Page last updated: 2024-12-08

nps-568

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Description

N-(2-chlorophenylpropyl)-1-(3-methoxyphenyl)ethylamine: NPS-568 is the ((R), HCl salt)-isomer; calcimimetic compound and calcium-sensing receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID158797
CHEMBL ID292376
SCHEMBL ID311950
MeSH IDM0427953
PubMed CID158796
CHEMBL ID2107572
SCHEMBL ID1178446
MeSH IDM0427953

Synonyms (74)

Synonym
nps r568
gtpl718
benzenepropanamine, 2-chloro-n-(1-(3-methoxyphenyl)ethyl)-, (r)-
tecalcet
r 568
tecalcet [inn]
(r)-2-chloro-n-(1-(3-methoxyphenyl)ethyl)benzenepropanamine
nps r 568
nps-r568
CHEMBL292376 ,
[3-(2-chloro-phenyl)-propyl]-[(r)-1-(3-methoxy-phenyl)-ethyl]-amine
bdbm50299670
(r)-3-(2-chlorophenyl)-n-(1-(3-methoxyphenyl)ethyl)propan-1-amine
3-(2-chlorophenyl)-n-[(1r)-1-(3-methoxyphenyl)ethyl]propan-1-amine
148717-54-8
8i16yle4us ,
unii-8i16yle4us
NCGC00344508-01
bdbm50432960
SCHEMBL311950
DTXSID90164084
(r)-n-(3-methoxy-alpha-phenylethyl) -3-(2-chlorophenyl)-1-propylamine
ZVQUCWXZCKWZBP-CQSZACIVSA-N
Q27088954
9ig ,
benzenepropanamine, 2-chloro-n-[(1r)-1-(3-methoxyphenyl)ethyl]-
AKOS040850283
D06020
tecalcet hydrochloride (usan)
177172-49-5
norcalcin (tn)
r-568
nps r-568
nps-r-568
n-(2-chlorophenylpropyl)-1-(3-methoxyphenyl)ethylamine
tecalcet hydrochloride
3-(2-chlorophenyl)-n-[(1r)-1-(3-methoxyphenyl)ethyl]propan-1-amine hydrochloride
norcalcin
tecalcet hcl
benzenepropanamine, 2-chloro-n-((1r)-1-(3-methoxyphenyl)ethyl)-, hydrochloride
krn 568
tecalcet hydrochloride
3-(2-chlorophenyl)-n-((1r)-1-(3-methoxyphenyl)ethyl)propan-1-amine hydrochloride
tecalcet hydrochloride [usan]
unii-3hp28r98lc
3hp28r98lc ,
3-(2-chlorophenyl)-n-((1r)-1-(3-methoxyphenyl)ethyl)propan-1-amine hydrochloride
krn-568
CHEMBL2107572
npsr-568
r 568 hydrochloride
smr004701455
MLS006010765
SCHEMBL1178446
2-chloro-n-[(1r)-1-(3-methoxyphenyl)ethyl]-benzenepropanamine hydrochloride
AKOS024457812
DTXSID10170263
AS-73997
[3-(2-chlorophenyl)propyl][(1r)-1-(3-methoxyphenyl)ethyl]amine hydrochloride
tecalcet(hydrochloride)
J-011257
177172-49-5 (hcl)
(r)-3-(2-chlorophenyl)-n-(1-(3-methoxyphenyl)ethyl)propan-1-amine hydrochloride
mfcd16038895
2-chloro-n-[(1r)-1-(3-methoxyphenyl)ethyl]-benzenepropanaminehydrochloride
r 568 hcl
benzenepropanamine, 2-chloro-n-[(1r)-1-(3-methoxyphenyl)ethyl]-, hydrochloride (1:1)
HY-10167A
CS-0002492
r-568 (hydrochloride)
Q27257225
tecalcet (hydrochloride)
CHA17249
(r)-3-(2-chlorophenyl)-n-(1-(3-methoxyphenyl)ethyl)propan-1-aminehydrochloride

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development of ring constrained analogues of the known calcimimetic R-568."( Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
Davis, J; Fotsch, C; Harrington, PE; Henley, C; Lott, FD; Lu, JY; Morony, S; Poon, SF; Reagan, JD; St Jean, DJ; Yang, Y, 2009
)
0.35
"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
" The first calcimimetic agent to be evaluated in clinical trials was R-568, but studies were discontinued because of its limited bioavailability and inconsistent pharmacokinetic profile."( Future role of calcimimetics in end-stage renal disease.
Goodman, WG; Turner, SA, 2002
)
0.31
" However, the low bioavailability of these first calcimimetics predicts a difficult clinical utilization."( Calcimimetic agents: review and perspectives.
Frazão, JM; Ureña, P, 2003
)
0.32
"Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development of ring constrained analogues of the known calcimimetic R-568."( Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
Davis, J; Fotsch, C; Harrington, PE; Henley, C; Lott, FD; Lu, JY; Morony, S; Poon, SF; Reagan, JD; St Jean, DJ; Yang, Y, 2009
)
0.35

