GPCRdb

Finalizing display...

Ligand source activities (1 row/activity)

Affinity
Potency

Search:

	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	pKi	None	-	8.20	3	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10358030
α-MSH	366	None	0	Human	Binding	pKi	None	-	8.20	3	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10493100
γ-MSH	1763	None	0	Human	Binding	pKd	None	-	8.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10358030
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	72.00	7.14	1	4	Binding affinity for Human Melanocortin 3 receptor expressed in L-cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
[D-Trp⁸]γ-MSH	1501	None	4	Human	Binding	IC50	=	71.00	7.15	1	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 3 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	=	40.00	7.40	1	4	Inhibition of [125I]NDP-MSH binding to Melanocortin 3 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	=	690.00	6.16	1	4	Binding affinity against human Melanocortin 3 receptor by gamma-MCH displacement.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030119t
ACTH	277	None	0	Human	Binding	pKi	=	-	7.06	-5	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7774675
ACTH	277	None	0	Human	Binding	pKi	=	7.06	8.15	-5	5	None	Drug Central	-	-	-	-	-	-	-
ACTH-(4-10)	218797	125I-NDP-MSH	0	Human	Binding	pKi	=	784.00	6.11	-7	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	=	784.00	6.11	-7	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	pKi	None	-	8.90	-2	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10493100
afamelanotide	302	None	19	Human	Binding	Ki	=	0.68	9.17	-2	8	Binding affinity towards human Melanocortin 3 receptor (hMC3R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00552-3
afamelanotide	302	None	19	Human	Binding	IC50	=	1.17	8.93	-2	8	Displacement of [125I]NDP-MSH from Melanocortin 3 receptor at 10 uM	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Binding	IC50	=	1.17	8.93	-2	8	Inhibitory concentration against human Melanocortin 3 receptor (hMC3R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Binding	IC50	=	3.30	8.48	-2	8	Inhibition of human Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030111j
afamelanotide	302	None	19	Human	Binding	IC50	=	2.90	8.54	-2	8	Binding affinity for Human Melanocortin 3 receptor expressed in L-cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
afamelanotide	302	None	19	Human	Binding	EC50	=	0.13	9.89	-2	8	Effective concentration required for the biological activity against human Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0303103
afamelanotide	302	None	19	Human	Binding	IC50	=	3.80	8.42	-2	8	Inhibitory activity against Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm00018a005
afamelanotide	302	None	19	Human	Binding	IC50	=	3.30	8.48	-2	8	Inhibition of [125I]NDP-MSH binding to Melanocortin 3 receptor expressed in HEK293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s

Showing 1 to 20 of 1,138 entries

Search:

	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	pIC50	=	-	8.20	1	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11150170
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	5.90	8.23	1	4	Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
[D-Trp⁸]γ-MSH	1501	None	4	Human	Functional	EC50	=	700.00	6.16	1	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 3 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	=	520.00	6.28	1	4	Effective concentration for intracellular cAMP accumulation in human melanocortin 3 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	=	3.70	8.43	1	4	Intracellular cAMP accumulation in human Melanocortin 3 receptor functional assay.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030119t
afamelanotide	302	None	19	Human	Functional	EC50	=	0.36	9.44	-15	8	In vitro agonist potency was evaluated in HEK293 cells transfected with human melanocortin receptor (hMC3R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/s0960-894x(03)00552-3
afamelanotide	302	None	19	Human	Functional	EC50	=	4.10	8.39	-15	8	effective concentration of peptide at 50% maximal cAMP accumulation on Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960840h
afamelanotide	302	None	19	Human	Functional	EC50	=	4.10	8.39	-15	8	Effective concentration that was able to generate 50% maximal intracellular cAMP in L-cells transfected with Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm960845e
afamelanotide	302	None	19	Human	Functional	EC50	=	0.80	9.10	-15	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	=	0.24	9.62	-15	8	Effective concentration required for intracellular cAMP accumulation against Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm000211e
afamelanotide	302	None	19	Human	Functional	EC50	=	0.13	9.88	-15	8	Evaluated for agonist activity at cloned Melanocortin 3 receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm00018a005
afamelanotide	302	None	19	Human	Functional	EC50	=	0.80	9.10	-15	8	Effective concentration for intracellular cAMP accumulation in human melanocortin 3 receptor expressing HEK 293 cells; (N = 4)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm049579s
afamelanotide	302	None	19	Human	Functional	EC50	=	6.80	8.17	-15	8	Agonist activity at EYFP-fused human MC3R 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	=	0.30	9.52	-15	8	Agonist activity at human MC3R 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	Rat	Functional	EC50	=	0.10	10.00	-1	8	Maximal agonist response at rat melanocortin 3 receptor (MC3R)	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm030452x
agouti-related protein	315	None	0	Human	Functional	pIC50	None	-	7.70	-39	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9819197
bremelanotide	720	None	23	Human	Functional	pEC50	=	8.62	8.06	-5	4	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	Drug Central	-	-	-	-	-	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	-
bremelanotide	720	None	23	Human	Functional	EC50	=	0.68	9.17	-5	4	Agonist activity at human MC3R expressed in HEK2936E cells assessed as cAMP production in presence of IBMX by time resolved fluorescence assay	ChEMBL	-	-	-	-	-	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.2c00793
bremelanotide	720	None	23	Human	Functional	EC50	=	0.68	9.17	-5	4	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	ChEMBL	-	-	-	-	-	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.1c00095
bremelanotide	720	None	23	Human	Functional	EC50	=	2.40	8.62	-5	4	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	ChEMBL	-	-	-	-	-	CCCC[C@H](NC(C)=O)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2cnc[nH]2)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.8b00170

Showing 1 to 20 of 555 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)