Assay ID | Title | Year | Journal | Article |
AID1902918 | Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in HEK293 cells by competitive binding assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID1239147 | Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP at 10 uM by luminescence counting relative to MT-II | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors. |
AID1743773 | Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID1902923 | Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
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. |
AID261679 | Inhibitory activity against hMC1R transfected in HEK293 cells | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
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. |
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. |
AID375549 | Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID261685 | Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID1169942 | Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1202911 | Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
AID108959 | Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
AID375546 | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID272317 | Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID272314 | Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID107387 | Metabotropic potency against Rana pipiens using frog skin bioassay; effect continued 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. |
AID1424717 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID1202967 | Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1480173 | Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
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. |
AID1169945 | Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1271087 | Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID1271083 | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
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. |
AID1169951 | Selectivity index, ratio of EC50 for mouse MC5R to EC50 for mouse MC1R | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1202975 | Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1369747 | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1202906 | Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
AID274317 | Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1424716 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID272313 | Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
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. |
AID102005 | Potency of compound was measured in lizard where (+) indicates peptide is prolonged acting. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues. |
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. |
AID1424713 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
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. |
AID1812562 | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID597028 | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
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. |
AID1424718 | Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID312478 | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
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. |
AID1369748 | Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1812561 | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID1902924 | Agonist activity at human MC3R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID1271082 | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID1812559 | Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID597022 | Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID1271084 | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID20351 | Relative rate determined by setting MTII equal to 1 and dividing the apparent k-1 by the MTII value | 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. |
AID274309 | Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in HEK293 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1169943 | Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1202969 | Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID109594 | Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
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. |
AID1369750 | Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1902927 | Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID1480172 | Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID1743775 | Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID1743780 | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID1902916 | Agonist activity at human MC1R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
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. |
AID1480164 | Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID9405 | Biological activity using the lizard skin (Anolis carolinensis) assay. The value indicates 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. |
AID1424721 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID108967 | Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor | 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. |
AID272326 | Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1812563 | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID1852344 | Selectivity ratio of EC50 for human MC4R to EC50 for human MC1R | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID108482 | Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
AID1424722 | Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
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. |
AID108603 | Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation | 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. |
AID274319 | Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
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. |
AID108627 | Relative potency of compound for EC50 against Melanocortin 1 receptor transfected into L-cells was determined with respect to EC50 of MTII | 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. |
AID1743779 | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID312480 | Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT2 | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID375547 | Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID1480166 | Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID272319 | Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1202976 | Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
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. |
AID1369757 | Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1202974 | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1852334 | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID15831 | Dissociation rate calculated from the first-order equation using the t1/2 value | 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. |
AID1202909 | Antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
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. |
AID1743778 | Selectivity index, ratio of EC50 for agonist activity at human MC4R expressed in HEK293 cells to IC50 for agonist activity at human MC3R expressed in HEK293 cells | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID274321 | Activity at human MC1R expressed in HEK293 cells assessed as activation of adenylate cyclase | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1852343 | Selectivity ratio of EC50 for human MC3R to EC50 for human MC1R | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID1202964 | Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1743774 | Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID23339 | Relative rate determined by setting MTII equal to 1 and dividing the apparent k-1 by the MTII value | 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. |
AID1169950 | Selectivity index, ratio of EC50 for mouse MC3R to EC50 for mouse MC1R | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID312476 | Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT2 | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID107389 | Metabotropic potency against Anolis carolinensis using lizard skin bioassay; effect continued 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. |
