LPAR3

Summary

LPAR3 (lysophosphatidic acid receptor 3, HGNC:14298) is a protein-coding gene on chromosome 1p22.3, encoding Lysophosphatidic acid receptor 3 (Q9UBY5). Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities.

This gene encodes a member of the G protein-coupled receptor family, as well as the EDG family of proteins. This protein functions as a cellular receptor for lysophosphatidic acid and mediates lysophosphatidic acid-evoked calcium mobilization. This receptor couples predominantly to G(q/11) alpha proteins.

Source: NCBI Gene 23566 — RefSeq curated summary.

At a glance

• GWAS associations: 10
• Clinical variants (ClinVar): 69 total
• Druggable target: yes
• MANE Select transcript: NM_012152

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14298
Approved symbol	LPAR3
Name	lysophosphatidic acid receptor 3
Location	1p22.3
Locus type	gene with protein product
Status	Approved
Aliases	LP-A3, Edg-7, RP4-678I3, HOFNH30, LPA3
Ensembl gene	ENSG00000171517
Ensembl biotype	protein_coding
OMIM	605106
Entrez	23566

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 11 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000370611, ENST00000440886, ENST00000491034, ENST00000930963, ENST00000930964, ENST00000930965, ENST00000930966, ENST00000942299, ENST00000942300, ENST00000942301, ENST00000942302, ENST00000942303

RefSeq mRNA: 1 — MANE Select: NM_012152 NM_012152

CCDS: CCDS700

Canonical transcript exons

ENST00000370611 — 3 exons

Exon	Start	End
ENSE00001672580	84893016	84893206
ENSE00001720988	84865385	84866138
ENSE00003891730	84811602	84814171

Expression profiles

Bgee: expression breadth ubiquitous, 170 present calls, max score 95.10.

FANTOM5 (CAGE): breadth broad, TPM avg 1.0747 / max 38.1654, expressed in 389 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
13011	1.0747	389

Top tissues by expression

258 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
bronchial epithelial cell	CL:0002328	95.10	gold quality
right uterine tube	UBERON:0001302	91.83	gold quality
epithelium of bronchus	UBERON:0002031	90.03	gold quality
bronchus	UBERON:0002185	89.18	gold quality
mucosa of paranasal sinus	UBERON:0005030	88.57	gold quality
dorsal root ganglion	UBERON:0000044	85.67	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	85.10	gold quality
trigeminal ganglion	UBERON:0001675	81.63	gold quality
cardiac atrium	UBERON:0002081	81.52	gold quality
right atrium auricular region	UBERON:0006631	81.49	gold quality
myocardium	UBERON:0002349	80.62	silver quality
cardiac muscle of right atrium	UBERON:0003379	79.88	silver quality
oviduct epithelium	UBERON:0004804	79.33	gold quality
fallopian tube	UBERON:0003889	78.82	gold quality
body of pancreas	UBERON:0001150	78.72	gold quality
endometrium	UBERON:0001295	78.10	gold quality
lower esophagus mucosa	UBERON:0035834	77.73	gold quality
urethra	UBERON:0000057	77.01	gold quality
prostate gland	UBERON:0002367	76.94	gold quality
nasal cavity mucosa	UBERON:0001826	76.79	gold quality
epithelium of nasopharynx	UBERON:0001951	76.20	gold quality
heart right ventricle	UBERON:0002080	75.99	silver quality
esophagus mucosa	UBERON:0002469	75.90	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	75.89	gold quality
gingival epithelium	UBERON:0001949	75.70	gold quality
heart left ventricle	UBERON:0002084	74.70	gold quality
cardiac ventricle	UBERON:0002082	74.64	gold quality
gingiva	UBERON:0001828	74.39	gold quality
nasal cavity epithelium	UBERON:0005384	74.11	silver quality
right testis	UBERON:0004534	73.96	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.67
E-GEOD-124858	no	1.47

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

23 targeting LPAR3, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-141-3P	99.94	72.79	2421
HSA-MIR-200A-3P	99.94	72.68	2420
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-26A-5P	99.78	73.52	2303
HSA-MIR-26B-5P	99.78	73.51	2305
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-4465	99.71	72.56	2096
HSA-MIR-646	99.68	67.84	1645
HSA-MIR-5700	99.64	69.88	2280
HSA-MIR-4519	99.48	66.10	859
HSA-MIR-5697	99.39	67.74	1249
HSA-MIR-155-5P	99.35	70.16	1509
HSA-MIR-190B-3P	99.33	68.29	1382
HSA-MIR-4641	99.28	66.64	744
HSA-MIR-3160-5P	99.28	69.07	1938
HSA-MIR-6737-3P	98.95	68.56	1577
HSA-MIR-7157-3P	98.95	68.70	1582
HSA-MIR-5008-3P	98.73	67.50	1433
HSA-MIR-4723-3P	97.67	65.91	1017
HSA-MIR-6769B-3P	97.41	65.53	1036
HSA-MIR-3183	97.40	65.68	978
HSA-MIR-4524B-3P	95.52	64.12	964

Literature-anchored findings (GeneRIF, showing 39)

