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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

anti-BrP-LPA	429	None	0	Human	Binding	pKi	=	-	6.12	-	1	Unclassified	Guide to Pharmacology	486.2	19	3	4	5.66	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)C[C@H](Br)P(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19509223
BrP-LPA	731	None	2	Human	Binding	pKi	=	-	6.09	-2	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	Binding	EC50	=	221.00	6.66	-	2	Agonist activity at human LPA1 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] 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/10.1039/C4MD00333K
CHEMBL117754	11065	None	23	Human	Binding	EC50	=	197.00	6.71	-	2	Agonist activity at human LPA1 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assay	ChEMBL	405.3	19	3	3	5.25	CCCCCCCC/C=C\CCCCCCCC(=O)NCCOP(=O)(O)O	https://dx.doi.org/10.1039/C4MD00333K
CHEMBL153043	45745	None	0	Human	Binding	EC50	=	24.00	7.62	-	6	Agonist activity at human LPA1 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	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	=	23.99	7.62	-	6	Agonist activity at human LPA1 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	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
CHEMBL181612	64603	None	0	Human	Binding	IC50	=	4230.00	5.37	-	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	615.4	24	4	4	8.22	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)CC(O)P(=O)(O)O	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL181917	64787	None	0	Human	Binding	IC50	=	3690.00	5.43	-	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	660.4	25	3	6	8.46	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL182446	65191	None	0	Human	Binding	IC50	=	114.00	6.94	12	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	676.4	28	3	7	7.86	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCOC)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL182446	65191	None	0	Human	Binding	Ki	=	35.00	7.46	12	2	Binding affinity towards Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	676.4	28	3	7	7.86	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCOC)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL183143	65593	None	0	Human	Binding	IC50	=	143.00	6.84	1	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	646.4	26	3	6	8.23	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL183143	65593	None	0	Human	Binding	Ki	=	26.00	7.58	1	2	Binding affinity towards Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	646.4	26	3	6	8.23	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL183221	65606	None	0	Human	Binding	IC50	=	84.00	7.08	2	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	700.3	26	3	6	8.78	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL183221	65606	None	0	Human	Binding	Ki	=	19.00	7.72	2	2	Binding affinity towards Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	700.3	26	3	6	8.78	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL185287	66673	None	0	Human	Binding	IC50	=	2840.00	5.55	-	2	Inhibitory concentration against Lysophosphatidic acid 1 (LPA1) receptor	ChEMBL	632.4	25	3	6	7.84	CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)n2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.05.023
CHEMBL188591	67378	None	0	Human	Binding	Ki	=	457.00	6.34	-11	3	Binding affinity for Lysophosphatidic acid receptor 1 expressed in RH7777 rat hepatoma cells	ChEMBL	292.2	13	2	2	4.57	CC/C=C/CCCCCCCCCCOP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL188859	67436	None	0	Human	Binding	Ki	=	788.00	6.10	-1	2	Binding affinity for Lysophosphatidic acid receptor 1 expressed in RH7777 rat hepatoma cells	ChEMBL	328.2	14	2	1	5.85	CCCCCCCCCCCCCCC(F)(F)P(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL190430	67647	None	0	Human	Binding	Ki	=	1146.00	5.94	-19	3	Binding affinity for Lysophosphatidic acid receptor 1 expressed in RH7777 rat hepatoma cells	ChEMBL	292.2	13	2	2	4.57	CCCC/C=C/CCCCCCCCOP(=O)(O)O	https://dx.doi.org/10.1021/jm049609r
CHEMBL201482	73410	None	0	Human	Binding	EC50	=	695.00	6.16	-	3	Activity at LPA1 receptor transfected RH7777 cells	ChEMBL	412.2	20	2	4	5.33	CCCCCCCCOC[C@H](COP(O)(O)=S)OCCCCCCCC	https://dx.doi.org/10.1016/j.bmcl.2005.10.031
CHEMBL2017139	73546	None	0	Human	Binding	EC50	=	16.60	7.78	-	6	Agonist activity at human LPA1 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	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

