afamelanotide [Ligand Id: 1324] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL441738 (Afamelanotida, Afamelanotide, CUV-1647, CUV1647, Melanotan, Melanotan-1, Melanotan i, Ndp-alpha-msh, (nle4,d-phe7)-.alpha.-msh, Scenesse) |
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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 | F | 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 | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 1 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | B | 9.54 | pIC50 | 0.29 | nM | IC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 receptor 1 expressed in HEK293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 24 hrs by beta-galactosidase reporter gene assay | F | 10.05 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2021) 64: 5577-5592 [PMID:33886285] |
| 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 melanocortin-1 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | F | 10.06 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2014) 57: 4615-4628 [PMID:24517312] |
| ChEMBL | Full agonist activity at mouse MC1R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | F | 10.29 | pEC50 | 0.05 | nM | EC50 | J Med Chem (2019) 62: 2738-2749 [PMID:30741545] |
| ChEMBL | Agonist activity at mouse MC1 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | F | 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 | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2018) 61: 3738-3744 [PMID:29578343] |
| 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 | 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 | 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 | 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 assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | F | 10.52 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2016) 59: 3112-3128 [PMID:26959173] |
| 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 | F | 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 | F | 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 | F | 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 assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay | F | 10.92 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2021) 64: 14860-14875 [PMID:34592820] |
| ChEMBL | 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 | F | 10.92 | pEC50 | 0.01 | nM | EC50 | ACS Med Chem Lett (2020) 11: 272-277 [PMID:32184956] |
| ChEMBL | Agonist activity against mouse MC1R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay | F | 11 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2023) 66: 8103-8117 [PMID:37307241] |
| 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] |
| ChEMBL | Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | F | 11 | pEC50 | 0.01 | nM | EC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| ChEMBL | Agonist activity at mouse MC1R by alphascreen cAMP assay | F | 11 | pEC50 | 0.01 | nM | EC50 | ACS Med Chem Lett (2020) 11: 1942-1948 [PMID:33062177] |
| 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 | F | 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 | F | 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 melanocortin receptor 3 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | B | 8.09 | pIC50 | 8.2 | nM | IC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | F | 9.38 | pEC50 | 0.41 | nM | EC50 | J Med Chem (2019) 62: 2738-2749 [PMID:30741545] |
| ChEMBL | 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 | F | 9.44 | pEC50 | 0.36 | nM | EC50 | J Med Chem (2021) 64: 5577-5592 [PMID:33886285] |
| 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 | F | 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 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 MC3R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | F | 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 | F | 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 | F | 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 stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | F | 9.72 | pEC50 | 0.19 | nM | EC50 | ACS Med Chem Lett (2020) 11: 272-277 [PMID:32184956] |
| ChEMBL | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | F | 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 by alphascreen cAMP assay | F | 10.05 | pEC50 | 0.09 | nM | EC50 | ACS Med Chem Lett (2020) 11: 1942-1948 [PMID:33062177] |