AID261686 | Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID25897 | Half-life determined by extrapolation of the slope until 50% of the peptide was bound relative to the specific binding | 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. |
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. |
AID108628 | Relative potency for inhibition of Melanocortin 1 receptor was determined relative to IC50 of MTII compound | 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. |
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. |
AID1902921 | Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID596854 | Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID321788 | Decrease in rat weight after 4 weeks | 2008 | Journal of medicinal chemistry, Feb-28, Volume: 51, Issue:4
| Backbone cyclic peptidomimetic melanocortin-4 receptor agonist as a novel orally administrated drug lead for treating obesity. |
AID261681 | Inhibitory activity against hMC4R transfected in HEK293 cells | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID108612 | Binding affinity towards human melanocortin receptor (hMC1R) using NDP-MSH as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
AID1202973 | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1852338 | Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID274322 | Activity at human MC3R expressed in HEK293 cells assessed as activation of adenylate cyclase | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
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. |
AID312474 | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1424726 | Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID1202963 | Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1271085 | Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID274310 | Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID312469 | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC1 receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1424720 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID1239144 | Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors. |
AID274318 | Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1271088 | Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
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. |
AID261683 | Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID274312 | Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
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. |
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. |
AID1852336 | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
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. |
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. |
AID272322 | Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1424724 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID312473 | Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID375552 | Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID1902925 | Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID1902919 | Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
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. |
AID272323 | Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1202977 | Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID375554 | Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID312471 | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1202968 | Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1271081 | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID1902922 | Agonist activity at human MC1R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID261684 | Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID1202905 | Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
AID1424712 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC1R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID1743776 | Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay relative to control | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID1812567 | Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID597027 | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID272327 | Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1202965 | Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1480163 | Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID1369752 | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
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. |
AID1202972 | Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells at 10 uM by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
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. |
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. |
AID312475 | Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT2 | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID163323 | Biological activity using the frog skin (Rana pipiens) assay. The value indicates 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. |
AID1424725 | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells at 10 uM after 40 mins by gamma counting analysis relative to control | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID375545 | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID109298 | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor | 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. |
AID1480174 | Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID597021 | Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
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. |
AID109118 | Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
AID108619 | The concentration that inhibits 50% specific binding was determined against the Melanocortin 1 receptor | 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. |
AID1239145 | Displacement of [125I]-[Nle4,D-Phe7]-alpha-MSH from human MC1 receptor expressed in A375 cells at 10 uM after 40 mins by luminescence counting relative to control | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors. |
AID1743781 | Selectivity index, ratio of Ki for human MC3R expressed in HEK293 cell membranes to Ki for human MC4R expressed in HEK293 cell membranes | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID272312 | Displacement of [125I]NDP-alphaMSH from human MC1 receptor expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
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. |
AID1902920 | Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID1202966 | Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID375551 | Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
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. |
AID1202913 | Antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
AID1852337 | Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
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. |
AID272318 | Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID261682 | Inhibitory activity against hMC5R transfected in HEK293 cells | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID274320 | Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID274323 | Activity at human MC5R expressed in HEK293 cells assessed as activation of adenylate cyclase | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1202971 | Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID1239146 | Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | 2015 | Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16
| Systematic Backbone Conformational Constraints on a Cyclic Melanotropin Ligand Leads to Highly Selective Ligands for Multiple Melanocortin Receptors. |
AID1480175 | Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID272316 | Activity at hMC1R transfected in HEK293 cells assessed as intracellular cAMP accumulation | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID597030 | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID1169947 | Selectivity index, ratio of EC50 for mouse MC3R to EC50 for mouse MC4R | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID108604 | Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor | 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. |
