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Assay Detail

CHEMBL4374585

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

Functional
DNA alkylating activity in human SKBR3 cells exhibiting increased cathepsin B activity and reduced GCPII expression assessed as reduction in cell viability incubated for 72 hrs by MTS assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Target

DNA (CHEMBL2311221)
Type NUCLEIC-ACID
Organism Homo sapiens

Publication

A small molecule drug conjugate (SMDC) of DUPA and a duocarmycin built on the solid phase.
Beekman AM, Cominetti MMD, Cartwright OC, Boger DL, Searcey M.
Medchemcomm (2019) 10 : 2170 -2174
PubMed 32879717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.05 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4443767 1 8.64
CHEMBL4452530 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4443767 IC50 = 2.3 nM 8.64
CHEMBL4452530 IC50 = 3560.0 nM 5.45