alpha-msh profile

ID Source	ID
PubMed CID	16133793
CHEBI ID	195325
SCHEMBL ID	20548027
SCHEMBL ID	22076809
MeSH ID	M0000797

Synonym
l-valinamide, n-acetyl-l-seryl-l-tyrosyl-l-seryl-l-methionyl-l-glutamyl-l-histidyl-l-phenylalanyl-l-arginyl-l-tryptophylglycyl-l-lysyl-l-prolyl-
ba 33761
unii-ovf025la77
ovf025la77 ,
alpha-intermedin
581-05-5
alpha-melanotropin (pig)
alpha-1-13-corticotropin, n-acetyl-13-l-valinamide-
alpha-melanotropin (macaca nemestrina)
alpha-melanotropin i (oncorhynchus keta)
alpha-melanotropin (ox)
alpha-melanotropin (swine)
alpha-melanotropin (human)
9002-79-3
melanotropin
.alpha.-melanotropin (ox)
.alpha.-msh
melantropin
n-acetyl-acth(1-13)-amide
.alpha.-melanotropin
.alpha.-melanotropin (sheep)
.alpha.-melanotropin (human)
melanotropin alpha
ac-l-ser-l-tyr-l-ser-l-met-l-glu-l-his-l-phe-l-arg-l-trp-gly-l-lys-l-pro-l-val-nh2
intermedin
n-ac-l-ser-l-tyr-l-ser-l-met-l-glu-l-his-l-phe-l-arg-l-trp-gly-l-lys-l-pro-l-val-nh2
n-acetyl-l-ser-l-tyr-l-ser-l-met-l-alpha-glu-l-his-l-phe-l-arg-l-trp-gly-l-lys-l-pro-l-valinamide
CHEBI:195325
active principle of the pars intermedia of the pituitary
.alpha.-melanotropin [mi]
valinamide, acetyl-l-seryl-l-tyrosyl-l-seryl-l-methionyl-l-glutamyl-l-histidyl-l-phenylalanyl-l-arginyl-l-tryptophyl-glycyl-l-lysyl-l-prolyl-, l-
intermedine [inn]
?-melanotropin
?-msh
AKOS024457181
czen-002
AS-57738
SCHEMBL20548027
SCHEMBL22076809

Excerpt	Relevance	Reference
" Ac-[Cys4,Cys10]-alpha-MSH4-12-NH2 (IV) was considerably more potent than the cyclic 4-11 melanotropin and was, in fact, equipotent or even slightly more potent than [Cys4,Cys10]-alpha-MSH and Ac-[Cys4,Cys10]-alpha-MSH4-13-NH2 over the linear portion of the dose-response in all three bioassays."	( Cyclic melanotropins. 5. Importance of the C-terminal tripeptide (Lys-Pro-Val). Castrucci, AM; Cody, WL; Hadley, ME; Hruby, VJ; Muska, BJ; Wilkes, BC, 1984)	0.61
" The biological activities of these derivatives were measured and compared on normal melanocytes (frog skins) and on transformed melanocytes (mouse melanoma adenylate cyclase), over the entire dose-response range."	( Synthesis and structure-function studies of melanocyte stimulating hormone analogues modified in the 2 and 4(7) positions: comparison of activities on frog skin melanophores and melanoma adenylate cyclase. Bregman, MD; Hadley, ME; Heward, CB; Hruby, VJ; Sawyer, TK; Yang, YC, 1980)	0.26

Role	Description
anti-inflammatory agent	Any compound that has anti-inflammatory effects.
[role 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]

