afamelanotide [Ligand Id: 1324] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL441738 (Scenesse, CUV1647, Afamelanotide, CUV-1647)
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  • MC1 receptor/Melanocortin receptor 1 in Human [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
  • MC1 receptor/Melanocortin receptor 1 in Mouse [ChEMBL: CHEMBL4077] [GtoPdb: 282] [UniProtKB: Q01727]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
  • MC3 receptor/Melanocortin receptor 3 in Mouse [ChEMBL: CHEMBL4774] [GtoPdb: 284] [UniProtKB: P33033]
  • MC3 receptor/Melanocortin receptor 3 in Rat [ChEMBL: CHEMBL4023] [GtoPdb: 284] [UniProtKB: P32244]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
  • MC4 receptor/Melanocortin receptor 4 in Mouse [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
  • MC5 receptor/Melanocortin receptor 5 in Mouse [ChEMBL: CHEMBL4489] [GtoPdb: 286] [UniProtKB: P41149]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Adenosine deaminase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1910] [GtoPdb: 1230] [UniProtKB: P00813]
ChEMBL Inhibition of human adenosine deaminase (ADA) B 7.8 pKi 16 nM Ki J. Med. Chem. (2004) 47: 3730-3743 [PMID:15239652]
MC1 receptor/Melanocortin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726]
ChEMBL Displacement of Eu-NDP-alphaMSH from human MC1 receptor expressed in human HCT116 cells after 1.5 hrs by time-resolved fluorescence analysis B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2011) 54: 8078-8084 [PMID:22011200]
ChEMBL Binding affinity towards human Melanocortin 1 receptor (hMC1R) B 9.3 pKi 0.5 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin B 10.34 pKi 0.05 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Displacement of [125I]NDP-MSH from Melanocortin 1 receptor at 10 uM B 9.29 pIC50 0.51 nM IC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL Inhibitory concentration against human Melanocortin 1 receptor (hMC1R) B 9.29 pIC50 0.51 nM IC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
GtoPdb - - 10 pIC50 - - - Eur. J. Pharmacol. (2002) 440: 141-57 [PMID:12007532];
Endocr. Rev. (1988) 9: 159-179 [PMID:3286233]
ChEMBL Agonist potency for human Melanocortin 1 receptor F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 2407-2410 [PMID:12161144]
ChEMBL Agonist activity against human melanocortin receptor hMC1R F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 133-137 [PMID:12467633]
ChEMBL effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 1 receptor F 9.72 pEC50 0.19 nM EC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 1 receptor F 9.72 pEC50 0.19 nM EC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
ChEMBL In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC1R) F 10.15 pEC50 0.07 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 10.15 pEC50 0.07 nM EC50 J Med Chem (2018) 61: 3738-3744 [PMID:29578343]
ChEMBL Evaluated for agonist activity at cloned mammalian human MSH1 receptor F 10.64 pEC50 0.02 nM EC50 J. Med. Chem. (1995) 38: 3454-3461 [PMID:7658432]
ChEMBL Effective concentration required for the biological activity against human Melanocortin 1 receptor B 10.64 pEC50 0.02 nM EC50 J. Med. Chem. (2003) 46: 4215-4231 [PMID:13678399]
MC1 receptor/Melanocortin receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4077] [GtoPdb: 282] [UniProtKB: Q01727]
ChEMBL Displacement of 125I-NDP-MSH from mouse MC1R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis B 9.51 pIC50 0.31 nM IC50 J. Med. Chem. (2016) 59: 3112-3128 [PMID:26959173]
ChEMBL Agonist activity on mouse melanocortin 1 receptor (mMC1R) stably expressed in HEK cells F 7.92 pEC50 12 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2079-2082 [PMID:12781199]
ChEMBL Effective concentration against mouse Melanocortin 1 receptor F 9.42 pEC50 0.38 nM EC50 J. Med. Chem. (2004) 47: 2194-2207 [PMID:15084118]
ChEMBL Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay F 10.04 pEC50 0.09 nM EC50 J. Med. Chem. (2014) 57: 9424-9434 [PMID:25347033]
ChEMBL Agonist activity at mouse melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs B 10.06 pEC50 0.09 nM EC50 J. Med. Chem. (2014) 57: 4615-4628 [PMID:24517312]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay F 10.06 pEC50 0.09 nM EC50 J. Med. Chem. (2008) 51: 5585-5593 [PMID:18800761]
