Page last updated: 2024-11-12

wz 811

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID11565518
CHEMBL ID237830
SCHEMBL ID589266
MeSH IDM0517160

Synonyms (32)

Synonym
wz 811
n,n''-di-2-pyridinyl-1,4-benzenedimethanamine
bdbm50225415
n-[[4-[(pyridin-2-ylamino)methyl]phenyl]methyl]pyridin-2-amine
CHEMBL237830 ,
wz-811
HY-15478
n1,n4-di-2-pyridinyl-1,4-benzenedimethanamine
wz811
S2912
55778-02-4
SCHEMBL589266
mfcd18086914
n,n'-(1,4-phenylenebis(methylene))dipyridin-2-amine
n,n'-(1,4-phenylenebis(methylene))bis(pyridin-2-amine)
AC-32781
AKOS024457893
DTXSID10468697
EX-A116
HMS3651F10
wz811, >=98% (hplc)
n,n''-(benzene-1,4-diyldimethanediyl)dipyridin-2-amine
n,n'-(1,4-phenylenebis(methylene))-bis(pyridin-2-amine)
n-[(4-{[(pyridin-2-yl)amino]methyl}phenyl)methyl]pyridin-2-amine
SW219530-1
BCP06492
FT-0700332
AS-16967
HMS3750C15
CCG-267383
1,4-bis(pyridine-2-aminomethyl)benzene
W0017
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-X-C chemokine receptor type 4Homo sapiens (human)IC50 (µMol)0.00100.00030.28766.2000AID1501134; AID604427
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-X-C chemokine receptor type 4Homo sapiens (human)EC50 (µMol)500,000.00020.00030.04410.0880AID303357
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
C-X-C chemokine receptor type 4Homo sapiens (human)EC (µMol)0.01000.01000.78001.0000AID1574049; AID605662
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

