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Ligand source activities (1 row/activity)

Affinity
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

BrP-LPA	731	None	2	Mouse	Binding	pKi	=	-	6.61	-1	5	Unclassified	Guide to Pharmacology	486.2	19	3	4	5.66	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19509223
CHEMBL115970	10184	None	0	Human	Binding	IC50	=	250.00	6.60	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	369.2	14	3	3	4.28	CCCCCCCCC(=O)c1ccc(CNCCCP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL116981	10576	None	0	Human	Binding	IC50	=	120.00	6.92	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	389.2	12	3	2	5.13	CCCCCCc1ccc(-c2ccc(CNCCCP(=O)(O)O)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL117007	10604	None	0	Human	Binding	IC50	=	2100.00	5.68	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	371.2	14	4	3	4.13	CCCCCCCCC(O)c1ccc(CNCCCP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL117403	11017	None	0	Human	Binding	IC50	=	700.00	6.16	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	371.2	13	3	4	3.47	CCCCCCCOC(=O)c1ccc(CNCCCP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL117715	11056	None	0	Human	Binding	IC50	=	57.00	7.24	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	421.2	15	3	4	4.75	CCCCCCCCOc1c(Cl)cc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL117723	11057	None	0	Human	Binding	IC50	=	80.00	7.10	-	6	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	465.1	15	3	4	4.85	CCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL118508	12323	None	0	Human	Binding	IC50	=	450.00	6.35	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	387.2	15	3	4	4.09	CCCCCCCCOc1ccc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL118783	12755	None	0	Human	Binding	IC50	=	33.00	7.48	-	3	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	451.1	14	3	4	4.46	CCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL118815	12805	None	0	Human	Binding	IC50	=	42.00	7.38	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	507.2	18	3	4	6.03	CCCCCCCCCCCOc1c(Br)cc(CNCCCP(=O)(O)O)cc1OC	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL118860	12851	None	3	Human	Binding	IC50	=	40.00	7.40	-	6	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	355.2	14	3	2	4.64	CCCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119116	13216	None	0	Human	Binding	IC50	=	6.60	8.18	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	425.1	14	3	3	5.39	CCCCCCCCOc1c(Cl)cc(CNCCCP(=O)(O)O)cc1Cl	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119239	13363	None	0	Human	Binding	IC50	=	1200.00	5.92	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	373.2	14	4	4	3.79	CCCCCCCCOc1ccc(CNCCCP(=O)(O)O)cc1O	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119256	13384	None	0	Human	Binding	IC50	=	26.00	7.58	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	341.2	13	3	2	4.25	CCCCCCCCc1ccc(CNCCCP(=O)(O)O)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119354	13511	None	0	Human	Binding	IC50	=	36.00	7.44	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	435.1	14	3	3	4.85	CCCCCCCCOc1ccc(CNCCCP(=O)(O)O)cc1Br	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119382	13549	None	0	Human	Binding	IC50	=	270.00	6.57	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	395.2	13	3	6	2.97	CCCCCCCn1nnc(-c2ccc(CNCCCP(=O)(O)O)cc2)n1	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119413	13600	None	0	Human	Binding	IC50	=	55.00	7.26	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	391.2	14	3	3	4.74	CCCCCCCCOc1ccc(CNCCCP(=O)(O)O)cc1Cl	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119440	13637	None	0	Human	Binding	IC50	=	15.00	7.82	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	385.2	14	3	3	4.70	CCCCCCCCOc1c(C)cc(CNCCCP(=O)(O)O)cc1C	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL119873	14190	None	0	Human	Binding	IC50	=	59.00	7.23	-	4	Binding affinity to human sphingosine 1-phosphate receptor 4 expressed in CHO cells was determined by using [33P]-S1P as radioligand	ChEMBL	375.2	14	3	3	4.22	CCCCCCCCOc1ccc(CNCCCP(=O)(O)O)cc1F	https://dx.doi.org/10.1016/j.bmcl.2004.04.070
CHEMBL1206092	14703	None	0	Human	Binding	EC50	=	1090.00	5.96	-	2	Activity at LPA2 receptor in RH7777 rat hepatoma cell line	ChEMBL	436.2	18	2	4	5.99	CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(O)(O)=S)O1	https://dx.doi.org/10.1016/j.bmcl.2005.08.096

Showing 1 to 20 of 79 entries

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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

2-oleoyl-LPA	85	None	0	Human	Functional	pEC50	None	-	8.00	1	4	Unclassified	Guide to Pharmacology	436.3	20	3	5	5.04	CCCCCCCC/C=C\CCCCCCCC(=O)OC(CO)COP(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/10922489
AM966	389	None	41	Human	Functional	pIC50	None	-	5.80	-81	7	Unclassified	Guide to Pharmacology	490.1	7	2	5	6.91	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1Cl	https://pubmed.ncbi.nlm.nih.gov/20649573
AM966	389	None	41	Human	Functional	IC50	=	1700.00	5.77	-81	7	Antagonist activity at human LPA2 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis	ChEMBL	490.1	7	2	5	6.91	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1Cl	https://dx.doi.org/10.1039/C4MD00333K
AM966	389	None	41	Mouse	Functional	pIC50	None	-	4.60	-1258	7	Unclassified	Guide to Pharmacology	490.1	7	2	5	6.91	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1Cl	https://pubmed.ncbi.nlm.nih.gov/20649573
BrP-LPA	731	None	2	Human	Functional	Ki	=	170.00	6.77	-	5	Antagonist activity at human LPA2 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay	ChEMBL	486.2	19	3	4	5.66	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O	https://dx.doi.org/10.1039/C4MD00255E
BrP-LPA	731	None	2	Mouse	Functional	pIC50	=	-	6.33	9	5	Unclassified	Guide to Pharmacology	486.2	19	3	4	5.66	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19509223
CHEMBL117529	11031	None	0	Human	Functional	EC50	=	1089.00	5.96	-5	2	Agonistic activity against lysophosphatidic acid receptor 2 using [35S]GTP-gamma-S as radioligand tested in vitro	ChEMBL	417.3	19	3	3	5.23	CCCCCCCC/C=C\CCCCCCCC(=O)NCCC(=O)P(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2004.04.061
CHEMBL117529	11031	None	0	Human	Functional	EC50	=	1089.00	5.96	-5	2	Agonist activity at LPA2 (unknown origin) by [35S]GTPgammaS binding assay	ChEMBL	417.3	19	3	3	5.23	CCCCCCCC/C=C\CCCCCCCC(=O)NCCC(=O)P(=O)(O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01287
CHEMBL117663	11048	None	0	Human	Functional	EC50	=	1960.00	5.71	-	1	Agonistic activity against lysophosphatidic acid receptor 2 using [35S]GTP-gamma-S as radioligand tested in vitro	ChEMBL	421.3	19	3	2	6.00	CCCCCCCC/C=C\CCCCCCCC(=O)NCCC(F)P(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2004.04.061
CHEMBL117754	11065	None	23	Human	Functional	EC50	=	30.00	7.52	6	2	Agonistic activity against lysophosphatidic acid receptor 2 using [35S]GTP-gamma-S as radioligand tested in vitro	ChEMBL	405.3	19	3	3	5.25	CCCCCCCC/C=C\CCCCCCCC(=O)NCCOP(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2004.04.061
CHEMBL117798	11096	None	0	Human	Functional	EC50	=	108.00	6.97	-2	2	Agonistic activity against lysophosphatidic acid receptor 2 using [35S]GTP-gamma-S as radioligand tested in vitro	ChEMBL	433.2	19	3	3	5.35	CCCCCCCC/C=C\CCCCCCCC(=O)NCCC(=O)P(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2004.04.061
CHEMBL1206181	14712	None	0	Human	Functional	IC50	=	40000.00	4.40	-91	4	Antagonist activity at human S1P4 receptor expressed in CHO cell membrane by FLIPR assay	ChEMBL	608.3	17	2	5	9.50	CCCCCCCCCCC#CC(O)c1ccccc1-c1ccc(Sc2ccc(OCCCC)cc2)c(S(=O)(=O)O)c1	https://dx.doi.org/10.1016/j.bmc.2007.02.048
CHEMBL1207343	14835	None	0	Human	Functional	IC50	=	6000.00	5.22	-47	4	Antagonist activity at human S1P4 receptor expressed in CHO cell membrane by FLIPR assay	ChEMBL	612.2	17	3	7	6.93	CCCCOc1ccc(Sc2ccc(-c3ccccc3C(O)C#CCOCCCCCCCO)cc2S(=O)(=O)O)cc1	https://dx.doi.org/10.1016/j.bmc.2007.02.048
CHEMBL187402	67130	None	0	Human	Functional	EC50	=	480.00	6.32	-16	2	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	308.2	13	2	2	4.69	CCCC/C=C/CCCCCCCCOP(O)(O)=S	https://dx.doi.org/10.1021/jm049609r
CHEMBL187459	67142	None	0	Human	Functional	EC50	=	244.00	6.61	-1	3	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	364.2	17	2	2	6.25	CCCCCCCC/C=C/CCCCCCCCOP(O)(O)=S	https://dx.doi.org/10.1021/jm049609r
CHEMBL188591	67378	None	0	Human	Functional	EC50	=	4100.00	5.39	-39	3	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	292.2	13	2	2	4.57	CC/C=C/CCCCCCCCCCOP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL190349	67638	None	0	Human	Functional	EC50	=	717.00	6.14	-22	2	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	264.1	11	2	2	3.79	CC/C=C/CCCCCCCCOP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL190430	67647	None	0	Human	Functional	EC50	=	397.00	6.40	-4	3	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	292.2	13	2	2	4.57	CCCC/C=C/CCCCCCCCOP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL190484	67653	None	0	Human	Functional	EC50	=	677.00	6.17	-25	2	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	280.1	11	2	2	3.91	CC/C=C/CCCCCCCCOP(O)(O)=S	https://dx.doi.org/10.1021/jm049609r
CHEMBL190999	67869	None	46	Human	Functional	IC50	=	5500.00	5.26	-1	2	Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA2 receptor	ChEMBL	278.2	13	2	1	4.87	CCCCCCCCCCCCCCP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r

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Ligand source activities (1 row/activity)