Assay Detail
Binding
CHEMBL5251380
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay
35
Total Activities
35
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 tyrosine-phosphorylation-regulated kinase 1B (CHEMBL5543) ↗| 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 | 35 | 7.40 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5070553 | — | — | 1 | 8.96 |
| CHEMBL4441878 | — | — | 1 | 8.96 |
| CHEMBL393525 | — | — | 1 | 8.47 |
| CHEMBL4784318 | CIRTUVIVINT | 1.0 | 1 | 8.44 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 8.34 |
| CHEMBL5285332 | — | — | 1 | 8.32 |
| CHEMBL5081787 | — | — | 1 | 8.27 |
| CHEMBL3589662 | — | — | 1 | 8.11 |
| CHEMBL3421968 | — | — | 1 | 8.08 |
| CHEMBL5289681 | — | — | 1 | 8.01 |
| CHEMBL4647659 | — | — | 1 | 7.92 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.89 |
| CHEMBL5283849 | — | — | 1 | 7.86 |
| CHEMBL4873449 | — | — | 1 | 7.62 |
| CHEMBL3894571 | — | — | 1 | 7.60 |
| CHEMBL5279705 | — | — | 1 | 7.59 |
| CHEMBL5091238 | — | — | 1 | 7.46 |
| CHEMBL4283240 | — | — | 1 | 7.42 |
| CHEMBL3298236 | — | — | 1 | 7.27 |
| CHEMBL1802358 | — | — | 1 | 7.26 |
| CHEMBL4292553 | — | — | 1 | 7.19 |
| CHEMBL1236620 | — | — | 1 | 7.09 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.03 |
| CHEMBL4297639 | LORECIVIVINT | 3.0 | 1 | 7.01 |
| CHEMBL5273528 | — | — | 1 | 6.98 |
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 6.83 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 6.66 |
| CHEMBL5086263 | — | — | 1 | 6.44 |
| CHEMBL5288391 | — | — | 1 | 6.44 |
| CHEMBL5288595 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5070553 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4441878 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL393525 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4784318 | CIRTUVIVINT | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1230165 | SILMITASERTIB | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5285332 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL5081787 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL3589662 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL3421968 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5289681 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4647659 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL5283849 | — | IC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4873449 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL3894571 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL5279705 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL5091238 | — | IC50 | = | 34.5 | nM | 7.46 |
| CHEMBL4283240 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL3298236 | — | IC50 | = | 53.5 | nM | 7.27 |
| CHEMBL1802358 | — | IC50 | = | 54.4 | nM | 7.26 |
| CHEMBL4292553 | — | IC50 | = | 64.4 | nM | 7.19 |
| CHEMBL1236620 | — | IC50 | = | 81.2 | nM | 7.09 |
| CHEMBL269538 | HARMINE | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4297639 | LORECIVIVINT | IC50 | = | 97.2 | nM | 7.01 |
| CHEMBL5273528 | — | IC50 | = | 103.7 | nM | 6.98 |
| CHEMBL140 | CURCUMIN | IC50 | = | 147.7 | nM | 6.83 |
| CHEMBL1614713 | CC-401 | IC50 | = | 218.2 | nM | 6.66 |
| CHEMBL5086263 | — | IC50 | = | 366.5 | nM | 6.44 |
| CHEMBL5288391 | — | IC50 | = | 363.9 | nM | 6.44 |
| CHEMBL5288595 | — | IC50 | = | 405.2 | nM | 6.39 |
| CHEMBL5093741 | — | IC50 | = | 514.2 | nM | 6.29 |
| CHEMBL1997924 | — | IC50 | = | 1138.0 | nM | 5.94 |
| CHEMBL3185434 | — | IC50 | = | 1248.0 | nM | 5.90 |
| CHEMBL5284529 | — | IC50 | = | 2803.0 | nM | 5.55 |
| CHEMBL297453 | EPIGALOCATECHIN GALLATE | IC50 | > | 10000.0 | nM | - |