• demonstrate that two biological fluids, blood plasma and seminal plasma, differentially activate LPA receptors (PMID:12123830)
• results suggested that lysophosphatidic acid (LPA) receptors LPA(2) and LPA(3) may be involved in VEGF expression mediated by LPA signals in human ovarian oncogenesis (PMID:12668280)
• data suggest that endothelial differentiation gene EDG-7 regulates Lysophosphatidic acid(LPA)-mediated mesangial cell proliferation and suggest that EDG-7 and EDG-2 LPA receptors play a diverse role in mesangial cell proliferation (PMID:15292052)
• expression of LPA-induced inflammatory response genes is mediated by LPA1 and LPA3 (PMID:17923111)
• Lysophosphatidic acid receptor 3 may contribute to the pathogenesis of rheumatoid arthritis through the modulation of fibroblast-like synoviocyte migration and cytokine production. (PMID:18006645)
• Lysophosphatidic acid might regulate VEGF-C and lymphatic marker expression in endothelial cells, which contributes to endothelial cell tube formation in vitro and in vivo, thus facilitating endothelial cell participation lymphangiogenesis. (PMID:18627789)
• Expression of LPA3 during ovarian carcinogenesis contributes to ovarian cancer aggressiveness, suggesting that the targeting of LPA production and action may have potential for the treatment of ovarian cancer. (PMID:19001604)
• Switching of LPA receptor expression from LPA3 to LPA1, may be involved in prostate cancer progression and/or androgen independence (PMID:19025891)
• LPA(1) receptor, LPA(2) and LPA(3) receptors-induced VASP phosphorylation is a critical mediator of tumor cell migration initiation (PMID:19081821)
• LPA-stimulated cell growth is mediated by distinct but overlapping receptors and signaling pathways in these two model ovarian cancer cell lines. (PMID:19420982)
• Data show that CLL cells express LPA receptors LPA(1-5) and VEGF receptors, and the plasma levels of VEGF are elevated in CLL patients. (PMID:19860625)
• show that human microglia express LPA receptor subtypes LPA(1), LPA(2), and LPA(3) on mRNA and protein level. LPA activation of C13NJ cells induced Rho and extracellular signal-regulated kinase activation and enhanced cellular ATP production. (PMID:19899077)
• Mutation in LPA3 gene indicate that the alterations in LPA receptor gene may play some role in pathogenesis in human osteosarcoma cells. (PMID:21116120)
• found that LPA receptor 2/3-mediated IL-8 expression occurs through Gi/PI3K/AKT, Gi/PKC and IkappaB/NF-kappaB signaling (PMID:21964883)
• study found that LPS induces both ATX and LPA3 expression in THP-1 cells; the PKR and SPK1-mediated pathways are involved in both ATX and LPA3 induction, resulting in the coordinate up-regulation of these two genes (PMID:22314276)
• LPA3 Receptor act as a negative regulator on cell motile and invasive abilities of colon cancer. (PMID:22763559)
• in the normal human menstrual cycle, lysophosphatidic acid receptor 3 messenger RNA and protein expression change, indicating that this gene may be related to the function of the endometrium. (PMID:22872026)
• High LPAR3 expression is associated with aggressiveness of breast carcinoma. (PMID:22922883)
• The results indicated that LPA(3) acts as a positive regulator of cell motility and invasion in sarcoma cells, suggesting that LPA signaling pathway via LPA(3) may be involved in the progression of sarcoma cells. (PMID:23167620)
• Findings indicate lysophosphatidic acid (LPA)-lysophosphatidic acid receptor-Galpha13 signaling node as a therapeutic target for pancreatic cancer treatment and control. (PMID:23508014)
• Lysophosphatidic acid (LPA) increased hepatocellular carcinoma cells cell invasion, which was LPA-receptor dependent. (PMID:23569130)
• LPA3 mRNA is clearly expressed in human PANC-1 tumor cells. (PMID:24061591)
• The results demonstrate LPA-stimulated migration in oral carcinoma cells through LPAR3, mediated further by PKC, which acts either in concert with or independently of EGFR transactivation (PMID:24928086)
• These data indicated that the expression of LPA receptor 3 was increased in human triple-negative breast cancers and is associated with tumor metastatic ability. (PMID:25209561)
• Suggest that LPA2 and LPA3 may function as a molecular switch and play opposing roles during megakaryopoiesis of K562 cells. (PMID:25463482)
• Expression profiles reveal LPAR3 (lysophosphatidic acid receptor 3) as a mediator for mitotic phosphorylation-driven pancreatic cell motility and invasion. Together, this work identifies YAP as a novel regulator of pancreatic cancer cell motility, invasion and metastasis. (PMID:26440309)
• The results indicate that LPA2 and LPA3 receptors play opposing roles during red blood cells differentiation. (PMID:27244685)
• myeloma cells stimulate mesenchymal stem cells (MSCs to produce autotaxin, an indispensable enzyme for the biosynthesis of lysophosphatidic acid, and LPA receptor 1 (LPA1) and 3 (LPA3) transduce opposite signals to MSCs to determine the fate of MSCs. (PMID:27641212)
• Using pharmacological activators and shRNA knockdown experiments, we demonstrate that activation of LPA3 inhibits megakaryopoiesis in human HSCs. In addition, pharmacological activation of LPA3 suppressed thrombopoiesis in zebrafish. (PMID:29239275)
• Study also identifies that LPAR3 increases miR-122-5p expression, which occurs mechanistically through the SH3 domain and helps explain why miR-122-5p increases are detected in cancer patient serum. LPAR3 is partially responsible for the production and secretion of miR-122-5p, found in the serum of a wide variety of patients with cancer. (PMID:30266753)
• LPAR3 was differently expressed in melanosis coli tissues.LPAR3 expression was related to cell apoptosis. (PMID:30559147)
• Lysophosphatidic acid receptor LPA3 prevents oxidative stress and cellular senescence in Hutchinson-Gilford progeria syndrome. (PMID:31714004)
• Effects of lysophosphatidic acid (LPA) receptor-2 (LPA2) and LPA3 on the regulation of chemoresistance to anticancer drug in lung cancer cells. (PMID:32006610)
• The Agpat4/LPA axis in colorectal cancer cells regulates antitumor responses via p38/p65 signaling in macrophages. (PMID:32296017)
• Roles of endothelial cells in the regulation of cell motility via lysophosphatidic acid receptor-2 (LPA2) and LPA3 in osteosarcoma cells. (PMID:33347862)
• Transcriptional regulation of lysophosphatidic acid receptors 2 and 3 regulates myeloid commitment of hematopoietic stem cells. (PMID:33406026)
• LPAR1 and aberrantly expressed LPAR3 differentially promote the migration and proliferation of malignant peripheral nerve sheath tumor cells. (PMID:36416236)
• LPA3 Receptor Phosphorylation Sites: Roles in Signaling and Internalization. (PMID:38791546)
• Lysophosphatidic Acid Receptor 3 (LPA3): Signaling and Phosphorylation Sites. (PMID:38928196)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	lpar3	ENSDARG00000101814
mus_musculus	Lpar3	ENSMUSG00000036832
rattus_norvegicus	Lpar3	ENSRNOG00000064204

