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Assay Detail

CHEMBL5325963

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

Binding
Inhibition of recombinant human DNA polymerase eta expressed in baculovirus expression system using primer/TAMRA-labeled reporter/BHQ2-labeled template as DNA substrate preincubated for 15 mins followed by substrate addition measured immediately by fluorescence based assay
2
Total Activities
2
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

DNA polymerase eta (CHEMBL5542)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Computer-aided identification, synthesis, and biological evaluation of DNA polymerase η inhibitors for the treatment of cancer.
Munafò F, Nigro M, Brindani N, Manigrasso J, Geronimo I, Ottonello G, Armirotti A, De Vivo M.
Eur J Med Chem (2023) 248 : 115044 -115044
PubMed 36621139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.17 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6246 ELLAGIC ACID 2.0 1 7.21
CHEMBL275938 AURINTRICARBOXYLIC ACID 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6246 ELLAGIC ACID IC50 = 62.0 nM 7.21
CHEMBL275938 AURINTRICARBOXYLIC ACID IC50 = 75.0 nM 7.12