GPCRdb

	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

[¹⁹Lys,²⁶Leu]-galparan	3708	None	0	Rat	Binding	pKd	=	-	9.15	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8738882
[²Ala]-galparan	3709	None	0	Rat	Binding	pKd	=	-	5.80	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8738882
[D-Trp²]galanin-(1-29)	1499	None	0	Human	Binding	Kd	=	0.40	9.40	5	4	Binding affinity to human GalR1	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm801088x
[N-Me,des-Sar]Gal-B2	2832	None	0	Human	Binding	pKi	=	-	6.44	-17	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/20121116
C7	777	None	0	Human	Binding	pKi	=	-	9.62	4	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9808667
C7	777	None	0	Human	Binding	pKi	=	-	9.62	4	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9880084
C7	777	None	0	Rat	Binding	pKi	=	-	8.68	-8	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9305929
C7	777	None	0	Rat	Binding	pKi	=	-	8.68	-8	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9722565
C7	777	None	0	Rat	Binding	pKi	=	-	8.68	-8	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8750821
C7	777	None	0	Mouse	Binding	pKi	=	-	8.86	-5	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9271210
C7	777	None	0	Mouse	Binding	pKi	=	-	8.86	-5	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9832122
CHEMBL1790054	63205	None	0	Human	Binding	Ki	=	3.30	8.48	19	2	Displacement of europium-labeled galanin from human GalR1 expressed in HEK293 EBNA cells	ChEMBL	2195.3	78	32	26	-3.15	CCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O	https://dx.doi.org/10.1021/jm801088x
CHEMBL180966	64303	None	12	Rat	Binding	IC50	=	3.00	8.52	-	1	Inhibition of [3H]glycine uptake at rat glycine transporter 1 expressed in african green monkey COS7 cells	ChEMBL	393.2	9	1	3	5.02	CN(CC[C@@H](Oc1ccc(-c2ccccc2)cc1)c1ccc(F)cc1)CC(=O)O	https://dx.doi.org/10.1016/j.bmcl.2008.10.104
CHEMBL1921902	68765	None	0	Human	Binding	IC50	=	8590.00	5.07	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	375.2	6	2	6	4.96	COc1ccc(Nc2cc(Nc3ccccc3)nc(N3CCCCC3)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921903	68766	None	0	Human	Binding	IC50	=	34860.00	4.46	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	429.2	6	2	6	5.85	FC(F)(F)Oc1cccc(Nc2cc(Nc3ccccc3)nc(N3CCCCC3)n2)c1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921989	68818	None	0	Human	Binding	IC50	=	6900.00	5.16	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	411.2	7	2	6	5.56	FC(F)Oc1cccc(Nc2cc(Nc3ccccc3)nc(N3CCCCC3)n2)c1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921991	68820	None	0	Human	Binding	IC50	=	6770.00	5.17	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	393.2	6	2	6	5.10	COc1ccc(Nc2cc(Nc3ccccc3)nc(N3CCCCC3)n2)cc1F	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921992	68821	None	0	Human	Binding	IC50	=	12800.00	4.89	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	430.2	6	1	7	4.16	COc1ccc(Nc2cc(N3CCN(c4ccccc4)CC3)nc(N3CCCC3)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921993	68822	None	0	Human	Binding	IC50	=	4600.00	5.34	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	391.2	7	2	7	4.58	COc1ccc(Nc2cc(Nc3cccc(OC)c3)nc(N3CCCC3)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033
CHEMBL1921995	68824	None	0	Human	Binding	IC50	=	27500.00	4.56	-	2	Displacement of [125I]galanin from GalR1 by gamma counting	ChEMBL	455.2	9	3	7	6.32	COc1ccc(Nc2cc(Nc3ccc(OC(F)F)cc3)nc(NC3CCCCC3)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.09.033

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

2,3-dihydro-1,4-dithiin-1,1,4,4-tetroxide	48	None	0	Human	Functional	pIC50	=	-	5.57	-	1	Unclassified	Guide to Pharmacology	182.0	0	0	4	-0.70	O=S1(=O)C=CS(=O)(=O)CC1	https://pubmed.ncbi.nlm.nih.gov/10896115
[Sar¹, D-Ala¹²]galanin(1-16)	3482	None	0	Human	Functional	pIC50	=	-	9.40	4	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11491429
alarin	327	None	0	Rat	Functional	pIC50	>	-	6.00	-1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/20880399
C7	777	None	0	Human	Functional	pIC50	=	-	8.59	1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941
C7	777	None	0	Human	Functional	pIC50	=	-	8.59	1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9685625
C7	777	None	0	Rat	Functional	pIC50	=	-	8.31	-1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941
C7	777	None	0	Rat	Functional	pIC50	=	-	8.31	-1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9108306
dithiipin-1,1,4,4-tetroxide analogue 7	1439	None	0	Human	Functional	pIC50	=	-	6.72	158	2	Unclassified	Guide to Pharmacology	286.0	1	0	4	1.53	Cc1ccc(C2=CS(=O)(=O)CCCS2(=O)=O)cc1	https://pubmed.ncbi.nlm.nih.gov/10896115
galanin	1715	None	0	Human	Functional	pIC50	=	-	9.89	1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9685625
galanin	1716	None	20	Human	Functional	pIC50	=	-	9.73	-1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11481429
galanin	1716	None	20	Human	Functional	pIC50	=	-	9.73	-1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941
galanin	1716	None	20	Human	Functional	pIC50	=	-	9.73	-1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9685625
galanin	1714	None	0	Human	Functional	pIC50	=	-	9.82	-2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941
galanin	1714	None	0	Human	Functional	pIC50	=	-	9.82	-2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9685625
galanin	1714	None	0	Rat	Functional	pIC50	=	-	10.19	2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941
galanin	1714	None	0	Rat	Functional	pIC50	=	-	10.19	2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9108306
galanin	1715	None	0	Rat	Functional	pIC50	=	-	9.43	-1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10601261
galanin	1715	None	0	Rat	Functional	pIC50	=	-	9.43	-1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/20880399
galanin	1715	None	0	Rat	Functional	pEC50	=	-	9.80	-1	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10601261
galanin	1716	None	20	Rat	Functional	pIC50	=	-	10.19	1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9168941

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Ligand source activities (1 row/activity)