Assay Detail
Binding
CHEMBL2072693
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CHK1 in human HT29 cells assessed as abrogation of camptothecin induced check point
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 7.39 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070713 | — | — | 1 | 8.10 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 8.00 |
| CHEMBL2070704 | — | — | 1 | 8.00 |
| CHEMBL487273 | — | — | 1 | 7.70 |
| CHEMBL2070700 | — | — | 1 | 7.70 |
| CHEMBL2070697 | — | — | 1 | 7.70 |
| CHEMBL2070710 | — | — | 1 | 7.70 |
| CHEMBL2070702 | — | — | 1 | 7.70 |
| CHEMBL2070699 | — | — | 1 | 7.70 |
| CHEMBL2070705 | — | — | 1 | 7.52 |
| CHEMBL2070701 | — | — | 1 | 7.52 |
| CHEMBL2070714 | — | — | 1 | 7.52 |
| CHEMBL2070716 | — | — | 1 | 7.40 |
| CHEMBL2070703 | — | — | 1 | 7.40 |
| CHEMBL2070708 | — | — | 1 | 7.22 |
| CHEMBL2070706 | — | — | 1 | 7.22 |
| CHEMBL2070698 | — | — | 1 | 7.10 |
| CHEMBL2070707 | — | — | 1 | 7.00 |
| CHEMBL2070711 | — | — | 1 | 6.82 |
| CHEMBL2070709 | — | — | 1 | 6.72 |
| CHEMBL2070712 | — | — | 1 | 6.70 |
| CHEMBL2070715 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070713 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2041933 | AZD-7762 | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2070704 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL487273 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070700 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070697 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070710 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070702 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070699 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2070705 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2070701 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2070714 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2070716 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2070703 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2070708 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2070706 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2070698 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2070707 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2070711 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2070709 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2070712 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2070715 | — | EC50 | = | 940.0 | nM | 6.03 |