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Assay Detail

CHEMBL977797

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

Binding
Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 2 (CHEMBL4015)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Allosteric transinhibition by specific antagonists in CCR2/CXCR4 heterodimers.
Sohy D, Parmentier M, Springael JY.
J Biol Chem (2007) 282 : 30062 -30069
PubMed 17715128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 10.25 10.40
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18442 PLERIXAFOR 4.0 2 10.40
CHEMBL41275 2 10.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18442 PLERIXAFOR IC50 = 0.04 nM 10.40
CHEMBL41275 IC50 = 0.08 nM 10.10
CHEMBL18442 PLERIXAFOR Inhibition = 87.1 % -
CHEMBL41275 Inhibition = 38.1 % -