GPCRdb

Finalizing display...

Ligand source activities (1 row/activity)

Affinity
Potency

Search:

	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

A-971432	215	None	30	Human	Binding	IC50	=	6.00	8.22	-	3	Displacement of [33P]S1P from S1P5 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
CHEMBL1090796	8023	None	0	Human	Binding	IC50	=	1360.00	5.87	-	4	Displacement of [33P]sphingosine-1-phosphate from human S1P5 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
CHEMBL1090829	8033	None	0	Human	Binding	IC50	=	184.00	6.74	-	3	Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	561.2	10	4	5	5.67	C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1093429	8413	None	0	Human	Binding	IC50	=	87.20	7.06	-	4	Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	538.1	10	4	5	4.76	C[C@](N)(COP(=O)(O)O)C(=O)Nc1ccc(OCCc2ccc(-c3ccccc3)cc2)c(C(F)(F)F)c1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1093823	8466	None	0	Human	Binding	IC50	=	9.60	8.02	-	4	Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting	ChEMBL	547.1	9	4	5	5.63	C[C@](N)(COP(=O)(O)O)c1nc(-c2ccc(OCc3ccc(-c4ccccc4)cc3)c(C(F)(F)F)c2)c[nH]1	https://dx.doi.org/10.1016/j.bmcl.2010.02.098
CHEMBL1095833	8719	None	24	Human	Binding	IC50	=	142.00	6.85	-	4	Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting	ChEMBL	460.1	8	2	6	4.27	CCC/N=C1\S/C(=C\c2ccc(OC[C@@H](O)CO)c(Cl)c2)C(=O)N1c1ccccc1C	https://dx.doi.org/10.1021/jm100181s
CHEMBL1161691	10294	None	0	Human	Binding	IC50	=	0.77	9.11	-	5	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes	ChEMBL	389.2	14	5	6	2.62	CCCCCCCCc1ccc(CCC(N)(CO)CO[PH](O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.07.049
CHEMBL117723	11057	None	0	Human	Binding	IC50	=	10.00	8.00	-	6	Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells	ChEMBL	465.1	15	3	4	4.85	CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1021/jm0492507
CHEMBL1180115	11410	None	0	Human	Binding	EC50	=	55.00	7.26	-	3	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand	ChEMBL	344.1	10	4	4	2.18	CCCCCCc1ccc(NC(=O)[C@@H](N)COP(=O)(O)O)cc1	https://dx.doi.org/10.1016/s0960-894x(03)00812-6
CHEMBL1180152	11415	None	0	Human	Binding	EC50	=	43.00	7.37	-	3	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand	ChEMBL	344.1	10	4	4	2.18	CCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1	https://dx.doi.org/10.1016/s0960-894x(03)00812-6
CHEMBL1180214	11420	None	0	Human	Binding	EC50	=	160.00	6.80	-	4	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand	ChEMBL	428.2	16	4	4	4.53	CCCCCCCCCCCCc1ccc(NC(=O)[C@H](N)COP(=O)(O)O)cc1	https://dx.doi.org/10.1016/s0960-894x(03)00812-6
CHEMBL1181601	11756	None	0	Human	Binding	EC50	=	77.00	7.11	-	3	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist	ChEMBL	383.2	11	4	4	3.96	CCCCCCCCc1ccc2[nH]c([C@@H](N)[C@@H](C)OP(=O)(O)O)nc2c1	https://dx.doi.org/10.1016/j.bmcl.2004.07.030
CHEMBL1181640	11765	None	0	Human	Binding	EC50	=	390.00	6.41	-	3	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand; partial agonist	ChEMBL	289.2	9	3	3	3.46	CCCCCCCCc1ccc2[nH]c([C@H](N)CO)nc2c1	https://dx.doi.org/10.1016/j.bmcl.2004.07.030
CHEMBL1181660	11770	None	0	Human	Binding	EC50	=	37.00	7.43	-	4	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	ChEMBL	395.2	12	4	4	4.09	CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)COP(=O)(O)O)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.05.097
CHEMBL1181688	11776	None	0	Human	Binding	EC50	=	29.00	7.54	-	4	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	ChEMBL	411.2	12	4	4	4.21	CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(O)(O)=S)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.05.097
CHEMBL1181694	11780	None	0	Human	Binding	EC50	=	26.00	7.58	-	4	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	ChEMBL	409.2	12	4	4	4.26	CCCCCCCCc1ccc(-c2c[nH]c(C(C)(N)COP(=O)(O)O)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.05.097
CHEMBL1181739	11783	None	0	Human	Binding	EC50	=	860.00	6.07	-	4	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	ChEMBL	315.2	10	3	3	3.97	CCCCCCCCc1ccc(-c2c[nH]c([C@H](N)CO)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.05.097
CHEMBL1181748	11786	None	0	Human	Binding	EC50	=	12.00	7.92	-	4	Effective concentration against sphingosine 1-phosphate receptor 5 determined by a [c-35S]-GTP binding assay	ChEMBL	395.2	12	4	4	4.09	CCCCCCCCc1ccc(-c2c[nH]c([C@@H](N)COP(=O)(O)O)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.05.097
CHEMBL1183918	12097	None	0	Human	Binding	EC50	=	645.50	6.19	-	4	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand; Not determined	ChEMBL	352.2	15	4	4	2.46	CCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O	https://dx.doi.org/10.1016/s0960-894x(03)00812-6
CHEMBL1183950	12104	None	2	Human	Binding	EC50	=	1220.00	5.91	-	3	In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand	ChEMBL	408.3	19	4	4	4.02	CCCCCCCCCCCCCCCCNC(=O)[C@@H](N)COP(=O)(O)O	https://dx.doi.org/10.1016/s0960-894x(03)00812-6

