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Assay Detail

CHEMBL3854641

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

Binding
Inhibition of human DNA polymerase kappa (19 to 526 residues)-mediated TLS past acrolein derived ring-opened reduced form of gamma-HOPdG lesions preincubated for 15 mins followed by DNA substrate addition measured after 30 mins in presence of dCTP and dGTP by radioactive gel-based primer extension assay
3
Total Activities
3
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 kappa (CHEMBL5365)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting the Translesion Synthesis Pathway for the Development of Anti-Cancer Chemotherapeutics.
Korzhnev DM, Hadden MK.
J Med Chem (2016) 59 : 9321 -9336
PubMed 27362876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.25 5.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL463914 MANOALIDE 1 5.25
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 5.25
CHEMBL3960997 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL463914 MANOALIDE IC50 = 5600.0 nM 5.25
CHEMBL1014 CANDESARTAN CILEXETIL IC50 = 5600.0 nM 5.25
CHEMBL3960997 IC50 = 5600.0 nM 5.25