LPAR4

Summary

LPAR4 (lysophosphatidic acid receptor 4, HGNC:4478) is a protein-coding gene on chromosome Xq21.1, encoding Lysophosphatidic acid receptor 4 (Q99677). Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities.

This gene encodes a member of the lysophosphatidic acid receptor family. It may also be related to the P2Y receptors, a family of receptors that bind purine and pyrimidine nucleotides and are coupled to G proteins. The encoded protein may play a role in monocytic differentiation.

Source: NCBI Gene 2846 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 52 total
• Druggable target: yes
• MANE Select transcript: NM_001278000

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4478
Approved symbol	LPAR4
Name	lysophosphatidic acid receptor 4
Location	Xq21.1
Locus type	gene with protein product
Status	Approved
Aliases	P2Y9, P2Y5-LIKE, P2RY9, LPA4
Ensembl gene	ENSG00000147145
Ensembl biotype	protein_coding
OMIM	300086
Entrez	2846

Gene structure

Transcript identifiers

Ensembl transcripts: 14 — 13 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000435339, ENST00000514744, ENST00000610214, ENST00000614823, ENST00000885310, ENST00000919745, ENST00000919746, ENST00000919747, ENST00000919748, ENST00000919749, ENST00000919750, ENST00000919751, ENST00000919752, ENST00000919753

RefSeq mRNA: 2 — MANE Select: NM_001278000 NM_001278000, NM_005296

CCDS: CCDS14441

Canonical transcript exons

ENST00000614823 — 5 exons

Exon	Start	End
ENSE00002028757	78750174	78750223
ENSE00002050864	78751210	78751311
ENSE00003703680	78750730	78750792
ENSE00003742495	78754791	78758714
ENSE00003917663	78747720	78748034

Expression profiles

Bgee: expression breadth ubiquitous, 170 present calls, max score 99.91.

FANTOM5 (CAGE): breadth broad, TPM avg 1.0640 / max 113.8635, expressed in 255 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
196788	1.0640	255

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	99.91	gold quality
buccal mucosa cell	CL:0002336	98.89	gold quality
tibia	UBERON:0000979	95.51	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	89.41	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	86.71	gold quality
ventricular zone	UBERON:0003053	79.63	gold quality
cartilage tissue	UBERON:0002418	77.77	gold quality
ganglionic eminence	UBERON:0004023	77.50	gold quality
hindlimb stylopod muscle	UBERON:0004252	73.59	gold quality
embryo	UBERON:0000922	70.08	gold quality
calcaneal tendon	UBERON:0003701	69.30	gold quality
tendon	UBERON:0000043	68.87	gold quality
tendon of biceps brachii	UBERON:0008188	68.47	silver quality
left ovary	UBERON:0002119	68.41	gold quality
ovary	UBERON:0000992	67.46	gold quality
monocyte	CL:0000576	67.42	gold quality
mononuclear cell	CL:0000842	67.04	gold quality
leukocyte	CL:0000738	67.00	gold quality
right ovary	UBERON:0002118	66.89	gold quality
cranial nerve II	UBERON:0000941	66.66	gold quality
mucosa of stomach	UBERON:0001199	65.53	gold quality
cortical plate	UBERON:0005343	63.56	gold quality
paraflocculus	UBERON:0005351	63.37	gold quality
endometrium epithelium	UBERON:0004811	62.94	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	62.85	gold quality
middle frontal gyrus	UBERON:0002702	62.76	silver quality
gall bladder	UBERON:0002110	61.34	gold quality
corpus callosum	UBERON:0002336	61.02	gold quality
apex of heart	UBERON:0002098	60.95	gold quality
smooth muscle tissue	UBERON:0001135	60.76	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.18

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): PITX2, RUNX2

miRNA regulators (miRDB)

93 targeting LPAR4, 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-3613-3P	100.00	76.36	7965
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-10523-5P	99.91	69.22	2038
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-345-3P	99.89	70.23	1421
HSA-MIR-548D-3P	99.87	70.67	4362
HSA-MIR-139-5P	99.80	69.50	1399
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-6885-3P	99.75	70.36	3187
HSA-MIR-7856-5P	99.75	69.99	2901
HSA-MIR-199A-3P	99.75	70.48	929
HSA-MIR-199B-3P	99.75	70.48	929
HSA-MIR-3129-5P	99.75	70.46	914
HSA-MIR-2681-5P	99.75	67.64	1655
HSA-MIR-6505-5P	99.73	69.25	1595
HSA-MIR-4677-5P	99.70	70.09	1940
HSA-MIR-670-5P	99.67	69.94	1565

