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Assay Detail

CHEMBL1806025

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

Functional
Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-87MG ATCC
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

Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
Zhu A, Zhan W, Liang Z, Yoon Y, Yang H, Grossniklaus HE, Xu J, Rojas M, Lockwood M, Snyder JP, Liotta DC, Shim H.
J Med Chem (2010) 53 : 8556 -8568
PubMed 21105715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.07 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802333 1 9.10
CHEMBL237830 1 8.74
CHEMBL1802329 1 8.27
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802333 IC50 = 0.8 nM 9.10
CHEMBL237830 IC50 = 1.8 nM 8.74
CHEMBL1802329 IC50 = 5.4 nM 8.27
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE IC50 = 695.0 nM 6.16