Assay Detail
Binding
CHEMBL5127379
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-fused human recombinant DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method
58
Total Activities
58
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 1B (CHEMBL5543) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 6.51 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5179655 | — | — | 1 | 7.85 |
| CHEMBL5195216 | — | — | 1 | 7.70 |
| CHEMBL5200518 | — | — | 1 | 7.70 |
| CHEMBL5181008 | — | — | 1 | 7.64 |
| CHEMBL1803085 | — | — | 1 | 7.62 |
| CHEMBL5196066 | — | — | 1 | 7.46 |
| CHEMBL1803084 | — | — | 1 | 7.28 |
| CHEMBL5195122 | — | — | 1 | 7.21 |
| CHEMBL1802358 | — | — | 1 | 7.21 |
| CHEMBL5199422 | — | — | 1 | 7.20 |
| CHEMBL5181355 | — | — | 1 | 7.14 |
| CHEMBL5208980 | — | — | 1 | 7.06 |
| CHEMBL5206143 | — | — | 1 | 7.05 |
| CHEMBL5179457 | — | — | 1 | 7.04 |
| CHEMBL5180765 | — | — | 1 | 7.00 |
| CHEMBL5170033 | — | — | 1 | 6.80 |
| CHEMBL5203292 | — | — | 1 | 6.72 |
| CHEMBL5206744 | — | — | 1 | 6.70 |
| CHEMBL5194689 | — | — | 1 | 6.60 |
| CHEMBL1802355 | — | — | 1 | 6.57 |
| CHEMBL1803079 | — | — | 1 | 6.51 |
| CHEMBL5191942 | — | — | 1 | 6.50 |
| CHEMBL5187753 | — | — | 1 | 6.48 |
| CHEMBL5207974 | — | — | 1 | 6.44 |
| CHEMBL5181028 | — | — | 1 | 6.39 |
| CHEMBL5201763 | — | — | 1 | 6.36 |
| CHEMBL1803082 | — | — | 1 | 6.32 |
| CHEMBL5200677 | — | — | 1 | 6.30 |
| CHEMBL5172170 | — | — | 1 | 6.28 |
| CHEMBL5205157 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5179655 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5195216 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5200518 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5181008 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1803085 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5196066 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1803084 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5195122 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL1802358 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5199422 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5181355 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL5208980 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5206143 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5179457 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL5180765 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5170033 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL5203292 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5206744 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5194689 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1802355 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1803079 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5191942 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5187753 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5207974 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5181028 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5201763 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1803082 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5200677 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5172170 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5205157 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1802843 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5194491 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5169780 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5193677 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5182235 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL5202202 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL5187895 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5173265 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL485053 | LEUCETTAMINE B | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5207630 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5193292 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5205905 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5209464 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5175458 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5179916 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1803069 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5169649 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5172199 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5184273 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5184877 | — | IC50 | > | 10000.0 | nM | - |