Literature-anchored findings (GeneRIF, showing 10)

• identified as the fourth lysophosphatidic acid (LPA) receptor; shares only 20-24% amino acid identities with Edg-2/LPA1, Edg-4/LPA2, and Edg-7/LPA3, and phylogenetic analysis also shows that p2y9/GPR23 is far distant from the Edg family (PMID:12724320)
• 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)
• LPA4 and LPA5 receptors induce osteoblastic differentiation of human mesenchymal stem cells (PMID:20069565)
• LPA4 gene mutation may play some role in the pathogenesis of colon cancer. (PMID:20890765)
• Our data suggest that LPA4 signaling potentially modulates malignant behavior of SQ-20B cells. (PMID:23467751)
• These results suggest that the diverse roles of LPA4, LPA5 and LPA6 are involved in the activation of tumor progression in pancreatic cancer cells. (PMID:25849892)
• Mutation in LPAR4 gene is associated with papillary thyroid carcinoma. (PMID:26941397)
• Study shows that due to the high LPAR2 and LPAR4 transcript and protein expression in endometriotic ovarian cysts and positive correlations of both these receptors with the PR-B and ERbeta, respectively, those receptors seem to be the most promising predictors of the endometriotic cysts. (PMID:29621954)
• Potential genetic biomarkers predict adverse pregnancy outcome during early and mid-pregnancy in women with systemic lupus erythematosus. (PMID:36465614)
• Pancreatic cancer cells upregulate LPAR4 in response to isolation stress to promote an ECM-enriched niche and support tumour initiation. (PMID:36646789)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	lpar4	ENSDARG00000089824
mus_musculus	Lpar4	ENSMUSG00000049929
rattus_norvegicus	Lpar4	ENSRNOG00000002428

Paralogs (16): P2RY10 (ENSG00000078589), GPR18 (ENSG00000125245), F2RL3 (ENSG00000127533), GPR55 (ENSG00000135898), LPAR6 (ENSG00000139679), GPR65 (ENSG00000140030), GPR17 (ENSG00000144230), CYSLTR2 (ENSG00000152207), F2RL2 (ENSG00000164220), F2RL1 (ENSG00000164251), CYSLTR1 (ENSG00000173198), GPR4 (ENSG00000177464), GPR35 (ENSG00000178623), F2R (ENSG00000181104), P2RY8 (ENSG00000182162), GPR20 (ENSG00000204882)

Protein

Protein identifiers

Lysophosphatidic acid receptor 4 — Q99677 (reviewed: Q99677)

Alternative names: G-protein coupled receptor 23, P2Y purinoceptor 9, P2Y5-like receptor, Purinergic receptor 9

All UniProt accessions (2): Q99677, V9GY74

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities. Transduces a signal by increasing the intracellular calcium ions and by stimulating adenylyl cyclase activity. The rank order of potency for agonists of this receptor is 1-oleoyl- > 1-stearoyl- > 1-palmitoyl- > 1-myristoyl- > 1-alkyl- > 1-alkenyl-LPA.

Subcellular location. Cell membrane.

Tissue specificity. High expression in ovary. Not detected in the brain regions thalamus, putamen, caudate, frontal cortex, pons, hypothalamus and hippocampus.

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

RefSeq proteins (2): NP_001264929, NP_005287 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (24 total): topological domain 8, transmembrane region 7, glycosylation site 4, sequence conflict 3, chain 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q99677-F1	82.68	0.61

Functional residue map

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

Disulfide bonds (1): 111–188

Glycosylation sites (4): 15, 24, 28, 183

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

ID	Pathway
R-HSA-416476	G alpha (q) signalling events
R-HSA-417957	P2Y 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-418038	Nucleotide-like (purinergic) receptors
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 139 (showing top): RORA1_01, REACTOME_P2Y_RECEPTORS, CHX10_01, MORF_RAD51L3, EVI1_05, MORF_CTSB, BLALOCK_ALZHEIMERS_DISEASE_UP, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, TGANTCA_AP1_C, PID_LYSOPHOSPHOLIPID_PATHWAY, CUI_TCF21_TARGETS_2_DN, MORF_ATF2, CTAWWWATA_RSRFC4_Q2, SAFFORD_T_LYMPHOCYTE_ANERGY, CAIRO_LIVER_DEVELOPMENT_UP

GO Biological Process (2): G protein-coupled receptor signaling pathway (GO:0007186), signal transduction (GO:0007165)

