Assay Detail
Binding
CHEMBL3105977
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Inhibition of rat recombinant 6xHis-tagged DYRK1A catalytic domain (1 to 502) expressed in Escherichia coli BL21 (DE3) using N-terminal fluorescein coupled KISGRLSPIMTEQ as substrate after 30 mins by HPLC analysis in presence of 50 uM ATP
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.38 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3102952 | — | — | 1 | 8.52 |
| CHEMBL3102951 | — | — | 1 | 7.93 |
| CHEMBL3102955 | — | — | 1 | 7.91 |
| CHEMBL3102953 | — | — | 1 | 7.84 |
| CHEMBL3102950 | — | — | 1 | 7.64 |
| CHEMBL3102954 | — | — | 1 | 7.41 |
| CHEMBL3102956 | — | — | 1 | 6.98 |
| CHEMBL3102957 | — | — | 1 | 6.82 |
| CHEMBL3102942 | — | — | 1 | 6.80 |
| CHEMBL3102944 | — | — | 1 | 6.55 |
| CHEMBL3102935 | — | — | 1 | 6.48 |
| CHEMBL3102859 | — | — | 1 | 6.39 |
| CHEMBL3102945 | — | — | 1 | 6.34 |
| CHEMBL3102938 | — | — | 1 | 6.02 |
| CHEMBL3102934 | — | — | 1 | 6.02 |
| CHEMBL3102940 | — | — | 1 | 5.93 |
| CHEMBL3102947 | — | — | 1 | 5.78 |
| CHEMBL3102943 | — | — | 1 | 5.76 |
| CHEMBL3102937 | — | — | 1 | 5.57 |
| CHEMBL3102946 | — | — | 1 | 5.54 |
| CHEMBL3102941 | — | — | 1 | 5.51 |
| CHEMBL3102939 | — | — | 1 | 5.45 |
| CHEMBL3102936 | — | — | 1 | 5.13 |
| CHEMBL3102949 | — | — | 1 | 4.83 |
| CHEMBL3102948 | — | — | 1 | 4.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3102952 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3102951 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL3102955 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL3102953 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL3102950 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL3102954 | — | IC50 | = | 39.1 | nM | 7.41 |
| CHEMBL3102956 | — | IC50 | = | 105.2 | nM | 6.98 |
| CHEMBL3102957 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3102942 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3102944 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3102935 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3102859 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3102945 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3102938 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3102934 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3102940 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL3102947 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL3102943 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL3102937 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3102946 | — | IC50 | = | 2880.0 | nM | 5.54 |
| CHEMBL3102941 | — | IC50 | = | 3080.0 | nM | 5.51 |
| CHEMBL3102939 | — | IC50 | = | 3590.0 | nM | 5.45 |
| CHEMBL3102936 | — | IC50 | = | 7490.0 | nM | 5.13 |
| CHEMBL3102949 | — | IC50 | = | 14630.0 | nM | 4.83 |
| CHEMBL3102948 | — | IC50 | = | 57780.0 | nM | 4.24 |