Assay Detail
Binding
CHEMBL868459
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Chk1
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 7.49 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381517 | — | — | 1 | 8.52 |
| CHEMBL207596 | — | — | 1 | 8.30 |
| CHEMBL207994 | — | — | 1 | 8.15 |
| CHEMBL206460 | — | — | 1 | 8.15 |
| CHEMBL208332 | — | — | 1 | 8.10 |
| CHEMBL379095 | — | — | 1 | 8.05 |
| CHEMBL207606 | — | — | 1 | 8.05 |
| CHEMBL205449 | — | — | 1 | 8.00 |
| CHEMBL206812 | — | — | 1 | 8.00 |
| CHEMBL379458 | — | — | 1 | 7.96 |
| CHEMBL202635 | — | — | 1 | 7.92 |
| CHEMBL207778 | — | — | 1 | 7.89 |
| CHEMBL207995 | — | — | 1 | 7.85 |
| CHEMBL208728 | — | — | 1 | 7.82 |
| CHEMBL206098 | — | — | 1 | 7.82 |
| CHEMBL207060 | — | — | 1 | 7.75 |
| CHEMBL206213 | — | — | 1 | 7.66 |
| CHEMBL206997 | — | — | 1 | 7.64 |
| CHEMBL206663 | — | — | 1 | 7.60 |
| CHEMBL205950 | — | — | 1 | 7.50 |
| CHEMBL205744 | — | — | 1 | 7.42 |
| CHEMBL205699 | — | — | 1 | 7.42 |
| CHEMBL206139 | — | — | 1 | 7.38 |
| CHEMBL205491 | — | — | 1 | 7.38 |
| CHEMBL205590 | — | — | 1 | 7.37 |
| CHEMBL205951 | — | — | 1 | 7.35 |
| CHEMBL381527 | — | — | 1 | 7.29 |
| CHEMBL202837 | — | — | 1 | 7.24 |
| CHEMBL377304 | — | — | 1 | 7.19 |
| CHEMBL205543 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381517 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL207596 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL206460 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL207994 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL208332 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL379095 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL207606 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL205449 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL206812 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL379458 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL202635 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL207778 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL207995 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL208728 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL206098 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL207060 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL206213 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL206997 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL206663 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL205950 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL205699 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL205744 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL206139 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL205491 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL205590 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL205951 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL381527 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL202837 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL377304 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL205543 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL210516 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL206143 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL208537 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL202838 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL381172 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL205754 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL383670 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL205088 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL207582 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL378800 | — | IC50 | = | 328.0 | nM | 6.48 |
| CHEMBL206558 | — | IC50 | = | 1365.0 | nM | 5.87 |
| CHEMBL425593 | — | IC50 | > | 10000.0 | nM | - |