Assay Detail
Binding
CHEMBL3705212
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Luciferin-Luciferase Assay: The activity of ROCKII (1-543) kinase is measured utilizing Cambrex PKLight ATP Detection Reagent, a homogeneous assay technology using luciferin-luciferase to quantify residual ATP. The assay is performed in 384-well low-volume, white, non-binding surface microtiter plates (Corning). The assay buffer is 25 mM HEPES, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4 and 0.5 mM DTT. Test compounds, dissolved in neat DMSO at 500 μg/mL, are serially diluted for dose response for a final starting concentration of 3 μg/mL in 1% DMSO of assay buffer. ROCKII (1-543) (62,408 Da) is diluted in assay buffer to a final concentration of 7.5 nM in a total volume of 15 μL.
80
Total Activities
79
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
Rho kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 80 | 8.20 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3680709 | — | — | 1 | 9.14 |
| CHEMBL3680716 | — | — | 1 | 8.96 |
| CHEMBL3680713 | — | — | 1 | 8.96 |
| CHEMBL3680707 | — | — | 1 | 8.96 |
| CHEMBL3680719 | — | — | 1 | 8.92 |
| CHEMBL3680737 | — | — | 1 | 8.92 |
| CHEMBL3680767 | — | — | 1 | 8.89 |
| CHEMBL3680727 | — | — | 1 | 8.89 |
| CHEMBL3680736 | — | — | 1 | 8.89 |
| CHEMBL3680759 | — | — | 1 | 8.89 |
| CHEMBL3680746 | — | — | 1 | 8.85 |
| CHEMBL3680714 | — | — | 1 | 8.85 |
| CHEMBL3680739 | — | — | 1 | 8.82 |
| CHEMBL3680731 | — | — | 1 | 8.82 |
| CHEMBL3680749 | — | — | 1 | 8.77 |
| CHEMBL3680762 | — | — | 1 | 8.77 |
| CHEMBL3680741 | — | — | 1 | 8.77 |
| CHEMBL3680721 | — | — | 1 | 8.74 |
| CHEMBL3680711 | — | — | 1 | 8.74 |
| CHEMBL3680720 | — | — | 1 | 8.74 |
| CHEMBL3680781 | — | — | 1 | 8.72 |
| CHEMBL3680718 | — | — | 1 | 8.72 |
| CHEMBL3680696 | — | — | 1 | 8.70 |
| CHEMBL3680729 | — | — | 1 | 8.68 |
| CHEMBL3680725 | — | — | 1 | 8.66 |
| CHEMBL3680732 | — | — | 1 | 8.60 |
| CHEMBL3680723 | — | — | 1 | 8.59 |
| CHEMBL3680708 | — | — | 1 | 8.59 |
| CHEMBL3680776 | — | — | 1 | 8.59 |
| CHEMBL3680724 | — | — | 1 | 8.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3680709 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL3680716 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3680707 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3680713 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3680719 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3680737 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3680767 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3680727 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3680736 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3680759 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3680746 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3680714 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3680739 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3680731 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3680741 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3680762 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3680749 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3680721 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3680711 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3680720 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3680781 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3680718 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3680696 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3680729 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3680725 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3680732 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3680723 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3680708 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3680776 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3680724 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3680801 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3680743 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3680763 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3680747 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3680695 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3680744 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3680710 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3680799 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3680699 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3680717 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3680794 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3680703 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3680702 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3680764 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL3680697 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3680798 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3680783 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3680802 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3680705 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3680745 | — | IC50 | = | 8.1 | nM | 8.09 |