Assay Detail
Binding
CHEMBL4604968
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His/GST-tagged GSK3beta (2 to 433 residues) expressed in baculovirus infected Sf9 cells using Ulight-glycogen synthase peptide as substrate incubated for 30 mins by TR-FRET LANCE method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.06 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4648047 | — | — | 1 | 6.20 |
| CHEMBL4640465 | — | — | 1 | 5.71 |
| CHEMBL4641631 | — | — | 1 | 5.25 |
| CHEMBL4091320 | — | — | 1 | 4.53 |
| CHEMBL4640598 | — | — | 1 | 4.35 |
| CHEMBL4641672 | — | — | 1 | 4.33 |
| CHEMBL4634969 | — | — | 1 | - |
| CHEMBL4648945 | — | — | 1 | - |
| CHEMBL4644898 | — | — | 1 | - |
| CHEMBL4638460 | — | — | 1 | - |
| CHEMBL4648742 | — | — | 1 | - |
| CHEMBL4645474 | — | — | 1 | - |
| CHEMBL4649473 | — | — | 1 | - |
| CHEMBL4641839 | — | — | 1 | - |
| CHEMBL4640031 | — | — | 1 | - |
| CHEMBL4636064 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4648047 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4640465 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4641631 | — | IC50 | = | 5640.0 | nM | 5.25 |
| CHEMBL4091320 | — | IC50 | = | 29600.0 | nM | 4.53 |
| CHEMBL4640598 | — | IC50 | = | 44480.0 | nM | 4.35 |
| CHEMBL4641672 | — | IC50 | = | 46500.0 | nM | 4.33 |
| CHEMBL4634969 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL4648945 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL4644898 | — | IC50 | > | 28500.0 | nM | - |
| CHEMBL4638460 | — | IC50 | > | 12400.0 | nM | - |
| CHEMBL4648742 | — | IC50 | > | 8300.0 | nM | - |
| CHEMBL4645474 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4649473 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4641839 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4640031 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4636064 | — | IC50 | > | 50000.0 | nM | - |