Assay Detail
Binding
CHEMBL5251383
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human DYRK1A 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 tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗| 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 | 8.64 | 10.17 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4647659 | — | — | 1 | 10.17 |
| CHEMBL5070553 | — | — | 1 | 10.07 |
| CHEMBL393525 | — | — | 1 | 10.05 |
| CHEMBL5285332 | — | — | 1 | 10.00 |
| CHEMBL4784318 | CIRTUVIVINT | 1.0 | 1 | 9.79 |
| CHEMBL4441878 | — | — | 1 | 9.73 |
| CHEMBL4848254 | — | — | 1 | 9.62 |
| CHEMBL5081787 | — | — | 1 | 9.60 |
| CHEMBL5289681 | — | — | 1 | 9.55 |
| CHEMBL5091238 | — | — | 1 | 9.54 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 9.11 |
| CHEMBL5093741 | — | — | 1 | 9.04 |
| CHEMBL5086263 | — | — | 1 | 8.93 |
| CHEMBL5279705 | — | — | 1 | 8.86 |
| CHEMBL3589662 | — | — | 1 | 8.62 |
| CHEMBL4873449 | — | — | 1 | 8.60 |
| CHEMBL3421968 | — | — | 1 | 8.59 |
| CHEMBL5283849 | — | — | 1 | 8.59 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 8.48 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.47 |
| CHEMBL3894571 | — | — | 1 | 8.29 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 8.26 |
| CHEMBL5273528 | — | — | 1 | 8.23 |
| CHEMBL4283240 | — | — | 1 | 8.22 |
| CHEMBL1802358 | — | — | 1 | 8.14 |
| CHEMBL3298236 | — | — | 1 | 7.91 |
| CHEMBL1232500 | — | — | 1 | 7.88 |
| CHEMBL4297639 | LORECIVIVINT | 3.0 | 1 | 7.70 |
| CHEMBL5095897 | — | — | 1 | 7.41 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4647659 | — | Kd | = | 0.067 | nM | 10.17 |
| CHEMBL5070553 | — | Kd | = | 0.086 | nM | 10.07 |
| CHEMBL393525 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL5285332 | — | Kd | = | 0.101 | nM | 10.00 |
| CHEMBL4784318 | CIRTUVIVINT | Kd | = | 0.163 | nM | 9.79 |
| CHEMBL4441878 | — | Kd | = | 0.188 | nM | 9.73 |
| CHEMBL4848254 | — | Kd | = | 0.24 | nM | 9.62 |
| CHEMBL5081787 | — | Kd | = | 0.252 | nM | 9.60 |
| CHEMBL5289681 | — | Kd | = | 0.283 | nM | 9.55 |
| CHEMBL5091238 | — | Kd | = | 0.292 | nM | 9.54 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 0.775 | nM | 9.11 |
| CHEMBL5093741 | — | Kd | = | 0.912 | nM | 9.04 |
| CHEMBL5086263 | — | Kd | = | 1.163 | nM | 8.93 |
| CHEMBL5279705 | — | Kd | = | 1.38 | nM | 8.86 |
| CHEMBL3589662 | — | Kd | = | 2.385 | nM | 8.62 |
| CHEMBL4873449 | — | Kd | = | 2.541 | nM | 8.60 |
| CHEMBL3421968 | — | Kd | = | 2.573 | nM | 8.59 |
| CHEMBL5283849 | — | Kd | = | 2.602 | nM | 8.59 |
| CHEMBL1614713 | CC-401 | Kd | = | 3.312 | nM | 8.48 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 3.349 | nM | 8.47 |
| CHEMBL3894571 | — | Kd | = | 5.151 | nM | 8.29 |
| CHEMBL269538 | HARMINE | Kd | = | 5.474 | nM | 8.26 |
| CHEMBL5273528 | — | Kd | = | 5.836 | nM | 8.23 |
| CHEMBL4283240 | — | Kd | = | 5.969 | nM | 8.22 |
| CHEMBL1802358 | — | Kd | = | 7.236 | nM | 8.14 |
| CHEMBL3298236 | — | Kd | = | 12.19 | nM | 7.91 |
| CHEMBL1232500 | — | Kd | = | 13.22 | nM | 7.88 |
| CHEMBL4297639 | LORECIVIVINT | Kd | = | 19.95 | nM | 7.70 |
| CHEMBL5095897 | — | Kd | = | 38.77 | nM | 7.41 |
| CHEMBL184574 | DEMETHYLBELLIDIFOLIN | Kd | = | 60.02 | nM | 7.22 |
| CHEMBL4292553 | — | Kd | = | 100.21 | nM | 7.00 |
| CHEMBL1236620 | — | Kd | = | 108.63 | nM | 6.96 |
| CHEMBL485053 | LEUCETTAMINE B | Kd | = | 273.32 | nM | 6.56 |
| CHEMBL1997924 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL140 | CURCUMIN | Kd | > | 1000.0 | nM | - |
| CHEMBL4783398 | — | Kd | > | 1000.0 | nM | - |
| CHEMBL5284529 | — | Kd | > | 1000.0 | nM | - |