Page last updated: 2024-12-10

np 118809

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Description

1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one: an N-type calcium channel blocker; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4988454
CHEMBL ID604710
SCHEMBL ID4180792
MeSH IDM0546841

Synonyms (45)

Synonym
STK411255
1-[4-(diphenylmethyl)piperazin-1-yl]-3,3-diphenylpropan-1-one
np-118809
39-1-b4
FT-0667690
mk-6721
nmed-160
mk6721
CHEMBL604710
z160
z-160
1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one
AKOS003297641
piperazine, 1-(diphenylmethyl)-4-(1-oxo-3,3-diphenylpropyl)-
41332-24-5
HY-14462
np118809
CS-1361
1-[4-[di(phenyl)methyl]piperazin-1-yl]-3,3-di(phenyl)propan-1-one
np 118809
gtpl7765
SCHEMBL4180792
TX3R141LEP ,
1-(4-benzhydryl-piperazin-1-yl)-3,3-diphenylpropan-1-one
1-[4-(diphenylmethyl)-1-piperazinyl]-3,3-diphenyl-1-propanone
DTXSID70407284
A1-19036
unii-tx3r141lep
VCPMZDWBEWTGNW-UHFFFAOYSA-N
1-(4-benzhydryl-piperazin-1-yl)-3,3-diphenyl-propan-1-one
mfcd03387795
NCGC00378879-01
DB12743
BCP08259
Z27755997
EX-A2422
np118809; 39-1b4
AS-49769
Q27088019
HMS3748O17
39-1b4
bdbm50461289
N10437
EN300-6492997
AC-36066

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.39190.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency4.77240.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency4.77240.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency4.77240.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Voltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)IC50 (µMol)45.00000.03201.04793.6000AID1391672
Voltage-dependent L-type calcium channel subunit beta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.11000.08000.09330.1100AID471769
Voltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)IC50 (µMol)6.15500.02980.06990.1100AID459232; AID459233
Voltage-dependent calcium channel subunit alpha-2/delta-1Rattus norvegicus (Norway rat)IC50 (µMol)0.11000.08000.09330.1100AID471769
Voltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)IC50 (µMol)19.55500.04004.113710.0000AID1391671; AID459232
Voltage-dependent N-type calcium channel subunit alpha-1BRattus norvegicus (Norway rat)IC50 (µMol)0.11000.08000.32001.0000AID471769
Voltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)IC50 (µMol)6.15500.11000.11000.1100AID459232; AID459233
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)12.20000.00032.25459.6000AID459233
Prostaglandin D2 receptor 2Homo sapiens (human)IC50 (µMol)0.11000.00040.10090.9600AID471769
[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)
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)INH7.40007.40007.40007.4000AID472043
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (116)

Processvia Protein(s)Taxonomy
muscle contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
muscle organ developmentVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
myoblast fusionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of heart contractionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
aldosterone biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to hormone stimulusVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cortisol biosynthetic processVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cellular response to potassium ionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
regulation of membrane potentialVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion importVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
inorganic cation transmembrane transportVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
positive regulation of acrosome reactionVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
calcium ion transportVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of calcium ion transportVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion transport into cytosolVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
membrane depolarization during bundle of His cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of membrane repolarization during action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
positive regulation of high voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
cellular response to amyloid-betaVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
modulation of chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
response to amyloid-betaVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
chemical synaptic transmissionVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
regulation of calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
cellular response to amyloid-betaVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
regulation of voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
chemical synaptic transmissionVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
chemotaxisProstaglandin D2 receptor 2Homo sapiens (human)
immune responseProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
calcium-mediated signalingProstaglandin D2 receptor 2Homo sapiens (human)
positive regulation of G protein-coupled receptor signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
negative regulation of male germ cell proliferationProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide signaling pathwayProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (46)

Processvia Protein(s)Taxonomy
voltage-gated monoatomic ion channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
low voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
metal ion bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
scaffold protein bindingVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activity involved in bundle of His cell action potentialVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
metal ion bindingVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
amyloid-beta bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
calcium ion bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
protein bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
ATP bindingVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
prostaglandin J receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
G protein-coupled receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin D receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
prostaglandin F receptor activityProstaglandin D2 receptor 2Homo sapiens (human)
neuropeptide bindingProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (38)

Processvia Protein(s)Taxonomy
plasma membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
membraneVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent T-type calcium channel subunit alpha-1HHomo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
sarcoplasmic reticulumVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
extracellular exosomeVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
neuronal dense core vesicleVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent calcium channel subunit alpha-2/delta-1Homo sapiens (human)
plasma membraneVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
synapseVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
neuronal cell bodyVoltage-dependent N-type calcium channel subunit alpha-1BHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
synapseVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit beta-1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
plasma membraneProstaglandin D2 receptor 2Homo sapiens (human)
neuron projectionProstaglandin D2 receptor 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (36)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID472030AUC (0 to infinity) in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472042Inhibition of human ERG current at 1 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472043Inhibition of human ERG current2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID459233Inhibition of L type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells in presence of -100 mV holding potential by whole-cell patch clamp method2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
AID472033Apparent oral clearance in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID1391671Inhibition of Cav2.2 in human SH-SY5Y cells assessed as decrease in KCl-induced calcium mobilization measured after 600 secs post compound addition and 300 secs post KCl addition in presence of CaV1 blocker nifedipine by calcium 4 dye-based FLIPR assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels.
AID1391672Inhibition of recombinant human Cav3.2-alpha1 expressed in HEK293T cells assessed as decrease in KCl-induced calcium mobilization measured after 600 secs post compound addition and 300 secs post KCl addition by calcium 4 dye-based FLIPR assay2018Bioorganic & medicinal chemistry, 07-15, Volume: 26, Issue:11
Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels.
AID472046Displacement of radioligand from mu opioid receptor at 10 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472038Half life in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472031Half life in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472026Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472029AUC (0 to 8 hrs) in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472027Selectivity ratio of IC50 for rat Voltage-dependent L-type calcium channel to IC50 for rat N-type calcium channel2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472044Displacement of radioligand from Voltage-dependent L-type calcium channel at 10 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472037AUC (0 to infinity) in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472041Analgesic activity against phse 2A portion of rat formalin-induced inflammatory pain model assessed as flinches at 25 mg/kg, ip2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472035Tmax in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472045Displacement of radioligand from cannabinoid CB1 receptor at 10 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472036AUC (0 to 8 hrs) in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472034Cmax in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID459237Analgesic activity in Sprague-Dawley rat assessed as inhibition of spinal nerve injury-induced thermal hyperalgesia at 30 mg/kg, po after 60-90 mins2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
AID472032Volume of distribution at steady state in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID471769Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472040Oral bioavailability in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472047Displacement of radioligand from voltage-gated sodium channel at 10 uM2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID472039Apparent oral clearance in rat at 10 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID459236Analgesic activity in Sprague-Dawley rat assessed as inhibition of spinal nerve injury-induced mechanical allodynia at 30 mg/kg, po after 60-90 mins2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
AID472028Cmax in rat at 2 mg/kg, iv2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
AID459232Inhibition of N type calcium channel alpha-1b/alpha-2-delta-1/beta-1b expressed in HEK293 cells at holding potential of -100 mV by whole-cell patch clamp method2010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
AID459235Aqueous solubility at pH 7.42010Bioorganic & medicinal chemistry letters, Feb-15, Volume: 20, Issue:4
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
AID1346693Rat Cav2.2 (Voltage-gated calcium channels)2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's3 (50.00)24.3611
2020's2 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.79

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.79 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.79)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]