| 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 increase in forskolin-induced cAMP accumulation preincubated for 2 hrs followed by biotinylated cAMP addition and subsequent incubation for 2 hrs by AlphaScreen assay | F | 10.05 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2017) 60: 805-813 [PMID:28045525] |
| ChEMBL | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | F | 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 | Agonist activity against mouse MC3R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay | F | 10.1 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2023) 66: 8103-8117 [PMID:37307241] |
| ChEMBL | Agonist activity at mouse MC3R expressed in HEK293 cells assessed as induction of cAMP level incubated for 2 hr by alphaScreen assay | F | 10.13 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2021) 64: 14860-14875 [PMID:34592820] |
| ChEMBL | Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | F | 10.15 | pEC50 | 0.07 | nM | EC50 | ACS Med Chem Lett (2021) 12: 115-120 [PMID:33488972] |
| 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 melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | F | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 USA (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 [125I]-NDP-MSH from human melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 | F | 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 | F | 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 | F | 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 melanocortin receptor 4 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | ACS Med Chem Lett (2020) 11: 272-277 [PMID:32184956] |
| ChEMBL | Agonist activity at mouse MC4R by alphascreen cAMP assay | F | 9.05 | pEC50 | 0.9 | nM | EC50 | ACS Med Chem Lett (2020) 11: 1942-1948 [PMID:33062177] |
| ChEMBL | 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 | F | 9.05 | pEC50 | 0.9 | nM | EC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | F | 9.06 | pEC50 | 0.87 | nM | EC50 | J Med Chem (2018) 61: 3738-3744 [PMID:29578343] |
| ChEMBL | Agonist activity against mouse MC4R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay | F | 9.14 | pEC50 | 0.72 | nM | EC50 | J Med Chem (2023) 66: 8103-8117 [PMID:37307241] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | F | 9.34 | pEC50 | 0.46 | nM | EC50 | J Med Chem (2016) 59: 3112-3128 [PMID:26959173] |
| ChEMBL | Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | F | 9.39 | pEC50 | 0.41 | nM | EC50 | J Med Chem (2017) 60: 8103-8114 [PMID:28813605] |
| ChEMBL | Agonist activity at mouse MC4R 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 | F | 9.41 | pEC50 | 0.39 | nM | EC50 | J Med Chem (2017) 60: 805-813 [PMID:28045525] |
| ChEMBL | Functional activity at the mouse melanocortin 4 receptor | F | 9.49 | pEC50 | 0.32 | nM | EC50 | J Med Chem (2001) 44: 2247-2252 [PMID:11405661] |
| ChEMBL | 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 | F | 9.52 | pEC50 | 0.3 | nM | EC50 | ACS Med Chem Lett (2021) 12: 115-120 [PMID:33488972] |
| ChEMBL | Effective concentration for maximum agonist response towards mouse melanocortin 4 receptor | F | 9.54 | pEC50 | 0.29 | nM | EC50 | J Med Chem (2004) 47: 1514-1526 [PMID:14998337] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | F | 9.55 | pEC50 | 0.28 | nM | EC50 | J Med Chem (2019) 62: 2738-2749 [PMID:30741545] |
| ChEMBL | In vitro activation of mouse recombinant Melanocortin-4 receptor. | B | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2002) 45: 2801-2810 [PMID:12061882] |
| ChEMBL | Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells | B | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| ChEMBL | Agonist activity to the mouse Melanocortin-4 receptor (mMC4R) | F | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2002) 45: 3073-3081 [PMID:12086493] |
| ChEMBL | Effective concentration against mouse melanocortin MC4 receptor | F | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2004) 47: 2194-2207 [PMID:15084118] |
| ChEMBL | Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2011) 54: 1379-1390 [PMID:21306168] |
| ChEMBL | Agonist activity at mouse MC4 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2013) 56: 2747-2763 [PMID:23432160] |
| ChEMBL | Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2014) 57: 9424-9434 [PMID:25347033] |
