Assay Detail
Binding
CHEMBL4151776
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His6-tagged human full length CDK2/N-terminal GST-tagged human full length Cyclin A using histone H1 and [gamma-32P]-ATP incubated for 30 mins by phosphorimage based assay
19
Total Activities
19
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
Development of Second-Generation CDK2 Inhibitors for the Prevention of Cisplatin-Induced Hearing Loss.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.21 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL518383 | — | — | 1 | 8.52 |
| CHEMBL456963 | — | — | 1 | 7.92 |
| CHEMBL457177 | — | — | 1 | 7.72 |
| CHEMBL510578 | — | — | 1 | 7.60 |
| CHEMBL497306 | — | — | 1 | 7.46 |
| CHEMBL507167 | — | — | 1 | 7.42 |
| CHEMBL1187319 | — | — | 1 | 7.36 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 7.33 |
| CHEMBL463579 | — | — | 1 | 7.05 |
| CHEMBL497477 | — | — | 1 | 6.96 |
| CHEMBL463580 | — | — | 1 | 6.85 |
| CHEMBL457388 | — | — | 1 | 6.85 |
| CHEMBL448316 | — | — | 1 | 6.12 |
| CHEMBL457208 | — | — | 1 | 5.80 |
| CHEMBL4160645 | — | — | 1 | - |
| CHEMBL4165150 | — | — | 1 | - |
| CHEMBL4175760 | — | — | 1 | - |
| CHEMBL4161715 | — | — | 1 | - |
| CHEMBL4172348 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL518383 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL456963 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL457177 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL510578 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL497306 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL507167 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL1187319 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL445813 | AT-7519 | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL463579 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL497477 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL463580 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL457388 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL448316 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL457208 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4160645 | — | IC50 | = | 760200.0 | nM | - |
| CHEMBL4165150 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4175760 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4161715 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4172348 | — | IC50 | > | 10000.0 | nM | - |