ChEMBL Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay B 10.3 pEC50 0.05 nM EC50 J. Med. Chem. (2013) 56: 2747-2763 [PMID:23432160]
ChEMBL Maximal agonist response of mouse melanocortin 1 receptor (MC1R) F 10.34 pEC50 0.05 nM EC50 J. Med. Chem. (2004) 47: 1514-1526 [PMID:14998337]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 10.4 pEC50 0.04 nM EC50 J Med Chem (2018) 61: 3738-3744 [PMID:29578343]
ChEMBL Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells B 10.42 pEC50 0.04 nM EC50 J. Med. Chem. (2002) 45: 5736-5744 [PMID:12477357]
ChEMBL Agonist activity to the mouse Melanocortin-1 receptor (mMC1R) F 10.42 pEC50 0.04 nM EC50 J. Med. Chem. (2002) 45: 3073-3081 [PMID:12086493]
ChEMBL In vitro activation of mouse recombinant Melanocortin-1 receptor. B 10.42 pEC50 0.04 nM EC50 J. Med. Chem. (2002) 45: 2801-2810 [PMID:12061882]
ChEMBL In vitro agonist potency for Mouse Melanocortin 1 receptor F 10.49 pEC50 0.03 nM EC50 J. Med. Chem. (2005) 48: 3328-3336 [PMID:15857138]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay B 10.52 pEC50 0.03 nM EC50 J. Med. Chem. (2016) 59: 3112-3128 [PMID:26959173]
ChEMBL Functional activity at the mouse melanocortin 1 receptor F 10.52 pEC50 0.03 nM EC50 J. Med. Chem. (2001) 44: 2247-2252 [PMID:11405661]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay F 10.64 pEC50 0.02 nM EC50 J. Med. Chem. (2004) 47: 6702-6710 [PMID:15615519]
ChEMBL Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay B 10.68 pEC50 0.02 nM EC50 J Med Chem (2017) 60: 8103-8114 [PMID:28813605]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay B 10.7 pEC50 0.02 nM EC50 J Med Chem (2017) 60: 4342-4357 [PMID:28453292]
ChEMBL Effective concentration for mouse Melanocortin-1 receptor B 10.74 pEC50 0.02 nM EC50 J. Med. Chem. (2005) 48: 3060-3075 [PMID:15828845]
ChEMBL Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay F 10.74 pEC50 0.02 nM EC50 J. Med. Chem. (2011) 54: 1379-1390 [PMID:21306168]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay B 10.82 pEC50 0.01 nM EC50 J Med Chem (2017) 60: 805-813 [PMID:28045525]
ChEMBL Agonistic activity against mouse MC1R F 10.85 pEC50 0.01 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5176-5181 [PMID:19635667]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay F 11 pEC50 0.01 nM EC50 J Med Chem (2018) 61: 7729-7740 [PMID:30035543]
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
GtoPdb - - 8.9 pKi - - - Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin B 9.11 pKi 0.78 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Binding affinity towards human Melanocortin 3 receptor (hMC3R) B 9.17 pKi 0.68 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Inhibitory activity against Melanocortin 3 receptor B 8.42 pIC50 3.8 nM IC50 J. Med. Chem. (1995) 38: 3454-3461 [PMID:7658432]
ChEMBL Inhibition of human Melanocortin 3 receptor B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2003) 46: 3728-3733 [PMID:12904077]
ChEMBL Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4) B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2005) 48: 1839-1848 [PMID:15771429]
ChEMBL Binding affinity for Human Melanocortin 3 receptor expressed in L-cells B 8.54 pIC50 2.9 nM IC50 J. Med. Chem. (2000) 43: 4998-5002 [PMID:11150170]
ChEMBL Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM B 8.93 pIC50 1.17 nM IC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL Inhibitory concentration against human Melanocortin 3 receptor (hMC3R) B 8.93 pIC50 1.17 nM IC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
ChEMBL Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay B 8.17 pEC50 6.8 nM EC50 J Med Chem (2017) 60: 8716-8730 [PMID:28972753]
ChEMBL effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor F 8.39 pEC50 4.1 nM EC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor F 8.39 pEC50 4.1 nM EC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
ChEMBL Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4) F 9.1 pEC50 0.8 nM EC50 J. Med. Chem. (2005) 48: 1839-1848 [PMID:15771429]
ChEMBL Effective concentration of peptide at 50% maximal cAMP generation F 9.1 pEC50 0.8 nM EC50 J. Med. Chem. (2003) 46: 3728-3733 [PMID:12904077]
