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Assay Detail

CHEMBL4036263

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Binding
Inhibition of recombinant human full length Cdc7 (1 to 574 residues)/human N-terminal GST-tagged ASK (1 to 674 residues) expressed in baculovirus expression system using N-terminal His-tagged MCM2 as substrate pretreated for 60 mins followed by 50 uM ATP addition by TR-FRET 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

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 7.95 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062209 1 8.82
CHEMBL4083927 1 8.77
CHEMBL4080673 1 8.25
CHEMBL4098392 1 7.11
CHEMBL4080367 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062209 IC50 = 1.5 nM 8.82
CHEMBL4083927 IC50 = 1.7 nM 8.77
CHEMBL4080673 IC50 = 5.6 nM 8.25
CHEMBL4098392 IC50 = 77.0 nM 7.11
CHEMBL4080367 IC50 = 150.0 nM 6.82