Paralogs (18): LPAR2 (ENSG00000064547), CNR1 (ENSG00000118432), MC3R (ENSG00000124089), S1PR4 (ENSG00000125910), GPR12 (ENSG00000132975), GPR6 (ENSG00000146360), GPR119 (ENSG00000147262), MC4R (ENSG00000166603), S1PR1 (ENSG00000170989), MC5R (ENSG00000176136), S1PR5 (ENSG00000180739), GPR3 (ENSG00000181773), MC2R (ENSG00000185231), CNR2 (ENSG00000188822), LPAR1 (ENSG00000198121), S1PR3 (ENSG00000213694), MC1R (ENSG00000258839), S1PR2 (ENSG00000267534)

Protein

Protein identifiers

Lysophosphatidic acid receptor 3 — Q9UBY5 (reviewed: Q9UBY5)

Alternative names: Lysophosphatidic acid receptor Edg-7

All UniProt accessions (1): Q9UBY5

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities. May play a role in the development of ovarian cancer. Seems to be coupled to the G(i)/G(o) and G(q) families of heteromeric G proteins.

Subcellular location. Cell membrane.

Tissue specificity. Most abundantly expressed in prostate, testes, pancreas, and heart, with moderate levels in lung and ovary. No detectable expression in brain, placenta, liver, skeletal muscle, kidney, spleen, thymus, small intestine, colon, or peripheral blood leukocytes.

Similarity. Belongs to the G-protein coupled receptor 1 family.

RefSeq proteins (1): NP_036284* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR004065	LPA_rcpt	Family
IPR005385	LPA_rcpt_EDG7	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (20 total): topological domain 8, transmembrane region 7, glycosylation site 2, chain 1, lipid moiety-binding region 1, sequence variant 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UBY5-F1	81.63	0.47

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 309

Glycosylation sites (2): 15, 172

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-416476	G alpha (q) signalling events
R-HSA-418594	G alpha (i) signalling events
R-HSA-419408	Lysosphingolipid and LPA receptors
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 163 (showing top): GSE45365_CD8A_DC_VS_CD11B_DC_IFNAR_KO_UP, GOBP_POSITIVE_REGULATION_OF_CALCIUM_ION_TRANSPORT, GOBP_REGULATION_OF_COLLATERAL_SPROUTING, GOBP_REGULATION_OF_DEVELOPMENTAL_GROWTH, GOBP_GROWTH, GOBP_POSITIVE_REGULATION_OF_MAPK_CASCADE, GOBP_NEUROGENESIS, GOBP_REGULATION_OF_NERVOUS_SYSTEM_DEVELOPMENT, GOBP_POSITIVE_REGULATION_OF_NERVOUS_SYSTEM_DEVELOPMENT, ACEVEDO_LIVER_CANCER_WITH_H3K27ME3_UP, GOBP_MONOATOMIC_CATION_TRANSPORT, GOBP_CELL_CELL_SIGNALING, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, GOBP_REGULATION_OF_ANATOMICAL_STRUCTURE_SIZE, GOBP_REGULATION_OF_CELL_PROJECTION_ORGANIZATION

GO Biological Process (12): G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), adenylate cyclase-activating G protein-coupled receptor signaling pathway (GO:0007189), positive regulation of cytosolic calcium ion concentration (GO:0007204), chemical synaptic transmission (GO:0007268), gene expression (GO:0010467), bleb assembly (GO:0032060), positive regulation of MAPK cascade (GO:0043410), collateral sprouting (GO:0048668), positive regulation of collateral sprouting (GO:0048672), positive regulation of calcium ion transport (GO:0051928), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (6): G-protein alpha-subunit binding (GO:0001965), G protein-coupled receptor activity (GO:0004930), phospholipid binding (GO:0005543), lipid binding (GO:0008289), lysophosphatidic acid receptor activity (GO:0070915), protein binding (GO:0005515)

