Assay Detail
Binding
CHEMBL912250
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Inhibition of human recombinant ROCK1 expressed in Sf9 cells at 10 mM
9
Total Activities
9
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 | Expert |
Publication
Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.69 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218719 | — | — | 1 | 8.30 |
| CHEMBL427058 | GSK-466317A | — | 1 | 8.10 |
| CHEMBL374453 | GSK-299115A | — | 1 | 8.10 |
| CHEMBL218720 | GSK-466314A | — | 1 | 8.05 |
| CHEMBL441702 | GSK-270822A | — | 1 | 8.05 |
| CHEMBL384073 | GSK-180736A | — | 1 | 7.85 |
| CHEMBL375312 | — | — | 1 | 7.85 |
| CHEMBL218654 | — | — | 1 | 7.29 |
| CHEMBL217910 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218719 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL427058 | GSK-466317A | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL374453 | GSK-299115A | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL218720 | GSK-466314A | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL441702 | GSK-270822A | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL384073 | GSK-180736A | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL375312 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL218654 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL217910 | — | IC50 | = | 2500.0 | nM | 5.60 |