LPAR3
gene geneOn this page
Also known as LP-A3Edg-7RP4-678I3HOFNH30LPA3
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
- Expression (HPA): Tissue enhanced — highest in fallopian tube, area postrema, dorsal motor vagal complex
- GTEx eGene: eQTL in 27 tissues, sQTL in 1 (q < 0.05)
- Constraint (gnomAD): pLI 0.78 (intermediate), LOEUF 0.62 (unconstrained)
- MANE Select transcript:
NM_012152 - Notable: 69 clinical variants but no curated precision-oncology (CIViC) evidence yet
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: 14 — 13 protein_coding, 1 protein_coding_CDS_not_defined
MANE Select: ENST00000370611
Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 2, TSL 3: 1
ENST00000370611, ENST00000440886, ENST00000491034, ENST00000930963, ENST00000930964, ENST00000930965, ENST00000930966, ENST00000942299, ENST00000942300, ENST00000942301, ENST00000942302, ENST00000942303, ENST00001028116, ENST00001145346
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.
Highest expression (Bgee): bronchial epithelial cell, uterine tube, epithelium of bronchus, bronchus, mucosa of paranasal sinus.
Genetic regulation across tissues (GTEx eQTL / sQTL)
LPAR3 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 27 tissues and its splicing (sQTL) in 1 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.
showing 20 of 28 significant tissue × QTL associations:
| Tissue | QTL | q-value | Slope | Lead variant |
|---|---|---|---|---|
| Cells Cultured fibroblasts | eqtl | 4.8e-52 | +0.44 | 1:84883501:T:C |
| Cells EBV-transformed lymphocytes | eqtl | 1.4e-34 | +1.00 | 1:84926641:C:T |
| Whole Blood | eqtl | 7.1e-23 | +0.49 | 1:84893289:C:T |
| Lung | eqtl | 4.1e-16 | -0.31 | 1:84873395:C:T |
| Spleen | eqtl | 2.7e-14 | +0.85 | 1:84926641:C:T |
| Esophagus Mucosa | eqtl | 3.7e-12 | -0.27 | 1:84888880:G:A |
| Skin Sun Exposed Lower leg | eqtl | 9.4e-09 | +0.24 | 1:84842841:T:G |
| Brain Cerebellar Hemisphere | eqtl | 4.5e-08 | +0.51 | 1:84777740:G:T |
| Skin Not Sun Exposed Suprapubic | eqtl | 5.8e-07 | +0.26 | 1:84842841:T:G |
| Brain Cerebellum | eqtl | 1.0e-05 | +0.41 | 1:84776811:C:T |
| Brain Cortex | eqtl | 1.7e-05 | +0.31 | 1:84761787:G:C |
| Brain Hippocampus | eqtl | 2.4e-05 | +0.35 | 1:84755059:C:CGT |
| Brain Anterior cingulate cortex BA24 | eqtl | 3.1e-05 | +0.35 | 1:84761787:G:C |
| Small Intestine Terminal Ileum | eqtl | 2.7e-04 | +0.55 | 1:84926641:C:T |
| Brain Frontal Cortex BA9 | eqtl | 4.1e-04 | +0.26 | 1:84762642:C:T |
| Minor Salivary Gland | eqtl | 1.1e-03 | +0.65 | 1:84842841:T:G |
| Colon Transverse | eqtl | 1.2e-03 | +0.19 | 1:84893414:G:A |
| Stomach | eqtl | 1.8e-03 | +0.29 | 1:84882814:T:G |
| Testis | eqtl | 3.1e-03 | +0.12 | 1:84873395:C:T |
| Thyroid | eqtl | 6.1e-03 | +0.21 | 1:84887029:T:A |
FANTOM5 promoters
1 alternative TSS:
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 13011 | 1.0747 | 389 |
Top tissues by expression
showing 100 of 258 tissues 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 |
| esophagus squamous epithelium | UBERON:0006920 | 73.72 | gold quality |
| heart | UBERON:0000948 | 73.37 | gold quality |
| squamous epithelium | UBERON:0006914 | 73.25 | gold quality |
| testis | UBERON:0000473 | 72.98 | gold quality |
| epithelium of esophagus | UBERON:0001976 | 72.87 | gold quality |
| pancreas | UBERON:0001264 | 72.68 | gold quality |
