afamelanotide [Ligand Id: 1324] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL441738 (Afamelanotide, CUV-1647, CUV1647, Melanotan, Melanotan-1, Melanotan i, 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 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 | 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 | 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 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 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 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 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 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 | 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 | 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 | 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 by alphascreen cAMP assay | F | 10.05 | pEC50 | 0.09 | nM | EC50 | ACS Med Chem Lett (2020) 11: 1942-1948 [PMID:33062177] |
| 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 | Agonistic activity against mouse MC3R | F | 10.05 | pEC50 | 0.09 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 5176-5181 [PMID:19635667] |
| 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 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 | J Med Chem (2020) 63: 2194-2208 [PMID:31845801] |
| 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 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 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 | 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 | 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 | 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 | 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 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 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 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-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 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 | 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 | 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 | 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
