Assay Detail
Binding
CHEMBL924433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Chk1 expressed in baculovirus by time-resolved fluorescence assay
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Serine/threonine-protein kinase Chk1 (CHEMBL4630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.82 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL249443 | — | — | 1 | 9.52 |
| CHEMBL249429 | — | — | 1 | 9.30 |
| CHEMBL249237 | — | — | 1 | 9.22 |
| CHEMBL250035 | — | — | 1 | 9.10 |
| CHEMBL249441 | — | — | 1 | 9.00 |
| CHEMBL250459 | — | — | 1 | 8.92 |
| CHEMBL250272 | — | — | 1 | 8.92 |
| CHEMBL249241 | — | — | 1 | 8.70 |
| CHEMBL249240 | — | — | 1 | 8.70 |
| CHEMBL249238 | — | — | 1 | 8.70 |
| CHEMBL249044 | — | — | 1 | 8.64 |
| CHEMBL400350 | — | — | 1 | 8.62 |
| CHEMBL400127 | — | — | 1 | 8.60 |
| CHEMBL249632 | — | — | 1 | 8.59 |
| CHEMBL249796 | — | — | 1 | 8.52 |
| CHEMBL428409 | — | — | 1 | 8.52 |
| CHEMBL249224 | — | — | 1 | 8.46 |
| CHEMBL250033 | — | — | 1 | 8.46 |
| CHEMBL401156 | — | — | 1 | 8.44 |
| CHEMBL249834 | — | — | 1 | 8.43 |
| CHEMBL400323 | — | — | 1 | 8.37 |
| CHEMBL249236 | — | — | 1 | 8.19 |
| CHEMBL428580 | — | — | 1 | 8.04 |
| CHEMBL250225 | — | — | 1 | 7.96 |
| CHEMBL249597 | — | — | 1 | 7.96 |
| CHEMBL248665 | — | — | 1 | 7.94 |
| CHEMBL249594 | — | — | 1 | 7.92 |
| CHEMBL249595 | — | — | 1 | 7.77 |
| CHEMBL250224 | — | — | 1 | 7.60 |
| CHEMBL399966 | — | — | 1 | 7.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL249443 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL249429 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL249237 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL250035 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL249441 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL250459 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL250272 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL249241 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL249240 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL249238 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL249044 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL400350 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL400127 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL249632 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL428409 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL249796 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL249224 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL250033 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL401156 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL249834 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL400323 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL249236 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL428580 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL249597 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL250225 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL248665 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL249594 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL249595 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL250224 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL399966 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL250222 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL248584 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL250029 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL399023 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL248995 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL248993 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL249401 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL400661 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL249400 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL248988 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL399902 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL250628 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL248992 | — | IC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL436640 | — | IC50 | = | 1080.0 | nM | 5.97 |