Assay Detail
Binding
CHEMBL3767308
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK5/p35NCK (unknown origin) using histone H1 as substrate in presence of [gamma-33P]ATP
5
Total Activities
5
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 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.89 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 7.35 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.39 |
| CHEMBL1801932 | — | — | 1 | 5.43 |
| CHEMBL3263773 | — | — | 1 | 5.30 |
| CHEMBL3763161 | — | — | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103840 | DINACICLIB | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 405.0 | nM | 6.39 |
| CHEMBL1801932 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3263773 | — | IC50 | = | 4960.0 | nM | 5.30 |
| CHEMBL3763161 | — | IC50 | = | 10700.0 | nM | 4.97 |