Assay Detail
Binding
CHEMBL5378446
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human DYRK1A assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis
44
Total Activities
43
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 1A (CHEMBL2292) ↗| 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 | 44 | 6.92 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085086 | — | — | 2 | 8.92 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 8.62 |
| CHEMBL5412105 | — | — | 1 | 8.44 |
| CHEMBL5428750 | — | — | 1 | 8.30 |
| CHEMBL5401556 | — | — | 1 | 7.96 |
| CHEMBL5395833 | — | — | 1 | 7.94 |
| CHEMBL5408047 | — | — | 1 | 7.78 |
| CHEMBL5435195 | — | — | 1 | 7.73 |
| CHEMBL5432405 | — | — | 1 | 7.69 |
| CHEMBL5403642 | — | — | 1 | 7.45 |
| CHEMBL5429359 | — | — | 1 | 7.44 |
| CHEMBL5422963 | — | — | 1 | 7.42 |
| CHEMBL1802358 | — | — | 1 | 7.38 |
| CHEMBL5406864 | — | — | 1 | 7.27 |
| CHEMBL5420112 | — | — | 1 | 7.13 |
| CHEMBL5417699 | — | — | 1 | 7.12 |
| CHEMBL5414174 | — | — | 1 | 7.10 |
| CHEMBL5422667 | — | — | 1 | 7.07 |
| CHEMBL5432194 | — | — | 1 | 7.06 |
| CHEMBL5429691 | — | — | 1 | 6.95 |
| CHEMBL5415554 | — | — | 1 | 6.71 |
| CHEMBL5406490 | — | — | 1 | 6.68 |
| CHEMBL5433334 | — | — | 1 | 6.64 |
| CHEMBL5397088 | — | — | 1 | 6.63 |
| CHEMBL5414086 | — | — | 1 | 6.40 |
| CHEMBL5415238 | — | — | 1 | 6.31 |
| CHEMBL5406672 | — | — | 1 | 6.30 |
| CHEMBL5421052 | — | — | 1 | 6.29 |
| CHEMBL5426876 | — | — | 1 | 6.02 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 5.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085086 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5412105 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5428750 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5401556 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL5395833 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5408047 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL5435195 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL5085086 | — | IC50 | = | 19.3 | nM | 7.71 |
| CHEMBL5432405 | — | IC50 | = | 20.3 | nM | 7.69 |
| CHEMBL5403642 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL5429359 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL5422963 | — | IC50 | = | 38.5 | nM | 7.42 |
| CHEMBL1802358 | — | IC50 | = | 41.6 | nM | 7.38 |
| CHEMBL5406864 | — | IC50 | = | 53.5 | nM | 7.27 |
| CHEMBL5420112 | — | IC50 | = | 74.4 | nM | 7.13 |
| CHEMBL5417699 | — | IC50 | = | 76.6 | nM | 7.12 |
| CHEMBL5414174 | — | IC50 | = | 78.7 | nM | 7.10 |
| CHEMBL5422667 | — | IC50 | = | 84.4 | nM | 7.07 |
| CHEMBL5432194 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5429691 | — | IC50 | = | 112.3 | nM | 6.95 |
| CHEMBL5415554 | — | IC50 | = | 196.1 | nM | 6.71 |
| CHEMBL5406490 | — | IC50 | = | 210.2 | nM | 6.68 |
| CHEMBL5433334 | — | IC50 | = | 228.8 | nM | 6.64 |
| CHEMBL5397088 | — | IC50 | = | 235.9 | nM | 6.63 |
| CHEMBL5414086 | — | IC50 | = | 399.3 | nM | 6.40 |
| CHEMBL5415238 | — | IC50 | = | 488.0 | nM | 6.31 |
| CHEMBL5406672 | — | IC50 | = | 505.9 | nM | 6.30 |
| CHEMBL5421052 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL5426876 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 1549.0 | nM | 5.81 |
| CHEMBL5404093 | — | IC50 | = | 1755.0 | nM | 5.76 |
| CHEMBL5426463 | — | IC50 | = | 3930.0 | nM | 5.41 |
| CHEMBL5401354 | — | IC50 | = | 4794.0 | nM | 5.32 |
| CHEMBL5430240 | — | IC50 | = | 5618.0 | nM | 5.25 |
| CHEMBL5435933 | — | IC50 | = | 7484.0 | nM | 5.13 |
| CHEMBL5413380 | — | IC50 | = | 8746.0 | nM | 5.06 |
| CHEMBL5439224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5429150 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5419583 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5424188 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426979 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5420099 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5432402 | — | IC50 | > | 10000.0 | nM | - |