| left testis | UBERON:0004533 | 72.43 | gold quality |
| stromal cell of endometrium | CL:0002255 | 72.01 | gold quality |
| cauda epididymis | UBERON:0004360 | 71.68 | gold quality |
| skin of hip | UBERON:0001554 | 71.66 | gold quality |
| corpus epididymis | UBERON:0004359 | 71.18 | gold quality |
| diaphragm | UBERON:0001103 | 71.06 | gold quality |
| skin of abdomen | UBERON:0001416 | 70.78 | gold quality |
| apex of heart | UBERON:0002098 | 70.35 | gold quality |
| tibia | UBERON:0000979 | 69.99 | gold quality |
| mouth mucosa | UBERON:0003729 | 69.91 | gold quality |
| minor salivary gland | UBERON:0001830 | 69.68 | gold quality |
| zone of skin | UBERON:0000014 | 69.56 | gold quality |
| saliva-secreting gland | UBERON:0001044 | 69.13 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 69.09 | gold quality |
| skin of leg | UBERON:0001511 | 69.04 | gold quality |
| vagina | UBERON:0000996 | 69.03 | gold quality |
| upper leg skin | UBERON:0004262 | 68.10 | gold quality |
| oral cavity | UBERON:0000167 | 68.07 | silver quality |
| palpebral conjunctiva | UBERON:0001812 | 67.83 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 67.41 | gold quality |
| tonsil | UBERON:0002372 | 66.41 | gold quality |
| mammalian vulva | UBERON:0000997 | 65.80 | silver quality |
| urinary bladder | UBERON:0001255 | 65.70 | gold quality |
| trachea | UBERON:0003126 | 65.05 | silver quality |
| upper arm skin | UBERON:0004263 | 64.99 | gold quality |
| seminal vesicle | UBERON:0000998 | 64.86 | silver quality |
| right frontal lobe | UBERON:0002810 | 64.71 | gold quality |
| islet of Langerhans | UBERON:0000006 | 64.44 | gold quality |
| vastus lateralis | UBERON:0001379 | 64.41 | gold quality |
| skeletal muscle tissue of rectus abdominis | UBERON:0004511 | 64.38 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 64.20 | gold quality |
| quadriceps femoris | UBERON:0001377 | 64.08 | gold quality |
| prefrontal cortex | UBERON:0000451 | 64.00 | gold quality |
| anterior cingulate cortex | UBERON:0009835 | 63.59 | gold quality |
| cingulate cortex | UBERON:0003027 | 63.55 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 63.45 | silver quality |
| Ammon’s horn | UBERON:0001954 | 63.30 | gold quality |
| penis | UBERON:0000989 | 62.90 | silver quality |
| dorsolateral prefrontal cortex | UBERON:0009834 | 62.83 | gold quality |
| frontal cortex | UBERON:0001870 | 62.80 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 62.61 | gold quality |
| Brodmann (1909) area 9 | UBERON:0013540 | 62.61 | gold quality |
| periodontal ligament | UBERON:0008266 | 62.41 | gold quality |
| female reproductive system | UBERON:0000474 | 62.36 | gold quality |
| superficial temporal artery | UBERON:0001614 | 62.29 | gold quality |
| right lung | UBERON:0002167 | 62.23 | gold quality |
| neocortex | UBERON:0001950 | 61.96 | gold quality |
| cerebral cortex | UBERON:0000956 | 61.81 | gold quality |
| hair follicle | UBERON:0002073 | 61.79 | gold quality |
| body of tongue | UBERON:0011876 | 61.79 | gold quality |
| mucosa of urinary bladder | UBERON:0001259 | 61.67 | gold quality |
| caput epididymis | UBERON:0004358 | 61.55 | silver quality |
| vena cava | UBERON:0004087 | 61.42 | gold quality |
| uterus | UBERON:0000995 | 61.09 | gold quality |
| saphenous vein | UBERON:0007318 | 60.99 | gold quality |