Class	Description
peptide hormone	Any peptide with hormonal activity in animals, whether endocrine, neuroendocrine, or paracrine.
[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	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Melanocortin receptor 4	Homo sapiens (human)	IC50 (µMol)	0.0176	0.0002	0.6413	6.1900	AID109128; AID109131; AID242142; AID242174; AID242411; AID242739
Melanocortin receptor 4	Homo sapiens (human)	Ki	0.0846	0.0000	0.3086	4.8860	AID259534; AID259535; AID259536; AID259537; AID259538; AID259539; AID259540; AID259541; AID259542; AID259543; AID473160; AID677161
Melanocortin receptor 5	Homo sapiens (human)	IC50 (µMol)	0.1777	0.0009	1.2566	9.5180	AID109428; AID109429; AID240566; AID242740
Melanocortin receptor 5	Homo sapiens (human)	Ki	0.1500	0.0005	3.5265	8.9290	AID677160
Melanocortin receptor 3	Homo sapiens (human)	IC50 (µMol)	0.0323	0.0012	0.0166	0.0832	AID108792; AID108794; AID242173; AID242738
Melanocortin receptor 3	Homo sapiens (human)	Ki	0.0460	0.0001	0.2452	2.8650	AID677159
Melanocyte-stimulating hormone receptor	Homo sapiens (human)	IC50 (µMol)	0.0032	0.0001	0.0376	0.6150	AID108616; AID242172
Melanocyte-stimulating hormone receptor	Homo sapiens (human)	Ki	0.0015	0.0000	0.0065	0.0370	AID677158
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Gamma-aminobutyric acid receptor subunit alpha-2	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0008	0.0001	1.4693	7.0000	AID109615
Adenosine receptor A2a	Rattus norvegicus (Norway rat)	EC50 (µMol)	0.0021	0.0000	0.1156	0.7200	AID246687
Melanocortin receptor 4	Homo sapiens (human)	EC50 (µMol)	0.0202	0.0000	0.0911	2.6000	AID108957; AID108965; AID108968; AID108970; AID108971; AID109462; AID1151513; AID1476414; AID1476420; AID246241; AID246372; AID246687; AID246736; AID259544; AID259545; AID259546; AID259547; AID259548; AID259549; AID259550; AID259551; AID259552; AID259553; AID266581; AID473151; AID677162
Melanocortin receptor 5	Homo sapiens (human)	EC50 (µMol)	0.0614	0.0002	0.1615	4.4000	AID109296; AID109302; AID1476417; AID246242; AID246373; AID246688; AID246737; AID473157
Melanocortin receptor 3	Mus musculus (house mouse)	EC50 (µMol)	0.0769	0.0001	0.2857	5.4000	AID108938; AID108939; AID109614; AID109615; AID109617; AID109618; AID1229381; AID1253333; AID1296535; AID1547511; AID221832; AID240040; AID240052; AID282351; AID320926; AID447386
Melanocortin receptor 5	Mus musculus (house mouse)	EC50 (µMol)	0.0886	0.0000	0.0321	1.4900	AID107044; AID107045; AID107046; AID107047; AID109445; AID109446; AID109449; AID1229385; AID1253335; AID1296537; AID1547516; AID221835; AID240042; AID240054; AID282355; AID320928; AID447388
Melanocortin receptor 3	Homo sapiens (human)	EC50 (µMol)	0.0039	0.0001	0.0127	0.2480	AID108777; AID108779; AID108781; AID108782; AID1476411; AID246240; AID246371; AID246686; AID246735; AID473154
Melanocortin receptor 4	Mus musculus (house mouse)	EC50 (µMol)	0.1499	0.0000	0.1247	2.4700	AID107033; AID107034; AID107035; AID107037; AID109276; AID109277; AID109281; AID1229383; AID1253334; AID1296536; AID1547514; AID221834; AID240041; AID240053; AID282353; AID320927; AID447387
Melanocyte-stimulating hormone receptor	Homo sapiens (human)	EC50 (µMol)	0.0006	0.0000	0.0080	0.2280	AID108474; AID108475; AID108481; AID108605; AID108606; AID108607; AID108608; AID108609; AID109453; AID246685; AID266580; AID473155; AID71942
Melanocyte-stimulating hormone receptor	Mus musculus (house mouse)	EC50 (µMol)	0.0196	0.0000	0.3004	7.6900	AID108633; AID108635; AID108636; AID108639; AID109599; AID109601; AID109602; AID1229379; AID1253332; AID1296534; AID1547509; AID221830; AID240039; AID240051; AID282350; AID320925; AID447385
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
diet induced thermogenesis	Melanocortin receptor 4	Homo sapiens (human)
energy reserve metabolic process	Melanocortin receptor 4	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Melanocortin receptor 4	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Melanocortin receptor 4	Homo sapiens (human)
feeding behavior	Melanocortin receptor 4	Homo sapiens (human)
insulin secretion	Melanocortin receptor 4	Homo sapiens (human)
response to insulin	Melanocortin receptor 4	Homo sapiens (human)
positive regulation of bone resorption	Melanocortin receptor 4	Homo sapiens (human)
regulation of eating behavior	Melanocortin receptor 4	Homo sapiens (human)
response to melanocyte-stimulating hormone	Melanocortin receptor 4	Homo sapiens (human)
negative regulation of feeding behavior	Melanocortin receptor 4	Homo sapiens (human)
regulation of grooming behavior	Melanocortin receptor 4	Homo sapiens (human)
regulation of metabolic process	Melanocortin receptor 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Melanocortin receptor 5	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Melanocortin receptor 5	Homo sapiens (human)
regulation of metabolic process	Melanocortin receptor 5	Homo sapiens (human)
regulation of heart rate	Melanocortin receptor 3	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Melanocortin receptor 3	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Melanocortin receptor 3	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Melanocortin receptor 3	Homo sapiens (human)
regulation of blood pressure	Melanocortin receptor 3	Homo sapiens (human)
circadian regulation of gene expression	Melanocortin receptor 3	Homo sapiens (human)
homoiothermy	Melanocortin receptor 3	Homo sapiens (human)
locomotor rhythm	Melanocortin receptor 3	Homo sapiens (human)
sodium ion homeostasis	Melanocortin receptor 3	Homo sapiens (human)
regulation of feeding behavior	Melanocortin receptor 3	Homo sapiens (human)
regulation of metabolic process	Melanocortin receptor 3	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathway	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
UV protection	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
positive regulation of protein kinase A signaling	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
sensory perception of pain	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
negative regulation of tumor necrosis factor production	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
intracellular signal transduction	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
melanin biosynthetic process	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
pigmentation	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
UV-damage excision repair	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
positive regulation of protein kinase C signaling	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
positive regulation of feeding behavior	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
regulation of metabolic process	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled adenosine receptor activity	Adenosine receptor A2a	Rattus norvegicus (Norway rat)
melanocortin receptor activity	Melanocortin receptor 4	Homo sapiens (human)
melanocyte-stimulating hormone receptor activity	Melanocortin receptor 4	Homo sapiens (human)
protein binding	Melanocortin receptor 4	Homo sapiens (human)
peptide hormone binding	Melanocortin receptor 4	Homo sapiens (human)
ubiquitin protein ligase binding	Melanocortin receptor 4	Homo sapiens (human)
neuropeptide binding	Melanocortin receptor 4	Homo sapiens (human)
protein binding	Melanocortin receptor 5	Homo sapiens (human)
hormone binding	Melanocortin receptor 5	Homo sapiens (human)
melanocortin receptor activity	Melanocortin receptor 5	Homo sapiens (human)
melanocortin receptor activity	Melanocortin receptor 3	Homo sapiens (human)
melanocyte-stimulating hormone receptor activity	Melanocortin receptor 3	Homo sapiens (human)
protein binding	Melanocortin receptor 3	Homo sapiens (human)
neuropeptide binding	Melanocortin receptor 3	Homo sapiens (human)
peptide hormone binding	Melanocortin receptor 3	Homo sapiens (human)
melanocortin receptor activity	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
melanocyte-stimulating hormone receptor activity	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
protein binding	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
G protein-coupled peptide receptor activity	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
ubiquitin protein ligase binding	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
hormone binding	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
Golgi membrane	Adenosine receptor A2a	Rattus norvegicus (Norway rat)
plasma membrane	Melanocortin receptor 4	Homo sapiens (human)
membrane	Melanocortin receptor 4	Homo sapiens (human)
plasma membrane	Melanocortin receptor 4	Homo sapiens (human)
cytoplasm	Melanocortin receptor 4	Homo sapiens (human)
plasma membrane	Melanocortin receptor 5	Homo sapiens (human)
plasma membrane	Melanocortin receptor 5	Homo sapiens (human)
cytoplasm	Melanocortin receptor 5	Homo sapiens (human)
plasma membrane	Melanocortin receptor 3	Homo sapiens (human)
cytoplasm	Melanocortin receptor 3	Homo sapiens (human)
plasma membrane	Melanocortin receptor 3	Homo sapiens (human)
plasma membrane	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
plasma membrane	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
cytoplasm	Melanocyte-stimulating hormone receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (228)

