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Assay Detail

CHEMBL4132836

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

Functional
Antagonist activity at CXCR4 in human U87-MG cells assessed as inhibition of CXCL12-induced cell proliferation after 1 hr by MTT assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
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 5 6.36 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168547 1 6.92
CHEMBL4173028 1 6.72
CHEMBL4176412 1 6.72
CHEMBL4165124 1 6.00
CHEMBL1381819 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168547 IC50 = 120.0 nM 6.92
CHEMBL4173028 IC50 = 190.0 nM 6.72
CHEMBL4176412 IC50 = 190.0 nM 6.72
CHEMBL4165124 IC50 = 1000.0 nM 6.00
CHEMBL1381819 IC50 = 3800.0 nM 5.42