Assay Detail
Binding
CHEMBL1646347
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MLCK by HTRF assay
10
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Myosin light chain kinase, smooth muscle (CHEMBL2428) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.15 | 6.77 |
| Ki | 5 | 6.02 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281948 | K-252A | — | 1 | 7.70 |
| CHEMBL428496 | WORTMANNIN | — | 1 | 6.77 |
| CHEMBL249089 | — | — | 1 | 6.52 |
| CHEMBL429298 | — | — | 1 | 5.42 |
| CHEMBL1641992 | — | — | 1 | 5.06 |
| CHEMBL38380 | FASUDIL | 3.0 | 2 | 4.67 |
| CHEMBL1641990 | — | — | 1 | 4.63 |
| CHEMBL1641989 | — | — | 1 | 4.60 |
| CHEMBL41631 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281948 | K-252A | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL428496 | WORTMANNIN | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL249089 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL429298 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL1641992 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL38380 | FASUDIL | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL1641990 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL1641989 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL38380 | FASUDIL | Ki | = | 36000.0 | nM | 4.44 |
| CHEMBL41631 | — | Ki | = | 110000.0 | nM | - |