Assay Detail
Binding
CHEMBL3396022
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Inhibition of human recombinant CDK2/Cyclin A using fluoresceinyl-Ahx-Pro-Val-Lys-Arg-Arg-Leu-(3ClPhe)-Gly as substrate after 45 mins by fluorescence polarization assay
32
Total Activities
32
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
Iterative conversion of cyclin binding groove peptides into druglike CDK inhibitors with antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 5.77 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3393763 | — | — | 1 | 8.00 |
| CHEMBL3393766 | — | — | 1 | 7.70 |
| CHEMBL3393765 | — | — | 1 | 7.70 |
| CHEMBL3393762 | — | — | 1 | 7.70 |
| CHEMBL3393760 | — | — | 1 | 7.30 |
| CHEMBL3393759 | — | — | 1 | 7.16 |
| CHEMBL3393761 | — | — | 1 | 6.75 |
| CHEMBL3393764 | — | — | 1 | 6.62 |
| CHEMBL3393779 | — | — | 1 | 6.16 |
| CHEMBL3098653 | — | — | 1 | 6.00 |
| CHEMBL3393780 | — | — | 1 | 5.87 |
| CHEMBL3393770 | — | — | 1 | 5.77 |
| CHEMBL3393778 | — | — | 1 | 5.76 |
| CHEMBL3393777 | — | — | 1 | 5.55 |
| CHEMBL3393786 | — | — | 1 | 5.43 |
| CHEMBL3393788 | — | — | 1 | 5.35 |
| CHEMBL3393768 | — | — | 1 | 5.29 |
| CHEMBL3393781 | — | — | 1 | 5.24 |
| CHEMBL3393784 | — | — | 1 | 5.24 |
| CHEMBL3393783 | — | — | 1 | 5.05 |
| CHEMBL3393787 | — | — | 1 | 4.79 |
| CHEMBL206763 | — | — | 1 | 4.72 |
| CHEMBL3393769 | — | — | 1 | 4.69 |
| CHEMBL3393773 | — | — | 1 | 4.69 |
| CHEMBL3393776 | — | — | 1 | 4.45 |
| CHEMBL3393767 | — | — | 1 | 4.37 |
| CHEMBL3393785 | — | — | 1 | 4.33 |
| CHEMBL3393782 | — | — | 1 | 4.00 |
| CHEMBL3393771 | — | — | 1 | - |
| CHEMBL3393772 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3393763 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3393766 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3393762 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3393765 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3393760 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3393759 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3393761 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3393764 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3393779 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3098653 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL3393780 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL3393770 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3393778 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL3393777 | — | IC50 | = | 2810.0 | nM | 5.55 |
| CHEMBL3393786 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL3393788 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3393768 | — | IC50 | = | 5190.0 | nM | 5.29 |
| CHEMBL3393781 | — | IC50 | = | 5820.0 | nM | 5.24 |
| CHEMBL3393784 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL3393783 | — | IC50 | = | 8950.0 | nM | 5.05 |
| CHEMBL3393787 | — | IC50 | = | 16390.0 | nM | 4.79 |
| CHEMBL206763 | — | IC50 | = | 18880.0 | nM | 4.72 |
| CHEMBL3393769 | — | IC50 | = | 20620.0 | nM | 4.69 |
| CHEMBL3393773 | — | IC50 | = | 20360.0 | nM | 4.69 |
| CHEMBL3393776 | — | IC50 | = | 35650.0 | nM | 4.45 |
| CHEMBL3393767 | — | IC50 | = | 43170.0 | nM | 4.37 |
| CHEMBL3393785 | — | IC50 | = | 46750.0 | nM | 4.33 |
| CHEMBL3393782 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL3393771 | — | IC50 | > | 180000.0 | nM | - |
| CHEMBL3393772 | — | IC50 | > | 180000.0 | nM | - |
| CHEMBL3393774 | — | IC50 | > | 180000.0 | nM | - |
| CHEMBL3393775 | — | IC50 | > | 180000.0 | nM | - |