Page last updated: 2024-12-07

melanotan-ii

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

Description

Melanotan-II, also known as MT-II, is a synthetic analog of the naturally occurring hormone α-melanocyte-stimulating hormone (α-MSH). It is a potent stimulator of melanogenesis, the process of melanin production in the skin. Melanotan-II is typically synthesized through a chemical process involving peptide synthesis techniques.

Research on Melanotan-II is primarily focused on its potential therapeutic applications:

* **Tanning:** Melanotan-II promotes melanin production, leading to tanning without sun exposure.
* **Skin Cancer Prevention:** Research suggests that melanotan-II might offer some protection against skin cancer by increasing melanin levels.
* **Erectile Dysfunction:** Some studies have shown that Melanotan-II can improve erectile function in men.
* **Other Potential Applications:** Research is ongoing to explore its potential use in treating conditions like obesity, depression, and inflammation.

However, it's important to note that Melanotan-II is not approved for medical use in most countries. Its use carries potential risks, including:

* **Side Effects:** Common side effects include nausea, vomiting, flushing, and darkening of the skin.
* **Safety Concerns:** There are concerns about the long-term effects of Melanotan-II use, and it can interact with certain medications.

Therefore, Melanotan-II should only be used under the supervision of a qualified healthcare professional.'

melanotan-II: synthetic cyclic heptapeptide, an analog of alpha-melanotropin (4,10); capable of stimulating melanin synthesis & promoting rapid tanning of skin; currently in trials for use in the prevention of sunlight-induced skin cancer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID92432
CHEMBL ID430239
CHEBI ID195326
SCHEMBL ID1047531
MeSH IDM0212250

Synonyms (35)

Synonym
mtii
(3s,6s,9r,12s,15s,23s)-9-benzyl-6-{3-[(diaminomethylidene)amino]propyl}-15-[(2s)-2-acetamidohexanamido]-12-(1h-imidazol-5-ylmethyl)-3-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide
gtpl1323
melanotan ii
melanotan-ii
l-lysinamide, n-acetyl-l-norleucyl-l-alpha-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-, cyclic (2-7)-peptide
NCGC00167281-01
bdbm50184359
ebi_340792
(3s,6s,9r,12s,15s,23s)-15-((s)-2-acetylamino-hexanoylamino)-9-benzyl-6-(3-guanidino-propyl)-12-(3h-imidazol-4-ylmethyl)-3-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18hexaaza-cyclotricosane-23-carboxylic acid amide
melatonan
CHEMBL430239 ,
121062-08-6
mt-ii
CHEBI:195326
(3s,6s,9r,12s,15s,23s)-15-[[(2s)-2-acetamidohexanoyl]amino]-9-benzyl-6-[3-(diaminomethylideneamino)propyl]-12-(1h-imidazol-5-ylmethyl)-3-(1h-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexazacyclotricosane-23-carboxamide
unii-upf5cj93x7
upf5cj93x7 ,
AKOS015994654
SCHEMBL1047531
HS-2017
melanotan ii acetate salt
DTXSID90153135
J-004435
bdbm50027084
(3s,6s,9r,12s,15s,23s)-12-((1h-imidazol-5-yl)methyl)-3-((1h-indol-3-yl)methyl)-15-((s)-2-acetamidohexanamido)-9-benzyl-6-(3-guanidinopropyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide
HY-P0267
melanotan (mt)-ii
melanotanii
(3s,6s,9r,12s,15s,23s)-12-((1h-imidazol-5-yl)methyl)-3-((1h-indol-3-yl)methyl)-15-((s)-2-acetamidohexanamido)-9-benzyl-6-(3-((diaminomethylene)amino)propyl)-2,5,8,11,14,17-hexaoxo-1,4,7,10,13,18-hexaazacyclotricosane-23-carboxamide
Q423855
EX-A7394
l-lysinamide, n-acetyl-l-norleucyl-l-.alpha.-aspartyl-l-histidyl-d-phenylalanyl-l-arginyl-l-tryptophyl-, cyclic (2->7)-peptide
melanotan ii [who-dd]
121062-08-6 (non-salt)

