Assay Detail
Binding
CHEMBL3379632
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CHK1 in HeLa S3 cells assessed as inhibition of phosphorylation at ser345 by AlphaScreen SureFire CHK1 (p-Ser345) assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa S3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.02 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3355074 | — | — | 1 | 7.43 |
| CHEMBL3355069 | — | — | 1 | 7.36 |
| CHEMBL3355072 | — | — | 1 | 7.10 |
| CHEMBL3355071 | — | — | 1 | 6.91 |
| CHEMBL3355073 | — | — | 1 | 6.80 |
| CHEMBL3355070 | — | — | 1 | 6.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3355074 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3355069 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3355072 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3355071 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL3355073 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3355070 | — | IC50 | = | 327.0 | nM | 6.49 |