Page last updated: 2024-12-10

4-phenyl-2-propionamidotetraline

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

Description

4-phenyl-2-propionamidotetraline: melatonin receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3976006
CHEMBL ID285718
CHEBI ID110160
SCHEMBL ID54783
MeSH IDM0295167

Synonyms (38)

Synonym
HMS3267A10
BRD-A67482312-001-01-8
n-(4-phenyltetralin-2-yl)propanamide
gtpl1358
4p-pdot
PDSP1_001822
NCGC00024953-02
PDSP2_001805
CHEBI:110160
4-p-pdot
n-(4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propionamide
bdbm50240440
n-(4-phenyl-1,2,3,4-tetrahydro-naphthalen-2-yl)-propionamide
CHEMBL285718 ,
L000075
4-phenyl-2-propionamidotetraline
n-(4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl)propanamide
134865-74-0
SCHEMBL54783
RCYLUNPFECYGDW-UHFFFAOYSA-N
4-phenyl-2-propionamido tetralin
cis-4-phenyl-2-propionamidotetralin
ah 024
620170-78-7
AKOS024456343
SR-01000597467-1
sr-01000597467
J-006616
HMS3676A15
HY-100609
CS-0019766
Q27073959
4-phenyl-2- propionamidotetralin
HMS3412A15
mfcd00901545
N17036
ah-024
P2587
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
tetralinsCompounds containing a tetralin skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency0.79430.003245.467312,589.2998AID2517
Chain A, Ferritin light chainEquus caballus (horse)Potency28.18385.623417.292931.6228AID485281
TDP1 proteinHomo sapiens (human)Potency23.10930.000811.382244.6684AID686978
regulator of G-protein signaling 4Homo sapiens (human)Potency23.77810.531815.435837.6858AID504845
[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)
Melatonin receptor type 1AHomo sapiens (human)Ki0.22160.00000.27359.1000AID1138127; AID239989; AID369281
Melatonin receptor type 1BHomo sapiens (human)Ki0.00070.00000.16289.1000AID1138128; AID239966; AID369282
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (18)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1AHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
mating behaviorMelatonin receptor type 1AHomo sapiens (human)
circadian rhythmMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1BHomo sapiens (human)
chemical synaptic transmissionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cGMP-mediated signalingMelatonin receptor type 1BHomo sapiens (human)
glucose homeostasisMelatonin receptor type 1BHomo sapiens (human)
camera-type eye developmentMelatonin receptor type 1BHomo sapiens (human)
negative regulation of neuron apoptotic processMelatonin receptor type 1BHomo sapiens (human)
negative regulation of vasoconstrictionMelatonin receptor type 1BHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, non-REM sleepMelatonin receptor type 1BHomo sapiens (human)
negative regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationMelatonin receptor type 1BHomo sapiens (human)
negative regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
positive regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
regulation of neuronal action potentialMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
protein bindingMelatonin receptor type 1AHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1AHomo sapiens (human)
hormone bindingMelatonin receptor type 1AHomo sapiens (human)
organic cyclic compound bindingMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1AHomo sapiens (human)
protein bindingMelatonin receptor type 1BHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneMelatonin receptor type 1AHomo sapiens (human)
receptor complexMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
synapseMelatonin receptor type 1BHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID369281Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.
AID415405Selectivity ratio, Ki for human MT1 receptor to Ki for human MT2 receptor2009Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8
Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
AID108023Relative Binding Affinity (pRA1) to cloned human Melatonin receptor type 1A, stably expressed in NIH3T3 rat fibroblast cells, determined using 2-[125I]iodomelatonin2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.
AID1138128Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in African green monkey COS7 cells2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID108056Relative Binding Affinity (pRA1) to cloned human Melatonin receptor type 1B, stably expressed in NIH3T3 rat fibroblast cells, determined using 2-[125I]iodomelatonin2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Three-dimensional quantitative structure-activity relationship studies on selected MT1 and MT2 melatonin receptor ligands: requirements for subtype selectivity and intrinsic activity modulation.
AID415404Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in cells2009Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8
Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
AID1138140Selectivity ratio of Ki for human recombinant MT1 receptor to Ki for human recombinant MT2 receptor2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID369282Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
2-[(2,3-dihydro-1H-indol-1-yl)methyl]melatonin analogues: a novel class of MT2-selective melatonin receptor antagonists.
AID1138127Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in African green monkey COS7 cells2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID239989Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.
AID239966Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor MT2 expressed in NIH3T3 rat fibroblast cells2005Journal of medicinal chemistry, Jun-16, Volume: 48, Issue:12
Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.
AID415403Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in cells2009Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8
Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
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.
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.
AID1346220Human MT1 receptor (Melatonin receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 355, Issue:3
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
AID1346274Human MT2 receptor (Melatonin receptors)1998FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Sep, Volume: 12, Issue:12
Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms.
AID1346220Human MT1 receptor (Melatonin receptors)1998FASEB journal : official publication of the Federation of American Societies for Experimental Biology, Sep, Volume: 12, Issue:12
Selective MT2 melatonin receptor antagonists block melatonin-mediated phase advances of circadian rhythms.
AID1346220Human MT1 receptor (Melatonin receptors)2003Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 367, Issue:6
New selective ligands of human cloned melatonin MT1 and MT2 receptors.
AID1346274Human MT2 receptor (Melatonin receptors)1997Naunyn-Schmiedeberg's archives of pharmacology, Mar, Volume: 355, Issue:3
Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.
AID1346274Human MT2 receptor (Melatonin receptors)2003Naunyn-Schmiedeberg's archives of pharmacology, Jun, Volume: 367, Issue:6
New selective ligands of human cloned melatonin MT1 and MT2 receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (70)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (5.71)18.2507
2000's33 (47.14)29.6817
2010's28 (40.00)24.3611
2020's5 (7.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.06

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 Index11.06 (24.57)
Research Supply Index4.30 (2.92)
Research Growth Index5.36 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.06)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.39%)5.53%
Reviews1 (1.39%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other70 (97.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]