Assay Detail
Binding
CHEMBL2188998
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CDK5/p25 using histone H1 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 | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 6.31 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2180854 | — | — | 1 | 7.60 |
| CHEMBL2180844 | — | — | 1 | 7.43 |
| CHEMBL2180852 | — | — | 1 | 7.40 |
| CHEMBL2180849 | — | — | 1 | 7.17 |
| CHEMBL2180863 | — | — | 1 | 7.16 |
| CHEMBL2180862 | — | — | 1 | 7.10 |
| CHEMBL2180855 | — | — | 1 | 7.05 |
| CHEMBL2180853 | — | — | 1 | 6.89 |
| CHEMBL2180869 | — | — | 1 | 6.77 |
| CHEMBL2180856 | — | — | 1 | 6.58 |
| CHEMBL2180866 | — | — | 1 | 6.37 |
| CHEMBL2180870 | — | — | 1 | 6.29 |
| CHEMBL2180867 | — | — | 1 | 6.28 |
| CHEMBL2180858 | — | — | 1 | 6.23 |
| CHEMBL2180850 | — | — | 1 | 6.16 |
| CHEMBL2180845 | — | — | 1 | 5.89 |
| CHEMBL2180847 | — | — | 1 | 5.82 |
| CHEMBL2180865 | — | — | 1 | 5.82 |
| CHEMBL2180868 | — | — | 1 | 5.77 |
| CHEMBL2180846 | — | — | 1 | 5.57 |
| CHEMBL2180843 | — | — | 1 | 5.40 |
| CHEMBL2180857 | — | — | 1 | 5.00 |
| CHEMBL2180851 | — | — | 1 | 5.00 |
| CHEMBL2180848 | — | — | 1 | 4.80 |
| CHEMBL2180864 | — | — | 1 | - |
| CHEMBL2180859 | — | — | 1 | - |
| CHEMBL2180861 | — | — | 1 | - |
| CHEMBL2180860 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2180854 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2180844 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL2180852 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2180849 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2180863 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2180862 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2180855 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2180853 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2180869 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2180856 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL2180866 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2180870 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2180867 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL2180858 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL2180850 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2180845 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL2180847 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2180865 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2180868 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2180846 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL2180843 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2180857 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2180851 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2180848 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2180864 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180859 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180861 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2180860 | — | IC50 | > | 10000.0 | nM | - |