| ChEMBL | Effective concentration for mouse Melanocortin-4 receptor | B | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
| ChEMBL | In vitro agonist potency for Mouse Melanocortin 4 receptor | F | 9.85 | pEC50 | 0.14 | nM | EC50 | J Med Chem (2005) 48: 3328-3336 [PMID:15857138] |
| ChEMBL | Agonistic activity against mouse MC4R | F | 9.85 | pEC50 | 0.14 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 5176-5181 [PMID:19635667] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay | F | 9.89 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2008) 51: 5585-5593 [PMID:18800761] |
| ChEMBL | 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 | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2021) 64: 5577-5592 [PMID:33886285] |
| ChEMBL | Agonist activity at mouse melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2014) 57: 4615-4628 [PMID:24517312] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells | F | 10.01 | pEC50 | 0.1 | nM | EC50 | J Med Chem (2008) 51: 1026-1034 [PMID:18220330] |
| MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032] | ||||||||
| ChEMBL | Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis | B | 8 | pKi | 9.9 | nM | Ki | J Med Chem (2011) 54: 8078-8084 [PMID:22011200] |
| ChEMBL | Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin | B | 9.32 | pKi | 0.48 | nM | Ki | J Med Chem (2012) 55: 1969-1977 [PMID:22335602] |
| ChEMBL | Inhibition of human melanocortin 5 receptor | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2003) 46: 3728-3733 [PMID:12904077] |
| ChEMBL | Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4 | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2005) 48: 1839-1848 [PMID:15771429] |
| GtoPdb | - | - | 9 | pIC50 | - | - | - | Eur J Pharmacol (2002) 440: 141-57 [PMID:12007532] |
| ChEMBL | Binding affinity for Human Melanocortin 5 receptor expressed in L-cells | B | 9.05 | pIC50 | 0.89 | nM | IC50 | J Med Chem (2000) 43: 4998-5002 [PMID:11150170] |
| ChEMBL | Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM | B | 9.07 | pIC50 | 0.86 | nM | IC50 | J Med Chem (1997) 40: 2133-2139 [PMID:9216831] |
| ChEMBL | Inhibitory concentration against human Melanocortin 5 receptor (hMC5R) | B | 9.07 | pIC50 | 0.86 | nM | IC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | F | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2017) 60: 8716-8730 [PMID:28972753] |
| ChEMBL | Effective concentration of peptide at 50% maximal cAMP generation | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2003) 46: 3728-3733 [PMID:12904077] |
| ChEMBL | Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4) | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2005) 48: 1839-1848 [PMID:15771429] |
| ChEMBL | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor | F | 9.24 | pEC50 | 0.58 | nM | EC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor | F | 9.24 | pEC50 | 0.58 | nM | EC50 | J Med Chem (1997) 40: 2133-2139 [PMID:9216831] |
| ChEMBL | Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2018) 61: 3738-3744 [PMID:29578343] |
| ChEMBL | Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor | F | 9.64 | pEC50 | 0.23 | nM | EC50 | J Med Chem (2000) 43: 4998-5002 [PMID:11150170] |
| MC5 receptor/Melanocortin receptor 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4489] [GtoPdb: 286] [UniProtKB: P41149] | ||||||||
| ChEMBL | Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| ChEMBL | Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells | F | 6.77 | pEC50 | 170 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 2079-2082 [PMID:12781199] |
| ChEMBL | 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 | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2021) 64: 5577-5592 [PMID:33886285] |
| ChEMBL | Full agonist activity at mouse MC5R expressed in HEK293 cells co-expressing CRE/beta-galactosidase reporter gene after 6 hrs by beta-galactosidase cAMP assay | F | 8.7 | pEC50 | 1.98 | nM | EC50 | J Med Chem (2019) 62: 2738-2749 [PMID:30741545] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay | F | 9.39 | pEC50 | 0.41 | nM | EC50 | J Med Chem (2018) 61: 3738-3744 [PMID:29578343] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay | F | 9.51 | pEC50 | 0.31 | nM | EC50 | J Med Chem (2016) 59: 3112-3128 [PMID:26959173] |
| ChEMBL | 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 | F | 9.52 | pEC50 | 0.3 | nM | EC50 | ACS Med Chem Lett (2020) 11: 272-277 [PMID:32184956] |
