Assay Detail
Binding
CHEMBL4034242
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length recombinant human His-tagged GSK3B recombinant in baculovirus expression system using Alexa-Fluor tracer-236 incubated for 60 mins by TR-FRET based Lantha-screen Eu kinase assay
33
Total Activities
33
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 |
Publication
Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 5.14 | 6.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4064316 | — | — | 1 | 6.18 |
| CHEMBL4069163 | — | — | 1 | 6.00 |
| CHEMBL4105629 | — | — | 1 | 5.94 |
| CHEMBL4091320 | — | — | 1 | 5.52 |
| CHEMBL4077010 | — | — | 1 | 5.32 |
| CHEMBL4072138 | — | — | 1 | 5.29 |
| CHEMBL4095674 | — | — | 1 | 5.12 |
| CHEMBL4095479 | — | — | 1 | 5.10 |
| CHEMBL4084955 | — | — | 1 | 5.04 |
| CHEMBL4075648 | — | — | 1 | 5.02 |
| CHEMBL1802401 | — | — | 1 | 5.00 |
| CHEMBL4065388 | — | — | 1 | 4.97 |
| CHEMBL4079572 | — | — | 1 | 4.91 |
| CHEMBL4098364 | — | — | 1 | 4.90 |
| CHEMBL4066075 | — | — | 1 | 4.86 |
| CHEMBL48082 | — | — | 1 | 4.83 |
| CHEMBL4087456 | — | — | 1 | 4.82 |
| CHEMBL4090889 | — | — | 1 | 4.80 |
| CHEMBL1802963 | — | — | 1 | 4.65 |
| CHEMBL4102903 | — | — | 1 | 4.51 |
| CHEMBL4095156 | — | — | 1 | - |
| CHEMBL269538 | HARMINE | 1.0 | 1 | - |
| CHEMBL4086818 | — | — | 1 | - |
| CHEMBL4073997 | — | — | 1 | - |
| CHEMBL4098505 | — | — | 1 | - |
| CHEMBL4080488 | — | — | 1 | - |
| CHEMBL4103831 | — | — | 1 | - |
| CHEMBL4068096 | — | — | 1 | - |
| CHEMBL4094549 | — | — | 1 | - |
| CHEMBL3421979 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4064316 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4069163 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4105629 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL4091320 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4077010 | — | IC50 | = | 4780.0 | nM | 5.32 |
| CHEMBL4072138 | — | IC50 | = | 5160.0 | nM | 5.29 |
| CHEMBL4095674 | — | IC50 | = | 7580.0 | nM | 5.12 |
| CHEMBL4095479 | — | IC50 | = | 7960.0 | nM | 5.10 |
| CHEMBL4084955 | — | IC50 | = | 9230.0 | nM | 5.04 |
| CHEMBL4075648 | — | IC50 | = | 9610.0 | nM | 5.02 |
| CHEMBL1802401 | — | IC50 | = | 9950.0 | nM | 5.00 |
| CHEMBL4065388 | — | IC50 | = | 10690.0 | nM | 4.97 |
| CHEMBL4079572 | — | IC50 | = | 12300.0 | nM | 4.91 |
| CHEMBL4098364 | — | IC50 | = | 12700.0 | nM | 4.90 |
| CHEMBL4066075 | — | IC50 | = | 13860.0 | nM | 4.86 |
| CHEMBL48082 | — | IC50 | = | 14810.0 | nM | 4.83 |
| CHEMBL4087456 | — | IC50 | = | 15290.0 | nM | 4.82 |
| CHEMBL4090889 | — | IC50 | = | 15840.0 | nM | 4.80 |
| CHEMBL1802963 | — | IC50 | = | 22450.0 | nM | 4.65 |
| CHEMBL4102903 | — | IC50 | = | 31010.0 | nM | 4.51 |
| CHEMBL4095156 | — | IC50 | - | — | - | |
| CHEMBL269538 | HARMINE | IC50 | - | — | - | |
| CHEMBL4086818 | — | IC50 | - | — | - | |
| CHEMBL4073997 | — | IC50 | - | — | - | |
| CHEMBL4098505 | — | IC50 | - | — | - | |
| CHEMBL4080488 | — | IC50 | - | — | - | |
| CHEMBL4103831 | — | IC50 | - | — | - | |
| CHEMBL4068096 | — | IC50 | - | — | - | |
| CHEMBL4094549 | — | IC50 | - | — | - | |
| CHEMBL3421979 | — | IC50 | - | — | - | |
| CHEMBL4074685 | — | IC50 | - | — | - | |
| CHEMBL4069088 | — | IC50 | - | — | - | |
| CHEMBL4066607 | — | IC50 | - | — | - |