CXCL12α   Click here for help

GtoPdb Ligand ID: 4358

Synonyms: CXCL12 α | SDF-1α | stromal cell-derived factor-1α
Immunopharmacology Ligand
Compound class: Endogenous peptide in human, mouse or rat
Comment: CXCL12-1α and β were the first isoforms of this chemokine identified. Both proteins contain a signal peptide sequence that mediates their secretion via the canonical intracellular secretory pathway. CXCL12 participates in a variety of processes central to homeostasis and physiology, exerting its biological effects by binding to the chemokine receptors CXCR4 and CXCR7.
Species: Human
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
Gene deletion of CXCL12 in mice is lethal in late stage embryonic development (E18.5) [7]. Lethal developmental defects affecting the central nervous system, heart and vasculature are observed with deletion of the ligand gene, or of the genes for the CXCL12 receptors (CXCR4 [14,17] and CXCR7 [12]).
Natural/Endogenous Targets
Target
ACKR3
CXCR3
CXCR4
Selectivity at GPCRs
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CXCR4 Ligand is endogenous in the given species Hs Agonist Full agonist 7.7 – 8.2 pKd - 3,6
⤷ pKd 7.7 – 8.2 [3,6]
CXCR3 Ligand is endogenous in the given species Hs Agonist Full agonist 6.4 pKi - 16
⤷ pKi 6.4 [16]
ACKR3 Ligand is endogenous in the given species Hs Agonist Agonist 7.5 – 7.9 pEC50 - 2,13
⤷ pEC50 7.5 – 7.9 [2,13]
CXCR4 Ligand is endogenous in the given species Hs Agonist Agonist 9.3 pIC50 - 1
⤷ pIC50 9.3 (IC50 5x10-10 M) [1]
Description: Measuring CXCL12-induced displacement of CXCR4-bound 125I-CXCL12 from membranes prepared from HEK293T cells expressing human CXCR4.
Other ligands which bind to or alter the activity of this ligand
Key to terms and symbols Click column headers to sort
Ligand Sp. Type Action Value Parameter Concentration range (M) Reference
olaptesed pegol Small molecule or natural product Primary target of this compound Hs Inhibitor Binding 7.2 pIC50 - 4
⤷ pIC50 7.2 (IC50 6.793x10-8 M) [4]
Description: Inhibition of CXCL12 binding to immobilised heparin in a Biacore competition assay.
LIT-927 Small molecule or natural product Primary target of this compound Hs Inhibitor Binding 6.6 pIC50 - 11
⤷ pIC50 6.6 (IC50 2.67x10-7 M) [11]
Description: Measuring competitive inhibition of CXCL12α binding to CXCR4 by test ligand, using FRET detection.