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Assay Detail

CHEMBL2173538

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

Functional
Antagonist activity at human recombinant CXCR4 expressed in CHO cells assessed as inhibition of SDF1a-induced electrical impedance by dielectric spectroscopic analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
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

Noncyclam tetraamines inhibit CXC chemokine receptor type 4 and target glioma-initiating cells.
Ros-Blanco L, Anido J, Bosser R, Esté J, Clotet B, Kosoy A, Ruíz-Ávila L, Teixidó J, Seoane J, Borrell JI.
J Med Chem (2012) 55 : 7560 -7570
PubMed 22909088 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.28 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE 1 6.58
CHEMBL2170444 1 6.46
CHEMBL2170299 1 6.10
CHEMBL2170443 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE IC50 = 260.0 nM 6.58
CHEMBL2170444 IC50 = 350.0 nM 6.46
CHEMBL2170299 IC50 = 790.0 nM 6.10
CHEMBL2170443 IC50 = 1100.0 nM 5.96