MT-II [Ligand Id: 1323] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL430239 (Melatonan) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MC1 receptor/Melanocortin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726] | ||||||||
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 9.88 | pKi | 0.13 | nM | Ki | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | B | 9.95 | pKi | 0.11 | nM | Ki | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| ChEMBL | Antagonist activity at human MC1 receptor expressed in A375 cells assessed as inhibition of MT-II-induced intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | F | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (2015) 58: 6359-6367 [PMID:26218460] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting method | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 1 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Binding affinity towards human melanocortin receptor (hMC1R) using NDP-MSH as radioligand | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC1 receptor expressed in HEK293 cells by gamma counting analysis | B | 9 | pIC50 | 1 | nM | IC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC1R expressed in HEK293 cells after 40 mins by gamma counting analysis | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | The concentration that inhibits 50% specific binding was determined against the Melanocortin 1 receptor | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| ChEMBL | The concentration that inhibits 50% specific binding was determined against the Melanocortin 1 receptor | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| GtoPdb | - | - | 9.4 | pIC50 | - | - | - |
Eur J Pharmacol (2002) 440: 141-57 [PMID:12007532]; J Med Chem (1989) 32: 174-179 [PMID:2535874] |
| ChEMBL | Inhibitory concentration against human Melanocortin 1 receptor (hMC1R) | B | 9.6 | pIC50 | 0.25 | nM | IC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Displacement of [125I]NDP-alphaMSH from human MC1 receptor expressed in HEK293 cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC1 receptor expressed in HEK293 cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC1R expressed in HEK293 cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Inhibitory activity against hMC1R transfected in HEK293 cells | B | 9.7 | pIC50 | 0.2 | nM | IC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in HEK293 cells | B | 10 | pIC50 | 0.1 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Agonist activity at human MC1 receptor expressed in A375 cells assessed as intracellular cAMP accumulation using [3H]-cAMP by luminescence counting | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2015) 58: 6359-6367 [PMID:26218460] |
| ChEMBL | Decrease in frog skin reflectivity (metabotropic activity). | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (1997) 40: 2740-2749 [PMID:9276019] |
| ChEMBL | Agonist activity at human melanocortin 1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Agonist activity at human MC1R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation measured after 3 mins | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Agonist activity at human MC1R expressed in HEK293 cells assessed as increase in intracellular cAMP accumulation | F | 8.99 | pEC50 | 1.02 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Activity at human MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | F | 8.99 | pEC50 | 1.02 | nM | EC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Activity at human MC1R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | F | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Agonist activity at human MC1R expressed in HEK293 cells after 3 mins by cAMP assay | F | 9 | pEC50 | 1 | nM | EC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Agonistic activity against human melanocortin receptor (hMC1R) for cAMP accumulation | F | 9.22 | pEC50 | 0.6 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation | F | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| ChEMBL | Activity against hMC1R transfected in HEK293 cells by intracellular cAMP accumulation | F | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Activity at hMC1R transfected in HEK293 cells assessed as intracellular cAMP accumulation | F | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Agonist activity at human MC1 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Agonist activity at human MC1R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | F | 9.52 | pEC50 | 0.3 | nM | EC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| 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 | Effective concentration against Melanocortin 1 receptor transfected into L-cells was determined by concentration of peptide for 50% maximal cAMP generation | F | 9.82 | pEC50 | 0.15 | nM | EC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| ChEMBL | Effective concentration for the effect of Melanocortin 1 receptor in the frog skin. | B | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| ChEMBL | Effective concentration for the effect of Melanocortin 1 receptor in the frog skin. | B | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (1995) 38: 4720-4729 [PMID:7473600] |
| ChEMBL | Decrease in frog skin reflectivity (metabotropic activity). | F | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (1997) 40: 2740-2749 [PMID:9276019] |
| ChEMBL | Decrease in frog skin reflectivity (metabotropic activity). | F | 10 | pEC50 | 0.1 | nM | EC50 | J Med Chem (1997) 40: 2740-2749 [PMID:9276019] |
