Assay Detail
Binding
CHEMBL5251384
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Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay
37
Total Activities
37
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
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 37 | 8.50 | 10.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784318 | CIRTUVIVINT | 1.0 | 1 | 10.74 |
| CHEMBL393525 | — | — | 1 | 10.25 |
| CHEMBL4441878 | — | — | 1 | 9.64 |
| CHEMBL4647659 | — | — | 1 | 9.60 |
| CHEMBL5070553 | — | — | 1 | 9.49 |
| CHEMBL5081787 | — | — | 1 | 9.40 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 9.27 |
| CHEMBL5279705 | — | — | 1 | 9.24 |
| CHEMBL5285332 | — | — | 1 | 9.21 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 9.07 |
| CHEMBL5289681 | — | — | 1 | 9.01 |
| CHEMBL1232500 | — | — | 1 | 8.89 |
| CHEMBL4873449 | — | — | 1 | 8.88 |
| CHEMBL5273528 | — | — | 1 | 8.86 |
| CHEMBL3298236 | — | — | 1 | 8.79 |
| CHEMBL5283849 | — | — | 1 | 8.76 |
| CHEMBL5091238 | — | — | 1 | 8.58 |
| CHEMBL1236620 | — | — | 1 | 8.55 |
| CHEMBL4848254 | — | — | 1 | 8.27 |
| CHEMBL4297639 | LORECIVIVINT | 3.0 | 1 | 8.23 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 8.22 |
| CHEMBL3589662 | — | — | 1 | 8.21 |
| CHEMBL3421968 | — | — | 1 | 8.13 |
| CHEMBL3894571 | — | — | 1 | 8.12 |
| CHEMBL1802358 | — | — | 1 | 8.07 |
| CHEMBL4283240 | — | — | 1 | 8.06 |
| CHEMBL1997924 | — | — | 1 | 7.99 |
| CHEMBL5095897 | — | — | 1 | 7.98 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.92 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | — | 1 | 7.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784318 | CIRTUVIVINT | Kd | = | 0.018 | nM | 10.74 |
| CHEMBL393525 | — | Kd | = | 0.056 | nM | 10.25 |
| CHEMBL4441878 | — | Kd | = | 0.228 | nM | 9.64 |
| CHEMBL4647659 | — | Kd | = | 0.254 | nM | 9.60 |
| CHEMBL5070553 | — | Kd | = | 0.326 | nM | 9.49 |
| CHEMBL5081787 | — | Kd | = | 0.395 | nM | 9.40 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 0.54 | nM | 9.27 |
| CHEMBL5279705 | — | Kd | = | 0.58 | nM | 9.24 |
| CHEMBL5285332 | — | Kd | = | 0.62 | nM | 9.21 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 0.851 | nM | 9.07 |
| CHEMBL5289681 | — | Kd | = | 0.968 | nM | 9.01 |
| CHEMBL1232500 | — | Kd | = | 1.273 | nM | 8.89 |
| CHEMBL4873449 | — | Kd | = | 1.306 | nM | 8.88 |
| CHEMBL5273528 | — | Kd | = | 1.387 | nM | 8.86 |
| CHEMBL3298236 | — | Kd | = | 1.626 | nM | 8.79 |
| CHEMBL5283849 | — | Kd | = | 1.754 | nM | 8.76 |
| CHEMBL5091238 | — | Kd | = | 2.607 | nM | 8.58 |
| CHEMBL1236620 | — | Kd | = | 2.789 | nM | 8.55 |
| CHEMBL4848254 | — | Kd | = | 5.381 | nM | 8.27 |
| CHEMBL4297639 | LORECIVIVINT | Kd | = | 5.889 | nM | 8.23 |
| CHEMBL1614713 | CC-401 | Kd | = | 5.966 | nM | 8.22 |
| CHEMBL3589662 | — | Kd | = | 6.22 | nM | 8.21 |
| CHEMBL3421968 | — | Kd | = | 7.353 | nM | 8.13 |
| CHEMBL3894571 | — | Kd | = | 7.635 | nM | 8.12 |
| CHEMBL1802358 | — | Kd | = | 8.51 | nM | 8.07 |
| CHEMBL4283240 | — | Kd | = | 8.703 | nM | 8.06 |
| CHEMBL1997924 | — | Kd | = | 10.19 | nM | 7.99 |
| CHEMBL5095897 | — | Kd | = | 10.4 | nM | 7.98 |
| CHEMBL269538 | HARMINE | Kd | = | 12.11 | nM | 7.92 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | Kd | = | 29.74 | nM | 7.53 |
| CHEMBL5093741 | — | Kd | = | 34.81 | nM | 7.46 |
| CHEMBL485053 | LEUCETTAMINE B | Kd | = | 36.89 | nM | 7.43 |
| CHEMBL5086263 | — | Kd | = | 41.81 | nM | 7.38 |
| CHEMBL4292553 | — | Kd | = | 70.8 | nM | 7.15 |
| CHEMBL4783398 | — | Kd | = | 112.24 | nM | 6.95 |
| CHEMBL5284529 | — | Kd | = | 200.5 | nM | 6.70 |
| CHEMBL140 | CURCUMIN | Kd | > | 1000.0 | nM | - |