Assay Detail
Binding
CHEMBL1960787
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay
6
Total Activities
6
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
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.60 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220241 | GSK-269962A | — | 1 | 8.80 |
| CHEMBL1956071 | — | — | 1 | 8.25 |
| CHEMBL559147 | Y-27632 | — | 1 | 6.82 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.52 |
| CHEMBL189657 | — | — | 1 | - |
| CHEMBL1956072 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220241 | GSK-269962A | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1956071 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL559147 | Y-27632 | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL38380 | FASUDIL | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL189657 | — | IC50 | < | 10.0 | nM | - |
| CHEMBL1956072 | — | IC50 | < | 10.0 | nM | - |