Assay Detail
Binding
CHEMBL5378445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CLK4 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis
45
Total Activities
44
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 protein kinase CLK4 (CHEMBL4203) ↗| 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 | 45 | 7.13 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5429691 | — | — | 1 | 8.68 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 8.30 |
| CHEMBL5412105 | — | — | 1 | 8.29 |
| CHEMBL5435855 | — | — | 1 | 8.27 |
| CHEMBL1802358 | — | — | 1 | 8.00 |
| CHEMBL5085086 | — | — | 2 | 7.94 |
| CHEMBL5414174 | — | — | 1 | 7.93 |
| CHEMBL5408047 | — | — | 1 | 7.87 |
| CHEMBL5428750 | — | — | 1 | 7.87 |
| CHEMBL5395833 | — | — | 1 | 7.85 |
| CHEMBL5401556 | — | — | 1 | 7.79 |
| CHEMBL5432405 | — | — | 1 | 7.72 |
| CHEMBL5429359 | — | — | 1 | 7.58 |
| CHEMBL5397088 | — | — | 1 | 7.43 |
| CHEMBL5417699 | — | — | 1 | 7.38 |
| CHEMBL5435195 | — | — | 1 | 7.28 |
| CHEMBL5403642 | — | — | 1 | 7.24 |
| CHEMBL5433334 | — | — | 1 | 7.23 |
| CHEMBL5406864 | — | — | 1 | 7.11 |
| CHEMBL5422667 | — | — | 1 | 6.82 |
| CHEMBL5422963 | — | — | 1 | 6.78 |
| CHEMBL5415554 | — | — | 1 | 6.78 |
| CHEMBL5414086 | — | — | 1 | 6.77 |
| CHEMBL5420112 | — | — | 1 | 6.72 |
| CHEMBL5406672 | — | — | 1 | 6.62 |
| CHEMBL5432194 | — | — | 1 | 6.61 |
| CHEMBL5406490 | — | — | 1 | 6.57 |
| CHEMBL485053 | LEUCETTAMINE B | — | 1 | 6.40 |
| CHEMBL5415238 | — | — | 1 | 6.24 |
| CHEMBL5421052 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5429691 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5412105 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5435855 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL1802358 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5085086 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5414174 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5085086 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5408047 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5428750 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5395833 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5401556 | — | IC50 | = | 16.3 | nM | 7.79 |
| CHEMBL5432405 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL5429359 | — | IC50 | = | 26.4 | nM | 7.58 |
| CHEMBL5397088 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5417699 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL5435195 | — | IC50 | = | 52.7 | nM | 7.28 |
| CHEMBL5403642 | — | IC50 | = | 57.8 | nM | 7.24 |
| CHEMBL5433334 | — | IC50 | = | 58.5 | nM | 7.23 |
| CHEMBL5406864 | — | IC50 | = | 77.1 | nM | 7.11 |
| CHEMBL5422667 | — | IC50 | = | 152.7 | nM | 6.82 |
| CHEMBL5415554 | — | IC50 | = | 165.6 | nM | 6.78 |
| CHEMBL5422963 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL5414086 | — | IC50 | = | 169.5 | nM | 6.77 |
| CHEMBL5420112 | — | IC50 | = | 189.3 | nM | 6.72 |
| CHEMBL5406672 | — | IC50 | = | 239.8 | nM | 6.62 |
| CHEMBL5432194 | — | IC50 | = | 245.2 | nM | 6.61 |
| CHEMBL5406490 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 396.2 | nM | 6.40 |
| CHEMBL5415238 | — | IC50 | = | 577.7 | nM | 6.24 |
| CHEMBL5421052 | — | IC50 | = | 673.1 | nM | 6.17 |
| CHEMBL5426876 | — | IC50 | = | 861.0 | nM | 6.07 |
| CHEMBL5424188 | — | IC50 | = | 1006.0 | nM | 6.00 |
| CHEMBL5430240 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL5426979 | — | IC50 | = | 4913.0 | nM | 5.31 |
| CHEMBL5404093 | — | IC50 | = | 6490.0 | nM | 5.19 |
| CHEMBL5420099 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5439224 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5432402 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5426463 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5429150 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5435933 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413380 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5419583 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5401354 | — | IC50 | > | 10000.0 | nM | - |