| olfactory bulb | UBERON:0002264 | 60.97 | gold quality |
| inferior vagus X ganglion | UBERON:0005363 | 60.85 | gold quality |
| lower lobe of lung | UBERON:0008949 | 60.82 | silver quality |
| dorsal plus ventral thalamus | UBERON:0001897 | 60.81 | gold quality |
| type B pancreatic cell | CL:0000169 | 60.73 | gold quality |
| pericardium | UBERON:0002407 | 60.69 | gold quality |
| lateral globus pallidus | UBERON:0002476 | 60.64 | gold quality |
| substantia nigra pars reticulata | UBERON:0001966 | 60.50 | gold quality |
| subthalamic nucleus | UBERON:0001906 | 60.42 | 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 |
HPA expression
RNA tissue specificity: Tissue enhanced
showing 60 of 72 HPA tissues / cells by nTPM:
| Tissue / cell | Axis | nTPM |
|---|---|---|
| Fallopian tube | tissue | 34.2 |
| Prostate | tissue | 12.6 |
| Cervix | tissue | 9.8 |
| Pancreas | tissue | 9.8 |
| Testis | tissue | 9.7 |
| Heart muscle | tissue | 8.8 |
| Postcentral gyrus | tissue | 7.2 |
| Hippocampus | tissue | 6.4 |
| Epididymis | tissue | 5.6 |
| Salivary gland | tissue | 5.4 |
| Vagina | tissue | 5.3 |
| Urinary bladder | tissue | 4.7 |
| Nucleus accumbens | tissue | 4.7 |
| Esophagus | tissue | 4.2 |
| Skin 1 | tissue | 3.7 |
| Choroid plexus | tissue | 3.3 |
| Endometrium 1 | tissue | 2.7 |
| Locus coeruleus | tissue | 2.3 |
| Thymus | tissue | 2.1 |
| Basal ganglia | tissue | 1.6 |
| Lung | tissue | 1.4 |
| Placenta | tissue | 1.3 |
| Adrenal gland | tissue | 1.3 |
| Cerebellum | tissue | 1.0 |
| Seminal vesicle | tissue | 0.9 |
| Putamen | tissue | 0.9 |
| Spinal cord | tissue | 0.9 |
| Tonsil | tissue | 0.9 |
| Breast | tissue | 0.8 |
| Cerebral cortex | tissue | 0.8 |
| Ventral forebrain | tissue | 0.8 |
| Olfactory bulb | tissue | 0.8 |
| Retrosplenial cortex | tissue | 0.8 |
| Prefrontal cortex | tissue | 0.7 |
| Ovary | tissue | 0.7 |
| Amygdala | tissue | 0.7 |
| Corpus callosum | tissue | 0.7 |
| Hippocampal formation | tissue | 0.7 |
| Entorhinal cortex | tissue | 0.7 |
| Retrosplenial and cingulate cortex | tissue | 0.7 |
| Temporal cortex | tissue | 0.7 |
| Occipital cortex | tissue | 0.7 |
| Insular cortex | tissue | 0.7 |
| Motor cortex | tissue | 0.6 |
| Medulla oblongata | tissue | 0.6 |
| Hypothalamus | tissue | 0.6 |
| Septum | tissue | 0.6 |
| Somatosensory cortex | tissue | 0.6 |
| Rectum | tissue | 0.5 |
| Colon | tissue | 0.5 |
| Superior colliculi | tissue | 0.5 |
| Substantia nigra | tissue | 0.5 |
| Gallbladder | tissue | 0.5 |
| Periaqueductal gray | tissue | 0.5 |
| Pons | tissue | 0.4 |
| Skeletal muscle | tissue | 0.4 |
| Midbrain | tissue | 0.4 |
| Thalamus | tissue | 0.4 |
| Stomach 1 | tissue | 0.3 |
| Bone marrow | tissue | 0.3 |
Brain sub-regions (HPA Brain Atlas): detected in 188; highest nTPM — Area postrema (17.2), Dorsal motor vagal complex (15.9), Nucleus gracilis (9.3), Nucleus tractus solitarii (9.1), Inferior parietal lobule (7.7).
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
Targeting LPAR3 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).
23 miRNAs:
| 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 |
Functional genomics
gnomAD constraint: pLI 0.778, LOEUF 0.623, missense Z 1.43 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD
Regional missense constraint (gnomAD RMC): no regional variation along ENST00000370611 — one region, missense o/e 0.86.
