Assay Detail
Binding
CHEMBL4309973
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.53 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261720 | — | — | 1 | 9.70 |
| CHEMBL1276446 | — | — | 1 | 8.15 |
| CHEMBL300389 | — | — | 1 | 8.00 |
| CHEMBL258805 | SU-9516 | 1.0 | 1 | 7.66 |
| CHEMBL367625 | — | — | 1 | 7.58 |
| CHEMBL409450 | 6BIO | — | 1 | 7.39 |
| CHEMBL319467 | — | — | 1 | 6.93 |
| CHEMBL64758 | — | — | 1 | 6.81 |
| CHEMBL298445 | — | — | 1 | 6.73 |
| CHEMBL215919 | — | — | 1 | 6.67 |
| CHEMBL310840 | — | — | 1 | 6.59 |
| CHEMBL3115681 | NARAZACICLIB | 2.0 | 1 | 6.57 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.42 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.39 |
| CHEMBL80713 | — | — | 1 | 6.38 |
| CHEMBL426972 | — | — | 1 | 6.34 |
| CHEMBL411491 | — | — | 1 | 6.13 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | — | 1 | 6.03 |
| CHEMBL477064 | — | — | 1 | 5.92 |
| CHEMBL393929 | — | — | 1 | 5.61 |
| CHEMBL265964 | — | — | 1 | 5.36 |
| CHEMBL261425 | — | — | 1 | 5.24 |
| CHEMBL1802728 | — | — | 1 | 5.06 |
| CHEMBL259389 | QUINOXALINE1 | — | 1 | 4.86 |
| CHEMBL133712 | — | — | 1 | 4.76 |
| CHEMBL2028998 | — | — | 1 | - |
| CHEMBL290904 | — | — | 1 | - |
| CHEMBL1331734 | — | — | 1 | - |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | - |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261720 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1276446 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL300389 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL258805 | SU-9516 | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL367625 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL409450 | 6BIO | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL319467 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL64758 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL298445 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL215919 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL310840 | — | IC50 | = | 258.0 | nM | 6.59 |
| CHEMBL3115681 | NARAZACICLIB | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL564829 | MILCICLIB | IC50 | = | 383.0 | nM | 6.42 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL80713 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL426972 | — | IC50 | = | 458.0 | nM | 6.34 |
| CHEMBL411491 | — | IC50 | = | 738.0 | nM | 6.13 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 936.0 | nM | 6.03 |
| CHEMBL477064 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL393929 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL265964 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL261425 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1802728 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL259389 | QUINOXALINE1 | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL133712 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL2028998 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL290904 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL1331734 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | IC50 | > | 20000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | IC50 | > | 10000.0 | nM | - |
| CHEMBL132904 | — | IC50 | > | 20000.0 | nM | - |