Assay Detail
Binding
CHEMBL5378452
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Inhibition of human recombinant DYRK2 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 2 (CHEMBL4376) ↗| 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 | 6.11 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085086 | — | — | 1 | 6.86 |
| CHEMBL5433334 | — | — | 1 | 6.78 |
| CHEMBL5406672 | — | — | 1 | 6.77 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 6.69 |
| CHEMBL5430240 | — | — | 1 | 6.24 |
| CHEMBL1802358 | — | — | 1 | 6.20 |
| CHEMBL5412105 | — | — | 1 | 6.20 |
| CHEMBL5432405 | — | — | 1 | 6.15 |
| CHEMBL5424188 | — | — | 1 | 6.11 |
| CHEMBL5403642 | — | — | 1 | 5.68 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 5.56 |
| CHEMBL5408047 | — | — | 1 | 5.55 |
| CHEMBL5426979 | — | — | 1 | 5.40 |
| CHEMBL5429359 | — | — | 1 | 5.36 |
| CHEMBL5413380 | — | — | 1 | - |
| CHEMBL5404093 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085086 | — | IC50 | = | 138.3 | nM | 6.86 |
| CHEMBL5433334 | — | IC50 | = | 165.1 | nM | 6.78 |
| CHEMBL5406672 | — | IC50 | = | 168.5 | nM | 6.77 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 202.4 | nM | 6.69 |
| CHEMBL5430240 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL1802358 | — | IC50 | = | 630.5 | nM | 6.20 |
| CHEMBL5412105 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL5432405 | — | IC50 | = | 711.6 | nM | 6.15 |
| CHEMBL5424188 | — | IC50 | = | 773.7 | nM | 6.11 |
| CHEMBL5403642 | — | IC50 | = | 2076.0 | nM | 5.68 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL5408047 | — | IC50 | = | 2843.0 | nM | 5.55 |
| CHEMBL5426979 | — | IC50 | = | 3965.0 | nM | 5.40 |
| CHEMBL5429359 | — | IC50 | = | 4364.0 | nM | 5.36 |
| CHEMBL5413380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5404093 | — | IC50 | > | 10000.0 | nM | - |