Assay Detail
Binding
CHEMBL5251366
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity protein kinase CLK2 (CHEMBL4225) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 56 | 6.56 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5091238 | — | — | 1 | 9.22 |
| CHEMBL393525 | — | — | 1 | 8.96 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 8.55 |
| CHEMBL4784318 | CIRTUVIVINT | 1.0 | 1 | 8.44 |
| CHEMBL4647659 | — | — | 1 | 8.23 |
| CHEMBL4297639 | LORECIVIVINT | 3.0 | 1 | 7.87 |
| CHEMBL4873449 | — | — | 1 | 7.84 |
| CHEMBL5070553 | — | — | 1 | 7.61 |
| CHEMBL5279705 | — | — | 1 | 7.48 |
| CHEMBL4441878 | — | — | 1 | 7.44 |
| CHEMBL5273528 | — | — | 1 | 7.39 |
| CHEMBL1236620 | — | — | 1 | 7.30 |
| CHEMBL5284529 | — | — | 1 | 7.09 |
| CHEMBL1997924 | — | — | 1 | 7.08 |
| CHEMBL5283849 | — | — | 1 | 7.05 |
| CHEMBL5285332 | — | — | 1 | 7.05 |
| CHEMBL5081787 | — | — | 1 | 7.02 |
| CHEMBL4754195 | — | — | 1 | 6.94 |
| CHEMBL5288391 | — | — | 1 | 6.83 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.73 |
| CHEMBL3298236 | — | — | 1 | 6.67 |
| CHEMBL4637319 | — | — | 1 | 6.57 |
| CHEMBL1232500 | — | — | 1 | 6.50 |
| CHEMBL5289681 | — | — | 1 | 6.42 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 6.39 |
| CHEMBL4283240 | — | — | 1 | 6.20 |
| CHEMBL4798421 | — | — | 1 | 6.11 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 5.94 |
| CHEMBL4848254 | — | — | 1 | 5.88 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | 3.0 | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5091238 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL393525 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4784318 | CIRTUVIVINT | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4647659 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4297639 | LORECIVIVINT | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL4873449 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL5070553 | — | IC50 | = | 24.7 | nM | 7.61 |
| CHEMBL5279705 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL4441878 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL5273528 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL1236620 | — | IC50 | = | 49.6 | nM | 7.30 |
| CHEMBL5284529 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL1997924 | — | IC50 | = | 82.8 | nM | 7.08 |
| CHEMBL5285332 | — | IC50 | = | 89.6 | nM | 7.05 |
| CHEMBL5283849 | — | IC50 | = | 89.7 | nM | 7.05 |
| CHEMBL5081787 | — | IC50 | = | 95.3 | nM | 7.02 |
| CHEMBL4754195 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL5288391 | — | IC50 | = | 146.6 | nM | 6.83 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 185.3 | nM | 6.73 |
| CHEMBL3298236 | — | IC50 | = | 211.4 | nM | 6.67 |
| CHEMBL4637319 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL1232500 | — | IC50 | = | 315.3 | nM | 6.50 |
| CHEMBL5289681 | — | IC50 | = | 380.5 | nM | 6.42 |
| CHEMBL1614713 | CC-401 | IC50 | = | 405.2 | nM | 6.39 |
| CHEMBL4283240 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4798421 | — | IC50 | = | 771.7 | nM | 6.11 |
| CHEMBL269538 | HARMINE | IC50 | = | 1152.0 | nM | 5.94 |
| CHEMBL4848254 | — | IC50 | = | 1328.0 | nM | 5.88 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | = | 1317.0 | nM | 5.88 |
| CHEMBL4783398 | — | IC50 | = | 1542.0 | nM | 5.81 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | IC50 | = | 1697.0 | nM | 5.77 |
| CHEMBL1802358 | — | IC50 | = | 1893.0 | nM | 5.72 |
| CHEMBL4292553 | — | IC50 | = | 1993.0 | nM | 5.70 |
| CHEMBL5086263 | — | IC50 | = | 2499.0 | nM | 5.60 |
| CHEMBL5095897 | — | IC50 | = | 2674.0 | nM | 5.57 |
| CHEMBL608533 | MIDOSTAURIN | IC50 | = | 2979.0 | nM | 5.53 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 3094.0 | nM | 5.51 |
| CHEMBL3421968 | — | IC50 | = | 3503.0 | nM | 5.46 |
| CHEMBL5286716 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL5288595 | — | IC50 | = | 4409.0 | nM | 5.36 |
| CHEMBL3589662 | — | IC50 | = | 5140.0 | nM | 5.29 |
| CHEMBL5272336 | — | IC50 | = | 5962.0 | nM | 5.22 |
| CHEMBL5093741 | — | IC50 | = | 6713.0 | nM | 5.17 |
| CHEMBL4288096 | — | IC50 | = | 8406.0 | nM | 5.08 |
| CHEMBL790 | CHLORHEXIDINE | IC50 | = | 9165.0 | nM | 5.04 |
| CHEMBL418971 | BISPHENOL A | IC50 | > | 10000.0 | nM | - |
| CHEMBL1682931 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3894571 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1094636 | NIRAPARIB | IC50 | > | 10000.0 | nM | - |