Assay Detail
Binding
CHEMBL4036257
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal GST-tagged ROCK1 catalytic domain (1 to 477 residues) expressed in baculovirus expression system using Biotin-STK2 as substrate pretreated for 5 mins followed by ATP addition after 2 hrs by TR-FRET assay
24
Total Activities
24
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 |
Publication
2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.39 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4065361 | — | — | 1 | 8.39 |
| CHEMBL4086790 | — | — | 1 | 7.40 |
| CHEMBL4083927 | — | — | 1 | 6.85 |
| CHEMBL4078941 | — | — | 1 | 6.80 |
| CHEMBL4105646 | — | — | 1 | 6.77 |
| CHEMBL4080367 | — | — | 1 | 6.75 |
| CHEMBL4078031 | — | — | 1 | 6.70 |
| CHEMBL4062209 | — | — | 1 | 6.58 |
| CHEMBL4070822 | — | — | 1 | 6.44 |
| CHEMBL4096077 | — | — | 1 | 6.43 |
| CHEMBL4080673 | — | — | 1 | 6.40 |
| CHEMBL4095460 | — | — | 1 | 6.38 |
| CHEMBL4068071 | — | — | 1 | 6.27 |
| CHEMBL4091694 | — | — | 1 | 6.21 |
| CHEMBL4087760 | — | — | 1 | 6.11 |
| CHEMBL4098392 | — | — | 1 | 6.09 |
| CHEMBL4084945 | — | — | 1 | 6.08 |
| CHEMBL4091279 | — | — | 1 | 6.03 |
| CHEMBL4103214 | — | — | 1 | 5.92 |
| CHEMBL4063842 | — | — | 1 | 5.82 |
| CHEMBL4073971 | — | — | 1 | 5.80 |
| CHEMBL4061122 | — | — | 1 | 5.80 |
| CHEMBL4081417 | — | — | 1 | 5.77 |
| CHEMBL4099435 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4065361 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4086790 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4083927 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4078941 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4105646 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4080367 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4078031 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4062209 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4070822 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4096077 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4080673 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4095460 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4068071 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4091694 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4087760 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL4098392 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4084945 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL4091279 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4103214 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4063842 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4073971 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4061122 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4081417 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4099435 | — | IC50 | = | 2100.0 | nM | 5.68 |