Assay Detail
Binding
CHEMBL1804241
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant GST-tagged DYRK1A using myelin protein as substrate and [gamma32]-ATP after 30 mins by scintillation counting
36
Total Activities
36
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
Synthesis, protein kinase inhibitory potencies, and in vitro antiproliferative activities of meridianin derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.22 | 7.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1802966 | — | — | 1 | 7.47 |
| CHEMBL1802967 | — | — | 1 | 7.41 |
| CHEMBL1802406 | — | — | 1 | 7.18 |
| CHEMBL1802963 | — | — | 1 | 7.17 |
| CHEMBL1802401 | — | — | 1 | 7.07 |
| CHEMBL1802404 | — | — | 1 | 7.02 |
| CHEMBL1802410 | — | — | 1 | 6.96 |
| CHEMBL46440 | MERIDIANIN D | — | 1 | 6.89 |
| CHEMBL1802391 | — | — | 1 | 6.72 |
| CHEMBL1802409 | — | — | 1 | 6.66 |
| CHEMBL1802403 | — | — | 1 | 6.60 |
| CHEMBL1802971 | — | — | 1 | 6.54 |
| CHEMBL1802965 | — | — | 1 | 6.48 |
| CHEMBL44541 | MERIDIANIN C | — | 1 | 6.48 |
| CHEMBL1802405 | — | — | 1 | 6.34 |
| CHEMBL48082 | — | — | 1 | 6.16 |
| CHEMBL1802396 | — | — | 1 | 6.09 |
| CHEMBL1802962 | — | — | 1 | 6.07 |
| CHEMBL1802399 | — | — | 1 | 6.07 |
| CHEMBL1802400 | — | — | 1 | 5.96 |
| CHEMBL1802395 | — | — | 1 | 5.90 |
| CHEMBL1802964 | — | — | 1 | 5.84 |
| CHEMBL1802392 | — | — | 1 | 5.73 |
| CHEMBL1802968 | — | — | 1 | 5.68 |
| CHEMBL1802408 | — | — | 1 | 5.64 |
| CHEMBL1802407 | — | — | 1 | 5.55 |
| CHEMBL1802390 | — | — | 1 | 5.51 |
| CHEMBL1802389 | — | — | 1 | 5.38 |
| CHEMBL1802397 | — | — | 1 | 5.25 |
| CHEMBL1802398 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1802966 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL1802967 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL1802406 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1802963 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1802401 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1802404 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1802410 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL46440 | MERIDIANIN D | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1802391 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1802409 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1802403 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1802971 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1802965 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL44541 | MERIDIANIN C | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1802405 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL48082 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1802396 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL1802399 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1802962 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL1802400 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1802395 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL1802964 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL1802392 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL1802968 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1802408 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL1802407 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1802390 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1802389 | — | IC50 | = | 4150.0 | nM | 5.38 |
| CHEMBL1802397 | — | IC50 | = | 5650.0 | nM | 5.25 |
| CHEMBL1802398 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL1802969 | — | IC50 | = | 8450.0 | nM | 5.07 |
| CHEMBL1802402 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1802972 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802970 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802393 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1802394 | — | IC50 | > | 10000.0 | nM | - |