Assay Detail
Binding
CHEMBL4034241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length recombinant human GST-tagged Dyrk1a expressed in baculovirus expression system using Alexa-Fluor tracer-236 incubated for 60 mins by TR-FRET based Lantha-screen Eu kinase assay
32
Total Activities
32
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 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 6.89 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4079572 | — | — | 1 | 9.00 |
| CHEMBL4084955 | — | — | 1 | 9.00 |
| CHEMBL4064316 | — | — | 1 | 8.10 |
| CHEMBL4105629 | — | — | 1 | 8.10 |
| CHEMBL4091320 | — | — | 1 | 8.00 |
| CHEMBL4069163 | — | — | 1 | 7.92 |
| CHEMBL3421979 | — | — | 1 | 7.72 |
| CHEMBL269538 | HARMINE | 1.0 | 1 | 7.39 |
| CHEMBL4073997 | — | — | 1 | 7.34 |
| CHEMBL4075648 | — | — | 1 | 7.21 |
| CHEMBL4087456 | — | — | 1 | 7.21 |
| CHEMBL4098505 | — | — | 1 | 7.16 |
| CHEMBL4080488 | — | — | 1 | 7.12 |
| CHEMBL1802963 | — | — | 1 | 7.10 |
| CHEMBL4077010 | — | — | 1 | 7.05 |
| CHEMBL4086818 | — | — | 1 | 7.03 |
| CHEMBL4095674 | — | — | 1 | 6.96 |
| CHEMBL4072138 | — | — | 1 | 6.86 |
| CHEMBL4090889 | — | — | 1 | 6.62 |
| CHEMBL4066607 | — | — | 1 | 6.56 |
| CHEMBL4094549 | — | — | 1 | 6.54 |
| CHEMBL4095156 | — | — | 1 | 6.46 |
| CHEMBL4065388 | — | — | 1 | 6.39 |
| CHEMBL4095479 | — | — | 1 | 6.35 |
| CHEMBL48082 | — | — | 1 | 6.23 |
| CHEMBL4066075 | — | — | 1 | 6.10 |
| CHEMBL4074685 | — | — | 1 | 5.69 |
| CHEMBL4068096 | — | — | 1 | 5.67 |
| CHEMBL4098364 | — | — | 1 | 5.54 |
| CHEMBL4069088 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4079572 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4084955 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4064316 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4105629 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4091320 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4069163 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3421979 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL269538 | HARMINE | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4073997 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4075648 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4087456 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4098505 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4080488 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL1802963 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4077010 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4086818 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4095674 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4072138 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4090889 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL4066607 | — | IC50 | = | 277.0 | nM | 6.56 |
| CHEMBL4094549 | — | IC50 | = | 285.0 | nM | 6.54 |
| CHEMBL4095156 | — | IC50 | = | 351.0 | nM | 6.46 |
| CHEMBL4065388 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL4095479 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL48082 | — | IC50 | = | 588.0 | nM | 6.23 |
| CHEMBL4066075 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4074685 | — | IC50 | = | 2024.0 | nM | 5.69 |
| CHEMBL4068096 | — | IC50 | = | 2142.0 | nM | 5.67 |
| CHEMBL4098364 | — | IC50 | = | 2904.0 | nM | 5.54 |
| CHEMBL4069088 | — | IC50 | = | 2939.0 | nM | 5.53 |
| CHEMBL4103831 | — | IC50 | = | 4335.0 | nM | 5.36 |
| CHEMBL4102903 | — | IC50 | = | 7957.0 | nM | 5.10 |