Assay Detail
Binding
CHEMBL2188997
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Inhibition of porcine brain GSK-3alpha/beta using YRRAAVPPSPSLSRHSSPHQpSEDEEE as substrate and [gamma-33P]-ATP after 30 mins by scintillation counting
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.54 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180854 | — | — | 1 | 7.66 |
| CHEMBL2180855 | — | — | 1 | 7.58 |
| CHEMBL2180852 | — | — | 1 | 7.37 |
| CHEMBL2180844 | — | — | 1 | 7.29 |
| CHEMBL2180853 | — | — | 1 | 7.12 |
| CHEMBL2180867 | — | — | 1 | 6.92 |
| CHEMBL2180868 | — | — | 1 | 6.89 |
| CHEMBL2180843 | — | — | 1 | 6.85 |
| CHEMBL2180850 | — | — | 1 | 6.82 |
| CHEMBL2180862 | — | — | 1 | 6.77 |
| CHEMBL2180849 | — | — | 1 | 6.77 |
| CHEMBL2180856 | — | — | 1 | 6.70 |
| CHEMBL2180847 | — | — | 1 | 6.57 |
| CHEMBL2180870 | — | — | 1 | 6.51 |
| CHEMBL2180846 | — | — | 1 | 6.48 |
| CHEMBL2180859 | — | — | 1 | 6.44 |
| CHEMBL2180865 | — | — | 1 | 6.42 |
| CHEMBL2180869 | — | — | 1 | 6.33 |
| CHEMBL2180863 | — | — | 1 | 6.29 |
| CHEMBL2180866 | — | — | 1 | 6.12 |
| CHEMBL2180864 | — | — | 1 | 6.12 |
| CHEMBL2180851 | — | — | 1 | 5.92 |
| CHEMBL2180858 | — | — | 1 | 5.89 |
| CHEMBL2180848 | — | — | 1 | 5.46 |
| CHEMBL2180845 | — | — | 1 | 5.40 |
| CHEMBL2180857 | — | — | 1 | 5.37 |
| CHEMBL2180861 | — | — | 1 | - |
| CHEMBL2180860 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180854 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2180855 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2180852 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2180844 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2180853 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2180867 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2180868 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2180843 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2180850 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2180862 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2180849 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2180856 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2180847 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2180870 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2180846 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2180859 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2180865 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2180869 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL2180863 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2180866 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2180864 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL2180851 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2180858 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2180848 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2180845 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2180857 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL2180861 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180860 | — | IC50 | > | 10000.0 | nM | - |