Assay ID	Title	Year	Journal	Article
AID266581	Activity at human MC4R by cAMP accumulation in SaoS2 cells	2006	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14	Design of cyclic peptides with agonist activity at melanocortin receptor-4.
AID108777	Effective concentration of peptide at 50% maximal cAMP generation	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID102006	Potency of compound was measured in lizard where (-) indicates peptide is not prolonged acting.	1995	Journal of medicinal chemistry, May-12, Volume: 38, Issue:10	Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID259544	Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID259537	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID246688	Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID473154	Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID245728	Percentage of cAMP accumulation at 10 uM compound relative to alpha-MSH for melanocortin receptor 4	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID1296537	Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID282350	Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay	2004	Journal 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.
AID240039	Effective concentration for mouse Melanocortin-1 receptor	2005	Journal 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.
AID473155	Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID9404	Biological activity using the lizard skin (Anolis carolinensis) assay. The value indicates no prolonged biological activity	2003	Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID108609	In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 1 receptor (hMC1R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID108779	Effective concentration required for the biological activity against human Melanocortin 3 receptor	2003	Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID259545	Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID259538	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID242738	Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID108633	Agonistic activity evaluated at melanocortin 1 receptor (MC1R) of mouse HEK293 cells	2003	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24	Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
AID47399	Inhibition of Candida albicans at 100 uM concentration.	2003	Journal of medicinal chemistry, Feb-27, Volume: 46, Issue:5	Novel alpha-melanocyte stimulating hormone peptide analogues with high candidacidal activity.
AID240051	In vitro agonist potency for Mouse Melanocortin 1 receptor	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID1253335	Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.
AID447388	Agonistic activity against mouse MC5R	2009	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17	Semi-rigid tripeptide agonists of melanocortin receptors.
AID259551	Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID71943	In vitro potency of compound to stimulate melanosome dispersion in frog (Rana pipiens) skin relative to alpha-MSH	1982	Journal of medicinal chemistry, Sep, Volume: 25, Issue:9	Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID246685	Effective concentration for intracellular cAMP accumulation in human melanocortin 1 receptor expressing HEK 293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108639	Evaluated for agonist activity against mouse Melanocortin 1 receptor using mMC1R assay	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID252624	Maximal effect on human melanocortin 4 receptor expressing HEK 293 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID252965	Concentration of compound at 50% maximum cAMP accumulation at human melanocortin-4 receptor	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID259552	Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID71819	Potency in the frog (Rana pipiens) skin bioassay relative to alpha-MSH	1985	Journal of medicinal chemistry, May, Volume: 28, Issue:5	Cyclic melanotropins. 9. 7-D-Phenylalanine analogues of the active-site sequence.
AID107390	Metabotropic potency against Anolis carolinensis using lizard skin bioassay; effect did not continue after the removal of the compound	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	Potent and prolonged acting cyclic lactam analogues of alpha-melanotropin: design based on molecular dynamics.
AID71948	Residual activity in lizard skin; p(-)	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID242739	Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID71945	Relative potency compared to alpha MSH in a frog skin bioassay.	1997	Journal 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.
AID252275	Maximum percent cAMP accumulation mediated by human melanocortin 4 receptor relative to alpha-MSH (1.9%) at 10 uM concentration	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID108608	Evaluated for agonist at cloned mammalian Melanocortin 1 receptor in frog (Rana pipiens) skin assay	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID252623	Maximal effect on human melanocortin 3 receptor expressing HEK 293 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID259549	Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108479	Relative potency against Melanocortin 1 receptor of frog skin with respect to MTII as standard	1995	Journal 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.
AID108475	Effective concentration required for maximum agonist response at melanocortin 1 receptor from frog skin.	2004	Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6	De novo design, synthesis, and pharmacology of alpha-melanocyte stimulating hormone analogues derived from somatostatin by a hybrid approach.
AID320926	Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.
AID108781	Evaluated for agonist activity at cloned Melanocortin 3 receptor	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID473153	Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay relative to melanocortin 2	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID259540	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID107046	Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)	2002	Journal 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.
AID1253333	Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.
AID266583	Selectivity for human MC4R over MC1R	2006	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14	Design of cyclic peptides with agonist activity at melanocortin receptor-4.
AID259534	Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID71944	Relative potency using frog skin bioassay system	1980	Journal of medicinal chemistry, Dec, Volume: 23, Issue:12	Synthesis and structure-function studies of melanocyte stimulating hormone analogues modified in the 2 and 4(7) positions: comparison of activities on frog skin melanophores and melanoma adenylate cyclase.
AID447387	Agonistic activity against mouse MC4R	2009	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17	Semi-rigid tripeptide agonists of melanocortin receptors.
AID259543	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109276	Compound was evaluated for its agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells	2003	Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12	Urea small molecule agonists on mouse melanocortin receptors.