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" This level of sensitivity allowed the determination of pharmacokinetic parameters, following intravenous administration of MT-II in rat."( Determination of melanotan-II in rat plasma by liquid chromatography/tandem mass spectrometry: determination of pharmacokinetic parameters in rat following intravenous administration.
Mock, S; Shen, X; Tamvakopoulos, C, 2002
)
0.65

Bioavailability

ExcerptReferenceRelevance
"Ultrastable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues."( Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
Ahmad Fuaad, A; Bauer, U; Cai, M; Cheneval, O; Craik, DJ; Cromm, PM; Daly, NL; Dellsén, A; Durek, T; Harvey, PJ; Hruby, VJ; Kaas, Q; Kessler, H; Knerr, L; Larsson, N; Österlund, T; Plowright, AT; Schroeder, CI; Weidmann, J; White, AM; Zhou, Y, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" Two subjects had increased pigmentation in the face, upper body and buttock, as measured by quantitative reflectance and by visual perception 1 week after MT-II dosing ended."( Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study.
Brooks, C; Dorr, RT; Hadley, ME; Hruby, VJ; Levine, N; Lines, R; Xiang, L, 1996
)
0.65
" Repetitive once daily oral dosing (0."( Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
Faier, A; Gabinet, Y; Gilon, C; Halbfinger, E; Haskell-Luevano, C; Hess, S; Hoffman, A; Lapidot, T; Linde, Y; Ovadia, O; Portillo, FP; Safrai, E; Shalev, DE; Swed, A; Winkler, I; Xiang, Z; Yarden, D, 2008
)
0.35
" She appeared assured in the self-administration of double dosage and self-management of nausea with benzodiazepines and by injecting before sleep."( An in-depth case examination of an exotic dancer's experience of melanotan.
Brennan, R; Van Hout, MC, 2014
)
0.4
" There are questions regarding the preparation, administration, and dosage of these substances."( Risks of unregulated use of alpha-melanocyte-stimulating hormone analogues: a review.
Bergman, W; Habbema, L; Halk, AB; Neumann, M, 2017
)
0.46
" Emergent themes included motivation for MT II use, misinformation in the context of using an unregulated product, product preparation and administration, dosing regimens, sunbed use, side effects and concerning practices associated with MT II use."( Melanotan II User Experience: A Qualitative Study of Online Discussion Forums.
Daly, S; Gilhooley, E; McKenna, D, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny molecular entity that contains carbon.
[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 (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Melanocortin receptor 4Homo sapiens (human)IC50 (µMol)0.00200.00020.64136.1900AID109118; AID109131; AID1202971; AID1271083; AID1369752; AID1424720; AID1902920; AID261681; AID272314; AID274311; AID312471; AID375545; AID597029
Melanocortin receptor 4Homo sapiens (human)Ki0.00090.00000.30864.8860AID1480165; AID1743780; AID1812562; AID1852336
Melanocortin receptor 5Homo sapiens (human)IC50 (µMol)0.01240.00091.25669.5180AID109429; AID1202975; AID1271084; AID1369755; AID1424724; AID1480166; AID1812563; AID1852340; AID1902921; AID261682; AID272315; AID274312; AID312478; AID375546; AID597030
Melanocortin receptor 3Homo sapiens (human)IC50 (µMol)0.00340.00120.01660.0832AID108794; AID1202967; AID1271082; AID1369749; AID1424716; AID1902919; AID261680; AID272313; AID274310; AID312470; AID375544; AID597028
Melanocortin receptor 3Homo sapiens (human)Ki0.01240.00010.24522.8650AID1480164; AID1743779; AID1812561; AID1852335
Melanocyte-stimulating hormone receptorHomo sapiens (human)IC50 (µMol)0.00110.00010.03760.6150AID108612; AID108616; AID108619; AID1202963; AID1239144; AID1271081; AID1369747; AID1424713; AID1902918; AID261679; AID272312; AID274309; AID312469; AID375543; AID597027
Melanocyte-stimulating hormone receptorHomo sapiens (human)Ki0.00010.00000.00650.0370AID1480163; AID1812560; AID1852334
[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)
Melanocortin receptor 4Homo sapiens (human)EC50 (µMol)0.00280.00000.09112.6000AID108959; AID108967; AID108968; AID1202973; AID1271087; AID1369753; AID1424722; AID1476414; AID1476420; AID1480174; AID1480175; AID1743775; AID1812559; AID1812567; AID1852339; AID1902925; AID261685; AID272318; AID274320; AID312474; AID375549; AID597021
Melanocortin receptor 5Homo sapiens (human)EC50 (µMol)0.00770.00020.16154.4000AID109298; AID109597; AID1202977; AID1271088; AID1369757; AID1424726; AID1476417; AID1902927; AID261686; AID272319; AID274319; AID312479; AID375550; AID597022
Melanocortin receptor 3Mus musculus (house mouse)EC50 (µMol)0.00020.00010.28575.4000AID109614; AID109617; AID1169943; AID1202906; AID240040; AID282351
Melanocortin receptor 5Mus musculus (house mouse)EC50 (µMol)0.00020.00000.03211.4900AID107044; AID107046; AID1169945; AID1202905; AID240042; AID282355
Melanocortin receptor 3Homo sapiens (human)EC50 (µMol)0.00630.00010.01270.2480AID108778; AID108779; AID109594; AID1202969; AID1271086; AID1369750; AID1424718; AID1476411; AID1480173; AID1743773; AID1812558; AID1852338; AID1902923; AID261684; AID272317; AID274318; AID312473; AID375548; AID597020
Urotensin-2 receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00330.00300.00320.0033AID375550
