IMIDE A | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL397022 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL243931 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL395016 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL240747 | GRANULATIMIDE | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL388037 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL244141 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL243930 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL244140 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL413188 | ISOGRANULATIMIDE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL394608 | — | IC50 | = | 893.0 | nM | 6.05 |
| CHEMBL388434 | — | IC50 | = | 904.0 | nM | 6.04 |
| CHEMBL244353 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL244142 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL230868 | — | IC50 | - | — | - |