ChEMBL In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R) F 9.44 pEC50 0.36 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Agonist activity at human MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 9.52 pEC50 0.3 nM EC50 J Med Chem (2018) 61: 3738-3744 [PMID:29578343]
ChEMBL Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor F 9.62 pEC50 0.24 nM EC50 J. Med. Chem. (2000) 43: 4998-5002 [PMID:11150170]
ChEMBL Evaluated for agonist activity at cloned Melanocortin 3 receptor F 9.88 pEC50 0.13 nM EC50 J. Med. Chem. (1995) 38: 3454-3461 [PMID:7658432]
ChEMBL Effective concentration required for the biological activity against human Melanocortin 3 receptor B 9.89 pEC50 0.13 nM EC50 J. Med. Chem. (2003) 46: 4215-4231 [PMID:13678399]
MC3 receptor/Melanocortin receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4774] [GtoPdb: 284] [UniProtKB: P33033]
ChEMBL Displacement of [125I]-NDP-MSH from mouse MC3R expressed in HEK293 cells after 1 hr by gamma counting B 8.28 pIC50 5.3 nM IC50 J Med Chem (2017) 60: 4342-4357 [PMID:28453292]
ChEMBL Displacement of 125I-NDP-MSH from mouse MC3R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis B 8.38 pIC50 4.18 nM IC50 J. Med. Chem. (2016) 59: 3112-3128 [PMID:26959173]
ChEMBL Compound was evaluated for its agonist activity on mouse melanocortin receptor 3 (mMC3R) stably expressed in HEK cells F 7.12 pEC50 75 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2079-2082 [PMID:12781199]
ChEMBL Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay F 9.09 pEC50 0.81 nM EC50 J. Med. Chem. (2014) 57: 9424-9434 [PMID:25347033]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay F 9.48 pEC50 0.33 nM EC50 J. Med. Chem. (2008) 51: 5585-5593 [PMID:18800761]
ChEMBL Agonist activity at mouse melanocortin-3 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs B 9.48 pEC50 0.33 nM EC50 J. Med. Chem. (2014) 57: 4615-4628 [PMID:24517312]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 9.48 pEC50 0.33 nM EC50 J Med Chem (2018) 61: 3738-3744 [PMID:29578343]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay B 9.62 pEC50 0.24 nM EC50 J. Med. Chem. (2016) 59: 3112-3128 [PMID:26959173]
ChEMBL Agonist activity at mouse MC3 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay B 9.64 pEC50 0.23 nM EC50 J. Med. Chem. (2013) 56: 2747-2763 [PMID:23432160]
ChEMBL Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay B 9.72 pEC50 0.19 nM EC50 J Med Chem (2017) 60: 8103-8114 [PMID:28813605]
ChEMBL Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay F 9.85 pEC50 0.14 nM EC50 J. Med. Chem. (2011) 54: 1379-1390 [PMID:21306168]
ChEMBL Functional activity at the mouse melanocortin 3 receptor F 10 pEC50 0.1 nM EC50 J. Med. Chem. (2001) 44: 2247-2252 [PMID:11405661]
ChEMBL Agonist activity to the mouse Melanocortin-3 receptor (mMC3R) F 10.01 pEC50 0.1 nM EC50 J. Med. Chem. (2002) 45: 3073-3081 [PMID:12086493]
ChEMBL In vitro activation of mouse recombinant Melanocortin-3 receptor. B 10.01 pEC50 0.1 nM EC50 J. Med. Chem. (2002) 45: 2801-2810 [PMID:12061882]
ChEMBL Activity in mouse melanocortin-3 receptor (mMC3R) stably expressed in HEK293 cells B 10.01 pEC50 0.1 nM EC50 J. Med. Chem. (2002) 45: 5736-5744 [PMID:12477357]
ChEMBL Effective concentration against mouse Melanocortin 3 receptor F 10.01 pEC50 0.1 nM EC50 J. Med. Chem. (2004) 47: 2194-2207 [PMID:15084118]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells assessed as increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay B 10.05 pEC50 0.09 nM EC50 J Med Chem (2017) 60: 805-813 [PMID:28045525]
ChEMBL Agonistic activity against mouse MC3R F 10.05 pEC50 0.09 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5176-5181 [PMID:19635667]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay B 10.05 pEC50 0.09 nM EC50 J Med Chem (2017) 60: 4342-4357 [PMID:28453292]
ChEMBL Effective concentration for mouse Melanocortin-3 receptor B 10.05 pEC50 0.09 nM EC50 J. Med. Chem. (2005) 48: 3060-3075 [PMID:15828845]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay F 10.07 pEC50 0.09 nM EC50 J. Med. Chem. (2004) 47: 6702-6710 [PMID:15615519]
ChEMBL In vitro agonist potency for Mouse Melanocortin 3 receptor F 10.15 pEC50 0.07 nM EC50 J. Med. Chem. (2005) 48: 3328-3336 [PMID:15857138]
ChEMBL Agonist activity at mouse MC3R expressed in HEK293 cells F 10.2 pEC50 0.06 nM EC50 J. Med. Chem. (2008) 51: 1026-1034 [PMID:18220330]