| ChEMBL | Agonist activity at mouse MC5 receptor expressed in HEK293 cells after 6 hrs by cAMP-based beta-galactosidase reporter gene assay | F | 9.55 | pEC50 | 0.28 | nM | EC50 | J Med Chem (2013) 56: 2747-2763 [PMID:23432160] |
| ChEMBL | Agonist activity at mouse melanocortin-5 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs | F | 9.59 | pEC50 | 0.26 | nM | EC50 | J Med Chem (2014) 57: 4615-4628 [PMID:24517312] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells by CRE/beta-galactosidase reporter gene assay | F | 9.59 | pEC50 | 0.26 | nM | EC50 | J Med Chem (2008) 51: 5585-5593 [PMID:18800761] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP level at 100 uM incubated for 2 hr by alphaScreen assay | F | 9.68 | pEC50 | 0.21 | nM | EC50 | J Med Chem (2021) 64: 14860-14875 [PMID:34592820] |
| ChEMBL | Agonist activity against mouse MC5R expressed in HEK293 cells assessed as increase in cAMP level incubated for 2 hrs by AlphaScreen assay | F | 9.72 | pEC50 | 0.19 | nM | EC50 | J Med Chem (2023) 66: 8103-8117 [PMID:37307241] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells assessed as induction of cAMP accumulation after 2 hrs by alpha screen assay | F | 9.74 | pEC50 | 0.18 | nM | EC50 | J Med Chem (2017) 60: 4342-4357 [PMID:28453292] |
| ChEMBL | Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as increase in cAMP accumulation after 2 hrs by AlphaScreen assay | F | 9.74 | pEC50 | 0.18 | nM | EC50 | J Med Chem (2017) 60: 8103-8114 [PMID:28813605] |
| ChEMBL | Agonistic activity against mouse MC5R | F | 9.77 | pEC50 | 0.17 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 5176-5181 [PMID:19635667] |
| ChEMBL | Inverse agonist activity at mouse MC5R expressed in HEK293 cells incubated for 2 hrs by AlphaScreen cAMP assay | F | 9.85 | pEC50 | 0.14 | nM | EC50 | J Med Chem (2018) 61: 7729-7740 [PMID:30035543] |
| ChEMBL | 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 | F | 9.89 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| ChEMBL | Agonist activity at mouse MC5R 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 | F | 9.96 | pEC50 | 0.11 | nM | EC50 | J Med Chem (2017) 60: 805-813 [PMID:28045525] |
| ChEMBL | Agonist activity at mouse MC5R by alphascreen cAMP assay | F | 9.96 | pEC50 | 0.11 | nM | EC50 | ACS Med Chem Lett (2020) 11: 1942-1948 [PMID:33062177] |
| ChEMBL | Effective concentration for mouse Melanocortin-5 receptor | B | 10.02 | pEC50 | 0.1 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
| ChEMBL | Functional activity at the mouse melanocortin 5 receptor | F | 10.07 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2001) 44: 2247-2252 [PMID:11405661] |
| ChEMBL | 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 | F | 10.1 | pEC50 | 0.08 | nM | EC50 | ACS Med Chem Lett (2021) 12: 115-120 [PMID:33488972] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells | F | 10.11 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2008) 51: 1026-1034 [PMID:18220330] |
| ChEMBL | In vitro agonist potency for Mouse Melanocortin 5 receptor | F | 10.11 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2005) 48: 3328-3336 [PMID:15857138] |
| ChEMBL | Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells | B | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| ChEMBL | Effective concentration against mouse Melanocortin 5 receptor | F | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2004) 47: 2194-2207 [PMID:15084118] |
| ChEMBL | In vitro activation of mouse recombinant Melanocortin-5 receptor. | B | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2002) 45: 2801-2810 [PMID:12061882] |
| ChEMBL | Agonist activity towards mouse Melanocortin-5 receptor (mMC5R) | F | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2002) 45: 3073-3081 [PMID:12086493] |
| ChEMBL | Maximum agonist response for mouse melanocortin 5 receptor (MC5R) | F | 10.19 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2004) 47: 1514-1526 [PMID:14998337] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay | F | 10.21 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| ChEMBL | Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells after 48 hrs by cAMP based beta-galactosidase reporter gene assay | F | 10.52 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2011) 54: 1379-1390 [PMID:21306168] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