| ChEMBL | Agonist activity at human melanocortin receptor 1 expressed in human T-Rex-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | F | 10.3 | pEC50 | <0.05 | nM | EC50 | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Agonist activity at human MC1R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | F | 10.5 | pEC50 | <0.03 | nM | EC50 | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| MC1 receptor/Melanocortin receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4077] [GtoPdb: 282] [UniProtKB: Q01727] | ||||||||
| ChEMBL | Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | B | 9.66 | pEC50 | 0.22 | nM | EC50 | ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138] |
| ChEMBL | Activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | F | 10.52 | pEC50 | 0.03 | nM | EC50 | J Med Chem (2014) 57: 9424-9434 [PMID:25347033] |
| ChEMBL | Effective concentration for mouse Melanocortin-1 receptor | B | 10.66 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
| ChEMBL | Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay | F | 10.68 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| ChEMBL | Agonist activity to the mouse Melanocortin-1 receptor (mMC1R) | F | 10.7 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2002) 45: 3073-3081 [PMID:12086493] |
| ChEMBL | Activity in mouse melanocortin-1 receptor stably expressed in HEK293 cells | B | 10.7 | pEC50 | 0.02 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968] | ||||||||
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 7.73 | pKi | 18.62 | nM | Ki | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC3R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | B | 7.77 | pKi | 16.98 | nM | Ki | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100] |
| ChEMBL | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Inhibitory concentration against human Melanocortin 3 receptor (hMC3R) | B | 8.07 | pIC50 | 8.56 | nM | IC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Displacement of [125I]NDP-alphaMSH from human MC3 receptor expressed in HEK293 cells | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC3 receptor expressed in HEK293 cells by gamma counting analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells | B | 8.72 | pIC50 | 1.9 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC3R expressed in HEK293 cells | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Inhibitory activity against hMC3R transfected in HEK293 cells | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC3 receptor expressed in HEK293 cells | B | 8.9 | pIC50 | 1.25 | nM | IC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 3 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC3R expressed in HEK293 cells after 40 mins by gamma counting method | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | F | 7.47 | pEC50 | 33.9 | nM | EC50 | J Med Chem (2017) 60: 8716-8730 [PMID:28972753] |
| ChEMBL | Agonistic activity against human melanocortin receptor (hMC3R) for cAMP accumulation | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | F | 7.77 | pEC50 | 16.98 | nM | EC50 | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Activity at human MC3 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | F | 8.29 | pEC50 | 5.1 | nM | EC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells after 3 mins by cAMP assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Activity at human MC3R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | F | 8.62 | pEC50 | 2.4 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Activity against hMC3R transfected in HEK293 cells by intracellular cAMP accumulation | F | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | F | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Activity at hMC3R transfected in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Agonist activity at human MC3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.73 | pEC50 | 1.85 | nM | EC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Agonist activity at human melanocortin 3 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | F | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | F | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Effective concentration required for the biological activity against human Melanocortin 3 receptor | B | 9.57 | pEC50 | 0.27 | nM | EC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| ChEMBL | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor | F | 9.62 | pEC50 | 0.24 | nM | EC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Agonist activity at human MC3R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | F | 9.69 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| ChEMBL | Agonist activity at human melanocortin receptor 3 expressed in human T-REx-293 cells assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | F | 10.21 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| MC3 receptor/Melanocortin receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4774] [GtoPdb: 284] [UniProtKB: P33033] | ||||||||
| ChEMBL | Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | B | 9.46 | pEC50 | 0.35 | nM | EC50 | ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138] |
| ChEMBL | Activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | F | 9.74 | pEC50 | 0.18 | nM | EC50 | J Med Chem (2014) 57: 9424-9434 [PMID:25347033] |
| ChEMBL | Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay | F | 9.77 | pEC50 | 0.17 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| ChEMBL | Agonist activity to the mouse Melanocortin-3 receptor (mMC3R) | F | 9.8 | pEC50 | 0.16 | 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 | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| ChEMBL | Effective concentration for mouse Melanocortin-3 receptor | B | 9.89 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
| MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | - | - | - |
J Med Chem (1989) 32: 174-179 [PMID:2535874]; Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100]; Biochemistry (2000) 39: 14900-11 [PMID:11101306] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC4R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting analysis | B | 8.64 | pIC50 | 2.3 | nM | IC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC4 receptor expressed in HEK293 cells by gamma counting analysis | B | 8.64 | pIC50 | 2.3 | nM | IC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Binding affinity towards human melanocortin receptor (hMC4R) using NDP-MSH as radioligand | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC4R expressed in HEK293 cells | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Displacement of [125I]NDP-alphaMSH from human MC4 receptor expressed in HEK293 cells | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Inhibitory activity against hMC4R transfected in HEK293 cells | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 4 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC4R expressed in HEK293 cells after 40 mins by gamma counting method | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC4 receptor expressed in HEK293 cells | B | 8.97 | pIC50 | 1.07 | nM | IC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Inhibitory concentration against human Melanocortin 4 receptor (hMC4R) | B | 9.14 | pIC50 | 0.72 | nM | IC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as effect on cAMP accumulation by cAMP split-luciferase reporter gene assay | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2021) 64: 357-369 [PMID:33190475] |
| ChEMBL | Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | F | 8.07 | pEC50 | 8.6 | nM | EC50 | J Med Chem (2017) 60: 8716-8730 [PMID:28972753] |
| 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 | 8.51 | pEC50 | 3.1 | nM | EC50 | J Med Chem (2017) 60: 8716-8730 [PMID:28972753] |
| ChEMBL | Activity at hMC4R transfected in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Activity against hMC4R transfected in HEK293 cells by intracellular cAMP accumulation | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Agonist activity at human melanocortin 4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.54 | pEC50 | 2.87 | nM | EC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | F | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Activity at human MC4R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | F | 8.64 | pEC50 | 2.3 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Agonist activity at human MC4 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | F | 8.68 | pEC50 | 2.1 | nM | EC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.68 | pEC50 | 2.1 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Agonist activity at human MC4R expressed in HEK293 cells after 3 mins by cAMP assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Agonistic activity against human melanocortin receptor (hMC4R) for cAMP accumulation | F | 9.22 | pEC50 | 0.6 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Agonist activity at human MC4R expressed in low doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 45 mins by HTRF method | F | 9.46 | pEC50 | 0.35 | nM | EC50 | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| ChEMBL | Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using low doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Effective concentration required for the biological activity against human Melanocortin 4 receptor | B | 10.24 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2003) 46: 4215-4231 [PMID:13678399] |
| ChEMBL | Agonist activity at human melanocortin receptor 4 expressed in human T-REx-293 cells using high doxycycline assessed as stimulation of intracellular cAMP accumulation incubated for 45 mins by LANCE cAMP assay | F | 10.3 | pEC50 | <0.05 | nM | EC50 | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Effective concentration for intracellular cAMP accumulation in L-cells expressing Melanocortin 4 receptor | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Agonist activity at human MC4R expressed in high doxycyclin-treated HEK293 cell membranes assessed as increase in cAMP production after 15 mins by HTRF method | F | 10.5 | pEC50 | <0.03 | nM | EC50 | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| MC4 receptor/Melanocortin receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450] | ||||||||
| ChEMBL | Agonist activity to the mouse Melanocortin-4 receptor (mMC4R) | F | 10.06 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2002) 45: 3073-3081 [PMID:12086493] |
| ChEMBL | Activity in mouse melanocortin-4 receptor stably expressed in HEK293 cells | B | 10.06 | pEC50 | 0.09 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| ChEMBL | Activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | F | 10.22 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2014) 57: 9424-9434 [PMID:25347033] |
| ChEMBL | Effective concentration for mouse Melanocortin-4 receptor | B | 10.28 | pEC50 | 0.05 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
| ChEMBL | Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | B | 10.3 | pEC50 | 0.05 | nM | EC50 | ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138] |
| ChEMBL | Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay | F | 10.4 | pEC50 | 0.04 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032] | ||||||||
