Assay Detail
Binding
CHEMBL3429819
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal GST-tagged ROCK2 expressed in baculovirus-infected insect cells using long S6 kinase peptide as substrate by radiometric assay in presence of [32P]ATP
40
Total Activities
40
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
Design, synthesis, and biological evaluation of novel, highly active soft ROCK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 8.54 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3426732 | — | — | 1 | 9.00 |
| CHEMBL3426622 | — | — | 1 | 8.96 |
| CHEMBL3426623 | — | — | 1 | 8.96 |
| CHEMBL3426641 | — | — | 1 | 8.92 |
| CHEMBL3426726 | — | — | 1 | 8.89 |
| CHEMBL3426642 | — | — | 1 | 8.85 |
| CHEMBL3426627 | — | — | 1 | 8.82 |
| CHEMBL3426633 | — | — | 1 | 8.80 |
| CHEMBL3426638 | — | — | 1 | 8.74 |
| CHEMBL3426629 | — | — | 1 | 8.74 |
| CHEMBL3426643 | — | — | 1 | 8.70 |
| CHEMBL3426634 | — | — | 1 | 8.68 |
| CHEMBL2440737 | — | — | 1 | 8.60 |
| CHEMBL3426632 | — | — | 1 | 8.59 |
| CHEMBL3426628 | — | — | 1 | 8.48 |
| CHEMBL3426636 | — | — | 1 | 8.48 |
| CHEMBL3426646 | — | — | 1 | 8.46 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 8.42 |
| CHEMBL3426635 | — | — | 1 | 8.26 |
| CHEMBL3426626 | — | — | 1 | 8.18 |
| CHEMBL3426630 | — | — | 1 | 8.15 |
| CHEMBL3426631 | — | — | 1 | 7.57 |
| CHEMBL559147 | Y-27632 | — | 1 | 7.27 |
| CHEMBL3426625 | — | — | 1 | - |
| CHEMBL3426624 | — | — | 1 | - |
| CHEMBL3426620 | — | — | 1 | - |
| CHEMBL3426637 | — | — | 1 | - |
| CHEMBL3426639 | — | — | 1 | - |
| CHEMBL3426640 | — | — | 1 | - |
| CHEMBL3426644 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3426732 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3426622 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3426623 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3426641 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3426726 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3426642 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3426627 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3426633 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3426638 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3426629 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3426643 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3426634 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL2440737 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3426632 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3426636 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3426628 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3426646 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3426621 | RIPASUDIL | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3426635 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3426626 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3426630 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3426631 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL559147 | Y-27632 | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3426731 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426730 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426729 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426728 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426727 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426725 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426724 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426723 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426647 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426645 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426644 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426640 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426639 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426637 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426620 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426624 | — | IC50 | < | 1.0 | nM | - |
| CHEMBL3426625 | — | IC50 | < | 1.0 | nM | - |