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Assay Detail

CHEMBL4707525

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

Functional
Antagonist activity at CXCR4 in human CD4-positive T cells assessed as inhibition of CXCL12-induced calcium signal incubated for 20 mins by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CD4+ve Th
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

Structural optimization of aminopyrimidine-based CXCR4 antagonists.
Zhu,F.; Wang,Y.; Du,Q.; Ge,W.; Li,Z.; Wang,X.; Fu,C.; Luo,L.; Tian,S.; Ma,H.; Zheng,J.; Zhang,Y.; Sun,X.; He,S.; Zhang,X.
Eur J Med Chem (2020) 187 : 111914 -111914
PubMed 31806538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.46 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4751485 1 10.70
CHEMBL18442 PLERIXAFOR 4.0 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4751485 IC50 = 0.02 nM 10.70
CHEMBL18442 PLERIXAFOR IC50 = 6.134 nM 8.21