Assay Detail
Binding
CHEMBL5252012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal 6-His tagged human recombinant GSK3-beta H355L mutant using FL-KRREILSRRP[ps]ERYR-NH2 as substrate incubated for 20 hrs
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2-<i>b</i>]pyridazines as Glycogen Synthase Kinase-3β (GSK-3β) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 8.63 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5266553 | — | — | 1 | 9.89 |
| CHEMBL5286391 | — | — | 1 | 9.54 |
| CHEMBL5288788 | — | — | 1 | 9.49 |
| CHEMBL5270555 | — | — | 1 | 9.43 |
| CHEMBL5282319 | — | — | 1 | 9.38 |
| CHEMBL5282376 | — | — | 1 | 9.37 |
| CHEMBL5273327 | — | — | 1 | 9.24 |
| CHEMBL5290040 | — | — | 1 | 9.15 |
| CHEMBL5270781 | — | — | 1 | 9.14 |
| CHEMBL5283650 | — | — | 1 | 9.11 |
| CHEMBL5316226 | — | — | 1 | 9.09 |
| CHEMBL5285422 | — | — | 1 | 9.06 |
| CHEMBL5282654 | — | — | 1 | 8.96 |
| CHEMBL5286737 | — | — | 1 | 8.85 |
| CHEMBL5285386 | — | — | 1 | 8.82 |
| CHEMBL5284042 | — | — | 1 | 8.80 |
| CHEMBL5274844 | — | — | 1 | 8.72 |
| CHEMBL5274596 | — | — | 1 | 8.59 |
| CHEMBL5276944 | — | — | 1 | 8.47 |
| CHEMBL5286819 | — | — | 1 | 8.46 |
| CHEMBL5272860 | — | — | 1 | 8.46 |
| CHEMBL5286669 | — | — | 1 | 8.44 |
| CHEMBL5277960 | — | — | 1 | 8.34 |
| CHEMBL5279845 | — | — | 1 | 8.28 |
| CHEMBL5286503 | — | — | 1 | 8.17 |
| CHEMBL5271404 | — | — | 1 | 8.15 |
| CHEMBL5271582 | — | — | 1 | 8.05 |
| CHEMBL5278224 | — | — | 1 | 7.85 |
| CHEMBL5269379 | — | — | 1 | 7.70 |
| CHEMBL5278638 | — | — | 1 | 7.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5266553 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5286391 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5288788 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL5270555 | — | IC50 | = | 0.37 | nM | 9.43 |
| CHEMBL5282319 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5282376 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL5273327 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL5290040 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5270781 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL5283650 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL5316226 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL5285422 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL5282654 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5286737 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5285386 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5284042 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5274844 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5274596 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5276944 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5286819 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5272860 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL5286669 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5277960 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL5279845 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5286503 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5271404 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5271582 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5278224 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5269379 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5278638 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5284564 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5266078 | — | IC50 | = | 220.0 | nM | 6.66 |