GO Molecular Function (4): lysophosphatidic acid binding (GO:0035727), lysophosphatidic acid receptor activity (GO:0070915), G protein-coupled receptor activity (GO:0004930), lipid binding (GO:0008289)

GO Cellular Component (3): plasma membrane (GO:0005886), nuclear body (GO:0016604), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-6 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor activity	1
signal transduction	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
phospholipid binding	1
anion binding	1
carbohydrate derivative binding	1
lysophosphatidic acid binding	1
bioactive lipid receptor activity	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
binding	1
membrane	1
cell periphery	1
nucleoplasm	1
intracellular membraneless organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

556 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LPAR4	LPAR1	P78351	947
LPAR4	LPAR2	Q9HBW0	888
LPAR4	LPAR3	Q9UBY5	881
LPAR4	GPR22	Q99680	864
LPAR4	ENPP2	Q13822	764
LPAR4	GNA12	Q03113	729
LPAR4	GDPD1	Q8N9F7	673
LPAR4	GDPD3	Q7L5L3	652
LPAR4	S1PR5	Q9H228	650
LPAR4	GNAQ	P50148	638
LPAR4	GNA13	Q14344	593
LPAR4	SPHK1	Q9NYA1	545
LPAR4	TRIP6	Q15654	453
LPAR4	S1PR3	Q99500	446
LPAR4	S1PR2	O95136	446

IntAct

10 interactions, top by confidence:

A	B	Type	Score
LPAR4	POTEF	psi-mi:“MI:0914”(association)	0.530
LPAR4	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
RAMP2	LPAR4	psi-mi:“MI:0915”(physical association)	0.400
LPAR4	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	LPAR4	psi-mi:“MI:0915”(physical association)	0.400
LPAR4	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
BCL6	CACNA1A	psi-mi:“MI:0914”(association)	0.350

BioGRID (58): SLC25A35 (Affinity Capture-MS), ACAD10 (Affinity Capture-MS), ATL3 (Affinity Capture-MS), ATM (Affinity Capture-MS), ARHGEF40 (Affinity Capture-MS), CAV1 (Affinity Capture-MS), TAMM41 (Affinity Capture-MS), SPG7 (Affinity Capture-MS), EFR3A (Affinity Capture-MS), PPTC7 (Affinity Capture-MS), MTX1 (Affinity Capture-MS), RTCA (Affinity Capture-MS), NLRX1 (Affinity Capture-MS), PPP2R5E (Affinity Capture-MS), BTAF1 (Affinity Capture-MS)

ESM2 similar proteins: A0A4W3GG95, A7YY44, B0F9W3, B0UXR0, B2GV46, B3G515, B5X337, E7FEL0, O00398, O46685, O70526, P21556, P25023, P25105, P25116, P26824, P30411, P30558, P32299, P43657, P46002, P46093, P49019, P50132, P56488, Q00991, Q15743, Q1JQB3, Q28642, Q3UFD7, Q4G072, Q4KLH9, Q61038, Q62035, Q80Z39, Q8BFQ3, Q8BFU7, Q8BLG2, Q8BMC0, Q8BUD0

Diamond homologs: A0A2L0VBG2, E7EM37, E9QJ73, O18821, O18935, O19012, O19014, O19025, O19032, O42329, O62169, O75388, O77700, O77713, O77715, O77721, O77830, O88634, P16395, P30968, P30969, P32236, P32237, P32251, P49651, P49922, P97288, Q01776, Q15722, Q19PY9, Q29003, Q2V2K5, Q6UNA4, Q6XKD3, Q8CH60, Q8JG69, Q8JG70, Q8MJ88, Q8NGA4, Q8SPZ1

SIGNOR signaling

9 interactions.

A	Effect	B	Mechanism
LPAR4	“up-regulates activity”	GNAS	binding
LPAR4	“up-regulates activity”	GNAL	binding
LPAR4	“up-regulates activity”	GNAI1	binding
LPAR4	“up-regulates activity”	GNAI3	binding
LPAR4	“up-regulates activity”	GNAO1	binding
LPAR4	“up-regulates activity”	GNAZ	binding
LPAR4	“up-regulates activity”	GNAQ	binding
LPAR4	“up-regulates activity”	GNA14	binding
“lysophosphatidic acid”	“up-regulates activity”	LPAR4	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	33
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

563 predictions. Top by Δscore:

