Assay Detail
Binding
CHEMBL5735650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: The DYRK1A kinase assay was run using the Ser/Thr 18 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologiesa Division of Thermo-Fisher). This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity which is represented as a ratio of coumarin emission/fluorescein emission.Briefly, recombinant DYRK1A kinase, ATP and Ser/Thr peptide 18 were prepared in 1× Kinase buffer to final concentrations of 0.19 μg/mL, 30 μM, and 4 μM respectively. The mixture was allowed to incubate with the representative compounds for one hour at room temperature. All reactions were performed in duplicate. Unphosphorylated (0% Control) and phosphorylated (100% control) forms of Ser/Thr 18 served as control reactions. Additionally, an 11-point dose-response curve of Staurosporine (1 uM top) was run to serve as a positive compound control.After incubation, Development Reagent A was diluted in Development Buffer then added to the reaction and allowed to further incubate for one hour at room temperature. The plate was read at Ex 400 Em 455 to detect the coumarin signal and Ex 400 Em 520 to measure the signal (EnVision Multilabel Plate Reader, PerkinElmer).
210
Total Activities
66
Compounds Tested
3
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
6-(5-membered heteroaryl)isoquinolin-3-yl-(5-membered heteroaryl) carboxamides and preparation and use thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 70 | 8.15 | 9.00 |
| kon | 70 | - | - |
| k_off | 70 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6056650 | — | — | 3 | 9.00 |
| CHEMBL5940869 | — | — | 3 | 9.00 |
| CHEMBL6036161 | — | — | 3 | 9.00 |
| CHEMBL4755579 | — | — | 6 | 8.70 |
| CHEMBL6045084 | — | — | 6 | 8.70 |
| CHEMBL4761662 | — | — | 6 | 8.70 |
| CHEMBL6063563 | — | — | 3 | 8.70 |
| CHEMBL5893883 | — | — | 3 | 8.70 |
| CHEMBL5886109 | — | — | 3 | 8.70 |
| CHEMBL4762838 | — | — | 3 | 8.70 |
| CHEMBL5996584 | — | — | 3 | 8.70 |
| CHEMBL4800296 | — | — | 3 | 8.70 |
| CHEMBL5992147 | — | — | 3 | 8.52 |
| CHEMBL5784059 | — | — | 3 | 8.52 |
| CHEMBL6015428 | — | — | 3 | 8.52 |
| CHEMBL4746707 | — | — | 3 | 8.52 |
| CHEMBL6000505 | — | — | 3 | 8.52 |
| CHEMBL5995698 | — | — | 3 | 8.52 |
| CHEMBL5920679 | — | — | 3 | 8.52 |
| CHEMBL4795948 | — | — | 3 | 8.52 |
| CHEMBL6059586 | — | — | 3 | 8.52 |
| CHEMBL5803825 | — | — | 3 | 8.40 |
| CHEMBL4787749 | — | — | 3 | 8.40 |
| CHEMBL5857120 | — | — | 3 | 8.40 |
| CHEMBL6038529 | — | — | 3 | 8.40 |
| CHEMBL5989365 | — | — | 3 | 8.40 |
| CHEMBL5994578 | — | — | 3 | 8.40 |
| CHEMBL5883539 | — | — | 3 | 8.30 |
| CHEMBL5842207 | — | — | 3 | 8.30 |
| CHEMBL5982070 | — | — | 3 | 8.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5940869 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6056650 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6036161 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4755579 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6045084 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5893883 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4762838 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4761662 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4800296 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4761662 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5996584 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5886109 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6063563 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6000505 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5992147 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4746707 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5920679 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5995698 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4795948 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6015428 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5784059 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6059586 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6045084 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL6038529 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5989365 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5857120 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5803825 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4787749 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5994578 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5982070 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5842207 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5883539 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5929615 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5957402 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6024982 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6040830 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6018003 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5783562 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5897434 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5752492 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5914139 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4754087 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6048132 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5860704 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5772142 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5792391 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5873194 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5782986 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5982831 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5933226 | — | EC50 | = | 15.0 | nM | 7.82 |