AID109277	Effective concentration against mouse melanocortin MC4 receptor	2004	Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9	Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID1476413	Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID246737	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID108606	Evaluated for agonist activity against human Melanocortin 1 receptor using hMC1-R assay	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID108782	In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 3 receptor (hMC3R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID108794	Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)	1997	Journal 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.
AID677162	Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID71797	Activity expressed as EC50 was measured in frog.	1995	Journal of medicinal chemistry, May-12, Volume: 38, Issue:10	Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID1296535	Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID1229381	Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	2015	ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5	Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
AID102016	Residual activity in lizard skin; p(-)	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID252625	Maximal effect on human melanocortin 5 receptor expressing HEK 293 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108605	Effective concentration required for the biological activity against human Melanocortin 1 receptor	2003	Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID259546	Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID240054	In vitro agonist potency for Mouse Melanocortin 5 receptor	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID108952	Percent activation of human melanocortin receptor human Melanocortin 4 receptor was determined at 10 uM	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID107047	Agonistic activity evaluated at melanocortin 5 receptor (MC5R) of mouse HEK293 cells	2003	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24	Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
AID109602	Agonist activity to the mouse Melanocortin-1 receptor (mMC1R)	2002	Journal 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.
AID252273	Maximum percent cAMP accumulation mediated by human melanocortin 5 receptor relative to alpha-MSH (17%) at 10 uM concentration	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID1151513	Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID168702	Ability to stimulate melanosome dispersion in vitro in the frog skin activity measured relative to alpha-MSH	1984	Journal of medicinal chemistry, Sep, Volume: 27, Issue:9	Cyclic melanotropins. 5. Importance of the C-terminal tripeptide (Lys-Pro-Val).
AID108971	In vitro cAMP accumulation in HEK cells transfected with human melanocortin receptor-4 (hMC4R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID282353	Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay	2004	Journal 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.
AID252964	Concentration of compound at 50% maximum cAMP accumulation at human melanocortin-3 receptor	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID101998	Potency in the lizard (Anolis carolinensis) skin bioassay relative to alpha-MSH	1985	Journal of medicinal chemistry, May, Volume: 28, Issue:5	Cyclic melanotropins. 9. 7-D-Phenylalanine analogues of the active-site sequence.
AID199132	Adenylate cyclase activity in vitro in the membrane fraction from S-91 mouse melanoma tumors activity measured relative to alpha-MSH	1984	Journal of medicinal chemistry, Sep, Volume: 27, Issue:9	Cyclic melanotropins. 5. Importance of the C-terminal tripeptide (Lys-Pro-Val).
AID473152	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay relative to melanocortin 2	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID109281	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 4 receptor (mMC4R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID101999	Activity expressed as EC50 was measured in lizard.	1995	Journal of medicinal chemistry, May-12, Volume: 38, Issue:10	Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID71932	In vitro potency relative to alpha-melanotropin (alpha-MSH), in the frog (Rana pipiens) skin bioassay	1987	Journal of medicinal chemistry, Nov, Volume: 30, Issue:11	alpha-Melanotropin: the minimal active sequence in the frog skin bioassay.
AID221835	Functional activity at the mouse melanocortin 5 receptor	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID259536	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID259535	Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID109617	Agonist activity to the mouse Melanocortin-3 receptor (mMC3R)	2002	Journal 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.
AID109131	Inhibitory concentration against human Melanocortin 4 receptor (hMC4R)	1997	Journal 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.
AID221832	Functional activity at the mouse melanocortin 3 receptor	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID259542	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID108772	In vitro cAMP accumulation in Y1 cells transfected with mouse Melanocortin 2 receptor (mMC2R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID259550	Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID1229383	Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	2015	ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5	Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
AID108629	Binding towards human Melanocortin 1 receptor (hMC1R) relative to alpha-MSH	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID108965	Effective concentration of peptide at 50% maximal cAMP generation	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID240052	In vitro agonist potency for Mouse Melanocortin 3 receptor	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID71816	Potency of compound was measured in frog where (-) indicates peptide is not prolonged acting.	1995	Journal of medicinal chemistry, May-12, Volume: 38, Issue:10	Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
AID246371	Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID1476411	Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID677161	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID107388	Metabotropic potency against Rana pipiens using frog skin bioassay; effect did not continue after the removal of the compound	1989	Journal of medicinal chemistry, Dec, Volume: 32, Issue:12	Potent and prolonged acting cyclic lactam analogues of alpha-melanotropin: design based on molecular dynamics.
AID108474	Effective concentration for the effect of Melanocortin 1 receptor in the frog skin.	1995	Journal 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.
AID34307	In vitro potency of compound to stimulate adenylate cyclase activity in melanoma cells relative to alpha-MSH	1982	Journal of medicinal chemistry, Sep, Volume: 25, Issue:9	Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID109614	Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells	2002	Journal 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.
AID107037	Agonistic activity evaluated at melanocortin 4 receptor (MC4R) of mouse HEK293 cells	2003	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24	Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
AID259548	Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID677159	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID24702	Determination of extrapolation of the slope until 50% of the peptide was bound relative to the specific binding.	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID1151515	Agonist activity at human melanocortin-4 receptor L106P mutant expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response at 1 uM after 6 hrs	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
