Assay Detail
Binding
CHEMBL3875859
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Inhibition of GST-tagged human recombinant CLK2 expressed in Escherichia coli using RS peptide as substrate incubated for 30 mins in presence of [gamma-33 P] ATP by liquid scintillation counting analysis
19
Total Activities
19
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 CLK2 (CHEMBL4225) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.06 | 7.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3885431 | — | — | 1 | 7.36 |
| CHEMBL3883660 | — | — | 1 | 7.10 |
| CHEMBL3883639 | — | — | 1 | 6.96 |
| CHEMBL3884821 | — | — | 1 | 6.82 |
| CHEMBL3884015 | — | — | 1 | 6.40 |
| CHEMBL3883414 | — | — | 1 | 6.21 |
| CHEMBL3885036 | — | — | 1 | 6.21 |
| CHEMBL3883820 | — | — | 1 | 5.96 |
| CHEMBL3885335 | — | — | 1 | 5.96 |
| CHEMBL3885328 | — | — | 1 | 5.80 |
| CHEMBL3884570 | — | — | 1 | 5.64 |
| CHEMBL3885360 | — | — | 1 | 5.55 |
| CHEMBL3883448 | — | — | 1 | 5.46 |
| CHEMBL3884627 | — | — | 1 | 5.46 |
| CHEMBL3884250 | — | — | 1 | 5.40 |
| CHEMBL3885316 | — | — | 1 | 5.34 |
| CHEMBL3753668 | — | — | 1 | 5.34 |
| CHEMBL3884845 | — | — | 1 | - |
| CHEMBL3884932 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3885431 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3883660 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3883639 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3884821 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3884015 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3883414 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3885036 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3883820 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3885335 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3885328 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL3884570 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3885360 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3883448 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3884627 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3884250 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL3885316 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3753668 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3884845 | — | IC50 | - | — | - | |
| CHEMBL3884932 | — | IC50 | - | — | - |