Assay Detail
Binding
CHEMBL5732962
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.
42
Total Activities
6
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 | 14 | - | - |
| k_off | 14 | - | - |
| IC50 | 7 | 5.31 | 6.48 |
| Ki | 7 | 6.74 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5768727 | — | — | 6 | 8.00 |
| CHEMBL5850670 | — | — | 6 | 7.40 |
| CHEMBL5858473 | — | — | 12 | 7.16 |
| CHEMBL6016872 | — | — | 6 | 6.58 |
| CHEMBL2005186 | BELUMOSUDIL | 4.0 | 6 | 6.30 |
| CHEMBL5850835 | — | — | 6 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5768727 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL5850670 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL5858473 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL6016872 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL5768727 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2005186 | BELUMOSUDIL | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5858473 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL5850670 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL5858473 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL5850835 | — | Ki | = | 2010.0 | nM | 5.70 |
| CHEMBL6016872 | — | IC50 | = | 6690.0 | nM | 5.17 |
| CHEMBL2005186 | BELUMOSUDIL | IC50 | = | 13110.0 | nM | 4.88 |
| CHEMBL5858473 | — | IC50 | = | 22530.0 | nM | 4.65 |
| CHEMBL5850835 | — | IC50 | = | 53450.0 | nM | 4.27 |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5850835 | — | kon | = | - | — | - |
| CHEMBL5850835 | — | k_off | = | - | s-1 | - |
| CHEMBL5850835 | — | kon | = | - | — | - |
| CHEMBL5850835 | — | k_off | = | - | s-1 | - |
| CHEMBL5850670 | — | kon | = | - | — | - |
| CHEMBL6016872 | — | k_off | = | - | s-1 | - |
| 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 | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL6016872 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5850670 | — | k_off | = | - | s-1 | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | k_off | = | - | s-1 | - |
| CHEMBL5850670 | — | kon | = | - | — | - |
| CHEMBL5850670 | — | k_off | = | - | s-1 | - |
| CHEMBL5768727 | — | kon | = | - | — | - |
| CHEMBL5858473 | — | kon | = | - | — | - |
| CHEMBL5768727 | — | k_off | = | - | s-1 | - |
| CHEMBL5768727 | — | kon | = | - | — | - |
| CHEMBL5768727 | — | k_off | = | - | s-1 | - |