Assay Detail
Binding
CHEMBL4325327
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged human ROCK1 catalytic domain (1 to 477 residues) expressed in baculovirus expression system using biotin-STK-substrate 2 as substrate preincubated with enzyme for 5 mins followed by ATP addition and measured after 2 hrs by TR-FRET assay
17
Total Activities
17
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
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.47 | 7.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4462898 | — | — | 1 | 7.02 |
| CHEMBL4569914 | — | — | 1 | 6.89 |
| CHEMBL4083927 | — | — | 1 | 6.85 |
| CHEMBL4589689 | — | — | 1 | 6.80 |
| CHEMBL4436649 | — | — | 1 | 6.66 |
| CHEMBL4542797 | — | — | 1 | 6.57 |
| CHEMBL4543158 | — | — | 1 | 6.47 |
| CHEMBL4440266 | — | — | 1 | 6.44 |
| CHEMBL4587191 | — | — | 1 | 6.43 |
| CHEMBL4439133 | — | — | 1 | 6.38 |
| CHEMBL4297644 | SIMUROSERTIB | 2.0 | 1 | 6.37 |
| CHEMBL4529213 | — | — | 1 | 6.35 |
| CHEMBL4572218 | — | — | 1 | 6.34 |
| CHEMBL4570191 | — | — | 1 | 6.28 |
| CHEMBL4462574 | — | — | 1 | 6.20 |
| CHEMBL4457256 | — | — | 1 | 6.12 |
| CHEMBL4561384 | — | — | 1 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4462898 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4569914 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4083927 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4589689 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4436649 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4542797 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4543158 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4440266 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4587191 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4439133 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4297644 | SIMUROSERTIB | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4529213 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4572218 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4570191 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4462574 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4457256 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4561384 | — | IC50 | = | 1500.0 | nM | 5.82 |