Assay Detail
Binding
CHEMBL913833
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant Chk1
52
Total Activities
49
Compounds Tested
2
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
Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 8.00 | 9.00 |
| Ki | 3 | 8.19 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373732 | — | — | 1 | 9.00 |
| CHEMBL219875 | — | — | 1 | 9.00 |
| CHEMBL220473 | — | — | 1 | 9.00 |
| CHEMBL373598 | — | — | 2 | 8.70 |
| CHEMBL222421 | — | — | 1 | 8.70 |
| CHEMBL375144 | — | — | 1 | 8.70 |
| CHEMBL223589 | — | — | 1 | 8.70 |
| CHEMBL223672 | — | — | 1 | 8.70 |
| CHEMBL219689 | — | — | 1 | 8.70 |
| CHEMBL219979 | — | — | 1 | 8.52 |
| CHEMBL373897 | — | — | 1 | 8.52 |
| CHEMBL223257 | — | — | 1 | 8.52 |
| CHEMBL223640 | — | — | 1 | 8.40 |
| CHEMBL220525 | — | — | 1 | 8.40 |
| CHEMBL223367 | — | — | 2 | 8.37 |
| CHEMBL374334 | — | — | 1 | 8.30 |
| CHEMBL219637 | — | — | 1 | 8.30 |
| CHEMBL223347 | — | — | 1 | 8.22 |
| CHEMBL223311 | — | — | 1 | 8.22 |
| CHEMBL375097 | — | — | 1 | 8.22 |
| CHEMBL375644 | — | — | 1 | 8.22 |
| CHEMBL413779 | — | — | 1 | 8.22 |
| CHEMBL223255 | — | — | 1 | 8.15 |
| CHEMBL387341 | — | — | 1 | 8.15 |
| CHEMBL374416 | — | — | 1 | 8.15 |
| CHEMBL220002 | — | — | 1 | 8.15 |
| CHEMBL376037 | — | — | 1 | 8.05 |
| CHEMBL222413 | — | — | 1 | 8.05 |
| CHEMBL223512 | — | — | 1 | 8.00 |
| CHEMBL219952 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373732 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL220473 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL219875 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL222421 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL223672 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL375144 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL223589 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL373598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL219689 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL223257 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL219979 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL373897 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL223640 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL220525 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL223367 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL373598 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL374334 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL219637 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL223367 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL223311 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL375097 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL375644 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL413779 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL223347 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL223255 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL374416 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL220002 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL387341 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL376037 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL222413 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL223512 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL219952 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL220034 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL223312 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL373837 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL223833 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL220035 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL223460 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL223460 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL223542 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL223879 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL219635 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL374417 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL222414 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL376526 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL223509 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL223565 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL438642 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL435750 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL223141 | — | IC50 | = | 266.0 | nM | 6.58 |