Assay Detail
Binding
CHEMBL4275366
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Inhibition of CDK6/Cyclin D3 (unknown origin) using FAM-labeled peptide as substrate after 40 mins
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.48 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL560817 | — | — | 1 | 8.00 |
| CHEMBL4290012 | — | — | 1 | 8.00 |
| CHEMBL4288758 | — | — | 1 | 7.70 |
| CHEMBL4286430 | — | — | 1 | 7.58 |
| CHEMBL4289852 | — | — | 1 | 7.44 |
| CHEMBL4278514 | — | — | 1 | 7.40 |
| CHEMBL4281557 | — | — | 1 | 7.35 |
| CHEMBL559845 | — | — | 1 | 7.24 |
| CHEMBL4287981 | — | — | 1 | 6.50 |
| CHEMBL556881 | — | — | 1 | 6.46 |
| CHEMBL4292180 | — | — | 1 | 6.33 |
| CHEMBL4281978 | — | — | 1 | 6.26 |
| CHEMBL562104 | — | — | 1 | 5.99 |
| CHEMBL4294798 | — | — | 1 | 5.63 |
| CHEMBL560818 | — | — | 1 | 5.60 |
| CHEMBL4287560 | — | — | 1 | 5.56 |
| CHEMBL4277343 | — | — | 1 | 5.24 |
| CHEMBL1098059 | — | — | 1 | 5.13 |
| CHEMBL4279646 | — | — | 1 | 5.11 |
| CHEMBL4283123 | — | — | 1 | 5.07 |
| CHEMBL4293299 | — | — | 1 | - |
| CHEMBL4294376 | — | — | 1 | - |
| CHEMBL4293228 | — | — | 1 | - |
| CHEMBL4286071 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL560817 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4290012 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4288758 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4286430 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4289852 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4278514 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4281557 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL559845 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4287981 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL556881 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4292180 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4281978 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL562104 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4294798 | — | IC50 | = | 2320.0 | nM | 5.63 |
| CHEMBL560818 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL4287560 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL4277343 | — | IC50 | = | 5790.0 | nM | 5.24 |
| CHEMBL1098059 | — | IC50 | = | 7360.0 | nM | 5.13 |
| CHEMBL4279646 | — | IC50 | = | 7760.0 | nM | 5.11 |
| CHEMBL4283123 | — | IC50 | = | 8560.0 | nM | 5.07 |
| CHEMBL4293299 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4294376 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4293228 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4286071 | — | IC50 | > | 10000.0 | nM | - |