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Assay Detail

CHEMBL4034965

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

Binding
Inhibition of Chk2 (unknown origin) by ELISA based spectrophotometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Serine/threonine-protein kinase Chk2 (CHEMBL2527)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Part I: Design, synthesis and biological evaluation of novel pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors with studying their activities alone and in combination with genotoxic drugs.
Galal SA, Abdelsamie AS, Shouman SA, Attia YM, Ali HI, Tabll A, El-Shenawy R, El Abd YS, Ali MM, Mahmoud AE, Abdel-Halim AH, Fyiad AA, Girgis AS, El-Diwani HI.
Eur J Med Chem (2017) 134 : 392 -405
PubMed 28433679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.64 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4072515 1 8.26
CHEMBL4093249 1 8.16
CHEMBL4063921 1 7.83
CHEMBL4085496 1 7.75
CHEMBL4090789 1 7.51
CHEMBL195041 1 7.50
CHEMBL4100980 1 7.49
CHEMBL4103039 1 7.48
CHEMBL4062848 1 7.47
CHEMBL4083002 1 7.32
CHEMBL4076911 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4072515 IC50 = 5.5 nM 8.26
CHEMBL4093249 IC50 = 6.9 nM 8.16
CHEMBL4063921 IC50 = 14.9 nM 7.83
CHEMBL4085496 IC50 = 17.9 nM 7.75
CHEMBL4090789 IC50 = 31.0 nM 7.51
CHEMBL195041 IC50 = 32.0 nM 7.50
CHEMBL4100980 IC50 = 32.5 nM 7.49
CHEMBL4103039 IC50 = 33.4 nM 7.48
CHEMBL4062848 IC50 = 33.8 nM 7.47
CHEMBL4083002 IC50 = 48.4 nM 7.32
CHEMBL4076911 IC50 = 52.8 nM 7.28