GO Cellular Component (6): cytoplasm (GO:0005737), plasma membrane (GO:0005886), cilium (GO:0005929), axon (GO:0030424), synapse (GO:0045202), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
GPCR downstream signalling	2
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	2
binding	2
cellular anatomical structure	2
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase activator activity	1
regulation of biological quality	1
anterograde trans-synaptic signaling	1
macromolecule biosynthetic process	1
plasma membrane bounded cell projection assembly	1
MAPK cascade	1
regulation of MAPK cascade	1
positive regulation of intracellular signal transduction	1
axonogenesis	1
developmental cell growth	1
developmental growth involved in morphogenesis	1
positive regulation of cell growth	1
positive regulation of developmental growth	1
collateral sprouting	1
regulation of collateral sprouting	1
positive regulation of axonogenesis	1
calcium ion transport	1
positive regulation of monoatomic ion transport	1
regulation of calcium ion transport	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
protein binding	1
transmembrane signaling receptor activity	1
lipid binding	1
lysophosphatidic acid binding	1
bioactive lipid receptor activity	1
intracellular anatomical structure	1
membrane	1
cell periphery	1
intraciliary transport particle	1
membrane-bounded organelle	1

Protein interactions and networks

STRING

860 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LPAR3	LPAR6	P43657	940
LPAR3	LIPH	Q8WWY8	885
LPAR3	LPAR4	Q99677	881
LPAR3	LPAR5	Q9H1C0	877
LPAR3	ENPP2	Q13822	795
LPAR3	GNAQ	P50148	777
LPAR3	PLA1A	Q53H76	755
LPAR3	POU2F3	Q9UKI9	719
LPAR3	GPR87	Q9BY21	671
LPAR3	GDPD1	Q8N9F7	671
LPAR3	GDPD3	Q7L5L3	664
LPAR3	RPA3	P35244	662
LPAR3	PTGS2	P35354	598
LPAR3	LIPG	Q9Y5X9	590
LPAR3	P2RY10	O00398	581

IntAct

175 interactions, top by confidence:

A	B	Type	Score
CD74	LPAR3	psi-mi:“MI:0915”(physical association)	0.600
LPAR3	SLC35C2	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	MRM1	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	CLDN9	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	CYBRD1	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	SCN3B	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	TMEM70	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	SHISAL1	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	CD79A	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	FNDC9	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	LHFPL5	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	TMEM41A	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	FAM210B	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	LIME1	psi-mi:“MI:0915”(physical association)	0.560
LPAR3	CYB561	psi-mi:“MI:0915”(physical association)	0.560
EDA	LPAR3	psi-mi:“MI:0915”(physical association)	0.560
TFEC	LPAR3	psi-mi:“MI:0915”(physical association)	0.560
TMEM79	LPAR3	psi-mi:“MI:0915”(physical association)	0.560
BCL2L13	LPAR3	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (66): LPAR3 (Two-hybrid), LPAR3 (Affinity Capture-RNA), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid), LPAR3 (Two-hybrid)

ESM2 similar proteins: A6NMU1, B3DH96, O01608, O13076, O17819, O17820, O97504, P32244, P32245, P33032, P34974, P35345, P37289, P41149, P41968, P43118, P52592, P54127, P61793, P61794, P70115, Q01718, Q0Z8I9, Q28031, Q28905, Q5QD16, Q5QD17, Q5QD24, Q5QD25, Q5QD29, Q5QNP2, Q64326, Q6W049, Q8HXX3, Q8HYN8, Q8HZ64, Q8K5E0, Q923Y7, Q92633, Q96RJ0

Diamond homologs: E7EM37, O02213, O02777, O08530, O42384, O73810, O95136, O95977, P14416, P18089, P19020, P19328, P20272, P20288, P21453, P21554, P22270, P24628, P28286, P30545, P30728, P30951, P34972, P34973, P35412, P35462, P46089, P46095, P46628, P47746, P47752, P47936, P48303, P51651, P52592, P52702, P52703, P53453, P56971, P60026

SIGNOR signaling

19 interactions.

A	Effect	B	Mechanism
LPAR3	up-regulates	GNA12	binding
LPAR3	up-regulates	GNA13	binding
“lysophosphatidic acids”	up-regulates	LPAR3	“chemical activation”
“3-[({4-[4-({[1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]phenyl}methyl)sulfanyl]propanoic acid”	down-regulates	LPAR3	“chemical inhibition”
LPAR3	“up-regulates activity”	GNAL	binding
LPAR3	“up-regulates activity”	GNAI1	binding
LPAR3	“up-regulates activity”	GNAI3	binding
LPAR3	“up-regulates activity”	GNAO1	binding
LPAR3	“up-regulates activity”	GNAZ	binding
LPAR3	“up-regulates activity”	GNAQ	binding
LPAR3	“up-regulates activity”	GNA14	binding
LPAR3	“up-regulates activity”	GNA15	binding
“lysophosphatidic acid”	“up-regulates activity”	LPAR3	“chemical activation”
LPAR3	up-regulates	GNAI1	binding
LPAR3	up-regulates	GNAQ	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

