ChEMBL ligand: CHEMBL2070241 (Bremelanotida, 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	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	8.72	pKi	1.91	nM	Ki	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	10.02	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]
ChEMBL	Agonist activity at human MC1R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	F	10.11	pEC50	0.08	nM	EC50	J Med Chem (2022) 65: 12956-12969 [PMID:36167503]
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 expressed in HEK2936E cell membrane measured after 16 to 23 hrs by 1450 microbeta trilux scintillation proximity assay	B	6.7	pKi	199.53	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	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]
ChEMBL	Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	F	9.17	pEC50	0.68	nM	EC50	J Med Chem (2022) 65: 12956-12969 [PMID:36167503]
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]
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	7.7	pKi	19.95	nM	Ki	J Med Chem (2022) 65: 12956-12969 [PMID:36167503]
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	Antagonist activity at human MC4R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	F	8.84	pEC50	1.45	nM	EC50	J Med Chem (2022) 65: 12956-12969 [PMID:36167503]
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	Agonist activity at human MC5R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	F	6.7	pIC50	199.53	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	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 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]