Assay Detail
Binding
CHEMBL3424979
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Inhibition of human full length C-terminal c-Myc tagged Dyrk1B phosphorylation overexpressed in monkey COS1 cells after 5 hrs by ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-1 |
| 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
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.38 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3421968 | — | — | 1 | 7.38 |
| CHEMBL3421970 | — | — | 1 | 7.08 |
| CHEMBL3421967 | — | — | 1 | 7.07 |
| CHEMBL3421971 | — | — | 1 | 6.78 |
| CHEMBL3421978 | — | — | 1 | 6.72 |
| CHEMBL3421980 | — | — | 1 | 6.71 |
| CHEMBL3421963 | — | — | 1 | 6.55 |
| CHEMBL3421981 | — | — | 1 | 6.42 |
| CHEMBL3421962 | — | — | 1 | 6.34 |
| CHEMBL3421976 | — | — | 1 | 6.09 |
| CHEMBL3421975 | — | — | 1 | 6.05 |
| CHEMBL3421977 | — | — | 1 | 5.67 |
| CHEMBL3421979 | — | — | 1 | 5.51 |
| CHEMBL3421636 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3421968 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3421970 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3421967 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3421971 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL3421978 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL3421980 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3421963 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL3421981 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL3421962 | — | IC50 | = | 453.0 | nM | 6.34 |
| CHEMBL3421976 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3421975 | — | IC50 | = | 898.0 | nM | 6.05 |
| CHEMBL3421977 | — | IC50 | = | 2118.0 | nM | 5.67 |
| CHEMBL3421979 | — | IC50 | = | 3069.0 | nM | 5.51 |
| CHEMBL3421636 | — | IC50 | = | 9965.0 | nM | 5.00 |