69 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	61
Likely benign	0
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

509 predictions. Top by Δscore:

Variant	Effect	Δscore
1:84814167:CGCCC:C	acceptor_gain	1.0000
1:84814169:CCC:C	acceptor_gain	1.0000
1:84814170:CCC:C	acceptor_gain	1.0000
1:84814170:CCCTG:C	acceptor_loss	1.0000
1:84814171:CCTG:C	acceptor_loss	1.0000
1:84814172:C:CC	acceptor_gain	1.0000
1:84814173:T:A	acceptor_loss	1.0000
1:84814168:GCCC:G	acceptor_gain	0.9900
1:84814169:CCCC:C	acceptor_gain	0.9900
1:84814170:CC:C	acceptor_gain	0.9900
1:84814171:CC:C	acceptor_gain	0.9900
1:84814175:C:CT	acceptor_gain	0.9900
1:84859231:A:AC	donor_gain	0.9900
1:84859232:A:C	donor_gain	0.9900
1:84865382:TA:T	donor_loss	0.9900
1:84865384:C:CT	donor_loss	0.9900
1:84865396:A:AC	donor_gain	0.9900
1:84814172:C:T	acceptor_gain	0.9800
1:84814176:A:T	acceptor_gain	0.9800
1:84837424:C:A	donor_gain	0.9800
1:84865383:A:AC	donor_gain	0.9800
1:84865384:C:CC	donor_gain	0.9800
1:84865684:G:GC	donor_gain	0.9800
1:84865380:CCTA:C	donor_gain	0.9700
1:84865680:CAGTG:C	donor_gain	0.9700
1:84865721:T:TA	donor_gain	0.9500
1:84837423:T:TA	donor_gain	0.9000
1:84865379:ACCT:A	donor_loss	0.9000
1:84852440:C:CT	donor_gain	0.8700
1:84852441:T:TT	donor_gain	0.8700

AlphaMissense

2349 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:84814154:A:G	W252R	0.999
1:84814154:A:T	W252R	0.999
1:84814164:A:C	F248L	0.999
1:84814164:A:T	F248L	0.999
1:84814166:A:G	F248L	0.999
1:84865664:A:G	W153R	0.999
1:84865664:A:T	W153R	0.999
1:84865893:A:C	D76E	0.999
1:84865893:A:T	D76E	0.999
1:84865894:T:A	D76V	0.999
1:84865894:T:C	D76G	0.999
1:84865894:T:G	D76A	0.999
1:84865895:C:G	D76H	0.999
1:84865908:A:C	N71K	0.999
1:84865908:A:T	N71K	0.999
1:84814039:G:C	P290R	0.998
1:84814039:G:T	P290H	0.998
1:84814041:G:C	N289K	0.998
1:84814041:G:T	N289K	0.998
1:84814053:G:C	N285K	0.998
1:84814053:G:T	N285K	0.998
1:84814157:A:G	C251R	0.998
1:84865614:G:C	C169W	0.998
1:84865620:C:A	W167C	0.998
1:84865620:C:G	W167C	0.998
1:84865622:A:G	W167R	0.998
1:84865622:A:T	W167R	0.998
1:84865762:A:C	L120W	0.998
1:84865785:G:C	S112R	0.998
1:84865785:G:T	S112R	0.998

dbSNP variants (sampled 300 via entrez): RS1000106500 (1:84886383 G>A,C), RS1000146030 (1:84817291 A>ACACACACACACACACACACC,ACACACACACACACACACC,ACACACACACACACAC,ACACACACACACACACC,ACACACACACACACC,ACACACACACACC,ACACACACACC,ACACACACC,ACACACC,ACACC), RS1000158546 (1:84838478 C>T), RS1000218027 (1:84861127 T>A), RS1000249346 (1:84861427 T>C), RS1000256424 (1:84880078 C>A,T), RS1000265888 (1:84848327 C>G), RS1000358820 (1:84874182 G>A), RS1000391357 (1:84874506 C>A), RS1000434286 (1:84890318 G>T), RS1000436108 (1:84883620 A>G), RS1000440428 (1:84823722 C>T), RS1000471799 (1:84823467 A>G), RS1000548867 (1:84862739 G>A,C,T), RS1000566040 (1:84869486 T>C)

Disease associations

OMIM: gene MIM:605106 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

10 associations (top):

Study	Trait	p-value
GCST000244_4	Type 1 diabetes	2.000000e-06
GCST001511_3	Economic and political preferences (time)	9.000000e-06
GCST001713_29	Dental caries	2.000000e-06
GCST001726_4	Lipoprotein-associated phospholipase A2 activity change in response to statin therapy	4.000000e-06
GCST002726_7	Glucose homeostasis traits	6.000000e-06
GCST003254_10	Urinary albumin-to-creatinine ratio in non-diabetics	7.000000e-06
GCST004490_23	Cerebrospinal fluid t-tau:AB1-42 ratio	2.000000e-08
GCST006979_988	Heel bone mineral density	3.000000e-11
GCST006979_989	Heel bone mineral density	1.000000e-12
GCST012490_175	Femur bone mineral density x serum urate levels interaction	3.000000e-08

