Page last updated: 2024-11-11

t-226296

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

Description

T-226296: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9865843
CHEMBL ID178707
SCHEMBL ID5582818
MeSH IDM0428509

Synonyms (21)

Synonym
n-(6-((dimethylamino)methyl)-5,6,7,8-tetrahydronaphthalen-2-yl)-4''-fluorobiphenyl-4-carboxamide
bdbm50150715
4''-fluoro-biphenyl-4-carboxylic acid (6-dimethylaminomethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-amide
4''''-fluoro-biphenyl-4-carboxylic acid (6-dimethylaminomethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-amide
gtpl1314
t226296
n-[6-(dimethylaminomethyl)-5,6,7,8-tetrahydronaphthalen-2-yl]-4-(4-fluorophenyl)benzamide
t 226296
PDSP2_000965
t-226296
PDSP1_000981 ,
CHEMBL178707 ,
GXAQELJVODWLDD-UHFFFAOYSA-N
4'-fluoro-n-[6-[(n,n-dimethylamino)methyl]-5,6,7,8-tetrahydro-2-naphthalenyl][1,1'-biphenyl]-4-carboxamide
4'-fluoro-n-[6-[(n,n-dimethylamino)methyl]-5,6,7,8-tetrahydro-2-naphthalenyl)[1,1'-biphenyl]-4-carboxamide
SCHEMBL5582818
n-(6-((dimethylamino)methyl)-5,6,7,8-tetrahydronaphthalen-2-yl)-4'-fluoro-[1,1'-biphenyl]-4-carboxamide
331758-35-1
Q27088915
n-[6-[(dimethylamino)methyl]-5,6,7,8-tetrahydronaphthalen-2-yl]-4-(4-fluorophenyl)benzamide
AKOS040749598

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" We attempted to replicate the effects previously reported with SNAP-7941 and expanded the investigation to three other orally bioavailable MCH-1 receptor antagonists with good brain penetration."( Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety.
Basso, AM; Bratcher, NA; Brune, ME; Collins, CA; Cowart, MD; Esbenshade, TA; Fox, GB; Gallagher, KB; Hancock, AA; Iyengar, R; Kym, PR; Rueter, LE; Schmidt, M; Souers, AJ; Sun, M; Vasudevan, A; Zhao, C, 2006
)
0.33
" Pharmacokinetic analysis confirmed that 2s had good oral bioavailability and brain penetrance."( Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
Asami, A; Endo, S; Imaeda, T; Ishihara, Y; Kamata, M; Kato, K; Miyamoto, M; Nagisa, Y; Nakano, Y; Ogino, H; Ora, T; Suzuki, N; Takekawa, S; Tanaka, T; Tawada, M; Terauchi, J; Watanabe, K; Yamashita, T, 2011
)
0.37
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Melanin-concentrating hormone receptor 1Rattus norvegicus (Norway rat)IC50 (µMol)0.02400.02400.02400.0240AID614322
Melanin-concentrating hormone receptor 1Homo sapiens (human)IC50 (µMol)0.11720.00050.23633.5000AID242077; AID242643; AID248949; AID353587; AID443384; AID551220; AID614320; AID614321; AID630087
Melanin-concentrating hormone receptor 1Homo sapiens (human)Ki0.02170.00280.01540.0380AID239711; AID307524
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (8)

Processvia Protein(s)Taxonomy
generation of precursor metabolites and energyMelanin-concentrating hormone receptor 1Homo sapiens (human)
cell surface receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationMelanin-concentrating hormone receptor 1Homo sapiens (human)
feeding behaviorMelanin-concentrating hormone receptor 1Homo sapiens (human)
positive regulation of calcium ion transportMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide signaling pathwayMelanin-concentrating hormone receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
signaling receptor bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
melanin-concentrating hormone receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
hormone bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
G protein-coupled receptor activityMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuropeptide bindingMelanin-concentrating hormone receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
plasma membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
ciliumMelanin-concentrating hormone receptor 1Homo sapiens (human)
ciliary membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
non-motile ciliumMelanin-concentrating hormone receptor 1Homo sapiens (human)
neuron projectionMelanin-concentrating hormone receptor 1Homo sapiens (human)
plasma membraneMelanin-concentrating hormone receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID1346168Human MCH1 receptor (Melanin-concentrating hormone receptors)2002European journal of pharmacology, Mar-08, Volume: 438, Issue:3
T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist.
AID614320Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
AID551401Suppression of spontaneous food intake in diet-induced obese C57BL/6 mouse model at 30 mg/kg, po after 24 hrs2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
AID630087Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells2011Bioorganic & medicinal chemistry, Nov-01, Volume: 19, Issue:21
Melanin-concentrating hormone receptor 1 antagonists: synthesis, structure-activity relationship, docking studies, and biological evaluation of 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
AID614321Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
AID239711Displacement of [125I]MCH from human Melanin-concentrating hormone 1 (MCH1) receptor modified for optimal expression in HEK293 cells2005Bioorganic & medicinal chemistry letters, Feb-15, Volume: 15, Issue:4
Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists.
AID614322Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
AID242077Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells2004Journal of medicinal chemistry, Jul-29, Volume: 47, Issue:16
A virtual screening approach to finding novel and potent antagonists at the melanin-concentrating hormone 1 receptor.
AID242643Concentration required to inhibit binding of [125I]-MCH radioligand to human Melanin-concentrating hormone receptor 1 in IMR-32 I3.4.2 cell membranes2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
AID248949Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader2004Bioorganic & medicinal chemistry letters, Oct-04, Volume: 14, Issue:19
Synthesis and evaluation of 2-amino-8-alkoxy quinolines as MCHr1 antagonists. Part 2.
AID252268Suppression of Melanin concentrating hormone receptor-stimulated food intake in lean rats after 30 mg/kg dose2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
AID307524Displacement of [125I][Phe13, Tyr19]MCH from human recombinant MCHR1 expressed in CHO cells2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
AID443384Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay2009Bioorganic & medicinal chemistry letters, Nov-01, Volume: 19, Issue:21
Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation.
AID551220Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists.
AID614324Antiobesity activity in KKAy mouse assessed as inhibition of food intake at 30 mg/kg, po after 2 hrs2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
AID353587Antagonist activity at MCH1R by [35S]GTPgammaS binding assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's12 (75.00)29.6817
2010's4 (25.00)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: 11.49

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 Index11.49 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index4.32 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.49)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (6.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (93.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]