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)
Mouse-model phenotypes
Observed phenotypes of the mouse ortholog (MGI:1929469) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 8 distinct phenotype terms.
| Mouse phenotype (MP) | Records |
|---|---|
| abnormal systemic arterial blood pressure | 1 |
| abnormal placenta morphology | 1 |
| impaired embryo implantation | 1 |
| decreased litter size | 1 |
| long gestation period | 1 |
| impaired spacing of implantation sites | 1 |
| delayed embryo implantation | 1 |
| decreased prostaglandin level | 1 |
Additional cross-species homologs
Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.
| Organism | UniProt | Identity | Method |
|---|---|---|---|
| Macaca fascicularis | Q95KH4 | 98.6% | Diamond |
| Xenopus laevis | Q9PU16 | 98.4% | Diamond |
| Ovis aries | P46628 | 97.8% | Diamond |
| Bos taurus | Q28031 | 97.8% | Diamond |
| Sus scrofa | Q684M3 | 86.7% | Diamond |
| Takifugu rubripes | Q9PUQ8 | 69.1% | Diamond |
Genomic neighbors (locus context)
Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).
| Symbol | Type | Entrez |
|---|---|---|
| SSX2IP | protein-coding | 117178 |
| MCOLN2 | protein-coding | 255231 |
| LINC01555 | ncRNA | 439927 |
| LINC01461 | ncRNA | 103695366 |
| DNAI3 | protein-coding | 126820 |
| MCOLN3 | protein-coding | 55283 |
| MIR4423 | ncRNA | 100616481 |
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
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9UBY5-F1 | 81.63 | 0.47 |
Human Protein Atlas
Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Lysolipids receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins
Protein evidence: Evidence at protein level
Subcellular location (HPA, imaging): plasma membrane; primary cilium
Antibody reliability (HPA): IF supported
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)
| Type | Positions |
|---|---|
| S-palmitoyl cysteine | 309 |
Glycosylation sites (2)
| Type | Positions |
|---|---|
| N-linked (glcnac…) asparagine | 15, 172 |
Function
Pathways and Gene Ontology
Reactome pathways
3 curated (TAS) of 8; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).
8 pathways:
| ID | Pathway | Evidence |
|---|---|---|
| R-HSA-418594 | G alpha (i) signalling events | curated |
| R-HSA-416476 | G alpha (q) signalling events | curated |
| R-HSA-419408 | Lysosphingolipid and LPA receptors | curated |
| R-HSA-373076 | Class A/1 (Rhodopsin-like receptors) | — |
| R-HSA-388396 | GPCR downstream signalling | — |
| R-HSA-500792 | GPCR ligand binding | — |
| R-HSA-162582 | Signal Transduction | — |
| R-HSA-372790 | Signaling by GPCR | — |
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 (8): 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), 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 (5): cytoplasm (GO:0005737), plasma membrane (GO:0005886), axon (GO:0030424), synapse (GO:0045202), membrane (GO:0016020)
Reactome top-level categories
5 top-level categories:
| 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
28 GO namespaces:
| 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 |
| 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 |
| neuron projection | 1 |
| cell junction | 1 |
Experimentally-supported GO annotations
GO terms backed by direct experimental evidence (ECO experimental codes) — 1 of 19 annotations. The rest are phylogenetic / computational / electronic (IEA).
1 experimentally-supported GO terms:
| GO term | NS | Evidence |
|---|---|---|
| plasma membrane | CC | direct assay |
Protein interactions and networks
STRING
showing 15 of 652 interactions by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| LPAR3 | LPAR6 | P43657 | 934 |
| LPAR3 | LIPH | Q8WWY8 | 883 |
| LPAR3 | LPAR5 | Q9H1C0 | 882 |
| LPAR3 | LPAR4 | Q99677 | 881 |
| LPAR3 | ENPP2 | Q13822 | 767 |
| LPAR3 | POU2F3 | Q9UKI9 | 697 |
| LPAR3 | GDPD1 | Q8N9F7 | 654 |
| LPAR3 | PLA1A | Q53H76 | 635 |
| LPAR3 | GDPD3 | Q7L5L3 | 629 |
| LPAR3 | GPR87 | Q9BY21 | 623 |
| LPAR3 | LIPG | Q9Y5X9 | 612 |
| LPAR3 | RPA3 | P35244 | 601 |
| LPAR3 | PTGS2 | P35354 | 585 |
| LPAR3 | P2RY10 | O00398 | 540 |
| LPAR3 | PLA2G4A | P47712 | 536 |
IntAct
Human interaction partners of LPAR3 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).