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0004827	economic and social preference
EFO:0004746	lipoprotein-associated phospholipase A(2) measurement
EFO:0004471	insulin sensitivity measurement
EFO:0007778	urinary albumin to creatinine ratio
EFO:0007708	t-tau:beta-amyloid 1-42 ratio measurement
EFO:0009270	heel bone mineral density
EFO:0004531	urate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL3250 (SINGLE PROTEIN), CHEMBL3885601 (PROTEIN FAMILY)

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Lysophospholipid (LPA) receptors

Most potent curated ligand interactions (21 total), top 21:

Ligand	Action	Affinity	Parameter
T13	Agonist	9.3	pEC50
α-fluoromethylenephosphonate	Agonist	9.3	pEC50
2-oleoyl-LPA	Agonist	8.0	pEC50
dodecyl-thiophosphate	Antagonist	7.89	pKi
CpY	Agonist	7.7	pEC50
alkyl OMPT	Agonist	7.21	pEC50
CpX	Agonist	7.2	pEC50
OMPT	Agonist	7.17	pEC50
dodecylphosphate	Antagonist	7.05	pKi
dioctanoylglycerol pyrophosphate	Agonist	6.97	pIC50
farnesyl diphosphate	Antagonist	6.81	pKd
VPC32183	Antagonist	6.76	pIC50
LPA	Agonist	6.69	pKd
Ki16425	Antagonist	6.44	pKi
VPC12249	Antagonist	6.37	pIC50
farnesyl monophosphate	Antagonist	6.3	pIC50
oleoyl-thiophosphate	Partial agonist	6.26	pEC50
H2L5186303	Antagonist	5.91	pIC50
AM966	Antagonist	5.7	pIC50
compound 12 [PMID: 19800804]	Antagonist	5.52	pIC50
NAEPA	Agonist	5.3	pEC50

Binding affinities (BindingDB)

12 measured of 14 human assays (14 total across all organisms); most potent 12 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-[4-[4-[1-methyl-5-[[(1R)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	18 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[4-[3-fluoro-4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	18 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	18 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
[(1R)-1-phenylethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate	IC50	18.8 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
[(1R)-1-[3-(trifluoromethyl)phenyl]ethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate	IC50	24.5 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[4-[4-[1-methyl-5-[1-[3-(trifluoromethyl)phenyl]ethoxycarbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	46 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
2-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]acetic acid	IC50	48 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
2-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]cyclohexyl]acetic acid	IC50	58 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[4-[4-[1-methyl-5-[[(2R)-3-methylbutan-2-yl]oxycarbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	70 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[4-[4-[1-methyl-5-[[(1S)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	2660 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
1-[3-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	IC50	4450 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists
[(1R)-1-phenylethyl] 2-[5-(4-bromophenyl)-3-methyltriazol-4-yl]acetate	IC50	21900 nM	US-9321738: N-alkyltriazole compounds as LPAR antagonists

ChEMBL bioactivities

209 potent at pChembl≥5 of 220 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.69	EC50	0.2042	nM	CHEMBL2335051
9.68	EC50	0.21	nM	CHEMBL2335051
9.65	EC50	0.2239	nM	CHEMBL2335052
9.64	EC50	0.23	nM	CHEMBL2335052
9.57	EC50	0.27	nM	CHEMBL357053
9.57	EC50	0.2692	nM	CHEMBL357053
9.56	EC50	0.2754	nM	CHEMBL2017139
9.55	EC50	0.28	nM	CHEMBL2017139
9.44	EC50	0.36	nM	CHEMBL2335049
9.44	EC50	0.3631	nM	CHEMBL2335049
9.43	EC50	0.37	nM	CHEMBL2335047
9.43	EC50	0.3715	nM	CHEMBL2335047
9.41	EC50	0.39	nM	CHEMBL2335050
9.40	EC50	0.3981	nM	CHEMBL2335050
9.36	EC50	0.44	nM	CHEMBL153043
9.35	EC50	0.4467	nM	CHEMBL153043
8.97	EC50	1.08	nM	CHEMBL2335048
8.97	EC50	1.072	nM	CHEMBL2335048
8.52	EC50	3	nM	CHEMBL201482
8.30	Ki	5	nM	CHEMBL202361
7.96	IC50	11	nM	CHEMBL202361
7.85	Ki	14	nM	THIOPHOSPHORIC ACID DODECYL ESTER
7.85	Ki	14	nM	CHEMBL190484
7.85	Ki	14	nM	CHEMBL187402
7.62	IC50	24	nM	CHEMBL2372286
7.57	Ki	27	nM	CHEMBL190349
7.57	IC50	27	nM	CHEMBL190484
7.55	IC50	28	nM	THIOPHOSPHORIC ACID DODECYL ESTER
7.55	IC50	28	nM	CHEMBL187402
7.52	IC50	30	nM	CHEMBL485119
7.50	IC50	32	nM	CHEMBL190349
7.45	IC50	35.6	nM	CHEMBL91058
7.41	Ki	39	nM	CHEMBL183143
7.41	Ki	39	nM	CHEMBL362053
7.41	Ki	39	nM	CHEMBL202185
7.40	Ki	40	nM	CHEMBL188591
7.40	IC50	40	nM	CHEMBL272087
7.32	Ki	48	nM	CHEMBL183221
7.32	Ki	48	nM	CHEMBL3218459
7.31	Ki	49	nM	THIOPHOSPHORIC ACID DECYL ESTER
7.30	Ki	50	nM	CHEMBL203986
7.30	IC50	49.6	nM	CHEMBL5907737
7.24	Ki	58	nM	CHEMBL190430
7.21	EC50	62	nM	CHEMBL3621961
7.19	IC50	65	nM	CHEMBL2182050
7.18	IC50	65.7	nM	CHEMBL2182050
7.17	Ki	67	nM	CHEMBL427017
7.12	Ki	76	nM	THIOPHOSPHORIC ACID TETRADECYL ESTER
7.11	EC50	77	nM	LYSOPHOSPHATIDIC ACID
7.11	EC50	77.62	nM	LYSOPHOSPHATIDIC ACID