Processvia Protein(s)Taxonomy
calcium-mediated signalingC-X-C chemokine receptor type 4Homo sapiens (human)
response to hypoxiaC-X-C chemokine receptor type 4Homo sapiens (human)
neuron migrationC-X-C chemokine receptor type 4Homo sapiens (human)
epithelial cell developmentC-X-C chemokine receptor type 4Homo sapiens (human)
dendritic cell chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
apoptotic processC-X-C chemokine receptor type 4Homo sapiens (human)
inflammatory responseC-X-C chemokine receptor type 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
neuron recognitionC-X-C chemokine receptor type 4Homo sapiens (human)
response to virusC-X-C chemokine receptor type 4Homo sapiens (human)
response to activityC-X-C chemokine receptor type 4Homo sapiens (human)
telencephalon cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of cell adhesionC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of vascular wound healingC-X-C chemokine receptor type 4Homo sapiens (human)
CXCL12-activated CXCR4 signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of programmed cell deathC-X-C chemokine receptor type 4Homo sapiens (human)
myelin maintenanceC-X-C chemokine receptor type 4Homo sapiens (human)
endothelial cell differentiationC-X-C chemokine receptor type 4Homo sapiens (human)
symbiont entry into host cellC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of oligodendrocyte differentiationC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of viral processC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painC-X-C chemokine receptor type 4Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painC-X-C chemokine receptor type 4Homo sapiens (human)
regulation of calcium ion transportC-X-C chemokine receptor type 4Homo sapiens (human)
cardiac muscle contractionC-X-C chemokine receptor type 4Homo sapiens (human)
endothelial tube morphogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to cytokine stimulusC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to organonitrogen compoundC-X-C chemokine receptor type 4Homo sapiens (human)
cellular response to xenobiotic stimulusC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cold-induced thermogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
response to tacrolimusC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of dendrite extensionC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of vasculature developmentC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of mesenchymal stem cell migrationC-X-C chemokine receptor type 4Homo sapiens (human)
response to ultrasoundC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of macrophage migration inhibitory factor signaling pathwayC-X-C chemokine receptor type 4Homo sapiens (human)
neurogenesisC-X-C chemokine receptor type 4Homo sapiens (human)
cell chemotaxisC-X-C chemokine receptor type 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationC-X-C chemokine receptor type 4Homo sapiens (human)
immune responseC-X-C chemokine receptor type 4Homo sapiens (human)
brain developmentC-X-C chemokine receptor type 4Homo sapiens (human)
calcium-mediated signalingC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
virus receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
actin bindingC-X-C chemokine receptor type 4Homo sapiens (human)
G protein-coupled receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
protein bindingC-X-C chemokine receptor type 4Homo sapiens (human)
coreceptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
C-X-C chemokine receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine bindingC-X-C chemokine receptor type 4Homo sapiens (human)
ubiquitin protein ligase bindingC-X-C chemokine receptor type 4Homo sapiens (human)
myosin light chain bindingC-X-C chemokine receptor type 4Homo sapiens (human)
small molecule bindingC-X-C chemokine receptor type 4Homo sapiens (human)
C-X-C motif chemokine 12 receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
ubiquitin bindingC-X-C chemokine receptor type 4Homo sapiens (human)
C-C chemokine receptor activityC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
lysosomeC-X-C chemokine receptor type 4Homo sapiens (human)
early endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
cytoplasmC-X-C chemokine receptor type 4Homo sapiens (human)
lysosomeC-X-C chemokine receptor type 4Homo sapiens (human)
early endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
late endosomeC-X-C chemokine receptor type 4Homo sapiens (human)
plasma membraneC-X-C chemokine receptor type 4Homo sapiens (human)
cell surfaceC-X-C chemokine receptor type 4Homo sapiens (human)
cell leading edgeC-X-C chemokine receptor type 4Homo sapiens (human)
cytoplasmic vesicleC-X-C chemokine receptor type 4Homo sapiens (human)
extracellular exosomeC-X-C chemokine receptor type 4Homo sapiens (human)
anchoring junctionC-X-C chemokine receptor type 4Homo sapiens (human)
protein-containing complexC-X-C chemokine receptor type 4Homo sapiens (human)
external side of plasma membraneC-X-C chemokine receptor type 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID605662Displacement of biotinylated-TN14003 from CXCL12 binding site of CXCR4 in human MDA-MB-231 cells assessed as concentration required to inhibit >50% using rhodamine staining2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID605664Antagonist activity at CXCR4 in human MDA-MB-231 cells assessed as inhibition of CXCL12-mediated cell invasion at 10 nM by madrigal cell invasion assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID1564384Toxicity in C57BL/6J mouse at 10 mg/kg, ip2019European journal of medicinal chemistry, Nov-01, Volume: 181Synthesis and evaluation of 2,5-furan, 2,5-thiophene and 3,4-thiophene-based derivatives as CXCR4 inhibitors.
AID1574050Inhibition of CXCR4-mediated chemotaxis in human MDA-MB-231 cells assessed as reduction in CXCL12alpha-induced cell invasion at 100 nM after 22 hrs by hematoxylin/eosin dye-based matrigel assay relative to control2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Synthesis and evaluation of 2,5-diamino and 2,5-dianilinomethyl pyridine analogues as potential CXCR4 antagonists.
AID303357Displacement of biotinylated TN14003 from CXCR4 in MDA-MB-231 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID604429Antagonist activity at human CCR5 expressed in human U87 cells expressing CD4 assessed as inhibition of CCL5-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID605663Antagonist activity at CXCR4 in human MDA-MB-231 cells assessed as inhibition of CXCL12-mediated cell invasion at 100 nM by madrigal cell invasion assay2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID604428Antagonist activity at human CCR3 expressed in human U87 cells expressing CD4 assessed as inhibition of CCL5-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID1574049Inhibition of biotinylated TN14003 binding to CXCR4 in human MDA-MB-231 cells preincubated for 10 mins followed by biotinylated-TN14003 addition measured after 30 mins by streptavidin-rhodamine staining based fluorescence microscopic analysis2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Synthesis and evaluation of 2,5-diamino and 2,5-dianilinomethyl pyridine analogues as potential CXCR4 antagonists.
AID1564383Antiinflammatory activity in C57BL/6J mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip daily dosed 30 mins after carrageenan challenge and measured after 74 hrs carrageenan challenge and 2 hrs post last dose by caliper method 2019European journal of medicinal chemistry, Nov-01, Volume: 181Synthesis and evaluation of 2,5-furan, 2,5-thiophene and 3,4-thiophene-based derivatives as CXCR4 inhibitors.
AID303358Antagonist activity at CXCR4 in human U87 cells assessed as inhibition of SDF1-induced modulation of cAMP production by TR-FRET assay2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID604427Antagonist activity at human CXCR4 expressed in human U87 cells expressing CD4 assessed as inhibition of CXCL12-induced cAMP production pretreated for 15 mins before forskolin challenge by TR-FRET analysis2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID1501134Binding affinity to CXCR4 in human MDA-MB-231 cells preincubated for 15 mins followed by biotinylated TN41003 addition measured after 30 mins by rhodamine staining-based assay2017European journal of medicinal chemistry, Oct-20, Volume: 139An update on small molecules targeting CXCR4 as starting points for the development of anti-cancer therapeutics.
AID604430Antiinflammatory activity in C57BL/6L mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip administered 30 mins before carrageenan challenge measured after 76 hrs2010Journal of medicinal chemistry, Dec-23, Volume: 53, Issue:24
Dipyrimidine amines: a novel class of chemokine receptor type 4 antagonists with high specificity.
AID303359Inhibition of SDF1-mediated invasion of human MDA-MB-231 cells2007Journal of medicinal chemistry, Nov-15, Volume: 50, Issue:23
Discovery of small molecule CXCR4 antagonists.
AID1574051Antiinflammatory activity in C57Bl/6J mouse assessed as inhibition of carrageenan-induced paw edema at 10 mg/kg, ip treated for 2 days measured 2 hrs post last dose by caliper method relative to control2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Synthesis and evaluation of 2,5-diamino and 2,5-dianilinomethyl pyridine analogues as potential CXCR4 antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's4 (80.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 25.21

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index25.21 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.63 (4.65)
Search Engine Demand Index17.79 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (25.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]