CXCL12α

Ligand id: 4358

Name: CXCL12α

Species: Human

View interactive charts of activity data from GtoPdb and ChEMBL (where available) 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 Hs Agonist Full agonist 7.7 – 8.2 pKd - 3,6
pKd 7.7 – 8.2 [3,6]
CXCR3 Hs Agonist Full agonist 6.4 pKi - 16
pKi 6.4 [16]
ACKR3 Hs Agonist Agonist 7.5 – 7.9 pEC50 - 2,13
pEC50 7.5 – 7.9 [2,13]
CXCR4 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 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 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.