AID320927	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.
AID259541	Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID240053	In vitro agonist potency for Mouse Melanocortin 4 receptor	2005	Journal of medicinal chemistry, May-05, Volume: 48, Issue:9	N-terminal fatty acylated His-dPhe-Arg-Trp-NH(2) tetrapeptides: influence of fatty acid chain length on potency and selectivity at the mouse melanocortin receptors and human melanocytes.
AID109599	Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells	2002	Journal 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.
AID108635	Compound was evaluated for its agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells	2003	Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12	Urea small molecule agonists on mouse melanocortin receptors.
AID108616	Inhibitory concentration against human Melanocortin 1 receptor (hMC1R)	1997	Journal 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.
AID473151	Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID677168	Half life in human	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID244182	Selectivity of human melanocortin subtype-5 receptor over human melanocortin-4 receptor was determined	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID221834	Functional activity at the mouse melanocortin 4 receptor	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID282355	Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay	2004	Journal 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.
AID107034	In vitro activation of mouse recombinant Melanocortin-4 receptor.	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID109449	Evaluated for agonist activity at cloned mammalian mouse Melanocortin 5 receptor	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID1476420	Agonist 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	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID109462	Agonist activity against human melanocortin receptor hMC4R	2003	Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1	Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.
AID1253332	Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.
AID109429	Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)	1997	Journal 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.
AID320928	Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.
AID108481	Agonist potency for human Melanocortin 1 receptor	2002	Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17	Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.
AID244213	Selectivity for human melanocortin 3 receptor over melanocortin 5 receptor expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID1229385	Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	2015	ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5	Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
AID102008	Biological potency relative to alpha-MSH was measured by using lizard skin bioassay	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID252966	Concentration of compound at 50% maximum cAMP accumulation at human melanocortin-5 receptor	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID1193612	Induction of melanin synthesis in mouse B16F10 cells after 48 hrs by fluorescence microscopy relative to control	2015	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7	Synthesis and melanogenesis evaluation of 3',4',7-trihydroxyflavanone derivatives and characterization of flavanone-BODIPY.
AID1476414	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID252622	Maximal effect on human melanocortin 1 receptor expressing HEK 293 cells	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID1547511	Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID1476419	Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID1547514	Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID246736	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID473160	Displacement of [3H] melanocortin-2 from human recombinant MC4 receptor expressed in CHO cells by scintillation counting	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID246373	Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID240042	Effective concentration for mouse Melanocortin-5 receptor	2005	Journal 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.
AID259547	Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID38590	Ability to stimulate melanosome dispersion in vitro in the lizard skin activity measured relative to alpha-MSH	1984	Journal of medicinal chemistry, Sep, Volume: 27, Issue:9	Cyclic melanotropins. 5. Importance of the C-terminal tripeptide (Lys-Pro-Val).
AID234900	Relative potency against cyclic-Adenosine monophosphate (c-AMP) relative to alpha-MSH	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID1229379	Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay	2015	ACS medicinal chemistry letters, May-14, Volume: 6, Issue:5	Synthesis and Pharmacology of α/β(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
AID473158	Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay relative to alpha melanocyte-stimulating hormone	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID1253334	Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay	2015	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22	A fragment of the Escherichia coli ClpB heat-shock protein is a micromolar melanocortin 1 receptor agonist.
AID102010	In vitro potency in lizard (Anolis carolinensis) skin bioassay relative to alpha-MSH	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID246686	Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID17057	Dissociation rate calculated from the first-order equation using t1/2 value	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID473157	Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID242740	Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID102001	Metabotropic activity in lizard skin (10e-9 M) bioassay, compared to the half-maximal effective dose of; response is not prolonged (-).	1992	Journal of medicinal chemistry, Jan, Volume: 35, Issue:1	Synthesis and biological activities of fatty acid conjugates of a cyclic lactam alpha-melanotropin.
AID1296536	Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID677160	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID71941	In vitro potency in frog (Rana pipiens) skin assay relative to alpha-MSH	1989	Journal of medicinal chemistry, Jan, Volume: 32, Issue:1	Design of potent linear alpha-melanotropin 4-10 analogues modified in positions 5 and 10.
AID259553	Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID107035	Agonist activity to the mouse Melanocortin-4 receptor (mMC4R)	2002	Journal 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.
AID246372	Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID246242	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID107044	Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells	2002	Journal 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.
AID102011	Decrease in lizard skin reflectivity (metabotropic activity).	1997	Journal 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.