PubChem BioAssay actives

173 with measured affinity, of 467 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
dihydroxy-(2-methoxy-3-octadecoxypropoxy)-sulfanylidene-lambda5-phosphane	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0002	uM
sodium [1-[hydroxy(oxido)phosphinothioyl]oxy-3-methoxypropan-2-yl] octadecanoate	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0002	uM
[(2S)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0003	uM
(3-dihydroxyphosphinothioyloxy-2-methoxypropyl) octadecanoate	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0003	uM
[(2R)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0004	uM
sodium (2-hexadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0004	uM
sodium (2-heptadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0004	uM
dihydroxy-[(2S)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0004	uM
dihydroxy-[(2R)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0011	uM
[(2R)-2,3-dioctoxypropoxy]-dihydroxy-sulfanylidene-lambda5-phosphane	260482: Activity at LPA3 receptor transfected RH7777 cells	ec50	0.0030	uM
[(2R)-3-dihydroxyphosphinothioyloxy-2-octanoyloxypropyl] octanoate	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.0050	uM
dodecoxy-dihydroxy-sulfanylidene-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0140	uM
[(E)-dodec-9-enoxy]-dihydroxy-sulfanylidene-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0140	uM
dihydroxy-sulfanylidene-[(E)-tetradec-9-enoxy]-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0140	uM
(2S)-2-[[(2R)-2-[(2-aminoacetyl)amino]-3-(2,4-dinitrophenyl)sulfanylpropanoyl]amino]pentanedioic acid	408399: Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration	ic50	0.0240	uM
[(E)-dodec-9-enyl] dihydrogen phosphate	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0270	uM
2,6-bis[[(E)-3-carboxyprop-2-enoyl]amino]benzoic acid	408399: Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration	ic50	0.0300	uM
[(2R)-3-[4-[(3-methoxyphenyl)methoxy]phenyl]-2-[[(Z)-octadec-9-enoyl]amino]propyl] dihydrogen phosphate	102985: In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines	ic50	0.0356	uM
[(2R)-2-octanoyloxy-3-phosphonooxypropyl] octanoate	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.0390	uM
[(2R)-3-[4-[(4-ethoxy-2-pyridinyl)methoxy]phenyl]-2-[[(Z)-octadec-9-enoyl]amino]propyl] dihydrogen phosphate	240661: Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptor	ki	0.0390	uM
[(2R)-3-[4-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methoxy]phenyl]-2-[[(Z)-octadec-9-enoyl]amino]propyl] dihydrogen phosphate	240661: Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptor	ki	0.0390	uM
[(E)-tetradec-11-enyl] dihydrogen phosphate	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0400	uM
2-[4-[[(3,5-dimethoxybenzoyl)-(3-phenylpropyl)amino]methyl]phenoxy]benzoic acid	320519: Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay	ic50	0.0400	uM
[(2R)-2-[[(Z)-octadec-9-enoyl]amino]-3-[4-[[4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methoxy]phenyl]propyl] dihydrogen phosphate	240661: Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptor	ki	0.0480	uM
[(2R)-2-(octadecanoylamino)-3-[4-[[4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methoxy]phenyl]propyl] dihydrogen phosphate	1118228: Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting	ki	0.0480	uM
decoxy-dihydroxy-sulfanylidene-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0490	uM
sodium 1-[4-[4-[3-[1-(2-chlorophenyl)ethoxycarbonylamino]furo[2,3-c]pyridin-2-yl]phenyl]phenyl]cyclopropane-1-carboxylate	1938508: Antagonist activity at human LPA3 receptor	ec50	0.0500	uM
sodium 1-[4-[4-[3-(1-phenylethoxycarbonylamino)furo[2,3-c]pyridin-2-yl]phenyl]phenyl]cyclopropane-1-carboxylate	1938508: Antagonist activity at human LPA3 receptor	ec50	0.0500	uM
[(2S)-2,3-dioctoxypropyl] dihydrogen phosphate	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.0500	uM
2-[7-[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]-2,3-dihydro-1H-inden-4-yl]acetic acid	1938508: Antagonist activity at human LPA3 receptor	ec50	0.0500	uM
[(E)-tetradec-9-enyl] dihydrogen phosphate	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0580	uM
[(1R)-1-[3-(trifluoromethyl)phenyl]ethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate	706181: Antagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assay	ic50	0.0650	uM
[(2S)-2,3-dioctoxypropoxy]-dihydroxy-sulfanylidene-lambda5-phosphane	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.0670	uM
dihydroxy-sulfanylidene-tetradecoxy-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.0760	uM
[(2R)-2-hydroxy-3-phosphonooxypropyl] (Z)-octadec-9-enoate	733690: Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay	ec50	0.0770	uM
[(2R)-3-[4-[(4-methoxy-2-pyridinyl)methoxy]phenyl]-2-[[(Z)-octadec-9-enoyl]amino]propyl] dihydrogen phosphate	240661: Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptor	ki	0.1020	uM
[(2S)-3-dihydroxyphosphinothioyloxy-2-octanoyloxypropyl] octanoate	260482: Activity at LPA3 receptor transfected RH7777 cells	ec50	0.1150	uM
N-[(2S)-3-dihydroxyphosphinothioyloxy-1-(octylamino)-1-oxopropan-2-yl]octanamide	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.1170	uM
N-[(2R)-3-dihydroxyphosphinothioyloxy-1-(octylamino)-1-oxopropan-2-yl]octanamide	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.1180	uM
[(2S)-2-octanoyloxy-3-phosphonooxypropyl] octanoate	260482: Activity at LPA3 receptor transfected RH7777 cells	ki	0.1190	uM
decyl dihydrogen phosphate	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.1210	uM
dodecyl dihydrogen phosphate	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.1210	uM
dec-9-enoxy-dihydroxy-sulfanylidene-lambda5-phosphane	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.1280	uM
1-[4-[4-[1-methyl-5-[[(1R)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	706181: Antagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assay	ic50	0.1320	uM
[(2R)-2-heptanoyloxy-3-phosphonooxypropyl] heptanoate	408407: Inhibition of LPA3 receptor	ic50	0.1430	uM
3-[[4-[4-[1-(2-chlorophenyl)ethoxycarbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]methylsulfanyl]propanoic acid	239112: Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells	ki	0.1480	uM
[(3R)-4-[4-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methoxy]phenyl]-3-[[(Z)-octadec-9-enoyl]amino]butyl]phosphonic acid	240661: Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptor	ki	0.1500	uM
[(2R)-2,3-dioctoxypropyl] dihydrogen phosphate	260482: Activity at LPA3 receptor transfected RH7777 cells	ec50	0.1640	uM
[(2R)-2-[[(Z)-octadec-9-enoyl]amino]-3-[4-(pyridin-2-ylmethoxy)phenyl]propyl] dihydrogen phosphate	102985: In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines	ic50	0.1750	uM
[(2R)-3-dihydroxyphosphinothioyloxy-2-heptanoyloxypropyl] heptanoate	408407: Inhibition of LPA3 receptor	ic50	0.1840	uM