Showing 1 to 20 of 169 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	=	-	6.70	-19	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
ACT-1016-0707	271	None	0	Human	Functional	pIC50	=	-	8.54	-	1	IC₅₀ value corrected for unbound fraction in a Tango assay.	Guide to Pharmacology	438.1	6	2	5	2.26	COc1cc(Cl)ncc1NC(=O)C1(c2ccccc2C(C)C)CN(S(N)(=O)=O)C1	https://pubmed.ncbi.nlm.nih.gov/38349250
alkyl OMPT	347	None	0	Human	Functional	pEC50	=	-	6.15	-8	2	Unclassified	Guide to Pharmacology	452.3	22	2	4	6.28	CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(O)(O)=S)OC	https://pubmed.ncbi.nlm.nih.gov/16892372
alkyl OMPT	347	None	0	Human	Functional	EC50	=	571.00	6.24	-8	2	Agonist activity at human LPA1 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis	ChEMBL	452.3	22	2	4	6.28	CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(O)(O)=S)OC	https://dx.doi.org/10.1039/C4MD00333K
AM095	373	None	42	Human	Functional	pIC50	=	-	6.05	5	2	Unclassified	Guide to Pharmacology	456.2	7	2	5	6.25	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1	https://pubmed.ncbi.nlm.nih.gov/21159750
AM095	373	None	42	Human	Functional	IC50	=	25.00	7.60	5	2	Antagonist activity at human LPA1 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	456.2	7	2	5	6.25	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1	https://dx.doi.org/10.1039/C4MD00333K
AM095	373	None	42	Human	Functional	IC50	=	150.00	6.82	5	2	Antagonist activity at LPA1 in human lung fibroblasts assessed as inhibition of LPA-induced contraction after 18 hrs by 3D collagen gel contraction assay	ChEMBL	456.2	7	2	5	6.25	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1	https://dx.doi.org/10.1021/jm301022v
AM095	373	None	42	Mouse	Functional	pIC50	=	-	6.11	-5	2	Unclassified	Guide to Pharmacology	456.2	7	2	5	6.25	Cc1noc(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1	https://pubmed.ncbi.nlm.nih.gov/21159750
AM966	389	None	41	Human	Functional	pIC50	=	-	7.25	-1	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/21159750
AM966	389	None	41	Human	Functional	IC50	=	17.00	7.77	-1	7	Antagonist activity at human LPA1 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	pEC50	None	-	7.70	1	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
amitriptyline	401	None	38	Human	Functional	pIC50	~	-	6.22	-1288	51	Unclassified	Guide to Pharmacology	277.2	3	0	1	4.17	CN(C)CCC=C1c2ccccc2CCc2ccccc21	https://pubmed.ncbi.nlm.nih.gov/32007501
anti-BrP-LPA	429	None	0	Human	Functional	pIC50	=	-	5.68	-	1	Unclassified	Guide to Pharmacology	486.2	19	3	4	5.66	CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)C[C@H](Br)P(=O)(O)O	https://pubmed.ncbi.nlm.nih.gov/19509223
BMS-986020	676	None	0	Human	Functional	pIC50	=	-	8.90	-	1	Unclassified	Guide to Pharmacology	482.2	7	2	5	6.74	Cc1noc(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)c1NC(=O)O[C@H](C)c1ccccc1	-
BMS-986278	689	None	0	Human	Functional	pKB	=	-	8.16	-	1	Unclassified	Guide to Pharmacology	445.2	8	1	8	3.19	CCCN(C)C(=O)OCc1c(-c2ccc(O[C@H]3CCC[C@H](C(=O)O)C3)c(C)n2)nnn1C	https://pubmed.ncbi.nlm.nih.gov/34709814
BrP-LPA	731	None	2	Human	Functional	pIC50	=	-	5.34	-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
BrP-LPA	731	None	2	Human	Functional	Ki	=	170.00	6.77	-9	5	Antagonist activity at human LPA1 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
CHEMBL117529	11031	None	0	Human	Functional	EC50	=	221.00	6.66	5	2	Agonist activity at LPA1R (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
CHEMBL117529	11031	None	0	Human	Functional	EC50	=	221.00	6.66	5	2	Agonistic activity against lysophosphatidic acid receptor 1 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
CHEMBL117754	11065	None	23	Human	Functional	EC50	=	197.00	6.71	-6	2	Agonistic activity against lysophosphatidic acid receptor 1 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

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Ligand source activities (1 row/activity)