ChEMBL ligand: CHEMBL2070241 (Bremelanotide, PT-141, PT-141 FREE BASE)
MC1 receptor/Melanocortin receptor 1 in Human [ChEMBL: CHEMBL3795] [GtoPdb: 282] [UniProtKB: Q01726] There should be some charts here, you may need to enable JavaScript!
MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968] There should be some charts here, you may need to enable JavaScript!
MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245] There should be some charts here, you may need to enable JavaScript!
MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032] There should be some charts here, you may need to enable JavaScript!

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]
GtoPdb	Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC1 receptor.	-	8.19	pKi	6.4	nM	Ki	J Med Chem (2012) 55: 1969-77 [PMID:22335602]
ChEMBL	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC1 receptor expressed in BHK570 cells after 90 mins in presence of ovalbumin	B	8.19	pKi	6.4	nM	Ki	J Med Chem (2012) 55: 1969-1977 [PMID:22335602]
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	8.72	pKi	1.91	nM	Ki	J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
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	8.72	pKi	1.91	nM	Ki	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	10.02	pEC50	0.1	nM	EC50	J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
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	10.11	pEC50	0.08	nM	EC50	J Med Chem (2021) 64: 9906-9915 [PMID:34197114]
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	6.7	pKi	199.53	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	6.72	pKi	190.55	nM	Ki	J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
ChEMBL	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor expressed in BHK570 cells after 1 hr in presence of ovalbumin	B	7.28	pKi	53	nM	Ki	J Med Chem (2012) 55: 1969-1977 [PMID:22335602]
GtoPdb	Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC3 receptor.	-	7.28	pKi	53	nM	Ki	J Med Chem (2012) 55: 1969-77 [PMID:22335602]
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	8.62	pEC50	2.4	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	9.17	pEC50	0.68	nM	EC50	J Med Chem (2021) 64: 9906-9915 [PMID:34197114]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
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	7.61	pKi	24.55	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	7.66	pKi	21.88	nM	Ki	J Med Chem (2021) 64: 9906-9915 [PMID:34197114]
GtoPdb	Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC4 receptor.	-	9.6	pKi	0.25	nM	Ki	J Med Chem (2012) 55: 1969-77 [PMID:22335602]; Obstet Gynecol (2019) 134: 899-908 [PMID:31599840]
ChEMBL	Displacement of [125I]-NAD-alpha-MSH from MC4 receptor after 2 hrs by gamma counting in presence of ovalbumin	B	9.6	pKi	0.25	nM	Ki	J Med Chem (2012) 55: 1969-1977 [PMID:22335602]
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	8.39	pEC50	4.07	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	8.84	pEC50	1.45	nM	EC50	J Med Chem (2021) 64: 9906-9915 [PMID:34197114]
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	9.61	pEC50	0.25	nM	EC50	J Med Chem (2018) 61: 3674-3684 [PMID:29605997]
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	9.7	pEC50	0.2	nM	EC50	J Med Chem (2012) 55: 1969-1977 [PMID:22335602]
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	9.92	pEC50	0.12	nM	EC50	J Med Chem (2021) 64: 9906-9915 [PMID:34197114]
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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	7.77	pKi	17	nM	Ki	J Med Chem (2012) 55: 1969-1977 [PMID:22335602]
GtoPdb	Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC5 receptor.	-	7.77	pKi	17	nM	Ki	J Med Chem (2012) 55: 1969-77 [PMID:22335602]
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	6.7	pIC50	199.53	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	6.71	pIC50	194.98	nM	IC50	J Med Chem (2018) 61: 3674-3684 [PMID:29605997]

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]