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Assay Detail

CHEMBL4036260

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Cdc7 in human HeLa cells assessed as reduction in MCM2 phosphorylation at ser40 residues after 7 hrs by Western blot analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cell division cycle 7-related protein kinase (CHEMBL5443)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time-dependent inhibitors of Cdc7 kinase.
Kurasawa O, Homma M, Oguro Y, Miyazaki T, Mori K, Uchiyama N, Iwai K, Ohashi A, Hara H, Yoshida S, Cho N.
Bioorg Med Chem (2017) 25 : 3658 -3670
PubMed 28533114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.74 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4080673 1 7.17
CHEMBL4083927 1 6.60
CHEMBL4062209 1 6.46
CHEMBL4098392 1 -
CHEMBL4080367 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4080673 IC50 = 67.0 nM 7.17
CHEMBL4083927 IC50 = 250.0 nM 6.60
CHEMBL4062209 IC50 = 350.0 nM 6.46
CHEMBL4098392 IC50 > 1000.0 nM -
CHEMBL4080367 IC50 > 1000.0 nM -