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Target Report Card

Target Name and Classification

Target ID CHEMBL2107
Preferred Name C-X-C chemokine receptor type 4
Synonyms C-X-C chemokine receptor type 4 | CD_antigen=CD184 | CXC-R4 | CXCR-4 | CXCR4 | FB22 | Fusin | HM89 | LAP-3 | LCR1 | LESTR | LPS-associated protein 3 | Leukocyte-derived seven transmembrane domain receptor | Lipopolysaccharide-associated protein 3 | NPYRL | SDF-1 receptor | Stromal cell-derived factor 1 receptor
Organism Homo sapiens
Species Group No
Protein Target Classification
  • membrane receptor > family a g protein-coupled receptor > peptide receptor (family a gpcr) > chemokine receptor > cxc chemokine receptor

Target Components

Component Description Relationship Accession
C-X-C chemokine receptor type 4 SINGLE PROTEIN P61073

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL18442 PLERIXAFOR C-X-C chemokine receptor type 4 partial agonist 4 DailyMed
CHEMBL3545348 BKT140 C-X-C chemokine receptor type 4 antagonist 3 PubMed PubMed PubMed
CHEMBL3544949 CTCE-9908 C-X-C chemokine receptor type 4 antagonist 2 Other PubMed
CHEMBL3545105 POL6326 C-X-C chemokine receptor type 4 antagonist 2 Other PubMed
CHEMBL3545224 BURIXAFOR C-X-C chemokine receptor type 4 antagonist 2 Other PubMed
CHEMBL3039543 ULOCUPLUMAB C-X-C chemokine receptor type 4 inhibitor 1 Other PMC
CHEMBL3545330 MSX-122 C-X-C chemokine receptor type 4 antagonist 1 PubMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000121966
Ensembl ENSG00000121966
GO Cellular Component GO:0005737 (cytoplasm)
GO:0005764 (lysosome)
GO:0005768 (endosome)
GO:0005769 (early endosome)
GO:0005770 (late endosome)
GO:0005886 (plasma membrane)
GO:0009986 (cell surface)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0030054 (cell junction)
GO:0031252 (cell leading edge)
GO:0031410 (cytoplasmic vesicle)
GO:0032991 (macromolecular complex)
GO:0070062 (extracellular exosome)
GO Molecular Function GO:0001618 (virus receptor activity)
GO:0003779 (actin binding)
GO:0004871 (signal transducer activity)
GO:0004930 (G-protein coupled receptor activity)
GO:0004950 (chemokine receptor activity)
GO:0005515 (protein binding)
GO:0015026 (coreceptor activity)
GO:0016494 (C-X-C chemokine receptor activity)
GO:0019955 (cytokine binding)
GO:0019957 (C-C chemokine binding)
GO:0031625 (ubiquitin protein ligase binding)
GO:0032027 (myosin light chain binding)
GO:0043130 (ubiquitin binding)
GO Biological Process GO:0000187 (activation of MAPK activity)
GO:0001666 (response to hypoxia)
GO:0002407 (dendritic cell chemotaxis)
GO:0006915 (apoptotic process)
GO:0006935 (chemotaxis)
GO:0006954 (inflammatory response)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007204 (positive regulation of cytosolic calcium ion concentration)
GO:0007411 (axon guidance)
GO:0009615 (response to virus)
GO:0016032 (viral process)
GO:0019064 (fusion of virus membrane with host plasma membrane)
GO:0019722 (calcium-mediated signaling)
GO:0030260 (entry into host cell)
GO:0043217 (myelin maintenance)
GO:0048714 (positive regulation of oligodendrocyte differentiation)
GO:0050920 (regulation of chemotaxis)
GO:0070098 (chemokine-mediated signaling pathway)
GO:0071345 (cellular response to cytokine stimulus)
Wikipedia CXCR4

Target Cross References - Protein

canSAR P61073
CGD Warts, hypogammaglobulinemia, infections, and myelokathexis (WHIM syndrome)
Human Protein Atlas ENSG00000121966
IntAct P61073
Guide to Pharmacology 71
Open Targets ENSG00000121966
PharmGKB PA27058
Pharos P61073 (Tclin)
Reactome R-HSA-173107 (Binding and entry of HIV virion.)
R-HSA-376176 (Signaling by ROBO receptors.)
R-HSA-380108 (Chemokine receptors bind chemokines.)
R-HSA-418594 (G alpha (i) signalling events.)
UniProt B2R5N0 O60835 P30991 P56438 P61073 Q53S69 Q9BXA0 Q9UKN2

Target Cross References - Domain

InterPro IPR000276 (GPCR_Rhodpsn.)
IPR000355 (Chemokine_rcpt.)
IPR001277 (CXCR4/ACKR2.)
IPR017452 (GPCR_Rhodpsn_7TM.)
IPR022726 (Chemokine_CXCR4_N_dom.)
Pfam PF00001 (7tm_1)
PF12109 (CXCR4_N)

Target Cross References - Structure

PDBe 3ODU 3OE0 3OE6 3OE8 3OE9 4RWS