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Assay Detail

CHEMBL4132832

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

Binding
Binding affinity to CXCR4 in human MDA-MB-231 cells preincubated for 15 mins followed by biotinylated TN41003 addition measured after 30 mins by rhodamine staining-based assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 4 (CHEMBL2107)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

An update on small molecules targeting CXCR4 as starting points for the development of anti-cancer therapeutics.
Grande F, Giancotti G, Ioele G, Occhiuzzi MA, Garofalo A.
Eur J Med Chem (2017) 139 : 519 -530
PubMed 28826086 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.56 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237830 1 9.52
CHEMBL4162225 1 8.10
CHEMBL4170138 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237830 IC50 = 0.3 nM 9.52
CHEMBL4162225 IC50 = 8.0 nM 8.10
CHEMBL4170138 IC50 = 8.9 nM 8.05