MC3 receptor/Melanocortin receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4023] [GtoPdb: 284] [UniProtKB: P32244]
ChEMBL Maximal agonist response at rat melanocortin 3 receptor (MC3R) F 10 pEC50 0.1 nM EC50 J. Med. Chem. (2004) 47: 1514-1526 [PMID:14998337]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL Displacement of Eu-NDP-alphaMSH from human MC4 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis B 7.72 pKi 19 nM Ki J. Med. Chem. (2011) 54: 8078-8084 [PMID:22011200]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287A expressed in HEK293 cells B 8.05 pKi 9 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
GtoPdb - - 8.8 pKi - - - Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100];
Biochemistry (2000) 39: 14900-11 [PMID:11101306];
Proc. Natl. Acad. Sci. U.S.A. (1980) 77: 5754-8 [PMID:6777774]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268A expressed in HEK293 cells B 8.89 pKi 1.3 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R I125A expressed in HEK293 cells B 8.92 pKi 1.2 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y287F expressed in HEK293 cells B 9.01 pKi 0.97 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Binding affinity towards human melanocortin 4 receptor (hMC4R) B 9.02 pKi 0.95 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Displacement of [125I]NDP-alpha-MSH from human wild type MC4R expressed in HEK293 cells B 9.09 pKi 0.82 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184A expressed in HEK293 cells B 9.2 pKi 0.63 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R I129A expressed in HEK293 cells B 9.2 pKi 0.63 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R I291A expressed in HEK293 cells B 9.2 pKi 0.63 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R Y268F expressed in HEK293 cells B 9.24 pKi 0.57 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of [125I]NDP-alpha-MSH from mutant MC4R F184L expressed in HEK293 cells B 9.25 pKi 0.56 nM Ki J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Displacement of radiolabeled NDPalpha-MSH from human MC4 receptor B 9.33 pKi 0.47 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human MC4 receptor by radioligand displacement assay B 9.36 pKi 0.44 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Displacement of [I125]-NDP-MSH from wild type human melanocortin-4 receptor expressed in HEK293 cells B 7.85 pIC50 14 nM IC50 J. Med. Chem. (2014) 57: 4615-4628 [PMID:24517312]
ChEMBL Displacement of [I125]-NDP-MSH from human melanocortin-4 receptor L106P mutant expressed in HEK293 cells B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2014) 57: 4615-4628 [PMID:24517312]
ChEMBL Inhibitory activity against human Melanocortin 4 receptor B 8.44 pIC50 3.6 nM IC50 J. Med. Chem. (1995) 38: 3454-3461 [PMID:7658432]
ChEMBL Binding affinity for Human Melanocortin 4 receptor expressed in L-cells B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2000) 43: 4998-5002 [PMID:11150170]
ChEMBL Displacement of [125I]NDP-MSH from Melanocortin 4 receptor at 10 uM B 8.94 pIC50 1.16 nM IC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL Inhibitory concentration against human Melanocortin 4 receptor (hMC4R) B 8.94 pIC50 1.16 nM IC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
ChEMBL Displacement of radiolabeled NDPalpha-MSH from human MC4 receptor B 9.28 pIC50 0.52 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human MC4 receptor by radioligand displacement assay B 9.32 pIC50 0.48 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Inhibition of [125I]NDP-MSH binding to Melanocortin 4 receptor expressed in HEK293 cells; (N = 4) B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (2005) 48: 1839-1848 [PMID:15771429]
ChEMBL Inhibition of human melanocortin 4 receptor B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (2003) 46: 3728-3733 [PMID:12904077]
