Assay Detail
Binding
CHEMBL4325331
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-fused full-length human CDC7 (1 to 574 end residues)/DBF4 (1 to 674 residues) expressed in baculovirus expression system using MCM2 as substrate preincubated with enzyme for 60 mins prior to 50 uM ATP addition by HTRF transcreener ADP assay
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
CDC7/DBF4 (Cell division cycle 7-related protein kinase/Activator of S phase kinase) (CHEMBL2111377) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 9.05 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4439133 | — | — | 1 | 9.39 |
| CHEMBL4297644 | SIMUROSERTIB | 2.0 | 1 | 9.27 |
| CHEMBL4570191 | — | — | 1 | 9.14 |
| CHEMBL4083927 | — | — | 1 | 8.77 |
| CHEMBL4436649 | — | — | 1 | 8.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4439133 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL4297644 | SIMUROSERTIB | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4570191 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL4083927 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4436649 | — | IC50 | = | 2.1 | nM | 8.68 |