Dosage Studied

ExcerptRelevanceReference
" NPS R-568 rapidly increased plasma calcitonin levels to a peak at 10 to 20 min after oral dosing (ED(50) 40 mg/kg)."( Calcimimetic compound NPS R-568 stimulates calcitonin secretion but selectively targets parathyroid gland Ca(2+) receptor in rats.
Conklin, RL; Fox, J; Lowe, SH; Nemeth, EF; Petty, BA, 1999
)
0.3
" To test this hypothesis, we compared two NPS R-568 dosing regimens in rats with chronic renal insufficiency induced by two intravenous injections of adriamycin."( Daily intermittent decreases in serum levels of parathyroid hormone have an anabolic-like action on the bones of uremic rats with low-turnover bone and osteomalacia.
Fox, J; Furuya, Y; Ishii, H; Nagano, N; Nemeth, EF; Wada, M, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency46.61280.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency37.22120.001310.157742.8575AID1259252; AID1259253
Interferon betaHomo sapiens (human)Potency46.61280.00339.158239.8107AID1347411
[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)
Extracellular calcium-sensing receptorHomo sapiens (human)EC50 (µMol)0.13700.02000.23341.0000AID441276; AID738057
Extracellular calcium-sensing receptorHomo sapiens (human)EC50 (µMol)0.08000.02000.23341.0000AID744122
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (61)

Processvia Protein(s)Taxonomy
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)
ossificationExtracellular calcium-sensing receptorHomo sapiens (human)
response to ischemiaExtracellular calcium-sensing receptorHomo sapiens (human)
detection of calcium ionExtracellular calcium-sensing receptorHomo sapiens (human)
intracellular calcium ion homeostasisExtracellular calcium-sensing receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
JNK cascadeExtracellular calcium-sensing receptorHomo sapiens (human)
chemosensory behaviorExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of cell population proliferationExtracellular calcium-sensing receptorHomo sapiens (human)
anatomical structure morphogenesisExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of gene expressionExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of insulin secretionExtracellular calcium-sensing receptorHomo sapiens (human)
bile acid secretionExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to hepatocyte growth factor stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
vasodilationExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of vasoconstrictionExtracellular calcium-sensing receptorHomo sapiens (human)
branching morphogenesis of an epithelial tubeExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of positive chemotaxisExtracellular calcium-sensing receptorHomo sapiens (human)
fat pad developmentExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeExtracellular calcium-sensing receptorHomo sapiens (human)
calcium ion importExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to vitamin DExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to glucose stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to hypoxiaExtracellular calcium-sensing receptorHomo sapiens (human)
response to fibroblast growth factorExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of calcium ion importExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to peptideExtracellular calcium-sensing receptorHomo sapiens (human)
chloride transmembrane transportExtracellular calcium-sensing receptorHomo sapiens (human)
regulation of calcium ion transportExtracellular calcium-sensing receptorHomo sapiens (human)
ossificationExtracellular calcium-sensing receptorHomo sapiens (human)
response to ischemiaExtracellular calcium-sensing receptorHomo sapiens (human)
detection of calcium ionExtracellular calcium-sensing receptorHomo sapiens (human)
intracellular calcium ion homeostasisExtracellular calcium-sensing receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayExtracellular calcium-sensing receptorHomo sapiens (human)
JNK cascadeExtracellular calcium-sensing receptorHomo sapiens (human)
chemosensory behaviorExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of cell population proliferationExtracellular calcium-sensing receptorHomo sapiens (human)
anatomical structure morphogenesisExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of gene expressionExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of insulin secretionExtracellular calcium-sensing receptorHomo sapiens (human)
bile acid secretionExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to hepatocyte growth factor stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
vasodilationExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of vasoconstrictionExtracellular calcium-sensing receptorHomo sapiens (human)
branching morphogenesis of an epithelial tubeExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of positive chemotaxisExtracellular calcium-sensing receptorHomo sapiens (human)
fat pad developmentExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeExtracellular calcium-sensing receptorHomo sapiens (human)
calcium ion importExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to vitamin DExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to glucose stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to hypoxiaExtracellular calcium-sensing receptorHomo sapiens (human)
response to fibroblast growth factorExtracellular calcium-sensing receptorHomo sapiens (human)
positive regulation of calcium ion importExtracellular calcium-sensing receptorHomo sapiens (human)
cellular response to peptideExtracellular calcium-sensing receptorHomo sapiens (human)
chloride transmembrane transportExtracellular calcium-sensing receptorHomo sapiens (human)
regulation of calcium ion transportExtracellular calcium-sensing receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Processvia Protein(s)Taxonomy
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)
phosphatidylinositol phospholipase C activityExtracellular calcium-sensing receptorHomo sapiens (human)
G protein-coupled receptor activityExtracellular calcium-sensing receptorHomo sapiens (human)
integrin bindingExtracellular calcium-sensing receptorHomo sapiens (human)
calcium ion bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein bindingExtracellular calcium-sensing receptorHomo sapiens (human)
amino acid bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein kinase bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein homodimerization activityExtracellular calcium-sensing receptorHomo sapiens (human)
transmembrane transporter bindingExtracellular calcium-sensing receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityExtracellular calcium-sensing receptorHomo sapiens (human)
G protein-coupled receptor activityExtracellular calcium-sensing receptorHomo sapiens (human)
integrin bindingExtracellular calcium-sensing receptorHomo sapiens (human)
calcium ion bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein bindingExtracellular calcium-sensing receptorHomo sapiens (human)
amino acid bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein kinase bindingExtracellular calcium-sensing receptorHomo sapiens (human)
protein homodimerization activityExtracellular calcium-sensing receptorHomo sapiens (human)
transmembrane transporter bindingExtracellular calcium-sensing receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
cell surfaceExtracellular calcium-sensing receptorHomo sapiens (human)
basolateral plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
apical plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
neuronal cell bodyExtracellular calcium-sensing receptorHomo sapiens (human)
axon terminusExtracellular calcium-sensing receptorHomo sapiens (human)
plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
cell surfaceExtracellular calcium-sensing receptorHomo sapiens (human)
basolateral plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
apical plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
neuronal cell bodyExtracellular calcium-sensing receptorHomo sapiens (human)
axon terminusExtracellular calcium-sensing receptorHomo sapiens (human)
plasma membraneExtracellular calcium-sensing receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (45)