Melanocortin receptor 4Mus musculus (house mouse)EC50 (µMol)0.00010.00000.12472.4700AID107033; AID107035; AID1169944; AID1202911; AID240041; AID282353
Melanocyte-stimulating hormone receptorHomo sapiens (human)EC50 (µMol)0.00610.00000.00800.2280AID108474; AID108482; AID108603; AID108604; AID1202965; AID1239146; AID1271085; AID1369748; AID1424714; AID1480172; AID1812557; AID1852337; AID1902916; AID261683; AID272316; AID274317; AID312472; AID375547; AID596854; AID71942
Melanocyte-stimulating hormone receptorMus musculus (house mouse)EC50 (µMol)0.00010.00000.30047.6900AID109599; AID109602; AID1169942; AID1202904; AID240039; AID282350
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
diet induced thermogenesisMelanocortin receptor 4Homo sapiens (human)
energy reserve metabolic processMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 4Homo sapiens (human)
feeding behaviorMelanocortin receptor 4Homo sapiens (human)
insulin secretionMelanocortin receptor 4Homo sapiens (human)
response to insulinMelanocortin receptor 4Homo sapiens (human)
positive regulation of bone resorptionMelanocortin receptor 4Homo sapiens (human)
regulation of eating behaviorMelanocortin receptor 4Homo sapiens (human)
response to melanocyte-stimulating hormoneMelanocortin receptor 4Homo sapiens (human)
negative regulation of feeding behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of grooming behaviorMelanocortin receptor 4Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 5Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 5Homo sapiens (human)
regulation of heart rateMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocortin receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayMelanocortin receptor 3Homo sapiens (human)
regulation of blood pressureMelanocortin receptor 3Homo sapiens (human)
circadian regulation of gene expressionMelanocortin receptor 3Homo sapiens (human)
homoiothermyMelanocortin receptor 3Homo sapiens (human)
locomotor rhythmMelanocortin receptor 3Homo sapiens (human)
sodium ion homeostasisMelanocortin receptor 3Homo sapiens (human)
regulation of feeding behaviorMelanocortin receptor 3Homo sapiens (human)
regulation of metabolic processMelanocortin receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelanocyte-stimulating hormone receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV protectionMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase A signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
sensory perception of painMelanocyte-stimulating hormone receptorHomo sapiens (human)
negative regulation of tumor necrosis factor productionMelanocyte-stimulating hormone receptorHomo sapiens (human)
intracellular signal transductionMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanin biosynthetic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
pigmentationMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIMelanocyte-stimulating hormone receptorHomo sapiens (human)
UV-damage excision repairMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of protein kinase C signalingMelanocyte-stimulating hormone receptorHomo sapiens (human)
positive regulation of feeding behaviorMelanocyte-stimulating hormone receptorHomo sapiens (human)
regulation of metabolic processMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
melanocortin receptor activityMelanocortin receptor 4Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 4Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 4Homo sapiens (human)
ubiquitin protein ligase bindingMelanocortin receptor 4Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 4Homo sapiens (human)
protein bindingMelanocortin receptor 5Homo sapiens (human)
hormone bindingMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 5Homo sapiens (human)
melanocortin receptor activityMelanocortin receptor 3Homo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocortin receptor 3Homo sapiens (human)
protein bindingMelanocortin receptor 3Homo sapiens (human)
neuropeptide bindingMelanocortin receptor 3Homo sapiens (human)
peptide hormone bindingMelanocortin receptor 3Homo sapiens (human)
melanocortin receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
melanocyte-stimulating hormone receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
protein bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
G protein-coupled peptide receptor activityMelanocyte-stimulating hormone receptorHomo sapiens (human)
ubiquitin protein ligase bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
hormone bindingMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneMelanocortin receptor 4Homo sapiens (human)
membraneMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 4Homo sapiens (human)
cytoplasmMelanocortin receptor 4Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 5Homo sapiens (human)
cytoplasmMelanocortin receptor 5Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
cytoplasmMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocortin receptor 3Homo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
plasma membraneMelanocyte-stimulating hormone receptorHomo sapiens (human)
cytoplasmMelanocyte-stimulating hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (248)

