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Assay Detail

CHEMBL4313178

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

Binding
Inhibition of human His6-tagged ERCC1-XPF endonuclease activity expressed in Escherichia coli BL21 (DE3) using [6-FAM-5'-CAGCGCTCGG(20T)CCGAGCGCTG-3'-dabcyl] as substrate measured after 30 mins in presence of 5% DMSO by fluorescence assay
2
Total Activities
2
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

Targeting DNA Repair in Tumor Cells via Inhibition of ERCC1-XPF.
Elmenoufy AH, Gentile F, Jay D, Karimi-Busheri F, Yang X, Soueidan OM, Weilbeer C, Mani RS, Barakat KH, Tuszynski JA, Weinfeld M, West FG.
J Med Chem (2019) 62 : 7684 -7696
PubMed 31369707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.11 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4470176 1 6.48
CHEMBL463783 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4470176 IC50 = 330.0 nM 6.48
CHEMBL463783 IC50 = 1860.0 nM 5.73