Assay Detail
Binding
CHEMBL4309972
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 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 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.99 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261720 | — | — | 1 | 9.70 |
| CHEMBL1276446 | — | — | 1 | 8.52 |
| CHEMBL300389 | — | — | 1 | 8.40 |
| CHEMBL259389 | QUINOXALINE1 | — | 1 | 8.00 |
| CHEMBL319467 | — | — | 1 | 7.85 |
| CHEMBL258805 | SU-9516 | 1.0 | 1 | 7.57 |
| CHEMBL411491 | — | — | 1 | 7.39 |
| CHEMBL367625 | — | — | 1 | 7.34 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.34 |
| CHEMBL3115681 | NARAZACICLIB | 2.0 | 1 | 7.26 |
| CHEMBL409450 | 6BIO | — | 1 | 7.16 |
| CHEMBL310840 | — | — | 1 | 7.15 |
| CHEMBL477064 | — | — | 1 | 7.15 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.96 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | — | 1 | 6.87 |
| CHEMBL64758 | — | — | 1 | 6.73 |
| CHEMBL80713 | — | — | 1 | 6.66 |
| CHEMBL393929 | — | — | 1 | 6.60 |
| CHEMBL215919 | — | — | 1 | 6.54 |
| CHEMBL426972 | — | — | 1 | 6.45 |
| CHEMBL265964 | — | — | 1 | 6.02 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.75 |
| CHEMBL298445 | — | — | 1 | 5.36 |
| CHEMBL132904 | — | — | 1 | 5.15 |
| CHEMBL261425 | — | — | 1 | 4.88 |
| CHEMBL290904 | — | — | 1 | - |
| CHEMBL2028998 | — | — | 1 | - |
| CHEMBL1331734 | — | — | 1 | - |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | - |
| CHEMBL133712 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261720 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1276446 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL300389 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL259389 | QUINOXALINE1 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL319467 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL258805 | SU-9516 | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL411491 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL367625 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3115681 | NARAZACICLIB | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL409450 | 6BIO | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL310840 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL477064 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL564829 | MILCICLIB | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL64758 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL80713 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL393929 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL215919 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL426972 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL265964 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL298445 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL132904 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL261425 | — | IC50 | = | 13200.0 | nM | 4.88 |
| CHEMBL290904 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2028998 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1331734 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | IC50 | > | 20000.0 | nM | - |
| CHEMBL133712 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL1802728 | — | IC50 | = | 407000.0 | nM | - |