Assay IDTitleYearJournalArticle
AID1902918Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in HEK293 cells by competitive binding assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1239147Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP at 10 uM by luminescence counting relative to MT-II2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
AID1743773Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1902923Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID108616Inhibitory concentration against human Melanocortin 1 receptor (hMC1R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID261679Inhibitory activity against hMC1R transfected in HEK293 cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID109131Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID282350Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID375549Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID261685Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID1169942Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1202911Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID108959Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID375546Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID272317Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID272314Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID107387Metabotropic potency against Rana pipiens using frog skin bioassay; effect continued after the removal of the compound1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Potent and prolonged acting cyclic lactam analogues of alpha-melanotropin: design based on molecular dynamics.
AID1424717Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID1202967Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1480173Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID101999Activity expressed as EC50 was measured in lizard.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID1169945Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1271087Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID1271083Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID240039Effective concentration for mouse Melanocortin-1 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID1169951Selectivity index, ratio of EC50 for mouse MC5R to EC50 for mouse MC1R2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1202975Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1369747Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1202906Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID274317Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1424716Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID272313Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID102011Decrease in lizard skin reflectivity (metabotropic activity).1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID102005Potency of compound was measured in lizard where (+) indicates peptide is prolonged acting.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID1476413Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1424713Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting analysis2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID102013Relative potency compared to alpha MSH in a lizard skin bioassay.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID1812562Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID597028Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID108779Effective concentration required for the biological activity against human Melanocortin 3 receptor2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID1424718Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID312478Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID108968Effective concentration required for the biological activity against human Melanocortin 4 receptor2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID1369748Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1812561Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1902924Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1271082Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID1812559Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID597022Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID1271084Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID20351Relative rate determined by setting MTII equal to 1 and dividing the apparent k-1 by the MTII value1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID274309Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in HEK293 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1169943Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1202969Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID109594Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID71942Decrease in frog skin reflectivity (metabotropic activity).1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID1369750Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1902927Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1480172Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1743775Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1743780Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1902916Agonist activity at human MC1R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1476419Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1480164Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID9405Biological activity using the lizard skin (Anolis carolinensis) assay. The value indicates prolonged biological activity2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID1424721Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID108967Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID272326Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1812563Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852344Selectivity ratio of EC50 for human MC4R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID108482Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID1424722Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID107044Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID108603Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID274319Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID240041Effective concentration for mouse Melanocortin-4 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID108627Relative potency of compound for EC50 against Melanocortin 1 receptor transfected into L-cells was determined with respect to EC50 of MTII1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID1743779Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID312480Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT22008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID375547Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1480166Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID272319Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1202976Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID109617Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID1369757Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1202974Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1852334Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID15831Dissociation rate calculated from the first-order equation using the t1/2 value1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID1202909Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID107046Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID1743778Selectivity index, ratio of EC50 for agonist activity at human MC4R expressed in HEK293 cells to IC50 for agonist activity at human MC3R expressed in HEK293 cells2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID274321Activity at human MC1R expressed in HEK293 cells assessed as activation of adenylate cyclase2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1852343Selectivity ratio of EC50 for human MC3R to EC50 for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1202964Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1743774Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID23339Relative rate determined by setting MTII equal to 1 and dividing the apparent k-1 by the MTII value1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID1169950Selectivity index, ratio of EC50 for mouse MC3R to EC50 for mouse MC1R2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID312476Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT22008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID107389Metabotropic potency against Anolis carolinensis using lizard skin bioassay; effect continued after the removal of the compound1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Potent and prolonged acting cyclic lactam analogues of alpha-melanotropin: design based on molecular dynamics.
