Assay Detail
Binding
CHEMBL4003765
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Inhibition of CLK mediated SF3B1 activation in human SK-MEL-2 cells assessed as MDM2-pre mRNA exon skipping after 4 hrs by luciferase reporter gene assay relative to control
24
Total Activities
22
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 |
Target
Dual specificity protein kinase CLK1 (CHEMBL4224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 5.05 | 6.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3108948 | — | — | 1 | 6.10 |
| CHEMBL4078898 | — | — | 2 | 5.52 |
| CHEMBL367625 | — | — | 1 | 5.38 |
| CHEMBL4066861 | — | — | 1 | 5.37 |
| CHEMBL4104505 | — | — | 1 | 5.35 |
| CHEMBL4094492 | — | — | 2 | 5.14 |
| CHEMBL1532768 | — | — | 1 | 5.11 |
| CHEMBL4102202 | — | — | 1 | 5.10 |
| CHEMBL4100324 | — | — | 1 | 5.01 |
| CHEMBL4088144 | — | — | 1 | 4.93 |
| CHEMBL286721 | AMINOPURVALANOL | — | 1 | 4.92 |
| CHEMBL4102101 | — | — | 1 | 4.92 |
| CHEMBL4073318 | — | — | 1 | 4.91 |
| CHEMBL4064123 | — | — | 1 | 4.89 |
| CHEMBL4091876 | — | — | 1 | 4.85 |
| CHEMBL4067013 | — | — | 1 | 4.76 |
| CHEMBL4104657 | — | — | 1 | 4.73 |
| CHEMBL4080283 | — | — | 1 | 4.66 |
| CHEMBL4082309 | — | — | 1 | 4.63 |
| CHEMBL4084116 | — | — | 1 | 4.58 |
| CHEMBL4089225 | — | — | 1 | - |
| CHEMBL4068034 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3108948 | — | EC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4078898 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL367625 | — | EC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4066861 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4104505 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4078898 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4094492 | — | EC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL1532768 | — | EC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4102202 | — | EC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4094492 | — | EC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4100324 | — | EC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4088144 | — | EC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4102101 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL286721 | AMINOPURVALANOL | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4073318 | — | EC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4064123 | — | EC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL4091876 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4067013 | — | EC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL4104657 | — | EC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL4080283 | — | EC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4082309 | — | EC50 | = | 23500.0 | nM | 4.63 |
| CHEMBL4084116 | — | EC50 | = | 26400.0 | nM | 4.58 |
| CHEMBL4068034 | — | EC50 | - | — | - | |
| CHEMBL4089225 | — | EC50 | - | — | - |