Assay Detail
Binding
CHEMBL1947437
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Chk2 using STK1 as substrate after 10 mins by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk2 (CHEMBL2527) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.09 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332551 | — | — | 1 | 8.10 |
| CHEMBL1947251 | — | — | 1 | 7.85 |
| CHEMBL1947252 | — | — | 1 | 7.85 |
| CHEMBL1947250 | — | — | 1 | 7.70 |
| CHEMBL1947253 | — | — | 1 | 7.55 |
| CHEMBL1944822 | — | — | 1 | 6.81 |
| CHEMBL1944823 | — | — | 1 | 6.77 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | — | 1 | 6.74 |
| CHEMBL1944821 | — | — | 1 | 6.56 |
| CHEMBL1947254 | — | — | 1 | 6.23 |
| CHEMBL1947255 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332551 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1947251 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1947252 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1947250 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1947253 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1944822 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL1944823 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL1944821 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL1947254 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL1947255 | — | IC50 | = | 1526.0 | nM | 5.82 |