Assay Detail
Binding
CHEMBL5136852
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ROCK in rat A7R5 cells assessed as cofilin serine 3 phosphorylation incubated for 1 hr by ICW assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | A7R5 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntington's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.63 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5206259 | — | — | 1 | 8.10 |
| CHEMBL4448806 | — | — | 1 | 8.05 |
| CHEMBL5192610 | — | — | 1 | 7.85 |
| CHEMBL5208605 | — | — | 1 | 7.82 |
| CHEMBL5186165 | — | — | 1 | 7.75 |
| CHEMBL5199904 | — | — | 1 | 7.48 |
| CHEMBL5181094 | — | — | 1 | 7.36 |
| CHEMBL5200987 | — | — | 1 | 7.15 |
| CHEMBL3580669 | — | — | 1 | 7.13 |
| CHEMBL4459800 | — | — | 1 | 7.11 |
| CHEMBL5169406 | — | — | 1 | 6.97 |
| CHEMBL5188032 | — | — | 1 | 6.91 |
| CHEMBL5183751 | — | — | 1 | 6.90 |
| CHEMBL5180112 | — | — | 1 | 6.79 |
| CHEMBL5209364 | — | — | 1 | 6.60 |
| CHEMBL5174891 | — | — | 1 | 6.58 |
| CHEMBL5176687 | — | — | 1 | 6.54 |
| CHEMBL5201650 | — | — | 1 | 6.49 |
| CHEMBL5171140 | — | — | 1 | 6.17 |
| CHEMBL5187325 | — | — | 1 | 6.14 |
| CHEMBL3581146 | — | — | 1 | 6.08 |
| CHEMBL5193152 | — | — | 1 | 6.02 |
| CHEMBL5184099 | — | — | 1 | 6.01 |
| CHEMBL5207169 | — | — | 1 | 5.99 |
| CHEMBL5209466 | — | — | 1 | 5.84 |
| CHEMBL559147 | Y-27632 | — | 1 | 5.52 |
| CHEMBL5171976 | — | — | 1 | 5.48 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 5.42 |
| CHEMBL5186844 | — | — | 1 | 5.37 |
| CHEMBL5205297 | — | — | 1 | 5.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5206259 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4448806 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5192610 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5208605 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5186165 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5199904 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5181094 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5200987 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3580669 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4459800 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5169406 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5188032 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL5183751 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5180112 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL5209364 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL5174891 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5176687 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL5201650 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL5171140 | — | IC50 | = | 673.0 | nM | 6.17 |
| CHEMBL5187325 | — | IC50 | = | 721.0 | nM | 6.14 |
| CHEMBL3581146 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL5193152 | — | IC50 | = | 963.0 | nM | 6.02 |
| CHEMBL5184099 | — | IC50 | = | 974.0 | nM | 6.01 |
| CHEMBL5207169 | — | IC50 | = | 1030.0 | nM | 5.99 |
| CHEMBL5209466 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL559147 | Y-27632 | IC50 | = | 3026.0 | nM | 5.52 |
| CHEMBL5171976 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL1233300 | HYDROXYFASUDIL | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL5186844 | — | IC50 | = | 4270.0 | nM | 5.37 |
| CHEMBL5205297 | — | IC50 | = | 4930.0 | nM | 5.31 |
| CHEMBL5197969 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5187811 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL5207486 | — | IC50 | > | 5000.0 | nM | - |