| Assay ID | Title | Year | Journal | Article |
|---|
| AID1512893 | Agonist activity at human FLAG-tagged MC4R expressed in HTLA cells assessed as induction of beta-arrestin recruitment after 18 hrs by Presto-tango assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors. |
| 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. |
| AID109119 | Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| 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. |
| AID109107 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| 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. |
| AID1296532 | Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| AID1483077 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| AID1296527 | Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | 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. |
| 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 |
| AID1296531 | Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| AID1424727 | Agonist activity at human MC5R expressed in HEK293 cells at 10 uM after 3 mins by cAMP assay relative to MT-2 | 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 |
| 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. |
| AID104102 | Effective concentration was measured against frog skin MCR cells at 10 e-4 10 e-12 M Concentration. | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| AID391370 | Selectivity for mouse MC5R over mouse MC3R by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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 |
| 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. |
| AID1512899 | Decrease in protein-protein interaction of mouse Nano-Luc-tagged MC4R/mouse Halo-tagged MC4R homodimer expressed in HEK293 cells at 10 uM up to 10 mins by BRET assay relative to control | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors. |
| AID391361 | Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay relative to Ac-His-DPhe7-Arg-Trp-NH2 peptide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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. |
| AID108611 | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| AID1776308 | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
| AID1424723 | Agonist activity at human MC4R expressed in HEK293 cells at 10 uM after 3 mins by cAMP assay relative to MT-2 | 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 |
| AID391368 | Selectivity for mouse MC4R over mouse MC3R by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist 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. |
| AID1296528 | Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis | 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. |
| 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. |
| 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. |
| AID391360 | Antagonist activity at mouse MC3R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| AID391362 | Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| AID71817 | Potency measured in frog where (-) indicates peptide is not long acting. | 1995 | Journal of medicinal chemistry, May-12, Volume: 38, Issue:10
| Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues. |
| AID1776311 | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
| 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. |
| AID1151520 | Agonist activity at human melanocortin-4 receptor I102S mutant 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). |
| AID1512898 | Decrease in protein-protein interaction of mouse Nano-Luc-tagged MC4R/mouse Halo-tagged MC4R homodimer expressed in HEK293 cells up to 10 mins by BRET assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors. |
| AID1296533 | Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| AID1483073 | Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| AID622004 | Displacement of Eu-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 2 hrs by time resolved fluorescence assay | 2011 | Journal of medicinal chemistry, Oct-27, Volume: 54, Issue:20
| Design, synthesis, and biological studies of efficient multivalent melanotropin ligands: tools toward melanoma diagnosis and treatment. |
| 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 |
| AID1483084 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| 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 |
| AID108795 | Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| 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. |
| AID1424715 | Agonist activity at human MC1R expressed in HEK293 cells at 10 uM after 3 mins by cAMP assay relative to MT-2 | 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 |
| 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). |
| AID1151514 | 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 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). |
| AID1296539 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| AID391363 | Antagonist activity at mouse MC4R expressed in HEK293 cells assessed as effect on MT2 peptide-induced response by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| AID1296530 | Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells at 100 uM incubated for 1 hr by gamma counting analysis | 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. |
| 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. |
| AID1296540 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| AID1512890 | Agonist activity at human FLAG-tagged MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the 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. |
| AID108614 | Displacement of [125I]NDP-MSH from Melanocortin 1 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| 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. |
| 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 |
| 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 |
| AID391364 | Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay relative to Ac-His-DPhe7-Arg-Trp-NH2 peptide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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. |
| 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. |
| AID1483081 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| 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. |
| 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. |
| 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. |
| 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 |
| 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. |
| AID391367 | Selectivity for mouse MC4R over mouse MC1R by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| AID1424719 | Agonist activity at human MC3R expressed in HEK293 cells at 10 uM after 3 mins by cAMP assay relative to MT-2 | 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 |
| 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. |
| AID391365 | Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| AID1483091 | Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| 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. |
| AID1151519 | Agonist activity at human melanocortin-4 receptor I69T mutant 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). |
| AID1296538 | Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| 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. |
| 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. |
| AID1151523 | Agonist activity at human melanocortin-4 receptor C271R mutant 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). |
| AID1151521 | Agonist activity at human melanocortin-4 receptor A219V mutant 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). |
| 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 |
| 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. |
| AID391354 | Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist 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. |
| 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. |
| AID1776305 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
| AID391369 | Selectivity for mouse MC5R over mouse MC1R by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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. |
| AID1296541 | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay relative to Ac-His-DPhe-Arg-Trp-NH2 | 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. |
| 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. |
| 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. |
| AID1512896 | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 2 hrs by AlphaScreen assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Developing a Biased Unmatched Bivalent Ligand (BUmBL) Design Strategy to Target the GPCR Homodimer Allosteric Signaling (cAMP over β-Arrestin 2 Recruitment) Within the Melanocortin Receptors. |
| AID1547512 | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation at 100 uM incubated for 2 hrs by cAMP Alpha-screen assay relative to control | 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. |
| 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. |
| AID109425 | Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM | 1997 | Journal of medicinal chemistry, Jul-04, Volume: 40, Issue:14
| Discovery of prototype peptidomimetic agonists at the human melanocortin receptors MC1R and MC4R. |
| AID391366 | Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay relative to Ac-His-DPhe7-Arg-Trp-NH2 peptide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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 |
| 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. |
| 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. |
| AID391356 | Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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. |
| 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 |
| 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. |
| 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. |
| AID1776302 | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | 2021 | Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
| Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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 |
| AID1483074 | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | 2017 | Journal of medicinal chemistry, 05-25, Volume: 60, Issue:10
| Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa |
| AID391355 | Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay relative to Ac-His-DPhe7-Arg-Trp-NH2 peptide | 2008 | Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
| Melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH2 modified at the para position of the benzyl side chain (DPhe): importance for mouse melanocortin-3 receptor agonist versus antagonist activity. |
| 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 |
| 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. |
| AID1151522 | Agonist activity at human melanocortin-4 receptor C271Y mutant 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). |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |