ArrestinDb

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Ligand source activities (1 row/activity)

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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

(1R,2S)-PHENYLPROPANOLAMINE	27120	Functional	13	Rat	Binding	pKi	=	10000.00	5.00	-38	42	-	PDSP KiDatabase	151.1	2	2	2	1.07	C[C@H](N)[C@H](O)c1ccccc1	-
(S)-3,4-DCPG	2079	None	36	Human	Binding	EC50	=	31.00	7.51	-	8	Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells	ChEMBL	239.0	4	4	4	0.17	N[C@H](C(=O)O)c1ccc(C(=O)O)c(C(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.8b01120
ADX88178	300	None	40	Human	Binding	EC50	=	1200.00	5.92	-	4	Positive allosteric modulation of mGluR8 (unknown origin)	ChEMBL	272.1	3	2	6	2.68	Cc1ccnc(Nc2nc(-c3cn[nH]c3)c(C)s2)n1	https://dx.doi.org/10.1016/j.bmcl.2022.129106
Cathinone, (-)	218812	Functional	0	Rat	Binding	pKi	=	10000.00	5.00	-13	40	-	PDSP KiDatabase	149.1	2	1	2	1.22	CC(N)C(=O)c1ccccc1	-
CHEMBL180822	64133	None	0	Human	Binding	Kd	=	6.30	8.20	-	1	Dissociation constant of radiolabeled compound against recombinant human Metabotropic glutamate receptor 8	ChEMBL	189.1	4	4	4	-1.66	N[C@H](C(=O)O)[C@@H]1C(C(=O)O)[C@@H]1CO	https://dx.doi.org/10.1016/j.bmcl.2004.10.093
CHEMBL197976	72197	None	1	Rat	Binding	Ki	=	63000.00	4.20	-8	3	Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells	ChEMBL	195.0	3	4	3	-1.04	N[C@H](C(=O)O)[C@H]1C[C@@H]1P(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2005.09.014
CHEMBL199626	72701	None	1	Rat	Binding	Ki	=	54000.00	4.27	-1	3	Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells	ChEMBL	195.0	3	4	3	-1.04	N[C@H](C(=O)O)[C@@H]1C[C@H]1P(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2005.09.014
CHEMBL2381640	90084	None	2	Human	Binding	EC50	=	6530.00	5.18	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	199.0	2	3	4	-1.31	N[C@@]1(C(=O)O)CC(=O)[C@@H]2[C@H]1[C@H]2C(=O)O	https://dx.doi.org/10.1021/jm4000165
CHEMBL2381641	90085	None	1	Human	Binding	EC50	=	1590.00	5.80	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	197.1	2	3	3	-0.33	C=C1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	https://dx.doi.org/10.1021/jm4000165
CHEMBL2381644	90088	None	0	Human	Binding	EC50	=	12400.00	4.91	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226.1	3	3	4	-0.20	[N-]=[N+]=N[C@@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@@H]21	https://dx.doi.org/10.1021/jm4000165
CHEMBL2381645	90089	None	0	Human	Binding	EC50	=	12000.00	4.92	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	226.1	3	3	4	-0.20	[N-]=[N+]=N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	https://dx.doi.org/10.1021/jm4000165
CHEMBL2381649	90093	None	0	Human	Binding	EC50	=	4300.00	5.37	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	242.1	3	4	4	-1.38	CC(=O)N[C@H]1C[C@@](N)(C(=O)O)[C@@H]2[C@@H](C(=O)O)[C@H]12	https://dx.doi.org/10.1021/jm4000165
CHEMBL2381652	90096	None	0	Human	Binding	EC50	=	11500.00	4.94	-	4	Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay	ChEMBL	203.1	2	3	3	-0.54	N[C@@]1(C(=O)O)C[C@@H](F)[C@H]2[C@H](C(=O)O)[C@H]21	https://dx.doi.org/10.1021/jm4000165
CHEMBL285843	99919	None	47	Human	Binding	IC50	=	5.10	8.29	1	8	Inhibitory concentration against [3H]1 binding to recombinant human Metabotropic glutamate receptor 8	ChEMBL	183.0	4	4	3	-1.03	NC(CCP(=O)(O)O)C(=O)O	https://dx.doi.org/10.1016/j.bmcl.2004.10.093
CHEMBL285843	99919	Functional	47	Human	Binding	pKi	=	400.00	6.40	1	8	-	PDSP KiDatabase	183.0	4	4	3	-1.03	NC(CCP(=O)(O)O)C(=O)O	-
CHEMBL285843	99919	Functional	47	Rat	Binding	pKi	=	1258.93	5.90	-4	8	-	PDSP KiDatabase	183.0	4	4	3	-1.03	NC(CCP(=O)(O)O)C(=O)O	-
CHEMBL285843	99919	3H-CPPG	47	Rat	Binding	pKi	=	2700.00	5.57	-4	8	-	PDSP KiDatabase	183.0	4	4	3	-1.03	NC(CCP(=O)(O)O)C(=O)O	-
CHEMBL3955188	150689	None	0	Human	Binding	IC50	=	26670.00	4.57	-	4	Binding affinity to mGluR8 (unknown origin) by FLIPR assay	ChEMBL	416.2	6	1	5	4.03	COc1ccc(-c2cc(C(N)=O)nc3cc(CCc4cnc(C)nc4)ccc23)c(F)c1	https://dx.doi.org/10.1021/acsmedchemlett.3c00175
CHEMBL404886	155755	None	0	Rat	Binding	IC50	=	5000.00	5.30	-	2	Displacement of [3H]-L-AP4 from rat mGluR8	ChEMBL	437.1	2	2	6	3.98	O=C1CC(c2cccc(-n3ccnn3)c2)=Nc2cc(O)c(C#Cc3ccc(F)cc3)cc2N1	https://dx.doi.org/10.1016/j.bmcl.2007.12.005
CHEMBL4160748	162172	None	38	Human	Binding	EC50	=	2600.00	5.58	-	5	Agonist activity at mGlu8 (unknown origin)	ChEMBL	357.1	2	0	4	4.32	COc1ccc(-c2c(C)nn3c(C(F)(F)F)cc(C)nc23)c(F)c1F	https://dx.doi.org/10.1039/C8MD00524A

Showing 1 to 20 of 64 entries

	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

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Ligand source activities (1 row/activity)