Assay Detail
Binding
CHEMBL2025930
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Inhibition of human His-puritin-tagged ROCK1 expressed in Sf9 cells after 1 hr by FRET-based enzyme-coupled assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 4.95 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2023154 | — | — | 1 | 6.19 |
| CHEMBL2023156 | — | — | 1 | 5.94 |
| CHEMBL2023160 | — | — | 1 | 5.85 |
| CHEMBL2023158 | — | — | 1 | 5.77 |
| CHEMBL2023153 | — | — | 1 | 5.66 |
| CHEMBL2023155 | — | — | 1 | 5.61 |
| CHEMBL2023152 | — | — | 1 | 5.58 |
| CHEMBL2023159 | — | — | 1 | 5.58 |
| CHEMBL2023151 | — | — | 1 | 5.54 |
| CHEMBL2023150 | — | — | 1 | 5.34 |
| CHEMBL2023157 | — | — | 1 | 5.04 |
| CHEMBL225282 | — | — | 1 | 4.86 |
| CHEMBL2023149 | — | — | 1 | 4.67 |
| CHEMBL2023161 | — | — | 1 | 4.51 |
| CHEMBL2023147 | — | — | 1 | 4.23 |
| CHEMBL503641 | — | — | 1 | 4.19 |
| CHEMBL2022282 | — | — | 1 | 4.14 |
| CHEMBL67352 | — | — | 1 | 4.12 |
| CHEMBL2023148 | — | — | 1 | 3.80 |
| CHEMBL17551 | — | — | 1 | 3.74 |
| CHEMBL1566648 | — | — | 1 | 3.57 |
| CHEMBL2023144 | — | — | 1 | - |
| CHEMBL2023145 | — | — | 1 | - |
| CHEMBL2023146 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2023154 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2023156 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL2023160 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL2023158 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL2023153 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL2023155 | — | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL2023152 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL2023159 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL2023151 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2023150 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL2023157 | — | IC50 | = | 9070.0 | nM | 5.04 |
| CHEMBL225282 | — | IC50 | = | 13900.0 | nM | 4.86 |
| CHEMBL2023149 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL2023161 | — | IC50 | = | 31010.0 | nM | 4.51 |
| CHEMBL2023147 | — | IC50 | = | 59100.0 | nM | 4.23 |
| CHEMBL503641 | — | IC50 | = | 65000.0 | nM | 4.19 |
| CHEMBL2022282 | — | IC50 | = | 72500.0 | nM | 4.14 |
| CHEMBL67352 | — | IC50 | = | 75500.0 | nM | 4.12 |
| CHEMBL2023148 | — | IC50 | = | 157100.0 | nM | 3.80 |
| CHEMBL17551 | — | IC50 | = | 181300.0 | nM | 3.74 |
| CHEMBL1566648 | — | IC50 | = | 270000.0 | nM | 3.57 |
| CHEMBL2023144 | — | IC50 | > | 400000.0 | nM | - |
| CHEMBL2023145 | — | IC50 | > | 400000.0 | nM | - |
| CHEMBL2023146 | — | IC50 | - | — | - |