showing 30 of 53 partners by confidence:
| Partner | Interaction type | MIscore | Records |
|---|---|---|---|
| CD74 | physical association | 0.600 | 4 |
| CREB3L1 | physical association | 0.560 | 5 |
| RETREG3 | physical association | 0.560 | 5 |
| AQP6 | physical association | 0.560 | 3 |
| ARL13B | physical association | 0.560 | 3 |
| ASZ1 | physical association | 0.560 | 3 |
| BCL2L13 | physical association | 0.560 | 3 |
| C16orf54 | physical association | 0.560 | 3 |
| CD53 | physical association | 0.560 | 3 |
| CD79A | physical association | 0.560 | 3 |
| CLDN2 | physical association | 0.560 | 3 |
| CLDN7 | physical association | 0.560 | 3 |
| CLDN9 | physical association | 0.560 | 3 |
| CLEC12B | physical association | 0.560 | 3 |
| CPLX4 | physical association | 0.560 | 3 |
| CYB561 | physical association | 0.560 | 3 |
| CYBRD1 | physical association | 0.560 | 3 |
| EDA | physical association | 0.560 | 3 |
| ERGIC3 | physical association | 0.560 | 3 |
| FAM209A | physical association | 0.560 | 3 |
| FFAR2 | physical association | 0.560 | 3 |
| FNDC9 | physical association | 0.560 | 3 |
| GJB5 | physical association | 0.560 | 3 |
| GORAB | physical association | 0.560 | 3 |
| GPX8 | physical association | 0.560 | 3 |
| JAGN1 | physical association | 0.560 | 3 |
| KCNC1 | physical association | 0.560 | 3 |
| KCNJ6 | physical association | 0.560 | 3 |
| LEPROTL1 | physical association | 0.560 | 3 |
| LHFPL5 | physical association | 0.560 | 3 |
BioGRID (67 interactions; top human partners by supporting records): APP (Reconstituted Complex), AQP6 (Two-hybrid), ARL13B (Two-hybrid), ASZ1 (Two-hybrid), BCL2L13 (Two-hybrid), C16orf54 (Two-hybrid), CD53 (Two-hybrid), CD74 (Two-hybrid), CD79A (Two-hybrid), CDC123 (Affinity Capture-MS), CHRNA4 (Affinity Capture-MS), CLDN2 (Two-hybrid), CLDN7 (Two-hybrid), CLDN9 (Two-hybrid), CLEC12B (Two-hybrid)
SIGNOR signaling
showing 15 of 19 signaling 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 |
Protein complexes (CORUM) (8)
Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).
8 complexes by size:
| Complex | Subunits | Members |
|---|---|---|
| LPAR1-LPAR3 complex | 2 | LPAR1, LPAR3 |
| LPAR2-LPAR3 complex | 2 | LPAR2, LPAR3 |
| ★ LPAR3-S1PR1 complex | 2 | LPAR3, S1PR1 |
| LPAR3-S1PR2 complex | 2 | LPAR3, S1PR2 |
| ★ LPAR3-S1PR3 complex | 2 | LPAR3, S1PR3 |
| GPR4-LPAR3 complex | 2 | GPR4, LPAR3 |
| GPR68-LPAR3 complex | 2 | GPR68, LPAR3 |
| Lysophosphatidic acid receptor 3 | 1 | LPAR3 |
Ligand–receptor pairs (CellPhoneDB) (1)
Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.
1 ligand–receptor pairs:
| Partner | This gene’s role | Signaling class |
|---|---|---|
| ADGRE5 | ligand | Signaling by Lysophosphatidic acid receptor |
Disease & clinical
Genetic variants
Variant evidence for LPAR3: 69 ClinVar records (0 pathogenic / likely pathogenic); 10 GWAS associations.
