Assay Detail
Binding
CHEMBL3778244
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human GST-tagged DYRK1B expressed in insect cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP
20
Total Activities
20
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 1B (CHEMBL5543) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.93 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3774448 | — | — | 1 | 7.22 |
| CHEMBL3775393 | — | — | 1 | 7.16 |
| CHEMBL568150 | — | — | 1 | 7.10 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 6.75 |
| CHEMBL3774830 | — | — | 1 | 6.52 |
| CHEMBL3775754 | — | — | 1 | 6.05 |
| CHEMBL3774704 | — | — | 1 | 5.98 |
| CHEMBL3775949 | — | — | 1 | 5.82 |
| CHEMBL3775538 | — | — | 1 | 5.78 |
| CHEMBL3775821 | — | — | 1 | 5.66 |
| CHEMBL3193172 | — | — | 1 | 5.58 |
| CHEMBL3775111 | — | — | 1 | 5.58 |
| CHEMBL1612487 | — | — | 1 | 5.42 |
| CHEMBL3774696 | — | — | 1 | 5.37 |
| CHEMBL3774667 | — | — | 1 | 5.28 |
| CHEMBL3774736 | — | — | 1 | 5.24 |
| CHEMBL3775193 | — | — | 1 | 5.17 |
| CHEMBL3775969 | — | — | 1 | 4.98 |
| CHEMBL571292 | — | — | 1 | - |
| CHEMBL38043 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3774448 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3775393 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL568150 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL269538 | HARMINE | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3774830 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL3775754 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3774704 | — | IC50 | = | 1050.0 | nM | 5.98 |
| CHEMBL3775949 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL3775538 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL3775821 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL3193172 | — | IC50 | = | 2630.0 | nM | 5.58 |
| CHEMBL3775111 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL1612487 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3774696 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL3774667 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL3774736 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL3775193 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL3775969 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL571292 | — | IC50 | - | — | - | |
| CHEMBL38043 | — | IC50 | > | 10000.0 | nM | - |