Assay Detail
Binding
CHEMBL3396023
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant CDK4/Cyclin D1 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 |
Target
Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 5.30 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3393763 | — | — | 1 | 7.40 |
| CHEMBL3393766 | — | — | 1 | 6.92 |
| CHEMBL3393765 | — | — | 1 | 6.75 |
| CHEMBL3393762 | — | — | 1 | 6.54 |
| CHEMBL3393760 | — | — | 1 | 6.18 |
| CHEMBL3393759 | — | — | 1 | 6.06 |
| CHEMBL3393761 | — | — | 1 | 5.78 |
| CHEMBL3393764 | — | — | 1 | 5.51 |
| CHEMBL3393770 | — | — | 1 | 5.04 |
| CHEMBL3393779 | — | — | 1 | 5.03 |
| CHEMBL3393768 | — | — | 1 | 4.80 |
| CHEMBL3393778 | — | — | 1 | 4.69 |
| CHEMBL3393777 | — | — | 1 | 4.67 |
| CHEMBL3098653 | — | — | 1 | 4.60 |
| CHEMBL3393773 | — | — | 1 | 4.54 |
| CHEMBL3393769 | — | — | 1 | 4.47 |
| CHEMBL3393767 | — | — | 1 | 4.39 |
| CHEMBL3393780 | — | — | 1 | 4.34 |
| CHEMBL3393783 | — | — | 1 | 4.11 |
| CHEMBL3393781 | — | — | 1 | 4.09 |
| CHEMBL3393776 | — | — | 1 | - |
| CHEMBL3393787 | — | — | 1 | - |
| CHEMBL3393786 | — | — | 1 | - |
| CHEMBL3393785 | — | — | 1 | - |
| CHEMBL3393784 | — | — | 1 | - |
| CHEMBL3393782 | — | — | 1 | - |
| CHEMBL3393774 | — | — | 1 | - |
| CHEMBL206763 | — | — | 1 | - |
| CHEMBL3393775 | — | — | 1 | - |
| CHEMBL3393771 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3393763 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3393766 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3393765 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3393762 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3393760 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3393759 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL3393761 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL3393764 | — | IC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL3393770 | — | IC50 | = | 9190.0 | nM | 5.04 |
| CHEMBL3393779 | — | IC50 | = | 9260.0 | nM | 5.03 |
| CHEMBL3393768 | — | IC50 | = | 15760.0 | nM | 4.80 |
| CHEMBL3393778 | — | IC50 | = | 20240.0 | nM | 4.69 |
| CHEMBL3393777 | — | IC50 | = | 21170.0 | nM | 4.67 |
| CHEMBL3098653 | — | IC50 | = | 25120.0 | nM | 4.60 |
| CHEMBL3393773 | — | IC50 | = | 28760.0 | nM | 4.54 |
| CHEMBL3393769 | — | IC50 | = | 33760.0 | nM | 4.47 |
| CHEMBL3393767 | — | IC50 | = | 40460.0 | nM | 4.39 |
| CHEMBL3393780 | — | IC50 | = | 45580.0 | nM | 4.34 |
| CHEMBL3393783 | — | IC50 | = | 78250.0 | nM | 4.11 |
| CHEMBL3393781 | — | IC50 | = | 81130.0 | nM | 4.09 |
| CHEMBL3393776 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393787 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393786 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393785 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393784 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393782 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393774 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL206763 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393775 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393771 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393772 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3393788 | — | IC50 | > | 100000.0 | nM | - |