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 |
SpliceAI
Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 27 predictions of 434):
| Position(s) | Effect | Δscore | Sites |
|---|---|---|---|
| 1:84814172–84814173 | acceptor_loss | 1.0000 | 2 |
| 1:84893014–84893015 | donor_loss | 1.0000 | 5 |
| 1:84814172–84814173 | acceptor_loss | 0.9900 | 4 |
| 1:84859232 | donor_gain | 0.9900 | |
| 1:84814176 | acceptor_gain | 0.9800 | |
| 1:84837424 | donor_gain | 0.9800 | |
| 1:84865383–84865384 | donor_loss | 0.9800 | 6 |
| 1:84866026 | donor_gain | 0.9700 | |
| 1:84866139–84866140 | acceptor_loss | 0.9600 | 5 |
| 1:84866139 | acceptor_loss | 0.9500 |
AlphaMissense
1,053 missense substitutions predicted likely pathogenic (of 2,349 scored), across 243 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:
| Residue | Likely-pathogenic substitutions | Mean am_pathogenicity | Max am_pathogenicity |
|---|---|---|---|
| M202 | 9 | 0.887 | 0.994 |
| M300 | 9 | 0.845 | 0.967 |
| D76 | 8 | 0.998 | 0.999 |
| N48 | 8 | 0.987 | 0.998 |
| N289 | 8 | 0.986 | 0.998 |
| F248 | 8 | 0.981 | 0.999 |
| D262 | 8 | 0.978 | 0.986 |
| D297 | 8 | 0.974 | 0.991 |
| N285 | 8 | 0.965 | 0.998 |
| D110 | 8 | 0.960 | 0.982 |
| F61 | 8 | 0.938 | 0.997 |
| F199 | 8 | 0.935 | 0.983 |
| H62 | 8 | 0.911 | 0.986 |
| F65 | 8 | 0.877 | 0.987 |
| N58 | 8 | 0.780 | 0.951 |
| C169 | 7 | 0.993 | 0.998 |
| C176 | 7 | 0.993 | 0.997 |
| W252 | 7 | 0.993 | 0.999 |
| W153 | 7 | 0.986 | 0.999 |
| W167 | 7 | 0.985 | 0.998 |
HPA cancer prognostics
RNA cancer specificity: Cancer enhanced (Ovary Serous Cystadenocarcinoma)
Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.
2 prognostic cancer types:
| Cancer | Prognostic | p-value |
|---|---|---|
| Ovary Serous Cystadenocarcinoma (TCGA) | favorable | 0.000489 |
| Bladder Urothelial Carcinoma (TCGA) | unfavorable | 0.000911 |
Disease associations
OMIM: gene MIM:605106 | disease phenotypes:
GWAS associations
10 associations:
| Study | Trait | p-value |
|---|---|---|
| GCST006979_764 | Heel bone mineral density | 1e-12 |
| GCST006979_763 | Heel bone mineral density | 3e-11 |
| GCST004490_13 | Cerebrospinal fluid t-tau:AB1-42 ratio | 2e-8 |
| GCST012490_435 | Femur bone mineral density x serum urate levels interaction | 3e-8 |
| GCST000244_4 | Type 1 diabetes | 2e-6 |
| GCST001713_22 | Dental caries | 2e-6 |
| GCST001726_4 | Lipoprotein-associated phospholipase A2 activity change in response to statin therapy | 4e-6 |
| GCST002726_32 | Glucose homeostasis traits | 6e-6 |
| GCST003254_10 | Urinary albumin-to-creatinine ratio in non-diabetics | 7e-6 |
| GCST001511_10 | Economic and political preferences (time) | 9e-6 |
EFO canonical traits (from GWAS)
7 canonical traits:
| 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 (CPIC guideline: no)
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)
146 measured of 201 human assays (201 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| CHEMBL4871014 | IC50 | 1 nM | |
| CHEMBL3975893 | IC50 | 3.5 nM | |
| 1-[4-[6-[5-[[6-(cyclopropoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-5-fluoro-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 8.61 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[[6-(cyclopropoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid | IC50 | 9.86 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL2335047 | EC50 | 10 nM | |
| CHEMBL2335050 | EC50 | 11 nM | |
| 1-[4-[5-fluoro-6-[5-[(6-isopropoxypyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 11.1 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL2335051 | EC50 | 12 nM | |
| (R)—N-(1-(1-(1H-indazol-5-yl)-3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]decan-8-yl)-3-methyl-1-oxobutan-2-yl)-2-fluoro-5-(trifluoromethyl)benzamide | IC50 | 14 nM | |
| CHEMBL357053 | EC50 | 15 nM | |
| 1-[4-[5-fluoro-6-[5-[[6-(1-fluoro-1-methyl-ethyl)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid Hydrochloride | IC50 | 16.7 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[4-[1-methyl-5-[[(1R)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid | IC50 | 17 nM | US-9321738: N-alkyltriazole compounds as LPAR antagonists |
| 1-[4-[6-[5-[[6-(cyclobutoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid | IC50 | 17.2 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[2-cyano-4-[6-[5-[[6-(cyclopropoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 17.9 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 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 |