AID242142	Inhibitory concentration to displace [125I]-NDP-alpha-MSH from human melanocortin 4 receptor expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID240566	Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108607	Evaluated for agonist activity at cloned mammalian human MSH1 receptor	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
AID245729	Percentage of cAMP accumulation at 10 uM compound relative to alpha-MSH for melanocortin receptor 5	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID109445	Compound was evaluated for its agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells	2003	Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12	Urea small molecule agonists on mouse melanocortin receptors.
AID1547516	Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID108636	Effective concentration against mouse Melanocortin 1 receptor	2004	Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9	Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID1476421	Agonist 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-MSH	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID246687	Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID109601	In vitro activation of mouse recombinant Melanocortin-1 receptor.	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID108939	Effective concentration against mouse Melanocortin 3 receptor	2004	Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9	Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID118292	Relative potency using melanoma adenylate cyclase bioassay system from S-91 melanoma tumors grown in DBA/2J mice	1980	Journal of medicinal chemistry, Dec, Volume: 23, Issue:12	Synthesis and structure-function studies of melanocyte stimulating hormone analogues modified in the 2 and 4(7) positions: comparison of activities on frog skin melanophores and melanoma adenylate cyclase.
AID200407	Metabotropic potency was measured as the minimal effective dose required to elicit the response relative to alpha-MSH(1.0) by using melanoma tyrosinase bioassay; response is not prolonged (-).	1992	Journal of medicinal chemistry, Jan, Volume: 35, Issue:1	Synthesis and biological activities of fatty acid conjugates of a cyclic lactam alpha-melanotropin.
AID473159	Displacement of [3H]dofetilide from human ERG expressed in CHO cells by patch clamp method	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID1296534	Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay	2016	Journal of medicinal chemistry, Apr-14, Volume: 59, Issue:7	An in Vitro and in Vivo Investigation of Bivalent Ligands That Display Preferential Binding and Functional Activity for Different Melanocortin Receptor Homodimers.
AID108957	Agonist potency towards human Melanocortin 4 receptor	2002	Bioorganic & medicinal chemistry letters, Sep-02, Volume: 12, Issue:17	Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: arginine substitution.
AID107033	Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells	2002	Journal 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.
AID71821	Biological potency relative to alpha-MSH was measured by using frog skin bioassay	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID240040	Effective concentration for mouse Melanocortin-3 receptor	2005	Journal 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.
AID677158	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin	2012	Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5	Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.
AID242411	Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID109128	Inhibition of human melanocortin 4 receptor	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID447385	Agonistic activity against mouse MC1R	2009	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17	Semi-rigid tripeptide agonists of melanocortin receptors.
AID22927	Relative rate was determined by setting alpha-MSH equal to 1 and dividing the apparent k E-1 by the alpha-MSH value	1996	Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2	Characterizations of the unusual dissociation properties of melanotropin peptides from the melanocortin receptor, hMC1R.
AID240041	Effective concentration for mouse Melanocortin-4 receptor	2005	Journal 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.
AID109296	Effective concentration of peptide at 50% maximal cAMP generation	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID320925	Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay	2008	Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5	The 1,4-benzodiazepine-2,5-dione small molecule template results in melanocortin receptor agonists with nanomolar potencies.
AID246241	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID71942	Decrease in frog skin reflectivity (metabotropic activity).	1997	Journal 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.
AID244212	Selectivity for human melanocortin 3 receptor over melanocortin 4 receptor expressed in CHO cells	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID71935	Evaluated for relative potency in stimulating melanosome dispersion against Frog skin melanophores (Rana pipiens)	1983	Journal of medicinal chemistry, Feb, Volume: 26, Issue:2	Structure-activity studies of highly potent cyclic [Cys4,Cys10]Melanotropin analogues.
AID447386	Agonistic activity against mouse MC3R	2009	Bioorganic & medicinal chemistry letters, Sep-01, Volume: 19, Issue:17	Semi-rigid tripeptide agonists of melanocortin receptors.
AID242173	Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID259539	Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells	2006	Journal of medicinal chemistry, Feb-09, Volume: 49, Issue:3	Mapping the binding site of melanocortin 4 receptor agonists: a hydrophobic pocket formed by I3.28(125), I3.32(129), and I7.42(291) is critical for receptor activation.
AID163322	Biological activity using the frog skin (Rana pipiens) assay. The value indicates no prolonged biological activity	2003	Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID109446	Effective concentration against mouse Melanocortin 5 receptor	2004	Journal of medicinal chemistry, Apr-22, Volume: 47, Issue:9	Identification of putative agouti-related protein(87-132)-melanocortin-4 receptor interactions by homology molecular modeling and validation using chimeric peptide ligands.
AID242172	Inhibition of [125I]NDP-MSH binding to Melanocortin 1 receptor expressed in HEK293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID109615	In vitro activation of mouse recombinant Melanocortin-3 receptor.	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID1476416	Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay relative to alpha-MSH	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID245727	Percentage of cAMP accumulation at 10 uM compound relative to alpha-MSH for melanocortin receptor 3	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID109453	Agonist activity against human melanocortin receptor hMC1R	2003	Bioorganic & medicinal chemistry letters, Jan-06, Volume: 13, Issue:1	Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH(2) at the human melanocortin-1 and -4 receptors: histidine substitution.
AID242174	Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4)	2005	Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6	Novel 3D pharmacophore of alpha-MSH/gamma-MSH hybrids leads to selective human MC1R and MC3R analogues.
AID108968	Effective concentration required for the biological activity against human Melanocortin 4 receptor	2003	Journal of medicinal chemistry, Sep-25, Volume: 46, Issue:20	Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
