Assay Detail
Binding
CHEMBL1102983
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Inhibition of human recombinant GSK3-beta assessed as [gamma33]ATP transfer to biotinylated CREB-peptide substrate after 1 hr by scintillation counting
32
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of potent and bioavailable GSK-3beta inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 7.55 | 9.40 |
| Kd | 1 | 10.28 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082152 | — | — | 2 | 10.28 |
| CHEMBL1082153 | — | — | 1 | 9.40 |
| CHEMBL1080901 | — | — | 1 | 9.25 |
| CHEMBL1082151 | — | — | 1 | 9.00 |
| CHEMBL54547 | — | — | 1 | 8.74 |
| CHEMBL1081973 | — | — | 1 | 8.74 |
| CHEMBL1088149 | — | — | 1 | 8.62 |
| CHEMBL1081294 | — | — | 1 | 8.49 |
| CHEMBL431933 | — | — | 1 | 8.44 |
| CHEMBL1081617 | — | — | 1 | 8.19 |
| CHEMBL1087242 | — | — | 1 | 8.18 |
| CHEMBL1087499 | — | — | 1 | 8.15 |
| CHEMBL1081972 | — | — | 1 | 8.09 |
| CHEMBL1088724 | — | — | 1 | 8.00 |
| CHEMBL26501 | RO-320432 | — | 1 | 7.70 |
| CHEMBL1087243 | — | — | 1 | 7.66 |
| CHEMBL53745 | — | — | 1 | 7.66 |
| CHEMBL1081616 | — | — | 1 | 7.51 |
| CHEMBL1081128 | — | — | 1 | 7.46 |
| CHEMBL1087380 | — | — | 1 | 7.38 |
| CHEMBL322970 | — | — | 1 | 7.11 |
| CHEMBL293542 | — | — | 1 | 7.05 |
| CHEMBL430574 | PAULLONE | — | 1 | 7.00 |
| CHEMBL1080933 | — | — | 1 | 6.66 |
| CHEMBL1086734 | — | — | 1 | 6.46 |
| CHEMBL1086732 | — | — | 1 | 6.14 |
| CHEMBL1081293 | — | — | 1 | 5.89 |
| CHEMBL1086733 | — | — | 1 | 5.70 |
| CHEMBL1081260 | — | — | 1 | 5.55 |
| CHEMBL1081261 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082152 | — | Kd | = | 0.053 | nM | 10.28 |
| CHEMBL1082153 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1080901 | — | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL1082152 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL1082151 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL54547 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1081973 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1088149 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1081294 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL431933 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1081617 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL1087242 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL1087499 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1081972 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL1088724 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL26501 | RO-320432 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL53745 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1087243 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1081616 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1081128 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1087380 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL322970 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL293542 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL430574 | PAULLONE | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1080933 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL1086734 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1086732 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1081293 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1086733 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1081260 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1081261 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL1080932 | — | IC50 | = | 8200.0 | nM | 5.09 |