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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

CHEMBL153043	45745	None	0	Human	Binding	EC50	=	4.90	8.31	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL153043	45745	None	0	Human	Binding	EC50	=	4.90	8.31	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2017139	73546	None	0	Human	Binding	EC50	=	3.30	8.48	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.85	CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2017139	73546	None	0	Human	Binding	EC50	=	3.31	8.48	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.85	CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335047	87558	None	0	Human	Binding	EC50	=	3.50	8.46	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335047	87558	None	0	Human	Binding	EC50	=	3.47	8.46	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335048	87559	None	0	Human	Binding	EC50	=	4.90	8.31	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335048	87559	None	0	Human	Binding	EC50	=	4.90	8.31	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335052	87560	None	0	Human	Binding	EC50	=	3.80	8.42	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2335052	87560	None	0	Human	Binding	EC50	=	3.80	8.42	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	454.3	23	2	4	6.50	CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2364959	89093	None	0	Human	Binding	EC50	=	2.40	8.62	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2364959	89093	None	0	Human	Binding	EC50	=	2.46	8.61	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2365070	89102	None	0	Human	Binding	EC50	=	3.80	8.42	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	426.3	21	2	4	5.72	CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2365070	89102	None	0	Human	Binding	EC50	=	3.80	8.42	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	426.3	21	2	4	5.72	CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2365071	89103	None	0	Human	Binding	EC50	=	4.50	8.35	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	440.3	22	2	4	6.12	CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL2365071	89103	None	0	Human	Binding	EC50	=	4.47	8.35	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	440.3	22	2	4	6.12	CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL357053	121145	None	0	Human	Binding	EC50	=	2.70	8.57	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL357053	121145	None	0	Human	Binding	EC50	=	2.69	8.57	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	468.3	22	2	5	6.03	CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL364797	125870	None	15	Human	Binding	EC50	=	84.00	7.08	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	410.2	19	3	5	4.48	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2013.01.002
CHEMBL364797	125870	None	15	Human	Binding	EC50	=	83.18	7.08	-	6	Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ChEMBL	410.2	19	3	5	4.48	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2013.01.002

Showing 1 to 20 of 25 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

[1-bromo-(3S)-hydrox-4-(palmitoyloxy)butyl]phosphate	31	None	0	Human	Functional	pIC50	=	-	6.58	-	1	Unclassified	Guide to Pharmacology	508.2	20	2	5	5.77	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O[Na]	https://pubmed.ncbi.nlm.nih.gov/18781939
AM966	389	None	41	Human	Functional	pIC50	None	-	5.10	-398	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 LPA4 receptor expressed in CHO 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
CHEMBL256470	95359	None	35	Human	Functional	IC50	=	6309.57	5.20	-58	9	Antagonist activity at human LPA4 receptor expressed in CHO cells assessed as inhibition of LPA-induced cAMP accumulation pretreated for 30 mins followed by LPA stimulation and measured after 1 hr	ChEMBL	499.1	6	1	7	4.11	Cc1csc2c(N[C@@H](C)CN3CCN(S(=O)(=O)c4ccc(Cl)c(Cl)c4)CC3)ncnc12	https://dx.doi.org/10.1021/acs.jmedchem.2c02087
CHEMBL3621964	123770	None	0	Human	Functional	IC50	=	266.00	6.58	4	4	Antagonist activity at human LPA4 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization by Fura-2 AM probe-based fluorometric analysis	ChEMBL	484.2	18	3	4	5.44	CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O	https://dx.doi.org/10.1039/C4MD00333K
CHEMBL3623936	123884	None	0	Human	Functional	Ki	=	170.00	6.77	-	4	Antagonist activity at human LPA4 receptor expressed in CHO cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay	ChEMBL	512.2	20	3	4	6.22	CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O	https://dx.doi.org/10.1039/C4MD00255E
CHEMBL5424552	196466	None	0	Human	Functional	IC50	=	23988.33	4.62	-50	3	Antagonist activity at human LPA4 receptor expressed in CHO cells assessed as inhibition of LPA-induced cAMP accumulation pretreated for 30 mins followed by LPA stimulation and measured after 1 hr	ChEMBL	525.1	7	2	11	2.75	COC(=O)Nc1nc(C)c(S(=O)(=O)N2CCN(C[C@H](C)Nc3ncnc4c(C)csc34)CC2)s1	https://dx.doi.org/10.1021/acs.jmedchem.2c02087
farnesyl diphosphate	1622	None	0	Human	Functional	pIC50	None	-	5.70	-12	4	Unclassified	Guide to Pharmacology	382.1	11	3	4	4.63	CC(C)=CCC/C(C)=C\CC/C(C)=C\COP(=O)(O)OP(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19366702
farnesyl monophosphate	1623	None	0	Human	Functional	pIC50	None	-	5.84	-29	4	Unclassified	Guide to Pharmacology	302.2	9	2	2	4.51	CC(C)=CCC/C(C)=C\CC/C(C)=C\COP(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19366702
LPA	2355	None	15	Human	Functional	EC50	=	570.00	6.24	-72	13	Agonist activity at LPA4 receptor (unknown origin) expressed in CHO cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assay	ChEMBL	436.3	20	3	5	5.04	CCCCCCCC/C=C\CCCCCCCC(=O)OCC(O)COP(=O)(O)O	https://dx.doi.org/10.1021/acs.jmedchem.6b01270
LYSOPHOSPHATIDIC ACID	4157	None	20	Mouse	Functional	EC50	=	260.00	6.58	-36	7	Agonist activity at mouse LPA4 expressed in CHO cells by Fura-2AM dye based Ca2+ mobilization assay	ChEMBL	436.3	20	3	5	5.04	CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O	https://dx.doi.org/10.1021/jm5007116

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Ligand source activities (1 row/activity)