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Assay Detail

CHEMBL5227434

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

Binding
Inhibition of Chk2 (unknown origin)
9
Total Activities
8
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

Fused-azepinones: Emerging scaffolds of medicinal importance.
Akunuri R, Vadakattu M, Bujji S, Veerareddy V, Madhavi YV, Nanduri S.
Eur J Med Chem (2021) 220 : 113445 -113445
PubMed 33901899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.29 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481333 1 8.10
CHEMBL1947252 1 7.85
CHEMBL1947250 1 7.70
CHEMBL1947253 1 7.55
CHEMBL361708 HYMENIALDISINE 1 7.38
CHEMBL1944822 1 6.81
CHEMBL1944823 1 6.77
CHEMBL255465 DEBROMOHYMENIALDISINE 2 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481333 IC50 = 8.0 nM 8.10
CHEMBL1947252 IC50 = 14.0 nM 7.85
CHEMBL1947250 IC50 = 20.0 nM 7.70
CHEMBL1947253 IC50 = 28.0 nM 7.55
CHEMBL361708 HYMENIALDISINE IC50 = 42.0 nM 7.38
CHEMBL1944822 IC50 = 156.0 nM 6.81
CHEMBL1944823 IC50 = 171.0 nM 6.77
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 180.0 nM 6.75
CHEMBL255465 DEBROMOHYMENIALDISINE IC50 = 183.0 nM 6.74