Assay Detail
Binding
CHEMBL1102102
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Inhibition of GSK3-beta assessed as NADH level after 10 mins by pyruvate kinase/lactate dehydrogenase coupled spectrophotometric assay
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 64 | 7.72 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088011 | — | — | 1 | 9.40 |
| CHEMBL1088145 | — | — | 1 | 9.40 |
| CHEMBL1080902 | — | — | 1 | 9.10 |
| CHEMBL1076701 | — | — | 1 | 8.72 |
| CHEMBL1086602 | — | — | 1 | 8.70 |
| CHEMBL1076721 | — | — | 1 | 8.70 |
| CHEMBL1080849 | — | — | 1 | 8.70 |
| CHEMBL1079966 | — | — | 1 | 8.70 |
| CHEMBL1081633 | — | — | 1 | 8.70 |
| CHEMBL1088021 | — | — | 1 | 8.52 |
| CHEMBL1086735 | — | — | 1 | 8.52 |
| CHEMBL1076755 | — | — | 1 | 8.43 |
| CHEMBL1082009 | — | — | 1 | 8.40 |
| CHEMBL1086736 | — | — | 1 | 8.35 |
| CHEMBL1081833 | — | — | 1 | 8.30 |
| CHEMBL1082188 | — | — | 1 | 8.19 |
| CHEMBL1081446 | — | — | 1 | 8.11 |
| CHEMBL1082010 | — | — | 1 | 8.10 |
| CHEMBL1079968 | — | — | 1 | 8.10 |
| CHEMBL1088725 | — | — | 1 | 8.10 |
| CHEMBL1081102 | — | — | 1 | 8.08 |
| CHEMBL1080847 | — | — | 1 | 8.05 |
| CHEMBL1082157 | — | — | 1 | 8.05 |
| CHEMBL1076695 | — | — | 1 | 8.05 |
| CHEMBL1081069 | — | — | 1 | 7.85 |
| CHEMBL1081071 | — | — | 1 | 7.80 |
| CHEMBL1076552 | — | — | 1 | 7.80 |
| CHEMBL1081632 | — | — | 1 | 7.75 |
| CHEMBL1076682 | — | — | 1 | 7.70 |
| CHEMBL1081630 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088011 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1088145 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL1080902 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1076701 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1086602 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1076721 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1080849 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1079966 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1081633 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1088021 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1086735 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1076755 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL1082009 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL1086736 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL1081833 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1082188 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL1081446 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL1082010 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1079968 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1088725 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1081102 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL1080847 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1082157 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1076695 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1081069 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1081071 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1076552 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1081632 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1076682 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1081630 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL388978 | STAUROSPORINE | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1082176 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1081432 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1081103 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL322970 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1082011 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1081631 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL1081278 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1079967 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL1081429 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1081447 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL1080848 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1086601 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL1081430 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL1081070 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1081431 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1080376 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL1080377 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL1088154 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL1076619 | — | Ki | = | 460.0 | nM | 6.34 |