Assay Detail
Binding
CHEMBL4037443
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Inhibition of CHK1 in human HT29 cells assessed as abrogation of camptothecin-induced G2/M phase arrest
28
Total Activities
28
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
Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 28 | 6.91 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059912 | — | — | 1 | 8.10 |
| CHEMBL4093952 | — | — | 1 | 8.00 |
| CHEMBL4079910 | — | — | 1 | 8.00 |
| CHEMBL4097937 | — | — | 1 | 7.92 |
| CHEMBL487273 | — | — | 1 | 7.72 |
| CHEMBL4098878 | — | — | 1 | 7.62 |
| CHEMBL1287920 | — | — | 1 | 7.58 |
| CHEMBL4067770 | — | — | 1 | 7.52 |
| CHEMBL4104102 | — | — | 1 | 7.52 |
| CHEMBL4088986 | — | — | 1 | 7.40 |
| CHEMBL4100776 | — | — | 1 | 7.30 |
| CHEMBL4096683 | — | — | 1 | 7.28 |
| CHEMBL4071952 | — | — | 1 | 7.22 |
| CHEMBL4105353 | — | — | 1 | 7.16 |
| CHEMBL4079391 | — | — | 1 | 6.96 |
| CHEMBL4066751 | — | — | 1 | 6.82 |
| CHEMBL4068572 | — | — | 1 | 6.68 |
| CHEMBL4089699 | — | — | 1 | 6.47 |
| CHEMBL4081097 | — | — | 1 | 6.41 |
| CHEMBL4082801 | — | — | 1 | 6.39 |
| CHEMBL4097424 | — | — | 1 | 6.08 |
| CHEMBL4081827 | — | — | 1 | 6.06 |
| CHEMBL4094277 | — | — | 1 | 5.64 |
| CHEMBL4066399 | — | — | 1 | 5.48 |
| CHEMBL4076939 | — | — | 1 | 5.43 |
| CHEMBL4104408 | — | — | 1 | 5.00 |
| CHEMBL4098331 | — | — | 1 | - |
| CHEMBL4078664 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059912 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4093952 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4079910 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4097937 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL487273 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4098878 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1287920 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4067770 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4104102 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4088986 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4100776 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4096683 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4071952 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4105353 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4079391 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4066751 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4068572 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4089699 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4081097 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4082801 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4097424 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4081827 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL4094277 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4066399 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4076939 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4104408 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4098331 | — | EC50 | - | — | - | |
| CHEMBL4078664 | — | EC50 | - | — | - |