| ChEMBL | Inhibitory concentration against human Melanocortin 5 receptor (hMC5R) | B | 7.36 | pIC50 | 43.6 | nM | IC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK2936E cell membrane measured after 16-23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 7.57 | pIC50 | 26.92 | nM | IC50 | J Med Chem (2021) 64: 9906-9915 [PMID:34197114] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC5R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay | B | 7.63 | pIC50 | 23.44 | nM | IC50 | J Med Chem (2018) 61: 3674-3684 [PMID:29605997] |
| ChEMBL | Displacement of [125I]NDP-alphaMSH from human MC5 receptor expressed in HEK293 cells | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Displacement of [125I][Nle4,Dphe7]-alpha-MSH from human MC5R expressed in HEK293 cells | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Displacement of 125I-labeled [Nle4,DPhe7]-alpha-MSH from human melanocortin 5 receptor expressed in HEK293 cells incubated for 40 mins by gamma counting analysis | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting method | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Inhibitory activity against hMC5R transfected in HEK293 cells | B | 8.12 | pIC50 | 7.5 | nM | IC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Displacement of [125I][Nle4,D-Phe7]alpha-MSH from human MC5 receptor expressed in HEK293 cells | B | 8.13 | pIC50 | 7.47 | nM | IC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by Wallac 1470 gamma counting | B | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Displacement of [125I]-NDP-alpha-MSH from human MC5 receptor expressed in HEK293 cells by gamma counting analysis | B | 8.38 | pIC50 | 4.2 | nM | IC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Displacement of [125I]-[Nle4,d-Phe7]-alpha-MSH from human MC5R expressed in HEK293 cells after 40 mins by gamma counting analysis | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| GtoPdb | - | - | 9 | pIC50 | - | - | - | Eur J Pharmacol (2002) 440: 141-57 [PMID:12007532] |
| ChEMBL | Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay | F | 7.47 | pEC50 | 33.9 | nM | EC50 | J Med Chem (2017) 60: 8716-8730 [PMID:28972753] |
| ChEMBL | Agonistic activity against human melanocortin receptor (hMC5R) for cAMP accumulation | F | 7.6 | pEC50 | 25 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1307-1311 [PMID:12657270] |
| ChEMBL | Activity at human MC5R expressed in HEK293 cells assessed by measuring intracellular cAMP accumulation | F | 8.1 | pEC50 | 8 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 5462-5467 [PMID:16931008] |
| ChEMBL | Agonist activity at human MC5R expressed in HEK293 cells after 3 mins by cAMP assay | F | 8.22 | pEC50 | 6 | nM | EC50 | Eur J Med Chem (2018) 151: 815-823 [PMID:29679901] |
| ChEMBL | Antagonist activity at human MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by luminescence counter | F | 8.24 | pEC50 | 5.7 | nM | EC50 | ACS Med Chem Lett (2015) 6: 192-197 [PMID:25699148] |
| ChEMBL | Agonist activity at human MC5R expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.24 | pEC50 | 5.7 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 3099-3102 [PMID:21486697] |
| ChEMBL | Agonist activity at human MC5R expressed in HEK293 cells assessed as stimulation of intracellular cAMP level | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2009) 52: 3627-3635 [PMID:19473029] |
| ChEMBL | Agonist activity at human melanocortin 5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation incubated for 3 mins in presence of IBMX | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2015) 58: 9773-9778 [PMID:26599352] |
| ChEMBL | Activity against hMC5R transfected in HEK293 cells by intracellular cAMP accumulation | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2006) 49: 1946-1952 [PMID:16539382] |
| ChEMBL | Agonist activity at human MC5R expressed in HEK293 cells assessed as induction of intracellular cAMP accumulation after 3 mins | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2018) 61: 4263-4269 [PMID:29660981] |
| ChEMBL | Activity at hMC5R transfected in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2006) 49: 6888-6896 [PMID:17154518] |
| ChEMBL | Agonist activity at human MC5 receptor expressed in HEK293 cells assessed as intracellular cAMP accumulation | F | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2008) 51: 187-195 [PMID:18088090] |
| ChEMBL | Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor | F | 8.83 | pEC50 | 1.48 | nM | EC50 | J Med Chem (1997) 40: 1738-1748 [PMID:9171884] |
| MC5 receptor/Melanocortin receptor 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4489] [GtoPdb: 286] [UniProtKB: P41149] | ||||||||
| ChEMBL | Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay | B | 9.24 | pEC50 | 0.57 | nM | EC50 | ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138] |
| ChEMBL | Activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation by CRE/beta-galactosidase reporter gene assay | F | 9.72 | pEC50 | 0.19 | nM | EC50 | J Med Chem (2014) 57: 9424-9434 [PMID:25347033] |
| ChEMBL | Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay | F | 9.74 | pEC50 | 0.18 | nM | EC50 | J Med Chem (2004) 47: 6702-6710 [PMID:15615519] |
| ChEMBL | Agonist activity towards mouse Melanocortin-5 receptor (mMC5R) | F | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2002) 45: 3073-3081 [PMID:12086493] |
| ChEMBL | Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells | B | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2002) 45: 5736-5744 [PMID:12477357] |
| ChEMBL | Effective concentration for mouse Melanocortin-5 receptor | B | 10.17 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2005) 48: 3060-3075 [PMID:15828845] |
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]
