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Assay Detail

CHEMBL3097223

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

Binding
Antagonist activity at CXCR4 in human PBMC assessed as inhibition of HIV-1 3B infection
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery of tetrahydroisoquinoline-based CXCR4 antagonists.
Truax VM, Zhao H, Katzman BM, Prosser AR, Alcaraz AA, Saindane MT, Howard RB, Culver D, Arrendale RF, Gruddanti PR, Evers TJ, Natchus MG, Snyder JP, Liotta DC, Wilson LJ.
ACS Med Chem Lett (2013) 4 : 1025 -1030
PubMed 24936240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.50 7.52
IC90 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL518924 MAVORIXAFOR 4.0 1 7.52
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE 1 7.52
CHEMBL3091687 2 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL518924 MAVORIXAFOR IC50 = 30.0 nM 7.52
CHEMBL2311028 PLERIXAFOR OCTAHYDROCHLORIDE IC50 = 30.0 nM 7.52
CHEMBL3091687 IC50 = 35.0 nM 7.46
CHEMBL3091687 IC90 = 240.0 nM -