Assay Detail
Binding
CHEMBL5732963
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Inhibition Assay: Kinase inhibition can be determined using an IMAP® assay (Molecular Devices). This assay method involves the use of a fluorescently-tagged peptide substrate. Phosphorylation of the tagged peptide by a kinase of interest promotes binding of the peptide to a trivalent metal-based nanoparticle via the specific, high affinity interaction between the phospho-group and the trivalent metal. Proximity to the nanoparticle results in increased fluorescence polarization Inhibition of the kinase by a kinase inhibitor prevents phosphorylation of the substrate and thereby limits binding of the fluorescently-tagged substrate to the nanoparticle. Such an assay can be compatible with a microwell assay format, allowing simultaneous determination of IC50 of multiple compounds.
48
Total Activities
7
Compounds Tested
4
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 |
|---|---|---|---|
| kon | 16 | - | - |
| k_off | 16 | - | - |
| IC50 | 8 | 5.87 | 6.33 |
| Ki | 8 | 7.27 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5858473 | — | — | 12 | 7.70 |
| CHEMBL5768727 | — | — | 6 | 7.70 |
| CHEMBL5850835 | — | — | 6 | 7.52 |
| CHEMBL2005186 | BELUMOSUDIL | 4.0 | 6 | 7.40 |
| CHEMBL5850670 | — | — | 6 | 7.22 |
| CHEMBL6016872 | — | — | 6 | 7.10 |
| CHEMBL5986438 | — | — | 6 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5768727 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5858473 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5850835 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2005186 | BELUMOSUDIL | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5850670 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL6016872 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL5986438 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5858473 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL5768727 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5858473 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5850835 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL2005186 | BELUMOSUDIL | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5850670 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL6016872 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL5986438 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL5858473 | — | IC50 | = | 4640.0 | nM | 5.33 |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5850835 | — | kon | = | - | — | - |
| CHEMBL5850835 | — | k_off | = | - | s-1 | - |
| CHEMBL5850835 | — | kon | = | - | — | - |
| CHEMBL5850835 | — | k_off | = | - | s-1 | - |
| CHEMBL6016872 | — | kon | = | - | — | - |
| CHEMBL5850670 | — | kon | = | - | — | - |
| CHEMBL6016872 | — | kon | = | - | — | - |
| CHEMBL6016872 | — | k_off | = | - | s-1 | - |
| CHEMBL2005186 | BELUMOSUDIL | kon | = | - | — | - |
| CHEMBL2005186 | BELUMOSUDIL | k_off | = | - | s-1 | - |
| CHEMBL2005186 | BELUMOSUDIL | kon | = | - | — | - |
| CHEMBL2005186 | BELUMOSUDIL | k_off | = | - | s-1 | - |
| CHEMBL5850670 | — | kon | = | - | — | - |
| CHEMBL5850670 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL6016872 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5768727 | — | k_off | = | - | s-1 | - |
| CHEMBL5768727 | — | kon | = | - | — | - |
| CHEMBL5768727 | — | k_off | = | - | s-1 | - |
| CHEMBL5768727 | — | kon | = | - | — | - |
| CHEMBL5986438 | — | k_off | = | - | s-1 | - |
| CHEMBL5986438 | — | kon | = | - | — | - |
| CHEMBL5850670 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5986438 | — | k_off | = | - | s-1 | - |
| CHEMBL5986438 | — | kon | = | - | — | - |