Variant	Effect	Δscore
X:78754789:A:AT	acceptor_loss	0.9900
X:78754790:G:GA	acceptor_loss	0.9900
X:78754789:A:AG	acceptor_gain	0.9800
X:78754790:G:GG	acceptor_gain	0.9800
X:78754790:GGA:G	acceptor_gain	0.9800
X:78751208:A:AG	acceptor_gain	0.9700
X:78751209:G:GG	acceptor_gain	0.9700
X:78751209:GC:G	acceptor_gain	0.9700
X:78754788:TAGG:T	acceptor_gain	0.9700
X:78754789:AGGA:A	acceptor_gain	0.9700
X:78754790:GGAG:G	acceptor_gain	0.9700
X:78747771:G:GT	donor_gain	0.9600
X:78750131:C:CA	acceptor_gain	0.9600
X:78747789:A:T	donor_gain	0.9500
X:78747788:G:T	donor_gain	0.9400
X:78751309:GTG:G	donor_gain	0.9400
X:78751309:GTGGT:G	donor_loss	0.9400
X:78751310:TGGTG:T	donor_loss	0.9400
X:78751312:GTG:G	donor_loss	0.9400
X:78751313:T:TC	donor_loss	0.9400
X:78751314:G:GG	donor_loss	0.9400
X:78751315:AG:A	donor_loss	0.9400
X:78751316:G:T	donor_loss	0.9400
X:78749084:C:T	donor_gain	0.9300
X:78750793:G:GG	donor_gain	0.9300
X:78751207:C:G	acceptor_gain	0.9300
X:78747795:A:G	donor_gain	0.9200
X:78751202:T:G	acceptor_loss	0.9100
X:78751204:TCACA:T	acceptor_loss	0.9100
X:78751205:CACAG:C	acceptor_loss	0.9100

AlphaMissense

2455 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
X:78755181:G:C	W104C	0.999
X:78755181:G:T	W104C	0.999
X:78755460:G:C	W197C	0.999
X:78755460:G:T	W197C	0.999
X:78755179:T:A	W104R	0.998
X:78755179:T:C	W104R	0.998
X:78755200:T:A	C111S	0.998
X:78755201:G:C	C111S	0.998
X:78755276:G:C	R136P	0.998
X:78755356:T:A	W163R	0.998
X:78755356:T:C	W163R	0.998
X:78755431:T:A	C188S	0.998
X:78755432:G:C	C188S	0.998
X:78755433:C:G	C188W	0.998
X:78755026:G:C	G53R	0.997
X:78755431:T:C	C188R	0.997
X:78755432:G:A	C188Y	0.997
X:78755443:T:C	F192L	0.997
X:78755445:C:A	F192L	0.997
X:78755445:C:G	F192L	0.997
X:78755008:A:C	S47R	0.996
X:78755010:T:A	S47R	0.996
X:78755010:T:G	S47R	0.996
X:78755111:T:C	L81P	0.996
X:78755123:A:C	D85A	0.996
X:78755201:G:A	C111Y	0.996
X:78755202:C:G	C111W	0.996
X:78755260:T:C	C131R	0.996
X:78755266:A:C	S133R	0.996
X:78755268:T:A	S133R	0.996

dbSNP variants (sampled 300 via entrez): RS1000323382 (X:78750440 T>C), RS1000479881 (X:78758735 C>A,G), RS1001056642 (X:78752902 A>T), RS1001505631 (X:78752012 GA>G,GAA), RS1001658216 (X:78746055 C>T), RS1001838269 (X:78757529 A>G), RS1002168263 (X:78756554 A>T), RS1002555130 (X:78753246 C>A), RS1002665859 (X:78748358 TAC>T), RS1002770927 (X:78758911 A>G), RS1002871499 (X:78757872 T>A), RS1003513559 (X:78756115 A>T), RS1003615900 (X:78747092 C>A), RS1003671216 (X:78746631 T>C), RS1004178408 (X:78747134 G>A)

Disease associations

OMIM: gene MIM:300086 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5968 (SINGLE PROTEIN)

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 (5 total), top 5:

Ligand	Action	Affinity	Parameter
LPA	Agonist	7.35	pKd
[1-bromo-(3S)-hydrox-4-(palmitoyloxy)butyl]phosphate	Antagonist	6.58	pIC50
farnesyl monophosphate	Antagonist	5.84	pIC50
farnesyl diphosphate	Antagonist	5.7	pIC50
AM966	Antagonist	5.1	pIC50

ChEMBL bioactivities

28 potent at pChembl≥5 of 30 total, top 28 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.62	EC50	2.4	nM	CHEMBL2335051
8.61	EC50	2.455	nM	CHEMBL2335051
8.57	EC50	2.7	nM	CHEMBL357053
8.57	EC50	2.692	nM	CHEMBL357053
8.48	EC50	3.3	nM	CHEMBL2017139
8.48	EC50	3.311	nM	CHEMBL2017139
8.46	EC50	3.5	nM	CHEMBL2335047
8.46	EC50	3.467	nM	CHEMBL2335047
8.42	EC50	3.8	nM	CHEMBL2335052
8.42	EC50	3.8	nM	CHEMBL2335049
8.42	EC50	3.802	nM	CHEMBL2335052
8.42	EC50	3.802	nM	CHEMBL2335049
8.35	EC50	4.5	nM	CHEMBL2335050
8.35	EC50	4.467	nM	CHEMBL2335050
8.31	EC50	4.9	nM	CHEMBL2335048
8.31	EC50	4.9	nM	CHEMBL153043
8.31	EC50	4.898	nM	CHEMBL2335048
8.31	EC50	4.898	nM	CHEMBL153043
8.09	EC50	8.1	nM	LYSOPHOSPHATIDIC ACID
8.09	EC50	8.128	nM	LYSOPHOSPHATIDIC ACID
7.08	EC50	84	nM	CHEMBL364797
7.08	EC50	83.18	nM	CHEMBL364797
6.77	Ki	170	nM	CHEMBL3621353
6.77	Ki	170	nM	CHEMBL3621354
6.58	IC50	266	nM	CHEMBL3621964
6.24	EC50	570	nM	CHEMBL1222042
5.70	EC50	2000	nM	CHEMBL5085657
5.20	IC50	6310	nM	CHEMBL256470

PubChem BioAssay actives

24 with measured affinity, of 76 total; 13 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
sodium [1-[hydroxy(oxido)phosphinothioyl]oxy-3-methoxypropan-2-yl] octadecanoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0024	uM
[(2S)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0027	uM
(3-dihydroxyphosphinothioyloxy-2-methoxypropyl) octadecanoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0033	uM
dihydroxy-[(2S)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0035	uM
dihydroxy-(2-methoxy-3-octadecoxypropoxy)-sulfanylidene-lambda5-phosphane	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0038	uM
sodium (2-hexadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0038	uM
sodium (2-heptadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0045	uM
[(2R)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0049	uM
dihydroxy-[(2R)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0049	uM
[(2R)-2-hydroxy-3-phosphonooxypropyl] (Z)-octadec-9-enoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0081	uM
[(2R)-2-hydroxy-3-phosphonooxypropyl] hexadecanoate	733689: Agonist activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0832	uM
(2-hydroxy-3-phosphonooxypropyl) (Z)-octadec-9-enoate	1431880: 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	ec50	0.5700	uM
N-[(2S)-1-[4-(3,4-dichlorophenyl)sulfonylpiperazin-1-yl]propan-2-yl]-7-methylthieno[3,2-d]pyrimidin-4-amine	2034263: 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	ic50	6.3096	uM

CTD chemical–gene interactions

22 total (human), top 22 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression, decreases methylation	6
trichostatin A	affects cotreatment, decreases expression	3
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tretinoin	decreases expression	2
methylmercuric chloride	decreases expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
bisphenol A	decreases methylation	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
4-aminophenylarsenoxide	affects binding, decreases reaction	1
epigallocatechin gallate	affects cotreatment, decreases expression	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, decreases expression	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
Resveratrol	affects cotreatment, increases expression	1
Arsenic Trioxide	affects binding, decreases reaction	1
Benzo(a)pyrene	affects methylation, decreases methylation	1
Copper	increases expression, affects cotreatment	1
Diethylhexyl Phthalate	decreases expression	1
Nickel	decreases expression	1
Polychlorinated Biphenyls	affects expression	1
Aflatoxin B1	decreases methylation	1

ChEMBL screening assays

21 unique, capped per target: 16 functional, 5 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1073936	Functional	Antagonist activity at LPA4 receptor expressed in CHO cells assessed as inhibition of LPA-induced intracellular calcium response	Structure-based drug design identifies novel LPA3 antagonists. — Bioorg Med Chem
CHEMBL2344987	Binding	Intrinsic activity at human LPA4 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425 relative to LPA	Phosphorothioate analogs of sn-2 radyl lysophosphatidic acid (LPA): metabolically stabilized LPA receptor agonists. — Bioorg Med Chem Lett

Cellosaurus cell lines

3 cell lines: 2 spontaneously immortalized cell line, 1 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_KA78	CHO-K1/P2Y9/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KX51	PathHunter CHO-K1 GPR23 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_ZK34	Tango GPR23-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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