Assay Detail
Binding
CHEMBL5378453
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Inhibition of human recombinant DYRK3 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis
16
Total Activities
16
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 3 (CHEMBL4575) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer's Disease Drug Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.88 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5412105 | — | — | 1 | 6.51 |
| CHEMBL5408047 | — | — | 1 | 6.31 |
| CHEMBL5085086 | — | — | 1 | 6.09 |
| CHEMBL5406672 | — | — | 1 | 6.08 |
| CHEMBL5433334 | — | — | 1 | 6.05 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 5.98 |
| CHEMBL5429359 | — | — | 1 | 5.86 |
| CHEMBL5403642 | — | — | 1 | 5.78 |
| CHEMBL1802358 | — | — | 1 | 5.73 |
| CHEMBL5432405 | — | — | 1 | 5.63 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 5.31 |
| CHEMBL5430240 | — | — | 1 | 5.27 |
| CHEMBL5424188 | — | — | 1 | - |
| CHEMBL5426979 | — | — | 1 | - |
| CHEMBL5413380 | — | — | 1 | - |
| CHEMBL5404093 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5412105 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5408047 | — | IC50 | = | 493.4 | nM | 6.31 |
| CHEMBL5085086 | — | IC50 | = | 806.0 | nM | 6.09 |
| CHEMBL5406672 | — | IC50 | = | 841.9 | nM | 6.08 |
| CHEMBL5433334 | — | IC50 | = | 889.2 | nM | 6.05 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 1052.0 | nM | 5.98 |
| CHEMBL5429359 | — | IC50 | = | 1377.0 | nM | 5.86 |
| CHEMBL5403642 | — | IC50 | = | 1651.0 | nM | 5.78 |
| CHEMBL1802358 | — | IC50 | = | 1847.0 | nM | 5.73 |
| CHEMBL5432405 | — | IC50 | = | 2364.0 | nM | 5.63 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 4866.0 | nM | 5.31 |
| CHEMBL5430240 | — | IC50 | = | 5323.0 | nM | 5.27 |
| CHEMBL5424188 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426979 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5404093 | — | IC50 | > | 10000.0 | nM | - |