Assay Detail
Binding
CHEMBL4024308
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal GST-tagged CDK4/Cyclin-D3 co-expressed in baculovirus infected sf21 cells using Rb substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method
43
Total Activities
43
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
Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 7.72 | 8.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4104221 | — | — | 1 | 8.32 |
| CHEMBL4072117 | — | — | 1 | 8.20 |
| CHEMBL4075513 | — | — | 1 | 8.14 |
| CHEMBL4095712 | — | — | 1 | 8.09 |
| CHEMBL4091353 | — | — | 1 | 8.09 |
| CHEMBL4083345 | — | — | 1 | 8.08 |
| CHEMBL4063500 | — | — | 1 | 8.06 |
| CHEMBL4094507 | — | — | 1 | 8.02 |
| CHEMBL4091971 | — | — | 1 | 8.00 |
| CHEMBL4092039 | — | — | 1 | 8.00 |
| CHEMBL4087464 | — | — | 1 | 8.00 |
| CHEMBL4069404 | — | — | 1 | 8.00 |
| CHEMBL4079980 | — | — | 1 | 8.00 |
| CHEMBL4090436 | — | — | 1 | 7.96 |
| CHEMBL4073953 | — | — | 1 | 7.96 |
| CHEMBL4068361 | — | — | 1 | 7.96 |
| CHEMBL4071369 | — | — | 1 | 7.92 |
| CHEMBL4068308 | — | — | 1 | 7.92 |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | 7.89 |
| CHEMBL4066630 | — | — | 1 | 7.89 |
| CHEMBL4072827 | — | — | 1 | 7.89 |
| CHEMBL4094446 | — | — | 1 | 7.80 |
| CHEMBL4065039 | — | — | 1 | 7.80 |
| CHEMBL4092722 | — | — | 1 | 7.75 |
| CHEMBL4075445 | — | — | 1 | 7.64 |
| CHEMBL4092163 | — | — | 1 | 7.62 |
| CHEMBL4064231 | — | — | 1 | 7.60 |
| CHEMBL4102249 | — | — | 1 | 7.58 |
| CHEMBL4087863 | — | — | 1 | 7.58 |
| CHEMBL4064314 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4104221 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4072117 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL4075513 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4095712 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL4091353 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4083345 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4063500 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4094507 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4079980 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4069404 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4087464 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4092039 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4091971 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4068361 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4073953 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4090436 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4071369 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4068308 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3545110 | RIBOCICLIB | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4066630 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4072827 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4094446 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4065039 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4092722 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4075445 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4092163 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4064231 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4102249 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4087863 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4064314 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4099786 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4067088 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4102189 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4084219 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4072901 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4095168 | — | IC50 | = | 857.0 | nM | 6.07 |
| CHEMBL4066089 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL4074698 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4066542 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4082598 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4073881 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4061437 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4083275 | — | IC50 | > | 5000.0 | nM | - |