Assay Detail
Binding
CHEMBL987092
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Inhibition of human recombinant ROCK1 kinase expressed in insect Sf9 cells by SPA
25
Total Activities
25
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
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.49 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483402 | — | — | 1 | 8.70 |
| CHEMBL483574 | — | — | 1 | 8.52 |
| CHEMBL483401 | — | — | 1 | 8.40 |
| CHEMBL520828 | — | — | 1 | 8.30 |
| CHEMBL485612 | — | — | 1 | 8.22 |
| CHEMBL521347 | — | — | 1 | 8.22 |
| CHEMBL483395 | — | — | 1 | 8.10 |
| CHEMBL485440 | — | — | 1 | 8.00 |
| CHEMBL521144 | — | — | 1 | 7.96 |
| CHEMBL384073 | GSK-180736A | — | 1 | 7.85 |
| CHEMBL485611 | — | — | 1 | 7.82 |
| CHEMBL520808 | — | — | 1 | 7.58 |
| CHEMBL519008 | — | — | 1 | 7.34 |
| CHEMBL483575 | — | — | 1 | 7.17 |
| CHEMBL485598 | GSK-317354A | — | 1 | 7.12 |
| CHEMBL485585 | — | — | 1 | 7.00 |
| CHEMBL483396 | — | — | 1 | 6.98 |
| CHEMBL485586 | — | — | 1 | 6.98 |
| CHEMBL519680 | — | — | 1 | 6.98 |
| CHEMBL483387 | — | — | 1 | 6.89 |
| CHEMBL520848 | — | — | 1 | 6.89 |
| CHEMBL483394 | — | — | 1 | 6.82 |
| CHEMBL485592 | — | — | 1 | 6.75 |
| CHEMBL483568 | — | — | 1 | 6.54 |
| CHEMBL520640 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483402 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL483574 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL483401 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL520828 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL485612 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL521347 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL483395 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL485440 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL521144 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL384073 | GSK-180736A | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL485611 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL520808 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL519008 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL483575 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL485598 | GSK-317354A | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL485585 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL483396 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL485586 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL519680 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL483387 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL520848 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL483394 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL485592 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL483568 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL520640 | — | IC50 | = | 863.0 | nM | 6.06 |