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Ligand source activities (1 row/activity)

Affinity
Potency

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

α-MSH	366	None	0	Human	Binding	pKd	None	-	6.90	-19	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12007532
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	2500.00	5.60	-3	4	Binding affinity for Human Melanocortin 5 receptor expressed in L-cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	2200.00	5.66	-3	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	330.00	6.48	-3	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	Ki	=	2100.00	5.68	-3	4	Binding affinity against human Melanocortin 5 receptor by gamma-MCH displacement.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030119t
ACTH	277	None	0	Human	Binding	pKi	>	-	5.00	-2187	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7774675
ACTH-(4-10)	218797	125I-NDP-MSH	0	Human	Binding	pKi	=	10000.00	5.00	-93	4	-	PDSP KiDatabase	961.4	29	13	12	-1.46	CSCCC(N)C(=O)NC(CCC(=O)O)C(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCC(=O)O	-
ACTH-(4-10)	218797	125I-[Nle4,D-Phe7]Alpha-MSH	0	Human	Binding	pKi	=	10000.00	5.00	-93	4	-	PDSP KiDatabase	961.4	29	13	12	-1.46	CSCCC(N)C(=O)NC(CCC(=O)O)C(=O)NC(Cc1cnc[nH]1)C(=O)NC(Cc1ccccc1)C(=O)NC(CCCN=C(N)N)C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)NCC(=O)O	-
afamelanotide	302	None	19	Human	Binding	IC50	=	0.86	9.07	-6	8	Displacement of [125I]NDP-MSH from Melanocortin 5 receptor at 10 uM	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Binding	IC50	=	0.86	9.07	-6	8	Inhibitory concentration against human Melanocortin 5 receptor (hMC5R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Binding	IC50	=	2.20	8.66	-6	8	Inhibition of human melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030111j
afamelanotide	302	None	19	Human	Binding	IC50	=	0.89	9.05	-6	8	Binding affinity for Human Melanocortin 5 receptor expressed in L-cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
afamelanotide	302	None	19	Human	Binding	IC50	=	2.20	8.66	-6	8	Inhibition of [125I]NDP-MSH binding to Melanocortin 5 receptor expressed in HEK293 cells; N = 4	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
afamelanotide	302	None	19	Human	Binding	Ki	=	9.90	8.00	-6	8	Displacement of Eu-NDP-alphaMSH from human MC5 receptor expressed in human HEK293 cells after 1.5 hrs by time-resolved fluorescence analysis	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm201226w
afamelanotide	302	None	19	Human	Binding	Ki	=	0.48	9.32	-6	8	Displacement of [125I]-NAD-alpha-MSH from human recombinant MC3 receptor human MC5 expressed in BHK570 cells after 1 hr in presence of ovalbumin	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm201489a
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.07	10.15	-	8	In vitro activation of mouse recombinant Melanocortin-5 receptor.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0104872
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.07	10.15	-	8	Activity in mouse melanocortin-5 receptor stably expressed in HEK293 cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm020296e
afamelanotide	302	None	19	Mouse	Binding	EC50	=	0.10	10.02	-	8	Effective concentration for mouse Melanocortin-5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049010r
afamelanotide	302	None	19	Mouse	Binding	IC50	=	140.00	6.85	-	8	Displacement of [125I]-NDP-MSH from mouse melanocortin receptor 5 expressed in HEK293 cell mebranes incubated for 1 hr by automatic gamma counting method	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.9b00860
agouti	314	None	0	Mouse	Binding	pKd	None	-	4.90	-5011	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9454589

Showing 1 to 20 of 984 entries

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	550.00	6.26	-17	4	Intracellular cAMP accumulation in human Melanocortin 5 receptor functional assay.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030119t
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	490.00	6.31	-17	4	Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	550.00	6.26	-17	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	390.00	6.41	-17	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
Ac-c[Cys-Glu-His-D-Phe-Arg-Trp-D-Cys]-Pro-Pro-Lys-Asp-NH₂	247	None	0	Human	Functional	pIC50	None	-	8.00	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12904077
afamelanotide	302	None	19	Human	Functional	pIC50	None	-	9.00	-13	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12007532
afamelanotide	302	None	19	Human	Functional	EC50	=	0.58	9.24	-13	8	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Functional	EC50	=	0.58	9.24	-13	8	Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Functional	EC50	=	1.00	9.00	-13	8	Effective concentration of peptide at 50% maximal cAMP generation	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030111j
afamelanotide	302	None	19	Human	Functional	EC50	=	0.23	9.64	-13	8	Effective concentration required for intracellular cAMP accumulation by Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
afamelanotide	302	None	19	Human	Functional	EC50	=	1.00	9.00	-13	8	Effective concentration for intracellular cAMP accumulation in human melanocortin 5 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
afamelanotide	302	None	19	Human	Functional	EC50	=	1.10	8.96	-13	8	Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.7b00353
afamelanotide	302	None	19	Human	Functional	EC50	=	0.40	9.40	-13	8	Agonist activity at human MC5R expressed in HEK293 cells assessed as increase in cAMP production incubated for 2 hrs by AlphaScreen assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.8b00251
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.06	10.19	-5	8	Maximum agonist response for mouse melanocortin 5 receptor (MC5R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030452x
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.07	10.15	-5	8	Agonist activity towards mouse Melanocortin-5 receptor (mMC5R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm010524p
afamelanotide	302	None	19	Mouse	Functional	EC50	=	170.00	6.77	-5	8	Agonist activity on mouse melanocortin 5 receptor (mMC5R) stably expressed in HEL cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00318-4
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.07	10.15	-5	8	Effective concentration against mouse Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0303608
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.09	10.07	-5	8	Functional activity at the mouse melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm010061n
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.08	10.11	-5	8	In vitro agonist potency for Mouse Melanocortin 5 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0490843
afamelanotide	302	None	19	Mouse	Functional	EC50	=	0.06	10.21	-5	8	Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0492756

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Ligand source activities (1 row/activity)