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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

(S)-FTY720-phosphate	3596	None	37	Human	Binding	IC50	=	0.28	9.55	-	6	Displacement of [33P]S1P from human S1P1R expressed in CHO cell membranes	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/ml100227q
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	19.95	7.70	-	6	Agonist activity at human S1P1 receptor expressed in CHO-K1 EDG1 cells by beta-arrestin recruitment assay	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.5b01512
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	3.98	8.40	-	6	Agonist activity at human S1P1 receptor expressed in RH7777 cells by [35S]GTP-gammaS accumulation assay	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.5b01512
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	0.02	10.70	-	6	Agonist activity at human recombinant S1P1 expressed in CHO cells assessed as stimulation of ERK phosphorylation incubated for 7 mins by microplate reader analysis	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.8b01695
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	0.07	10.15	-	6	Agonist activity at human recombinant C-terminal GFP-fused S1P1 expressed in CHO cells assessed as induction of receptor internalization incubated for 50 mins by fluorescence based confocal laser scanning microscopic analysis	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.8b01695
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	0.28	9.55	-	6	Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b00089
(S)-FTY720-phosphate	3596	None	37	Human	Binding	EC50	=	0.40	9.40	-	6	Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2015.11.090
A-971432	215	None	30	Human	Binding	EC50	=	398.11	6.40	-	3	Modulation of S1PR1 (unknown origin)	ChEMBL	365.1	6	1	3	4.09	O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1	https://dx.doi.org/10.1016/j.ejmech.2023.115182
A-971432	215	None	30	Human	Binding	IC50	=	362.00	6.44	-	3	Displacement of [33P]S1P from S1P1 receptor (unknown origin) expressed in HEK cell membranes after 45 to 60 mins by scintillation counting based RLB method	ChEMBL	365.1	6	1	3	4.09	O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1	https://dx.doi.org/10.1021/acs.jmedchem.5b00928
AMISELIMOD	133577	None	22	Human	Binding	EC50	=	0.08	10.10	-	1	Modulation of S1PR1 (unknown origin)	ChEMBL	377.2	12	3	4	3.67	CCCCCCCOc1ccc(CCC(N)(CO)CO)cc1C(F)(F)F	https://dx.doi.org/10.1016/j.ejmech.2023.115182
ASP4058	502	None	23	Human	Binding	EC50	=	7.94	8.10	-	4	Modulation of S1PR1 (unknown origin)	ChEMBL	442.1	4	1	5	5.63	C[C@H](Oc1ccc(-c2nc(-c3ccc4[nH]cnc4c3)no2)cc1C(F)(F)F)C(F)(F)F	https://dx.doi.org/10.1016/j.ejmech.2023.115182
ASP4058	502	None	23	Human	Binding	pIC50	=	-	8.13	-	4	In a GTPγS binding assay.	Guide to Pharmacology	442.1	4	1	5	5.63	C[C@H](Oc1ccc(-c2nc(-c3ccc4[nH]cnc4c3)no2)cc1C(F)(F)F)C(F)(F)F	https://pubmed.ncbi.nlm.nih.gov/25347187
AUY954	524	None	19	Human	Binding	EC50	=	1.20	8.92	-	7	Activation of human recombinant S1P1 expressed in CHO cell membranes after 120 mins by GTP-gamma-35S-binding assay	ChEMBL	455.1	7	2	3	6.82	O=C(O)CCNCc1ccc2sc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)cc2c1	https://dx.doi.org/10.1016/j.bmcl.2018.10.042
cenerimod	878	None	36	Human	Binding	EC50	=	1.00	9.00	-	1	Modulation of S1PR1 (unknown origin)	ChEMBL	453.2	9	2	8	4.07	CCc1cc(-c2noc(-c3cc(OC)nc(C4CCCC4)c3)n2)cc(C)c1OC[C@@H](O)CO	https://dx.doi.org/10.1016/j.ejmech.2023.115182
CHEMBL1088819	7703	None	0	Human	Binding	IC50	=	3.40	8.47	-	2	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	495.2	10	4	6	3.61	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C#N)c1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1088820	7704	None	0	Human	Binding	IC50	=	0.80	9.10	-	2	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	504.1	10	4	5	4.39	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(Cl)c1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1089127	7763	None	0	Human	Binding	IC50	=	1.30	8.89	-	2	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	548.1	10	4	5	4.50	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(Br)c1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1090673	8000	None	0	Human	Binding	IC50	=	150.00	6.82	-	1	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	513.2	11	5	6	2.84	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(N)=O)c1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1090782	8022	None	0	Human	Binding	IC50	=	500.00	6.30	-	1	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	527.2	11	5	6	3.10	CNC(=O)c1cc(NC(=O)[C@@](C)(N)COP(=O)(O)O)ccc1OCCc1ccc(-c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1090796	8023	None	0	Human	Binding	IC50	=	4.14	8.38	-	4	Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	482.2	10	4	5	3.93	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(C(=O)CCc2ccc(-c3ccccc3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098

Showing 1 to 20 of 985 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)