CTD chemical–gene interactions

37 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression	6
trichostatin A	affects cotreatment, increases expression	3
sodium arsenite	affects methylation, increases expression	3
bisphenol A	decreases expression, increases expression	2
mercuric bromide	decreases expression, affects cotreatment	2
entinostat	increases expression, affects cotreatment	2
Benzo(a)pyrene	affects methylation, increases methylation	2
Phenylmercuric Acetate	decreases expression, affects cotreatment	2
Tobacco Smoke Pollution	decreases expression	2
Tretinoin	decreases expression	2
Aflatoxin B1	decreases expression, decreases methylation	2
FR900359	decreases phosphorylation	1
quercitrin	increases expression	1
11-nor-delta(9)-tetrahydrocannabinol-9-carboxylic acid	affects methylation, increases abundance	1
potassium chromate(VI)	increases expression	1
nickel sulfate	increases expression	1
lysophosphatidic acid	affects binding, decreases reaction, increases activity	1
CGP 52608	affects binding, increases reaction	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression, decreases expression	1
dorsomorphin	affects cotreatment, increases expression, decreases expression	1
Sunitinib	decreases expression	1
Vorinostat	increases expression	1
Acetaminophen	decreases expression	1
Glyphosate	increases expression, decreases expression	1
Arsenic	affects methylation	1
Cadmium	increases abundance, decreases expression	1
Cannabinoids	affects methylation, increases abundance	1
Bucladesine	affects cotreatment, increases expression	1
Estradiol	affects cotreatment, increases expression	1
Progesterone	increases expression	1

ChEMBL screening assays

74 unique, capped per target: 56 functional, 18 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1064668	Functional	Agonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as effect on intracellular calcium response at 10 uM	Structure-based drug design identifies novel LPA3 antagonists. — Bioorg Med Chem
CHEMBL1064670	Binding	Binding affinity to LPA3	Structure-based drug design identifies novel LPA3 antagonists. — Bioorg Med Chem

Cellosaurus cell lines

8 cell lines: 4 cancer cell line, 3 transformed cell line, 1 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B3A9	Abcam HEK293T LPAR3 KO	Transformed cell line	Female
CVCL_D8PD	Ubigene HCT 116 LPAR3 KO	Cancer cell line	Male
CVCL_D9IQ	Ubigene HEK293 LPAR3 KO	Transformed cell line	Female
CVCL_KW98	PathHunter CHO-K1 EDG7 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LA25	PathHunter U2OS EDG7 Activated GPCR Internalization	Cancer cell line	Female
CVCL_XA29	GeneBLAzer EDG7-NFAT-bla HEK 293T	Transformed cell line	Female
CVCL_YK53	U2OS LPAR3 HiTSeeker	Cancer cell line	Female
CVCL_ZK32	Tango EDG7-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.