AID252274	Maximum percent cAMP accumulation mediated by human melanocortin 3 receptor relative to alpha-MSH (1.1%) at 10 uM concentration	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID108773	Percent activation of human melanocortin receptor Melanocortin 3 receptor was determined at 10 uM	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID221830	Functional activity at the mouse melanocortin 1 receptor	2001	Journal of medicinal chemistry, Jun-21, Volume: 44, Issue:13	Characterization of melanocortin NDP-MSH agonist peptide fragments at the mouse central and peripheral melanocortin receptors.
AID1476417	Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	2017	Journal of medicinal chemistry, 11-09, Volume: 60, Issue:21	Click-Chemistry-Mediated Synthesis of Selective Melanocortin Receptor 4 Agonists.
AID246240	Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
AID102013	Relative potency compared to alpha MSH in a lizard skin bioassay.	1997	Journal 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.
AID109618	Agonistic activity evaluated at melanocortin 3 receptor (MC3R) of mouse HEK293 cells	2003	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 13, Issue:24	Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
AID1547509	Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay	2020	ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3	Single Nucleotide Polymorphisms in the Melanocortin His-Phe-Arg-Trp Sequences Decrease Tetrapeptide Potency and Efficacy.
AID282351	Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay	2004	Journal 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.
AID109428	Inhibition of human melanocortin 5 receptor	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID107045	In vitro activation of mouse recombinant Melanocortin-5 receptor.	2002	Journal of medicinal chemistry, Jun-20, Volume: 45, Issue:13	Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
AID109289	Percent activation of human melanocortin receptor Melanocortin 5 receptor was determined at 10 uM	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID102009	Evaluated for relative potency in stimulating melanosome dispersion against Lizard skin (Anolis carolinensis).	1983	Journal of medicinal chemistry, Feb, Volume: 26, Issue:2	Structure-activity studies of highly potent cyclic [Cys4,Cys10]Melanotropin analogues.
AID244181	Selectivity of human melanocortin subtype-3 receptor over human melanocortin-4 receptor was determined	2005	Bioorganic & medicinal chemistry letters, Jan-03, Volume: 15, Issue:1	Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
AID108938	Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells	2003	Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12	Urea small molecule agonists on mouse melanocortin receptors.
AID109302	In vitro cAMP accumulation in HEK cells transfected with human Melanocortin 5 receptor (hMC5R)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Aryl piperazine melanocortin MC4 receptor agonists.
AID102012	In vitro potency of compound to stimulate melanosome dispersion in lizard skin relative to alpha-MSH	1982	Journal of medicinal chemistry, Sep, Volume: 25, Issue:9	Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
AID266580	Activity at human MC1R by cAMP accumulation in SaoS2 cells	2006	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 16, Issue:14	Design of cyclic peptides with agonist activity at melanocortin receptor-4.
AID246735	Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)	2005	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 15, Issue:15	Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subt
AID473156	Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay relative to alpha melanocyte-stimulating hormone	2010	Journal of medicinal chemistry, Apr-22, Volume: 53, Issue:8	Discovery of a selective small-molecule melanocortin-4 receptor agonist with efficacy in a pilot study of sexual dysfunction in humans.
AID108792	Inhibition of human Melanocortin 3 receptor	2003	Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17	Structure-activity relationships of novel cyclic alpha-MSH/beta-MSH hybrid analogues that lead to potent and selective ligands for the human MC3R and human MC5R.
AID108970	Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptor	1995	Journal of medicinal chemistry, Sep-01, Volume: 38, Issue:18	Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	8 (16.33)	18.7374
1990's	7 (14.29)	18.2507
2000's	25 (51.02)	29.6817
2010's	8 (16.33)	24.3611
2020's	1 (2.04)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	49 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase Ib Study to Confirm the Pharmacokinetics and Melanogenic Potential of Controlled-Release Bioresorbable Implants of Afamelanotide in Healthy Volunteers [NCT03634137]	Phase 1	24 participants (Actual)	Interventional	2009-09-30	Completed
The Role of Alpha Melanocyte Stimulating Hormone in Ocular Disease [NCT03451578]		54 participants (Actual)	Interventional	2018-03-06	Completed
A Phase 3, Randomized, Double-Blind Trial of Two Formulations of Setmelanotide (Daily and Weekly) With a Crossover to Open-Label Once Weekly Setmelanotide in Patients With Specific Gene Defects in the Melanocortin-4 Receptor Pathway Who Are Currently on a [NCT05194124]	Phase 3	20 participants (Actual)	Interventional	2021-12-21	Completed
[NCT00004496]	Phase 1	45 participants (Anticipated)	Interventional	1999-02-28	Completed
A Phase IIb, Multicenter, Open-Label, Prospective Study of Bremelanotide in Diabetic Kidney Disease to Assess the Efficacy in Reducing Urinary Protein and Maintaining Podocyte Density and Function [NCT05709444]	Phase 2	45 participants (Anticipated)	Interventional	2022-12-26	Recruiting
Validation of the Concept of the Autoantibodies Directed Against the Neuropeptides Involved in Food Intake Regulation on the Incidental Cases of Eating Disorders [NCT03510533]		320 participants (Anticipated)	Interventional	2018-05-31	Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Substance	Relationship Strength	Studies	Classes	Roles
melanotan-ii 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	3.87	12	organic molecular entity
acth (4-10) ACTH (4-10): part of ACTH molecule containing amino acids 4-10 of total 39 amino acid chain; heptapeptide common to MSH & ACTH; RN given refers to glycine cpd	1.96	1
phenylalanylarginine phenylalanylarginine: RN given refers to all (L)-isomer. Phe-Arg : A dipeptide composed of L-phenylalanine and L-arginine joined by a peptide linkage.	1.97	1	dipeptide	metabolite
butin butin: isolated from seeds of Butea monosperma; structure given in first source. butin : A trihydroxyflavanone in which the three hydroxy substituents are located at positions 3', 4' and 7. It is found in Acacia mearnsii, Vernonia anthelmintica and Dalbergia odorifera and has a protective affect against oxidative stress-induced mitochondrial dysfunction.	2.11	1	flavanones
ml 00253764 2-(2-(2-(5-bromo-2-methoxyphenyl)ethyl)-3-fluorophenyl)-4,5-dihydro-1H-imidazole: structure in first source	2.03	1
shu 9119 SHU 9119: an agouti mimetic; structure in first source	1.98	1
bremelanotide bremelanotide: a synthetic peptide analogue of alpha-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system;	2.07	1	oligopeptide
acetyl-histidyl-phenylalanyl-arginyl-tryptophanamide [no description available]	3.27	6
ac-his-dphe-arg-trp-nh2 [no description available]	3.82	11
msh, 4-nle-7-phe-alpha- [no description available]	4.62	26	polypeptide	dermatologic drug

