GPCRdb

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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

1DMe	32	None	0	Human	Binding	pKi	None	-	9.10	3	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11024015
1DMe	32	None	0	Human	Binding	pKi	None	-	9.10	3	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12242085
1DMe	32	None	0	Human	Binding	pKi	None	-	9.10	3	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12421602
BIBP3226	631	None	27	Human	Binding	pKi	None	-	6.50	-39	4	Unclassified	Guide to Pharmacology	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://pubmed.ncbi.nlm.nih.gov/11024015
BIBP3226	631	None	27	Human	Binding	pKi	None	-	6.50	-39	4	Unclassified	Guide to Pharmacology	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://pubmed.ncbi.nlm.nih.gov/11325787
BIBP3226	631	None	27	Human	Binding	Ki	=	250.00	6.60	-39	4	Displacement of [3H]EYF from human NPFF2 expressed in CHO cells by radioligand binding assay	ChEMBL	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.5b00925
BIBP3226	631	None	27	Human	Binding	Ki	=	84.00	7.08	-39	4	Binding affinity to human NPFF2 receptor expressed in CHO cells	ChEMBL	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.5b00925
CHEMBL115479	210961	None	0	Rat	Binding	Ki	=	33.00	7.48	-	1	Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF	ChEMBL	-	-	-	-	-	CC(C)C[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/jm00047a005
CHEMBL116185	210972	None	0	Rat	Binding	Ki	=	20.90	7.68	-	1	Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF	ChEMBL	-	-	-	-	-	NC(=O)CC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/jm00047a005
CHEMBL117975	211049	None	0	Rat	Binding	Ki	=	64.00	7.19	-	1	Binding affinity for NPPF receptor in rat spinal cord membranes using the radioligand [125I]-[Tyr1]NPFF	ChEMBL	-	-	-	-	-	NC(=O)CC[C@H](N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/jm00047a005
CHEMBL1672379	211289	None	0	Human	Binding	IC50	=	0.79	9.10	-	2	Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR2 after 2 hrs	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/ml1002053
CHEMBL2165920	211792	None	25	Human	Binding	Ki	=	23.00	7.64	-10	2	Displacement of [125I]EYF from human NPFFR2 expressed in CHO cells by gamma-counter method	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.0c00643
CHEMBL2165920	211792	None	25	Human	Binding	Ki	=	0.90	9.05	-10	2	Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.1c00256
CHEMBL2204019	83575	None	0	Human	Binding	Ki	=	2015.00	5.70	-10	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	424.2	11	6	4	0.26	N=C(N)NCCC[C@@H](NC(=O)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049
CHEMBL2208294	84178	None	0	Human	Binding	Ki	=	141.00	6.85	-1	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	474.2	11	6	4	1.41	N=C(N)NCCC[C@H](NC(=O)c1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049
CHEMBL2208296	84179	None	0	Human	Binding	Ki	=	136.00	6.87	2	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	463.2	11	7	4	0.74	N=C(N)NCCC[C@H](NC(=O)c1ccc2cc[nH]c2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049
CHEMBL2208299	84180	None	0	Human	Binding	Ki	=	227.00	6.64	-15	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	514.3	13	6	4	1.78	N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049
CHEMBL2208303	84182	None	0	Human	Binding	Ki	=	117.00	6.93	-60	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	450.2	12	6	4	0.66	N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049
CHEMBL2208303	84182	None	0	Human	Binding	Ki	=	175.00	6.76	-60	2	Displacement of [125I]-1DMeNPFF from recombinant human NPFF2 receptor expressed in CHO cells by TopCount scintillation counting method	ChEMBL	450.2	12	6	4	0.66	N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.1c00256
CHEMBL2208304	84183	None	0	Human	Binding	Ki	=	1620.00	5.79	-23	2	Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF2 receptor expressed in CHO cells by scintillation counting	ChEMBL	450.2	12	6	4	0.66	N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.bmcl.2012.10.049

Showing 1 to 20 of 172 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

AC263093	239	None	0	Human	Functional	pEC50	=	-	5.55	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/20354177
BIBP3226	631	None	27	Human	Functional	EC50	=	233.00	6.63	-20	4	Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://dx.doi.org/10.1021/jm300535s
BIBP3226	631	None	27	Human	Functional	EC50	=	113.00	6.95	-20	4	Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	473.2	11	5	4	2.38	NC(N)=NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165920	211792	None	25	Human	Functional	EC50	=	1.70	8.77	21	2	Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165921	82140	None	0	Human	Functional	EC50	=	1256.00	5.90	3	2	Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	374.0	3	3	3	3.54	N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165921	82140	None	0	Human	Functional	EC50	=	1661.00	5.78	3	2	Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	374.0	3	3	3	3.54	N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165922	82141	None	0	Human	Functional	EC50	=	301.00	6.52	-	2	Agonist activity at human NPFF2 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	220.2	2	3	2	1.67	N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165922	82141	None	0	Human	Functional	EC50	=	8332.00	5.08	-	2	Agonist activity at human NPFF2 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	220.2	2	3	2	1.67	N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165922	82141	None	0	Human	Functional	EC50	=	8860.00	5.05	-	2	Agonist activity at human NPFF2 receptor D6.59A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	220.2	2	3	2	1.67	N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165922	82141	None	0	Human	Functional	EC50	=	2449.00	5.61	-	2	Agonist activity at human NPFF2 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	220.2	2	3	2	1.67	N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2	https://dx.doi.org/10.1021/jm300535s
CHEMBL2165922	82141	None	0	Human	Functional	EC50	=	298.00	6.53	-	2	Agonist activity at human NPFF2 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting	ChEMBL	220.2	2	3	2	1.67	N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2	https://dx.doi.org/10.1021/jm300535s
CHEMBL262202	212991	None	24	Human	Functional	EC50	=	517.00	6.29	77	2	Agonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cyclic cAMP accumulation	ChEMBL	-	-	-	-	-	CSCC[C@H](NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.0c00643
CHEMBL326770	213748	None	3	Human	Functional	EC50	=	309.00	6.51	-	4	Agonist activity at human NPFFR2 expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cyclic cAMP accumulation	ChEMBL	-	-	-	-	-	NC(=O)CC[C@H](NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1021/acs.jmedchem.0c00643
CHEMBL3361433	116578	None	0	Human	Functional	EC50	=	645.00	6.19	4	4	Antagonist activity at human NPFF2 receptor expressed in CHO cells assessed as reversal of 1DMe-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control	ChEMBL	443.3	8	4	3	3.26	N=C(N)NCC(=O)NCC1(Cc2cccc3ccccc23)CCN(Cc2ccccc2)CC1	https://dx.doi.org/10.1021/jm500989n
CHEMBL4442534	170122	None	0	Human	Functional	EC50	=	251.19	6.60	-1	3	Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003
CHEMBL4442534	170122	None	0	Human	Functional	EC50	=	250.00	6.60	-1	3	Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003
CHEMBL4442534	170122	None	0	Human	Functional	IC50	=	190.00	6.72	-1	3	Antagonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003
CHEMBL4449491	170612	None	0	Human	Functional	EC50	=	158.49	6.80	2	4	Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003
CHEMBL4449491	170612	None	0	Human	Functional	IC50	=	520.00	6.28	2	4	Antagonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003
CHEMBL4449491	170612	None	0	Human	Functional	EC50	=	170.00	6.77	2	4	Agonist activity at NPFF2 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins	ChEMBL	1164.6	30	12	11	2.66	N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O	https://dx.doi.org/10.1016/j.bmc.2019.01.003

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Ligand source activities (1 row/activity)