AID261686Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID25897Half-life determined by extrapolation of the slope until 50% of the peptide was bound relative to the specific binding1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID1476420Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID108628Relative potency for inhibition of Melanocortin 1 receptor was determined relative to IC50 of MTII compound1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID109614Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID1902921Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID596854Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID321788Decrease in rat weight after 4 weeks2008Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity.
AID261681Inhibitory activity against hMC4R transfected in HEK293 cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID108612Binding affinity towards human melanocortin receptor (hMC1R) using NDP-MSH as radioligand2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID1202973Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1852338Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID274322Activity at human MC3R expressed in HEK293 cells assessed as activation of adenylate cyclase2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID109599Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID312474Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1424726Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID1202963Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1271085Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID274310Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID312469Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC1 receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1424720Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID1239144Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
AID274318Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1271088Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID71945Relative potency compared to alpha MSH in a frog skin bioassay.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
AID261683Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID274312Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID282355Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID1476421Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1852336Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID1476411Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID282351Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID272322Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1424724Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID312473Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID375552Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH22009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1902925Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1902919Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID240040Effective concentration for mouse Melanocortin-3 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID272323Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1202977Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID375554Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH22009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID312471Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1202968Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1271081Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID1902922Agonist activity at human MC1R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID261684Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID1202905Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1424712Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC1R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID1743776Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay relative to control2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID1812567Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID597027Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID272327Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1202965Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1480163Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1369752Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID108794Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1202972Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID282353Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay2004Journal of medicinal chemistry, Dec-30, Volume: 47, Issue:27
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
AID108479Relative potency against Melanocortin 1 receptor of frog skin with respect to MTII as standard1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID312475Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT22008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID163323Biological activity using the frog skin (Rana pipiens) assay. The value indicates prolonged biological activity2003Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID1424725Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID375545Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID109298Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1480174Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID597021Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID107035Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID109118Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID108619The concentration that inhibits 50% specific binding was determined against the Melanocortin 1 receptor1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID1239145Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC1 receptor expressed in A375 cells at 10 uM after 40 mins by luminescence counting relative to control2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
AID1743781Selectivity index, ratio of Ki for human MC3R expressed in HEK293 cell membranes to Ki for human MC4R expressed in HEK293 cell membranes2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID272312Displacement of [125I]NDP-alphaMSH from human MC1 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID240042Effective concentration for mouse Melanocortin-5 receptor2005Journal of medicinal chemistry, Apr-21, Volume: 48, Issue:8
Structure-activity relationships of the unique and potent agouti-related protein (AGRP)-melanocortin chimeric Tyr-c[beta-Asp-His-DPhe-Arg-Trp-Asn-Ala-Phe-Dpr]-Tyr-NH2 peptide template.
AID1902920Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID1202966Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID375551Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH22009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1476417Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1202913Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID1852337Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID108474Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.1995Journal of medicinal chemistry, Nov-10, Volume: 38, Issue:23
Topographical modification of melanotropin peptide analogues with beta-methyltryptophan isomers at position 9 leads to differential potencies and prolonged biological activities.
