Assay Detail
Binding
CHEMBL1000361
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Inhibition of Chk1 kinase assessed as GST-Cdc25 phosphorylation by Western blot determination
64
Total Activities
64
Compounds Tested
1
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
Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 6.65 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455192 | — | — | 1 | 8.70 |
| CHEMBL516488 | — | — | 1 | 8.52 |
| CHEMBL452336 | — | — | 1 | 8.30 |
| CHEMBL508541 | — | — | 1 | 7.92 |
| CHEMBL512341 | — | — | 1 | 7.75 |
| CHEMBL508515 | — | — | 1 | 7.68 |
| CHEMBL518048 | — | — | 1 | 7.57 |
| CHEMBL454908 | — | — | 1 | 7.54 |
| CHEMBL517744 | — | — | 1 | 7.52 |
| CHEMBL512012 | — | — | 1 | 7.46 |
| CHEMBL519238 | — | — | 1 | 7.44 |
| CHEMBL214253 | — | — | 1 | 7.33 |
| CHEMBL462011 | — | — | 1 | 7.28 |
| CHEMBL519891 | — | — | 1 | 7.27 |
| CHEMBL472542 | — | — | 1 | 7.27 |
| CHEMBL486665 | — | — | 1 | 7.26 |
| CHEMBL214005 | — | — | 1 | 7.25 |
| CHEMBL470117 | — | — | 1 | 7.23 |
| CHEMBL520904 | — | — | 1 | 7.11 |
| CHEMBL472209 | — | — | 1 | 7.11 |
| CHEMBL471156 | — | — | 1 | 7.06 |
| CHEMBL508516 | — | — | 1 | 7.02 |
| CHEMBL486868 | — | — | 1 | 6.96 |
| CHEMBL472208 | — | — | 1 | 6.92 |
| CHEMBL511992 | — | — | 1 | 6.92 |
| CHEMBL411662 | — | — | 1 | 6.77 |
| CHEMBL488054 | — | — | 1 | 6.75 |
| CHEMBL511280 | — | — | 1 | 6.70 |
| CHEMBL487891 | — | — | 1 | 6.70 |
| CHEMBL453347 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455192 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL516488 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL452336 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL508541 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL512341 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL508515 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL518048 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL454908 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL517744 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL512012 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL519238 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL214253 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL462011 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL472542 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL519891 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL486665 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL214005 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL470117 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL520904 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL472209 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL471156 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL508516 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL486868 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL472208 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL511992 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL411662 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL488054 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL511280 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL487891 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL453347 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL452079 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL209388 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL520240 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL488899 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL529897 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL521051 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL470113 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL510668 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL471163 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL462170 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL511991 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL513079 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL379975 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL471157 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL471329 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL461134 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL461116 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL529669 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL508412 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL487031 | — | IC50 | = | 850.0 | nM | 6.07 |