ChEMBL Binding affinity to human MC4 receptor by radioligand displacement assay B 9.7 pIC50 0.2 nM IC50 Bioorg. Med. Chem. (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [125I]NDP-alpha-MSH from human recombinant MC4 receptor expressed in CHO cells B 9.82 pIC50 0.15 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [125I]NDP-a-MSH from human recombinant MC4 receptor expressed in CHO cells measured after 120 mins by scintillation counting method B 9.82 pIC50 0.15 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation F 8.05 pEC50 9 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL 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 B 8.19 pEC50 6.4 nM EC50 J Med Chem (2017) 60: 8716-8730 [PMID:28972753]
ChEMBL Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation F 8.29 pEC50 5.1 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation F 8.7 pEC50 2 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation F 8.82 pEC50 1.5 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation F 8.85 pEC50 1.4 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation F 8.92 pEC50 1.2 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation F 8.96 pEC50 1.1 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation F 8.96 pEC50 1.1 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist potency towards human Melanocortin 4 receptor F 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2002) 12: 2407-2410 [PMID:12161144]
ChEMBL Agonist activity against human melanocortin receptor hMC4R F 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 133-137 [PMID:12467633]
ChEMBL Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation F 9 pEC50 1 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor F 9.14 pEC50 0.72 nM EC50 J. Med. Chem. (1997) 40: 1738-1748 [PMID:9171884]
ChEMBL effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 4 receptor F 9.14 pEC50 0.72 nM EC50 J. Med. Chem. (1997) 40: 2133-2139 [PMID:9216831]
ChEMBL In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC4R) F 9.29 pEC50 0.51 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2647-2650 [PMID:12873485]
ChEMBL Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation F 9.29 pEC50 0.51 nM EC50 J. Med. Chem. (2006) 49: 911-922 [PMID:16451057]
ChEMBL Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay B 9.4 pEC50 0.4 nM EC50 J Med Chem (2017) 60: 8716-8730 [PMID:28972753]
ChEMBL Effective concentration required for intracellular cAMP accumulation by Melanocortin 4 receptor F 9.7 pEC50 0.2 nM EC50 J. Med. Chem. (2000) 43: 4998-5002 [PMID:11150170]
ChEMBL Effective concentration for intracellular cAMP accumulation in human melanocortin 4 receptor expressing HEK 293 cells; (N = 4) F 9.7 pEC50 0.2 nM EC50 J. Med. Chem. (2005) 48: 1839-1848 [PMID:15771429]
ChEMBL Agonist activity at human recombinant MC4 receptor expressed in BHK570 cells assessed as induction of cMAP accumulation in presence of 0.1% human serum albumin F 9.85 pEC50 0.14 nM EC50 J. Med. Chem. (2012) 55: 1969-1977 [PMID:22335602]
ChEMBL Agonist activity at human MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 9.89 pEC50 0.13 nM EC50 J Med Chem (2018) 61: 3738-3744 [PMID:29578343]
ChEMBL Effective concentration of peptide at 50% maximal cAMP generation F 10.7 pEC50 0.02 nM EC50 J. Med. Chem. (2003) 46: 3728-3733 [PMID:12904077]
ChEMBL Effective concentration required for the biological activity against human Melanocortin 4 receptor B 10.77 pEC50 0.02 nM EC50 J. Med. Chem. (2003) 46: 4215-4231 [PMID:13678399]
ChEMBL Evaluated for agonist activity at cloned mammalian Melanocortin 4 receptor F 10.77 pEC50 0.02 nM EC50 J. Med. Chem. (1995) 38: 3454-3461 [PMID:7658432]
MC4 receptor/Melanocortin receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450]
ChEMBL Inhibitory concentration towards melanocortin MC4 receptor by displacing radioligand [125I]-NDP-MSH; ND = not determined B 8.37 pIC50 4.22 nM IC50 J. Med. Chem. (2004) 47: 2194-2207 [PMID:15084118]
ChEMBL Displacement of [125I]-NDP-MSH from mouse MC4R expressed in HEK293 cells after 1 hr by gamma counting B 8.7 pIC50 2 nM IC50 J Med Chem (2017) 60: 4342-4357 [PMID:28453292]
ChEMBL Displacement of 125I-NDP-MSH from mouse MC4R expressed in HEK293 cells incubated for 1 hr by gamma counting analysis B 8.96 pIC50 1.09 nM IC50 J. Med. Chem. (2016) 59: 3112-3128 [PMID:26959173]
ChEMBL Agonist activity on mouse melanocortin 4 receptor (mMC4R) stably expressed in HEL cells F 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. Lett. (2003) 13: 2079-2082 [PMID:12781199]
ChEMBL Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay B 9.06 pEC50 0.87 nM