Assay Detail
Binding
CHEMBL4669837
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Inhibition of ROCK1 (unknown origin)
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 5.74 | 6.85 |
| IC50 | 2 | 6.67 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 7.30 |
| CHEMBL1605605 | — | — | 1 | 6.85 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.03 |
| CHEMBL2005186 | BELUMOSUDIL | 4.0 | 1 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3426621 | RIPASUDIL | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1605605 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL38380 | FASUDIL | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2005186 | BELUMOSUDIL | Ki | = | 24000.0 | nM | 4.62 |