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 expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 9.88 | pKi | 0.13 | nM | Ki | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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 | Displacement of sCy5-MT-I from human MC1R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis | B | 10 | pKi | 0.1 | nM | Ki | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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 by competitive binding assay | B | 8.72 | pIC50 | 1.9 | nM | IC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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][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]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 | 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][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 | 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 MC1R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | F | 8.36 | pEC50 | 4.4 | nM | EC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 | 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 | 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 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 MC1R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay | F | 10.2 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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 HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | F | 10.5 | pEC50 | <0.03 | nM | EC50 | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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 expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 7.73 | pKi | 18.62 | nM | Ki | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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 | Displacement of sCy5-MT-I from human MC3R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis | B | 9.03 | pKi | 0.93 | nM | Ki | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in HEK293 cells by competitive binding assay | B | 8.01 | pIC50 | 9.8 | nM | IC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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]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]-[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-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 | 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,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 | 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 | 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 | 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 | 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 maximal intracellular cAMP accumulation by fluorescence based analysis | F | 8.51 | pEC50 | 3.1 | nM | EC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 | 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 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 | 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 | Agonist activity at human MC3R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay | F | 9.4 | pEC50 | 0.4 | nM | EC50 | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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] |
| ChEMBL | Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | F | 10.21 | pEC50 | 0.06 | nM | EC50 | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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]-NDP-alpha-MSH from human MC4R expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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 sCy5-MT-I from human MC4R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis | B | 10.47 | pKi | 0.03 | nM | Ki | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in HEK293 cells by competitive binding assay | B | 8.13 | pIC50 | 7.4 | nM | IC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 | 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][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 | 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 human MC4R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | F | 8.25 | pEC50 | 5.6 | nM | EC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 | 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 | 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 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 MC4R stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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 | Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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 | Displacement of sCy5-MT-I from human MC5R stably expressed in human HEK293 cells incubated for 2 hrs by Cheng-Prusoff equation based FACS analysis | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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 | Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay | F | 7.57 | pIC50 | 26.92 | nM | IC50 | J Med Chem (2022) 65: 12956-12969 [PMID:36167503] |
| 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-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 | 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 | 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 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]-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]-[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] |
| ChEMBL | Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in HEK293 cells by competitive binding assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 stably expressed in human Flp-In-293 cells assessed as cAMP accumulation incubated for 45 mins in presence of IBMX by Lance Ultra cAMP assay | F | 8.2 | pEC50 | 6.31 | nM | EC50 | J Med Chem (2023) 66: 3273-3283 [PMID:36808973] |
| 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 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 | 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 MC5R expressed in HEK293 cells assessed as maximal intracellular cAMP accumulation by fluorescence based analysis | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2022) 65: 4007-4017 [PMID:35188390] |
| 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 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]
