Assay Detail
Binding
CHEMBL942709
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Chk1
39
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 8.61 | 9.52 |
| Ki | 1 | 8.40 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL399916 | — | — | 1 | 9.52 |
| CHEMBL400397 | — | — | 1 | 9.52 |
| CHEMBL400805 | — | — | 1 | 9.52 |
| CHEMBL249363 | — | — | 1 | 9.52 |
| CHEMBL401196 | — | — | 1 | 9.00 |
| CHEMBL437772 | — | — | 1 | 9.00 |
| CHEMBL401337 | — | — | 1 | 9.00 |
| CHEMBL248553 | — | — | 1 | 9.00 |
| CHEMBL248554 | — | — | 1 | 9.00 |
| CHEMBL248555 | — | — | 1 | 9.00 |
| CHEMBL249364 | — | — | 1 | 9.00 |
| CHEMBL249156 | — | — | 1 | 9.00 |
| CHEMBL249764 | — | — | 1 | 8.70 |
| CHEMBL398757 | — | — | 1 | 8.70 |
| CHEMBL249765 | — | — | 1 | 8.70 |
| CHEMBL400574 | — | — | 1 | 8.70 |
| CHEMBL248755 | — | — | 1 | 8.70 |
| CHEMBL400693 | — | — | 1 | 8.70 |
| CHEMBL400575 | — | — | 1 | 8.52 |
| CHEMBL248952 | — | — | 1 | 8.52 |
| CHEMBL400806 | — | — | 1 | 8.52 |
| CHEMBL250173 | — | — | 1 | 8.52 |
| CHEMBL400668 | — | — | 1 | 8.52 |
| CHEMBL248951 | — | — | 1 | 8.40 |
| CHEMBL248757 | — | — | 2 | 8.40 |
| CHEMBL249971 | — | — | 1 | 8.40 |
| CHEMBL400804 | — | — | 1 | 8.40 |
| CHEMBL249972 | — | — | 1 | 8.22 |
| CHEMBL398875 | — | — | 1 | 8.22 |
| CHEMBL248953 | — | — | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL399916 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL400397 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL400805 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL249363 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL249364 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL249156 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL248555 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL248554 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL248553 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL401337 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL437772 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL401196 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL249765 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL248755 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL400574 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL400693 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL249764 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL398757 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL250173 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL400806 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL400668 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL400575 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL248952 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL249971 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL248757 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL248757 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL400804 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL248951 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL249972 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL375097 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL248953 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL398875 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL375097 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL220002 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL249155 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL249154 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL250375 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL248756 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL374417 | — | IC50 | = | 28.0 | nM | 7.55 |