Assay IDTitleYearJournalArticle
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
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.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC 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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID45799Compound was evaluated for accumulation of [3H]- IP in CHO (CaSR) cells expressing rat cloned calcium sensing receptor2000Bioorganic & medicinal chemistry letters, Sep-04, Volume: 10, Issue:17
N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor.
AID437457Inhibition of hyperparathyroidism in Sprague-Dawley rat pharmacodynamic model assessed as decrease in PTH levels at 30 mg/kg, po2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID738057Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
New potent calcimimetics: I. Discovery of a series of novel trisubstituted ureas.
AID437453Mean residence time in Sprague-Dawley rat at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID437455Cmax in Sprague-Dawley rat at 2 mg/kg, po2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID437452Volume of distribution at steady state in Sprague-Dawley rat at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID437454AUC in Sprague-Dawley rat at 2 mg/kg, po2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID437456Oral bioavailability in Sprague-Dawley rat at 2 mg/kg2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID437451Clearance in Sprague-Dawley rat at 0.5 mg/kg, iv2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID441276Activity at human CaSR expressed in HEK293 cells assessed as calcium release by FLIPR assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl)methanamines as potent and efficacious type II calcimimetics.
AID45800Maximal stimulation of [3H]-inositol phosphates production in CHO cells expressing rat Calcium sensing receptor (CaSR) at 10 mM [Ca2+]2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor.
AID1346721Human CaS receptor (Calcium-sensing receptor)2012Endocrinology, Mar, Volume: 153, Issue:3
Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.
AID1346721Human CaS receptor (Calcium-sensing receptor)1998Proceedings of the National Academy of Sciences of the United States of America, Mar-31, Volume: 95, Issue:7
Calcimimetics with potent and selective activity on the parathyroid calcium receptor.
AID1346721Human CaS receptor (Calcium-sensing receptor)2015British journal of pharmacology, Jan, Volume: 172, Issue:1
Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics.
AID744122Positive allosteric modulation of human CaSR expressed in CHO cells assessed as increase in intracellular calcium level after 5 hrs by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
New potent calcimimetics: II. Discovery of benzothiazole trisubstituted ureas.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (169)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's16 (9.47)18.2507
2000's84 (49.70)29.6817
2010's54 (31.95)24.3611
2020's15 (8.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.26

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 Index16.26 (24.57)
Research Supply Index5.12 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials4 (2.47%)5.53%
Reviews0 (0.00%)6.00%
Reviews35 (21.60%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies2 (1.23%)4.05%
Observational0 (0.00%)0.25%
Observational1 (0.62%)0.25%
Other15 (100.00%)84.16%
Other120 (74.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]