AID1369749 | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1812557 | Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID108778 | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor | 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. |
AID1852335 | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID272325 | Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1169946 | Selectivity index, ratio of EC50 for mouse MC1R to EC50 for mouse MC4R | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
AID1369753 | Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
AID1271086 | Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | 2015 | Journal of medicinal chemistry, Dec-24, Volume: 58, Issue:24
| Discovery of Novel Potent and Selective Agonists at the Melanocortin-3 Receptor. |
AID1202970 | Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID274311 | Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID1852342 | Selectivity ratio of Ki for human MC4R to Ki for human MC1R | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
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. |
AID1743777 | Selectivity index, ratio of EC50 for agonist activity at human MC3R expressed in HEK293 cells to IC50 for agonist activity at human MC4R expressed in HEK293 cells | 2021 | Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
| Structure-Based Design of Melanocortin 4 Receptor Ligands Based on the SHU-9119-hMC4R Cocrystal Structure†. |
AID375553 | Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level relative to Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID1852339 | Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID597020 | Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID375544 | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID312472 | Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1812560 | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID597029 | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Cyclic lactam hybrid α-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors. |
AID375548 | Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID109597 | Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation | 2003 | Bioorganic & medicinal chemistry letters, Apr-07, Volume: 13, Issue:7
| Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution. |
AID1202978 | Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation at 10 uM by luminescence counter relative to MT-II | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist. |
AID272324 | Activity at hMC1R transfected in HEK293 cells assessed as intracellular cAMP accumulation relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
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. |
AID71815 | Potency measured in frog where (+) indicates peptide is long acting. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues. |
AID1169944 | Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | 2014 | Journal of medicinal chemistry, Nov-26, Volume: 57, Issue:22
| 1,4-disubstituted-[1,2,3]triazolyl-containing analogues of MT-II: design, synthesis, conformational analysis, and biological activity. |
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. |
AID375543 | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC1R expressed in HEK293 cells | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID1424714 | Agonist activity at human MC1R expressed in HEK293 cells after 3 mins by cAMP assay | 2018 | European journal of medicinal chemistry, May-10, Volume: 151 | Replacement of Arg with Nle and modified D-Phe in the core sequence of MSHs, Ac-His-D-Phe-Arg-Trp-NH |
AID312477 | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation at 10 uM relative to MT2 | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1902917 | Agonist activity at human MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
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. |
AID1852340 | Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
AID312470 | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID274324 | Activity at human MC4R expressed in HEK293 cells assessed as activation of adenylate cyclase | 2006 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 16, Issue:20
| Design, synthesis, and biological evaluation of a new class of small molecule peptide mimetics targeting the melanocortin receptors. |
AID272315 | Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1902926 | Agonist activity at human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation at 10 uM by fluorescence based analysis relative to control | 2022 | Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
| CLIPSing Melanotan-II to Discover Multiple Functionally Selective hMCR Agonists. |
AID272321 | Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID261680 | Inhibitory activity against hMC3R transfected in HEK293 cells | 2006 | Journal of medicinal chemistry, Mar-23, Volume: 49, Issue:6
| Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities. |
AID312479 | Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
| Structure-activity relationships of cyclic lactam analogues of alpha-melanocyte-stimulating hormone (alpha-MSH) targeting the human melanocortin-3 receptor. |
AID1480165 | Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | 2018 | Journal of medicinal chemistry, 04-26, Volume: 61, Issue:8
| Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1. |
AID1369755 | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method | 2018 | Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
| Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors. |
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. |
AID375550 | Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | 2009 | Journal of medicinal chemistry, Jun-25, Volume: 52, Issue:12
| Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. |
AID1202904 | Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | 2015 | ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
| Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor. |
AID272320 | Displacement of [125I]NDP-alphaMSH from human MC1 receptor expressed in HEK293 cells relative to MT2 | 2006 | Journal of medicinal chemistry, Nov-16, Volume: 49, Issue:23
| Design, synthesis, and biological evaluation of new cyclic melanotropin peptide analogues selective for the human melanocortin-4 receptor. |
AID1812558 | Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | 2021 | Journal of medicinal chemistry, 07-22, Volume: 64, Issue:14
| Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework. |
AID1852341 | Selectivity ratio of Ki for human MC3R to Ki for human MC1R | 2022 | Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
| Late-Stage Functionalization with Cysteine Staples Generates Potent and Selective Melanocortin Receptor-1 Agonists. |
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. |
AID1346171 | Human MC4 receptor (Melanocortin receptors) | 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. |
AID1346231 | Human MC1 receptor (Melanocortin receptors) | 2002 | European journal of pharmacology, Apr-12, Volume: 440, Issue:2-3
| The role of melanocortins in body weight regulation: opportunities for the treatment of obesity. |
AID1346180 | Human MC5 receptor (Melanocortin receptors) | 2002 | European journal of pharmacology, Apr-12, Volume: 440, Issue:2-3
| The role of melanocortins in body weight regulation: opportunities for the treatment of obesity. |
AID1346171 | Human MC4 receptor (Melanocortin receptors) | 1999 | European journal of pharmacology, Aug-13, Volume: 378, Issue:3
| Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat. |
AID1346178 | Human MC3 receptor (Melanocortin receptors) | 1999 | European journal of pharmacology, Aug-13, Volume: 378, Issue:3
| Characterization of melanocortin receptor ligands on cloned brain melanocortin receptors and on grooming behavior in the rat. |
AID1346231 | Human MC1 receptor (Melanocortin receptors) | 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. |
AID1346171 | Human MC4 receptor (Melanocortin receptors) | 2000 | Biochemistry, Dec-05, Volume: 39, Issue:48
| Molecular determinants of ligand binding to the human melanocortin-4 receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |