ArrestinDb

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Ligand source activities (1 row/activity)

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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

CHEMBL4781545	182185	None	0	Human	Binding	Ki	=	15.85	7.80	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	365.1	5	2	2	4.89	O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL4781545	182185	None	0	Human	Binding	Ki	=	25.12	7.60	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	365.1	5	2	2	4.89	O=C(O)Cc1ccccc1NC(=O)c1cccc(-c2ccc(Cl)cc2)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5394500	194991	None	0	Human	Binding	Ki	=	1258.93	5.90	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	453.1	7	1	4	6.86	O=C(O)CCc1cccc(Oc2ccc(Oc3cccc4cnccc34)cc2C(F)(F)F)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5394500	194991	None	0	Human	Binding	Ki	=	7943.28	5.10	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	453.1	7	1	4	6.86	O=C(O)CCc1cccc(Oc2ccc(Oc3cccc4cnccc34)cc2C(F)(F)F)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5399663	195262	None	0	Human	Binding	Kd	=	560.00	6.25	-	1	Binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as dissociation constant incubated for 15 mins by BRET assay	ChEMBL	651.3	12	3	10	4.26	Cc1cc(CN2CCN(CCNC3C=CC([N+](=O)[O-])c4nonc43)CC2)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5399663	195262	None	0	Human	Binding	Kd	=	310.00	6.51	-	1	Binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as dissociation constant incubated for 5 mins by NanoBRET assay	ChEMBL	651.3	12	3	10	4.26	Cc1cc(CN2CCN(CCNC3C=CC([N+](=O)[O-])c4nonc43)CC2)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5412414	195873	None	0	Human	Binding	Ki	=	501.19	6.30	1	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	418.2	13	4	6	2.50	NCCCCCCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5412414	195873	None	0	Human	Binding	Ki	=	501.19	6.30	1	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	418.2	13	4	6	2.50	NCCCCCCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5412414	195873	None	0	Mouse	Binding	Ki	=	630.96	6.20	-1	2	Competitive binding affinity to N-terminal Nluc-tagged mouse succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	418.2	13	4	6	2.50	NCCCCCCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5425639	196510	None	0	Human	Binding	Ki	=	794.33	6.10	1	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	347.1	8	3	5	2.00	CCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5425639	196510	None	0	Human	Binding	Ki	=	501.19	6.30	1	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	347.1	8	3	5	2.00	CCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5425639	196510	None	0	Mouse	Binding	Ki	=	630.96	6.20	-1	2	Competitive binding affinity to N-terminal Nluc-tagged mouse succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	347.1	8	3	5	2.00	CCOc1ccc(-c2ccc(C(=O)N[C@@H](CC(=O)O)C(=O)O)o2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5426854	196567	None	0	Human	Binding	Ki	=	39.81	7.40	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	457.2	7	2	4	4.29	Cc1cc(CN2CCN(C)CC2)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5426854	196567	None	0	Human	Binding	Ki	=	50.12	7.30	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	457.2	7	2	4	4.29	Cc1cc(CN2CCN(C)CC2)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5430997	196727	None	3	Human	Binding	Ki	=	316.23	6.50	5	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	398.1	7	3	5	2.31	O=C(O)C[C@H](NC(=O)c1cccc(-c2ccc(OC(F)(F)F)cc2)n1)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5430997	196727	None	3	Human	Binding	Ki	=	251.19	6.60	5	2	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	398.1	7	3	5	2.31	O=C(O)C[C@H](NC(=O)c1cccc(-c2ccc(OC(F)(F)F)cc2)n1)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5430997	196727	None	3	Mouse	Binding	Ki	=	1584.89	5.80	-5	2	Competitive binding affinity to N-terminal Nluc-tagged mouse succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	398.1	7	3	5	2.31	O=C(O)C[C@H](NC(=O)c1cccc(-c2ccc(OC(F)(F)F)cc2)n1)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5432512	196804	None	0	Human	Binding	Ki	=	39.81	7.40	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ChEMBL	379.1	5	2	2	5.20	Cc1cc(Cl)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5432512	196804	None	0	Human	Binding	Ki	=	31.62	7.50	-	1	Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ChEMBL	379.1	5	2	2	5.20	Cc1cc(Cl)ccc1-c1cccc(C(=O)Nc2ccccc2CC(=O)O)c1	https://dx.doi.org/10.1021/acs.jmedchem.3c00552
CHEMBL5438140	197076	None	0	Human	Binding	Kd	=	990.00	6.00	1	2	Binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells using assessed as dissociation constant incubated with for 30 mins by NanoBRET assay	ChEMBL	624.2	19	5	12	3.69	O=C(O)C[C@H](NC(=O)c1ccc(-c2ccc(OCCCCCCNCCNc3ccc([N+](=O)[O-])c4nonc34)cc2)o1)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.3c00552

Showing 1 to 20 of 33 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)