AID272318Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID261682Inhibitory activity against hMC5R transfected in HEK293 cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID274320Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID274323Activity at human MC5R expressed in HEK293 cells assessed as activation of adenylate cyclase2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1202971Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID1239146Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting2015Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors.
AID1480175Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID272316Activity at hMC1R transfected in HEK293 cells assessed as intracellular cAMP accumulation2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID597030Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID1169947Selectivity index, ratio of EC50 for mouse MC3R to EC50 for mouse MC4R2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID108604Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1369749Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1812557Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID108778Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1852335Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID272325Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1169946Selectivity index, ratio of EC50 for mouse MC1R to EC50 for mouse MC4R2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1369753Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID1271086Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX2015Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor.
AID1202970Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID274311Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID1852342Selectivity ratio of Ki for human MC4R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID71797Activity expressed as EC50 was measured in frog.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID1743777Selectivity index, ratio of EC50 for agonist activity at human MC3R expressed in HEK293 cells to IC50 for agonist activity at human MC4R expressed in HEK293 cells2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†.
AID375553Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH22009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1852339Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID597020Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID375544Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID312472Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1812560Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID597029Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
AID375548Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID109597Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation2003Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
AID1202978Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
AID272324Activity at hMC1R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1476416Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID71815Potency measured in frog where (+) indicates peptide is long acting.1995Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID1169944Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay2014Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity.
AID1476414Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay2017Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21
Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID375543Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC1R expressed in HEK293 cells2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1424714Agonist activity at human MC1R expressed in HEK293 cells after 3 mins by cAMP assay2018European journal of medicinal chemistry, May-10, Volume: 151Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH
AID312477Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT22008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1902917Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID109429Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Biological and conformational examination of stereochemical modifications using the template melanotropin peptide, Ac-Nle-c[Asp-His-Phe-Arg-Trp-Ala-Lys]-NH2, on human melanocortin receptors.
AID1852340Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID312470Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID274324Activity at human MC4R expressed in HEK293 cells assessed as activation of adenylate cyclase2006Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors.
AID272315Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1902926Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists.
AID272321Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID261680Inhibitory activity against hMC3R transfected in HEK293 cells2006Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
AID312479Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor.
AID1480165Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay2018Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
AID1369755Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors.
AID107033Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells2002Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-D-Phe-Arg-Trp-NH2 at the mouse melanocortin receptors. 4. Modifications at the Trp position.
AID375550Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level2009Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor.
AID1202904Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
AID272320Displacement of [125I]NDP-alphaMSH from human MC1 receptor expressed in HEK293 cells relative to MT22006Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor.
AID1812558Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay2021Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
AID1852341Selectivity ratio of Ki for human MC3R to Ki for human MC1R2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists.
AID109602Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors: part 2 modifications at the Phe position.
AID1346171Human MC4 receptor (Melanocortin receptors)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID1346231Human MC1 receptor (Melanocortin receptors)2002European journal of pharmacology, Apr-12, Volume: 440, Issue:2-3
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
AID1346180Human MC5 receptor (Melanocortin receptors)2002European journal of pharmacology, Apr-12, Volume: 440, Issue:2-3
The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.
AID1346171Human MC4 receptor (Melanocortin receptors)1999European journal of pharmacology, Aug-13, Volume: 378, Issue:3
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
AID1346178Human MC3 receptor (Melanocortin receptors)1999European journal of pharmacology, Aug-13, Volume: 378, Issue:3
Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat.
AID1346231Human MC1 receptor (Melanocortin receptors)1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID1346171Human MC4 receptor (Melanocortin receptors)2000Biochemistry, Dec-05, Volume: 39, Issue:48
Molecular determinants of ligand binding to the human melanocortin-4 receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (193)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902 (1.04)18.7374
1990's14 (7.25)18.2507
2000's86 (44.56)29.6817
2010's71 (36.79)24.3611
2020's20 (10.36)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 86.10

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index86.10 (24.57)
Research Supply Index5.30 (2.92)
Research Growth Index5.62 (4.65)
Search Engine Demand Index159.61 (26.88)
Search Engine Supply Index2.12 (0.95)

This Compound (86.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (2.04%)5.53%
Reviews9 (4.59%)6.00%
Case Studies17 (8.67%)4.05%
Observational1 (0.51%)0.25%
Other165 (84.18%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]