Assay Detail
Binding
CHEMBL5378454
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant DYRK4 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 4 (CHEMBL1075115) ↗| 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 | 5.72 | 6.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 6.41 |
| CHEMBL1802358 | — | — | 1 | 6.29 |
| CHEMBL5412105 | — | — | 1 | 6.29 |
| CHEMBL5085086 | — | — | 1 | 6.28 |
| CHEMBL5432405 | — | — | 1 | 5.91 |
| CHEMBL5433334 | — | — | 1 | 5.59 |
| CHEMBL5406672 | — | — | 1 | 5.54 |
| CHEMBL5403642 | — | — | 1 | 5.44 |
| CHEMBL5429359 | — | — | 1 | 5.32 |
| CHEMBL5408047 | — | — | 1 | 5.29 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 5.20 |
| CHEMBL5430240 | — | — | 1 | 5.06 |
| CHEMBL5424188 | — | — | 1 | - |
| CHEMBL5426979 | — | — | 1 | - |
| CHEMBL5413380 | — | — | 1 | - |
| CHEMBL5404093 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 388.0 | nM | 6.41 |
| CHEMBL1802358 | — | IC50 | = | 507.4 | nM | 6.29 |
| CHEMBL5412105 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL5085086 | — | IC50 | = | 524.7 | nM | 6.28 |
| CHEMBL5432405 | — | IC50 | = | 1223.0 | nM | 5.91 |
| CHEMBL5433334 | — | IC50 | = | 2563.0 | nM | 5.59 |
| CHEMBL5406672 | — | IC50 | = | 2862.0 | nM | 5.54 |
| CHEMBL5403642 | — | IC50 | = | 3618.0 | nM | 5.44 |
| CHEMBL5429359 | — | IC50 | = | 4783.0 | nM | 5.32 |
| CHEMBL5408047 | — | IC50 | = | 5177.0 | nM | 5.29 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 6374.0 | nM | 5.20 |
| CHEMBL5430240 | — | IC50 | = | 8703.0 | nM | 5.06 |
| CHEMBL5424188 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426979 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5404093 | — | IC50 | > | 10000.0 | nM | - |