Assay Detail
Binding
CHEMBL1034478
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Inhibition of human GSK3-beta
33
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.09 | 9.85 |
| Ki | 1 | 10.05 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL461262 | — | — | 1 | 10.05 |
| CHEMBL564450 | — | — | 1 | 9.85 |
| CHEMBL362558 | LY-2090314 | 2.0 | 1 | 8.96 |
| CHEMBL362814 | — | — | 1 | 8.80 |
| CHEMBL549953 | — | — | 1 | 8.70 |
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | — | 2 | 8.55 |
| CHEMBL182419 | — | — | 1 | 8.30 |
| CHEMBL105477 | — | — | 1 | 8.22 |
| CHEMBL562023 | — | — | 1 | 8.15 |
| CHEMBL337300 | — | — | 1 | 8.05 |
| CHEMBL361708 | HYMENIALDISINE | — | 1 | 8.00 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.82 |
| CHEMBL126077 | INDIRUBIN-3-MONOXIME | — | 1 | 7.66 |
| CHEMBL559559 | — | — | 1 | 7.52 |
| CHEMBL102714 | SB-216763 | — | 1 | 7.47 |
| CHEMBL549804 | — | — | 1 | 7.44 |
| CHEMBL540245 | — | — | 1 | 7.41 |
| CHEMBL562089 | — | — | 1 | 7.40 |
| CHEMBL557354 | — | — | 1 | 7.19 |
| CHEMBL322970 | — | — | 1 | 7.11 |
| CHEMBL564006 | — | — | 1 | 7.10 |
| CHEMBL259850 | — | — | 1 | 7.00 |
| CHEMBL325353 | — | — | 1 | 7.00 |
| CHEMBL557273 | — | — | 1 | 6.80 |
| CHEMBL44541 | MERIDIANIN C | — | 1 | 5.70 |
| CHEMBL554082 | — | — | 1 | 5.62 |
| CHEMBL554295 | — | — | 1 | 5.52 |
| CHEMBL550950 | — | — | 1 | 5.22 |
| CHEMBL178179 | — | — | 1 | 4.66 |
| CHEMBL77002 | — | — | 1 | 4.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL461262 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL564450 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL362558 | LY-2090314 | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL362814 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL549953 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL6291 | BISINDOLYLMALEIMIDE IX | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL182419 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL105477 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL562023 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL337300 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL361708 | HYMENIALDISINE | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL126077 | INDIRUBIN-3-MONOXIME | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL559559 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL102714 | SB-216763 | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL549804 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL540245 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL562089 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL557354 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL322970 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL564006 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL259850 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL325353 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL557273 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL44541 | MERIDIANIN C | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL554082 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL554295 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL550950 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL178179 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL77002 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL48082 | — | IC50 | = | 350000.0 | nM | 3.46 |
| CHEMBL50226 | — | IC50 | = | 420000.0 | nM | 3.38 |