Assay Detail
Binding
CHEMBL5323879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CHK1 (unknown origin) using peptide substrate S1 and ATP as substrate incubated for 1 hr by HTRF assay
52
Total Activities
52
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 Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 52 | 7.12 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428756 | — | — | 1 | 8.29 |
| CHEMBL5409504 | — | — | 1 | 8.12 |
| CHEMBL5426241 | — | — | 1 | 8.12 |
| CHEMBL5421825 | — | — | 1 | 8.12 |
| CHEMBL5431016 | — | — | 1 | 8.07 |
| CHEMBL5403690 | — | — | 1 | 8.01 |
| CHEMBL5427417 | — | — | 1 | 8.00 |
| CHEMBL5413462 | — | — | 1 | 7.97 |
| CHEMBL5411251 | — | — | 1 | 7.97 |
| CHEMBL5409206 | — | — | 1 | 7.93 |
| CHEMBL5433322 | — | — | 1 | 7.90 |
| CHEMBL5439250 | — | — | 1 | 7.88 |
| CHEMBL5408927 | — | — | 1 | 7.87 |
| CHEMBL5427282 | — | — | 1 | 7.86 |
| CHEMBL5410841 | — | — | 1 | 7.75 |
| CHEMBL5419654 | — | — | 1 | 7.72 |
| CHEMBL5089164 | — | — | 1 | 7.58 |
| CHEMBL5438311 | — | — | 1 | 7.57 |
| CHEMBL4169078 | SRA-737 | 1.0 | 1 | 7.54 |
| CHEMBL5412757 | — | — | 1 | 7.46 |
| CHEMBL5430670 | — | — | 1 | 7.45 |
| CHEMBL5439334 | — | — | 1 | 7.39 |
| CHEMBL5420872 | — | — | 1 | 7.24 |
| CHEMBL5433221 | — | — | 1 | 7.23 |
| CHEMBL5410542 | — | — | 1 | 7.21 |
| CHEMBL5424522 | — | — | 1 | 7.17 |
| CHEMBL5439325 | — | — | 1 | 7.10 |
| CHEMBL5401396 | — | — | 1 | 7.06 |
| CHEMBL5394796 | — | — | 1 | 7.06 |
| CHEMBL5425583 | — | — | 1 | 7.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5428756 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5409504 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5421825 | — | IC50 | = | 7.61 | nM | 8.12 |
| CHEMBL5426241 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5431016 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5403690 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5427417 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL5413462 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL5411251 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5409206 | — | IC50 | = | 11.66 | nM | 7.93 |
| CHEMBL5433322 | — | IC50 | = | 12.55 | nM | 7.90 |
| CHEMBL5439250 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5408927 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5427282 | — | IC50 | = | 13.97 | nM | 7.86 |
| CHEMBL5410841 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5419654 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5089164 | — | IC50 | = | 26.26 | nM | 7.58 |
| CHEMBL5438311 | — | IC50 | = | 26.65 | nM | 7.57 |
| CHEMBL4169078 | SRA-737 | IC50 | = | 28.9 | nM | 7.54 |
| CHEMBL5412757 | — | IC50 | = | 34.53 | nM | 7.46 |
| CHEMBL5430670 | — | IC50 | = | 35.16 | nM | 7.45 |
| CHEMBL5439334 | — | IC50 | = | 41.09 | nM | 7.39 |
| CHEMBL5420872 | — | IC50 | = | 57.97 | nM | 7.24 |
| CHEMBL5433221 | — | IC50 | = | 58.49 | nM | 7.23 |
| CHEMBL5410542 | — | IC50 | = | 61.6 | nM | 7.21 |
| CHEMBL5424522 | — | IC50 | = | 66.86 | nM | 7.17 |
| CHEMBL5439325 | — | IC50 | = | 80.12 | nM | 7.10 |
| CHEMBL5401396 | — | IC50 | = | 87.25 | nM | 7.06 |
| CHEMBL5394796 | — | IC50 | = | 86.51 | nM | 7.06 |
| CHEMBL5425583 | — | IC50 | = | 96.01 | nM | 7.02 |
| CHEMBL5395135 | — | IC50 | = | 124.4 | nM | 6.91 |
| CHEMBL5428637 | — | IC50 | = | 134.65 | nM | 6.87 |
| CHEMBL5431718 | — | IC50 | = | 158.55 | nM | 6.80 |
| CHEMBL5433344 | — | IC50 | = | 206.3 | nM | 6.69 |
| CHEMBL5415961 | — | IC50 | = | 219.3 | nM | 6.66 |
| CHEMBL5432487 | — | IC50 | = | 223.45 | nM | 6.65 |
| CHEMBL5409205 | — | IC50 | = | 227.25 | nM | 6.64 |
| CHEMBL5407292 | — | IC50 | = | 250.45 | nM | 6.60 |
| CHEMBL5428033 | — | IC50 | = | 301.3 | nM | 6.52 |
| CHEMBL5398690 | — | IC50 | = | 335.8 | nM | 6.47 |
| CHEMBL5433681 | — | IC50 | = | 362.25 | nM | 6.44 |
| CHEMBL5438895 | — | IC50 | = | 765.15 | nM | 6.12 |
| CHEMBL5432385 | — | IC50 | = | 827.0 | nM | 6.08 |
| CHEMBL5398934 | — | IC50 | = | 951.8 | nM | 6.02 |
| CHEMBL5401693 | — | IC50 | = | 1064.0 | nM | 5.97 |
| CHEMBL5420001 | — | IC50 | = | 1088.7 | nM | 5.96 |
| CHEMBL5440060 | — | IC50 | = | 1967.0 | nM | 5.71 |
| CHEMBL5408938 | — | IC50 | = | 1949.0 | nM | 5.71 |
| CHEMBL5420169 | — | IC50 | = | 2005.0 | nM | 5.70 |
| CHEMBL5429443 | — | IC50 | = | 2019.0 | nM | 5.70 |