Assay Detail
Binding
CHEMBL3424978
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Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins
22
Total Activities
22
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
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 | 22 | 7.94 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3421963 | — | — | 1 | 9.00 |
| CHEMBL3421962 | — | — | 1 | 8.70 |
| CHEMBL3421981 | — | — | 1 | 8.52 |
| CHEMBL3421968 | — | — | 1 | 8.52 |
| CHEMBL3421969 | — | — | 1 | 8.40 |
| CHEMBL3421967 | — | — | 1 | 8.40 |
| CHEMBL3421970 | — | — | 1 | 8.30 |
| CHEMBL3421978 | — | — | 1 | 8.15 |
| CHEMBL3421980 | — | — | 1 | 8.15 |
| CHEMBL3421966 | — | — | 1 | 8.05 |
| CHEMBL3421971 | — | — | 1 | 8.05 |
| CHEMBL3421976 | — | — | 1 | 7.92 |
| CHEMBL3421977 | — | — | 1 | 7.85 |
| CHEMBL3421964 | — | — | 1 | 7.80 |
| CHEMBL3421979 | — | — | 1 | 7.77 |
| CHEMBL3421975 | — | — | 1 | 7.68 |
| CHEMBL3421973 | — | — | 1 | 7.60 |
| CHEMBL3421965 | — | — | 1 | 7.47 |
| CHEMBL388853 | — | — | 1 | 7.37 |
| CHEMBL3421636 | — | — | 1 | 7.07 |
| CHEMBL3421974 | — | — | 1 | 7.01 |
| CHEMBL3421972 | — | — | 1 | 6.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3421963 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3421962 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3421981 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3421968 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3421969 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3421967 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3421970 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3421978 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3421980 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3421966 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3421971 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3421976 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3421977 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3421964 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3421979 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3421975 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3421973 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3421965 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL388853 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3421636 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3421974 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3421972 | — | IC50 | = | 140.0 | nM | 6.85 |