Assay Detail
ADMET
CHEMBL4014112
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Inhibition of recombinant human DYRK1A expressed in insect cells using RRRFRPASPLRGPPK peptide as substrate after 40 mins in presence of [gamma-33P]-ATP by scintillation counting
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.30 | 7.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL408982 | — | — | 1 | 7.15 |
| CHEMBL4096379 | — | — | 1 | 6.97 |
| CHEMBL4083249 | — | — | 1 | 6.86 |
| CHEMBL4104765 | — | — | 1 | 6.85 |
| CHEMBL4094600 | — | — | 1 | 6.75 |
| CHEMBL4088668 | — | — | 1 | 6.71 |
| CHEMBL4067143 | — | — | 1 | 6.61 |
| CHEMBL4072795 | — | — | 1 | 6.59 |
| CHEMBL4104122 | — | — | 1 | 6.55 |
| CHEMBL4069124 | — | — | 1 | 6.39 |
| CHEMBL4079878 | — | — | 1 | 6.38 |
| CHEMBL4081470 | — | — | 1 | 5.94 |
| CHEMBL4093503 | — | — | 1 | 5.88 |
| CHEMBL4060440 | — | — | 1 | 5.88 |
| CHEMBL4086890 | — | — | 1 | 5.87 |
| CHEMBL4064426 | — | — | 1 | 5.75 |
| CHEMBL4092984 | — | — | 1 | 5.54 |
| CHEMBL4082710 | — | — | 1 | 5.47 |
| CHEMBL4063617 | — | — | 1 | 5.47 |
| CHEMBL4059498 | — | — | 1 | - |
| CHEMBL4078073 | — | — | 1 | - |
| CHEMBL4102344 | — | — | 1 | - |
| CHEMBL4072220 | — | — | 1 | - |
| CHEMBL4100703 | — | — | 1 | - |
| CHEMBL4074986 | — | — | 1 | - |
| CHEMBL4101671 | — | — | 1 | - |
| CHEMBL4085242 | — | — | 1 | - |
| CHEMBL4104093 | — | — | 1 | - |
| CHEMBL4086182 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL408982 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4096379 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4083249 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4104765 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4094600 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4088668 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL4067143 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL4072795 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL4104122 | — | IC50 | = | 283.0 | nM | 6.55 |
| CHEMBL4069124 | — | IC50 | = | 404.0 | nM | 6.39 |
| CHEMBL4079878 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4081470 | — | IC50 | = | 1139.0 | nM | 5.94 |
| CHEMBL4093503 | — | IC50 | = | 1318.0 | nM | 5.88 |
| CHEMBL4060440 | — | IC50 | = | 1303.0 | nM | 5.88 |
| CHEMBL4086890 | — | IC50 | = | 1337.0 | nM | 5.87 |
| CHEMBL4064426 | — | IC50 | = | 1756.0 | nM | 5.75 |
| CHEMBL4092984 | — | IC50 | = | 2872.0 | nM | 5.54 |
| CHEMBL4082710 | — | IC50 | = | 3360.0 | nM | 5.47 |
| CHEMBL4063617 | — | IC50 | = | 3356.0 | nM | 5.47 |
| CHEMBL4059498 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4078073 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4102344 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4072220 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4100703 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4074986 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4101671 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4085242 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4104093 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4086182 | — | IC50 | > | 10000.0 | nM | - |