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Assay Detail

CHEMBL4036255

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

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 10 mins followed by ATP addition by TR-FRET assay
25
Total Activities
25
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 25 8.23 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083927 1 9.15
CHEMBL4087760 1 8.96
CHEMBL4078941 1 8.92
CHEMBL4070822 1 8.85
CHEMBL4080673 1 8.82
CHEMBL4095460 1 8.80
CHEMBL4062209 1 8.66
CHEMBL4078031 1 8.62
CHEMBL4084945 1 8.60
CHEMBL4086790 1 8.57
CHEMBL4091279 1 8.57
CHEMBL4068071 1 8.57
CHEMBL4103214 1 8.41
CHEMBL4081417 1 8.39
CHEMBL4098392 1 8.35
CHEMBL4096077 1 8.33
CHEMBL4091694 1 8.29
CHEMBL4105646 1 8.15
CHEMBL4080367 1 7.92
CHEMBL4061122 1 7.82
CHEMBL4099435 1 7.60
CHEMBL4063842 1 7.12
CHEMBL4065361 1 6.89
CHEMBL4073971 1 6.85
CHEMBL4062454 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083927 IC50 = 0.7 nM 9.15
CHEMBL4087760 IC50 = 1.1 nM 8.96
CHEMBL4078941 IC50 = 1.2 nM 8.92
CHEMBL4070822 IC50 = 1.4 nM 8.85
CHEMBL4080673 IC50 = 1.5 nM 8.82
CHEMBL4095460 IC50 = 1.6 nM 8.80
CHEMBL4062209 IC50 = 2.2 nM 8.66
CHEMBL4078031 IC50 = 2.4 nM 8.62
CHEMBL4084945 IC50 = 2.5 nM 8.60
CHEMBL4086790 IC50 = 2.7 nM 8.57
CHEMBL4091279 IC50 = 2.7 nM 8.57
CHEMBL4068071 IC50 = 2.7 nM 8.57
CHEMBL4103214 IC50 = 3.9 nM 8.41
CHEMBL4081417 IC50 = 4.1 nM 8.39
CHEMBL4098392 IC50 = 4.5 nM 8.35
CHEMBL4096077 IC50 = 4.7 nM 8.33
CHEMBL4091694 IC50 = 5.1 nM 8.29
CHEMBL4105646 IC50 = 7.0 nM 8.15
CHEMBL4080367 IC50 = 12.0 nM 7.92
CHEMBL4061122 IC50 = 15.0 nM 7.82
CHEMBL4099435 IC50 = 25.0 nM 7.60
CHEMBL4063842 IC50 = 75.0 nM 7.12
CHEMBL4065361 IC50 = 130.0 nM 6.89
CHEMBL4073971 IC50 = 140.0 nM 6.85
CHEMBL4062454 IC50 = 290.0 nM 6.54