Condition	Relationship Strength	Studies
B16 Melanoma [description not available]	1.98	1
Malignant Melanoma [description not available]	2.67	3
Melanoma A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)	2.67	3
Experimental Neoplasms [description not available]	1.95	1
Impotence [description not available]	2.44	2
Erectile Dysfunction The inability in the male to have a PENILE ERECTION due to psychological or organ dysfunction.	2.44	2
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	2.02	1

alpha-msh

Cross-References

Synonyms (39)

Research Excerpts

Dosage Studied

Roles (1)

Drug Classes (1)

Protein Targets (11)

Inhibition Measurements

Activation Measurements

Biological Processes (33)

Molecular Functions (9)

Ceullar Components (4)

Bioassays (228)

Research

Studies (49)

Market Indicators

Research Demand Index: 63.31

Study Types

Clinical Trials (6)

Trial Overview

alpha-msh

Cross-References

Synonyms (39)

Research Excerpts

Dosage Studied

Roles (1)

Drug Classes (1)

Protein Targets (11)

Inhibition Measurements

Activation Measurements

Biological Processes (33)

Molecular Functions (9)

Ceullar Components (4)

Bioassays (228)

Research

Studies (49)

Market Indicators

Research Demand Index: 63.31

Study Types

Clinical Trials (6)

Trial Overview

Related Drugs (10)

Related Conditions (7)