Assay Detail
Binding
CHEMBL3386997
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Inhibition of human recombinant ROCK-2 using KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK as substrate after 40 mins by scintillation counting analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.56 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL406821 | — | — | 1 | 8.30 |
| CHEMBL1956071 | — | — | 1 | 8.15 |
| CHEMBL3338837 | — | — | 1 | 7.96 |
| CHEMBL2147538 | — | — | 1 | 7.89 |
| CHEMBL3338839 | — | — | 1 | 7.85 |
| CHEMBL3338840 | — | — | 1 | 7.85 |
| CHEMBL3338842 | — | — | 1 | 7.70 |
| CHEMBL3338838 | — | — | 1 | 7.64 |
| CHEMBL1214929 | — | — | 1 | 7.58 |
| CHEMBL559147 | Y-27632 | — | 1 | 7.05 |
| CHEMBL3338843 | — | — | 1 | 7.00 |
| CHEMBL3338841 | — | — | 1 | 6.92 |
| CHEMBL3338844 | — | — | 1 | 6.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL406821 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1956071 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3338837 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2147538 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3338839 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3338840 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3338842 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3338838 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1214929 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL559147 | Y-27632 | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3338843 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3338841 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3338844 | — | IC50 | = | 432.0 | nM | 6.37 |