Assay Detail
Binding
CHEMBL3889022
Review assay metadata, readout intent, target linkage, and publication context from the same page.
HotSpot Technology Assay: The DYRK1A and DYRK1B kinase assays to determine IC50 values were performed by Reaction Biology Corporation using HotSpot technology Worldwide website: reactionbiology.com, Malvern, PA). Kinase reaction with specific kinase/ substrate pair along with required cofactors was carried out in 20 mM Hepes pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/ml BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO. Purified recombinant kinase was incubated with serial 3-fold dilutions of test compounds starting at a final concentration of 10 μM. Reaction was initiated by addition of a mixture of ATP (Sigma, St. Louis MO) and 33P ATP (Perkin Elmer, Waltham MA) to a final concentration of 10 μM and was carried out at room temperature for 120 min, followed by spotting of the reaction onto P81 ion exchange filter paper (Whatman Inc., Piscataway, NJ). Unbound phosphate was removed by extensive washing of filters in 0.75% Phosphoric acid.
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
DYRK1 inhibitors and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 65 | 7.18 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386770 | — | — | 1 | 9.80 |
| CHEMBL2386747 | — | — | 1 | 9.66 |
| CHEMBL3894571 | — | — | 1 | 9.44 |
| CHEMBL2386748 | — | — | 1 | 9.03 |
| CHEMBL2386764 | — | — | 1 | 9.01 |
| CHEMBL3971170 | — | — | 1 | 9.00 |
| CHEMBL2386762 | — | — | 1 | 8.95 |
| CHEMBL2386753 | — | — | 1 | 8.78 |
| CHEMBL2386763 | — | — | 1 | 8.74 |
| CHEMBL3915647 | — | — | 1 | 8.56 |
| CHEMBL2386744 | — | — | 1 | 8.44 |
| CHEMBL2386766 | — | — | 1 | 8.41 |
| CHEMBL3905538 | — | — | 1 | 8.37 |
| CHEMBL3983413 | — | — | 1 | 8.35 |
| CHEMBL2386749 | — | — | 1 | 8.31 |
| CHEMBL2386760 | — | — | 1 | 8.29 |
| CHEMBL2386754 | — | — | 1 | 8.22 |
| CHEMBL2386765 | — | — | 1 | 8.22 |
| CHEMBL3912295 | — | — | 1 | 8.10 |
| CHEMBL2386752 | — | — | 1 | 8.06 |
| CHEMBL2386743 | — | — | 1 | 8.02 |
| CHEMBL2386761 | — | — | 1 | 7.88 |
| CHEMBL2386751 | — | — | 1 | 7.87 |
| CHEMBL3898860 | — | — | 1 | 7.76 |
| CHEMBL2386769 | — | — | 1 | 7.74 |
| CHEMBL2386759 | — | — | 1 | 7.58 |
| CHEMBL3909052 | — | — | 1 | 7.48 |
| CHEMBL2386755 | — | — | 1 | 7.47 |
| CHEMBL3940669 | — | — | 1 | 7.46 |
| CHEMBL2386768 | — | — | 1 | 7.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386770 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL2386747 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3894571 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL2386748 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL2386764 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL3971170 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL2386762 | — | IC50 | = | 1.13 | nM | 8.95 |
| CHEMBL2386753 | — | IC50 | = | 1.65 | nM | 8.78 |
| CHEMBL2386763 | — | IC50 | = | 1.81 | nM | 8.74 |
| CHEMBL3915647 | — | IC50 | = | 2.76 | nM | 8.56 |
| CHEMBL2386744 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL2386766 | — | IC50 | = | 3.89 | nM | 8.41 |
| CHEMBL3905538 | — | IC50 | = | 4.25 | nM | 8.37 |
| CHEMBL3983413 | — | IC50 | = | 4.44 | nM | 8.35 |
| CHEMBL2386749 | — | IC50 | = | 4.91 | nM | 8.31 |
| CHEMBL2386760 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL2386754 | — | IC50 | = | 6.02 | nM | 8.22 |
| CHEMBL2386765 | — | IC50 | = | 6.06 | nM | 8.22 |
| CHEMBL3912295 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2386752 | — | IC50 | = | 8.63 | nM | 8.06 |
| CHEMBL2386743 | — | IC50 | = | 9.53 | nM | 8.02 |
| CHEMBL2386761 | — | IC50 | = | 13.08 | nM | 7.88 |
| CHEMBL2386751 | — | IC50 | = | 13.64 | nM | 7.87 |
| CHEMBL3898860 | — | IC50 | = | 17.48 | nM | 7.76 |
| CHEMBL2386769 | — | IC50 | = | 18.26 | nM | 7.74 |
| CHEMBL2386759 | — | IC50 | = | 26.2 | nM | 7.58 |
| CHEMBL3909052 | — | IC50 | = | 33.2 | nM | 7.48 |
| CHEMBL2386755 | — | IC50 | = | 33.93 | nM | 7.47 |
| CHEMBL3940669 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL2386768 | — | IC50 | = | 35.64 | nM | 7.45 |
| CHEMBL2386767 | — | IC50 | = | 39.03 | nM | 7.41 |
| CHEMBL3954779 | — | IC50 | = | 40.76 | nM | 7.39 |
| CHEMBL2386750 | — | IC50 | = | 42.7 | nM | 7.37 |
| CHEMBL3916163 | — | IC50 | = | 47.5 | nM | 7.32 |
| CHEMBL3982462 | — | IC50 | = | 54.84 | nM | 7.26 |
| CHEMBL3970062 | — | IC50 | = | 66.82 | nM | 7.17 |
| CHEMBL3906791 | — | IC50 | = | 79.85 | nM | 7.10 |
| CHEMBL3900000 | — | IC50 | = | 123.5 | nM | 6.91 |
| CHEMBL3921510 | — | IC50 | = | 124.7 | nM | 6.90 |
| CHEMBL3921110 | — | IC50 | = | 128.8 | nM | 6.89 |
| CHEMBL3957886 | — | IC50 | = | 142.5 | nM | 6.85 |
| CHEMBL3931248 | — | IC50 | = | 146.6 | nM | 6.83 |
| CHEMBL2386757 | — | IC50 | = | 194.4 | nM | 6.71 |
| CHEMBL3960099 | — | IC50 | = | 298.9 | nM | 6.52 |
| CHEMBL2386756 | — | IC50 | = | 431.2 | nM | 6.37 |
| CHEMBL2386758 | — | IC50 | = | 436.1 | nM | 6.36 |
| CHEMBL3893495 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3930050 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3904523 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3975059 | — | IC50 | = | 500.0 | nM | 6.30 |