Showing 1 to 20 of 256 entries

Search:

	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	Functional	EC50	=	0.34	9.47	-3	6	Agonist activity at human S1P5R	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/ml100301k
(S)-FTY720-phosphate	3596	None	37	Human	Functional	EC50	=	0.30	9.52	-3	6	Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/jm050242f
(S)-FTY720-phosphate	3596	None	37	Human	Functional	EC50	=	0.67	9.17	-3	6	Agonist activity at human recombinant S1P5 expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 45 mins by liquid scintillation counting 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.8b01695
(S)-FTY720-phosphate	3596	None	37	Human	Functional	EC50	=	0.36	9.44	-3	6	Agonist activity at recombinant human S1P5 receptor expressed in Chem-1 cells assessed as calcium flux measured for 180 secs by FLIPR 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/acsmedchemlett.0c00631
(S)-FTY720-phosphate	3596	None	37	Human	Functional	EC50	=	63.10	7.20	-3	6	Agonist activity at human S1P5 receptor expressed in CHO-K1 aequorin cells assessed as calcium accumulation of by luminescence assay in presence of cofactor coelenterazine	ChEMBL	387.2	14	4	4	3.32	CCCCCCCCc1ccc(CC[C@](N)(CO)COP(=O)(O)O)cc1	https://dx.doi.org/10.1021/jm200609t
(S)-FTY720-phosphate	3596	None	37	Human	Functional	EC50	=	0.36	9.44	-3	6	Agonist activity at human S1P5 receptor assessed as effect on calcium mobilization by Gq dependent whole cell 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.2010.02.006
A-971432	215	None	30	Human	Functional	pEC50	=	-	8.39	74	3	In a forskolin-induced cAMP inhibition assay in S1P₅-transfected CHO cells.	Guide to Pharmacology	365.1	6	1	3	4.09	O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1	https://pubmed.ncbi.nlm.nih.gov/26509640
A-971432	215	None	30	Human	Functional	EC50	=	4.10	8.39	74	3	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay	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
A-971432	215	None	30	Human	Functional	EC50	=	5.70	8.24	74	3	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay	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
A-971432	215	None	30	Human	Functional	pEC50	=	-	8.24	74	3	In a GTPγS assay using membranes from S1P₅-transfected HEK293 cells.	Guide to Pharmacology	365.1	6	1	3	4.09	O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1	https://pubmed.ncbi.nlm.nih.gov/26509640
A-971432	215	None	30	Human	Functional	pEC50	=	-	8.24	74	3	In a GTPγS assay using membranes from S1P₅-transfected HEK293 cells.	Guide to Pharmacology	365.1	6	1	3	4.09	O=C(O)C1CN(Cc2ccc(OCc3ccc(Cl)c(Cl)c3)cc2)C1	https://pubmed.ncbi.nlm.nih.gov/29688337
AFD(R)	303	None	0	Human	Functional	pEC50	=	-	8.85	1	4	Unclassified	Guide to Pharmacology	373.2	13	3	4	3.79	CCCCCCCOc1ccc(CC[C@@](C)(N)COP(=O)(O)O)cc1	https://pubmed.ncbi.nlm.nih.gov/11967257
AFD(R)	303	None	0	Human	Functional	pEC50	=	-	8.85	1	4	Unclassified	Guide to Pharmacology	373.2	13	3	4	3.79	CCCCCCCOc1ccc(CC[C@@](C)(N)COP(=O)(O)O)cc1	https://pubmed.ncbi.nlm.nih.gov/14732717
AFD(R)	303	None	0	Human	Functional	EC50	=	2.00	8.70	1	4	Binding potency at human S1P5 receptor by [35S]GTP-gamma-S binding assay	ChEMBL	373.2	13	3	4	3.79	CCCCCCCOc1ccc(CC[C@@](C)(N)COP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2005.09.038
ASP4058	502	None	23	Human	Functional	pEC50	=	-	8.12	-1	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	Functional	pEC50	=	-	6.47	-380	7	Unclassified	Guide to Pharmacology	455.1	7	2	3	6.82	O=C(O)CCNCc1ccc2sc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)cc2c1	https://pubmed.ncbi.nlm.nih.gov/17114004
AUY954	524	None	19	Mouse	Functional	pEC50	None	-	6.50	-354	7	Unclassified	Guide to Pharmacology	455.1	7	2	3	6.82	O=C(O)CCNCc1ccc2sc(-c3ccc(-c4ccccc4)c(C(F)(F)F)c3)cc2c1	https://pubmed.ncbi.nlm.nih.gov/17114004
CHEMBL1080865	6125	None	0	Human	Functional	EC50	=	142.00	6.85	-11	3	Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL	350.2	7	2	5	3.23	CCCN(CC1CC1)c1cc(C(=O)Nc2ccc3[nH]ncc3c2)ncn1	https://dx.doi.org/10.1016/j.bmcl.2010.01.102
CHEMBL1081645	6267	None	0	Human	Functional	EC50	=	191.00	6.72	-7	3	Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL	380.2	6	2	5	4.29	Cc1cc(O)ccc1NC(=O)c1cc(N(CC2CC2)C2CCCCC2)ncn1	https://dx.doi.org/10.1016/j.bmcl.2010.01.102
CHEMBL1081654	6272	None	0	Human	Functional	EC50	=	258.00	6.59	4	2	Agonist activity at S1P5 receptor expressed in CHO cells after 60 mins by [35S]-GTPgammaS binding assay	ChEMBL	326.2	4	3	5	3.49	Cc1cc(O)ccc1NC(=O)c1cc(NC2CCCCC2)ncn1	https://dx.doi.org/10.1016/j.bmcl.2010.01.102

Showing 1 to 20 of 270 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)