| CHEMBL1222042 | IC50 | 20 nM | |
| CHEMBL2182063 | IC50 | 20 nM | |
| 1-[4-[6-[1-methyl-5-[(6-propan-2-ylpyrazin-2-yl)amino]pyrazol-4-yl]-3-pyridinyl]phenyl]cyclopropane-1-carboxylic acid | IC50 | 20.6 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[[6-(cyclopropoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]-2-(trifluoromethyl)phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 22 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[4-[5-[(6-isopropylpyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]phenyl]phenyl]cyclopropanecarboxylic Acid | IC50 | 23.6 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 2-(2-(2-aminoacetamido)-3-(2,4-dinitrophenylthio)propanamido)pentanedioic acid | IC50 | 24 nM | |
| [(1R)-1-[3-(trifluoromethyl)phenyl]ethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate | IC50 | 24 nM | US-9321738: N-alkyltriazole compounds as LPAR antagonists |
| CHEMBL2182064 | IC50 | 24 nM | |
| CHEMBL153043 | EC50 | 24 nM | |
| 1-[4-[2-[5-[(6-isopropylpyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]pyrimidin-5-yl]phenyl]cyclopropanecarboxylic acid | IC50 | 24 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[[6-(1,1-difluoroethyl)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 24.4 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL2335049 | EC50 | 26 nM | |
| 1-[4-[6-[5-[[6-(3,3-difluorocyclobutoxy)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid | IC50 | 26.9 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[(6-isopropoxypyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]-2-methyl-phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 27.1 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 3-[4’-(3-Carboxy-acryloylamino)-biphenyl-4-ylcarbamoyl]-acrylic acid | IC50 | 28.3 nM | |
| 1-[3-cyano-4-[6-[5-[(6-isopropylpyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 29.3 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[(6-isopropoxypyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 29.3 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[3-methyl-4-[6-[1-methyl-5-[(6-propan-2-ylpyrazin-2-yl)amino]pyrazol-4-yl]-3-pyridinyl]phenyl]cyclopropane-1-carboxylic acid | IC50 | 30.9 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL2335048 | EC50 | 31 nM | |
| CHEMBL2182061 | IC50 | 35 nM | |
| 1-[4-[6-[1-methyl-5-[[6-(trifluoromethyl)pyrazin-2-yl]amino]pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid | IC50 | 36.3 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| (3-Octadec-9-enoylamino-propionyl)-phosphonothioic acid | EC50 | 40 nM | |
| CHEMBL2182023 | IC50 | 41 nM | |
| 1-[3-(cyanomethyl)-4-[6-[5-[(6-isopropylpyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 42.9 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[[6-(1-fluoro-1-methyl-ethyl)pyrazin-2-yl]amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 44 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[6-[5-[(6-isopropylpyrazin-2-yl)amino]-1-methyl-pyrazol-4-yl]-3-pyridyl]-3-(methoxymethyl)phenyl]cyclopropanecarboxylic Acid; Hydrochloride | IC50 | 45.8 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 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 |
| 1-[6-[6-[1-methyl-5-[(6-propan-2-ylpyrazin-2-yl)amino]pyrazol-4-yl]-3-pyridinyl]-3-pyridinyl]cyclopropane-1-carboxylic acid | IC50 | 48 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL404575 | IC50 | 50 nM | |
| 1-[4-[4-[5-[(6-chloropyrazin-2-yl)amino]-1-methylpyrazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid | IC50 | 52.9 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| 1-[4-[4-[1-methyl-5-[[6-(2-methylpropyl)pyrazin-2-yl]amino]pyrazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid | IC50 | 54.7 nM | US-11365185: Lysophosphatidic acid receptor 1 (LPAR1) inhibitor compounds |
| CHEMBL2182065 | IC50 | 57 nM | |
| Phosphoric acid mono-[2-((Z)-octadec-9-enoylamino)-ethyl] ester | IC50 | 60 nM |
ChEMBL bioactivities
209 potent at pChembl≥5 of 220 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
173 with measured affinity, of 471 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 | increases methylation, affects methylation | 2 |
| Phenylmercuric Acetate | affects cotreatment, decreases expression | 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 | decreases expression, increases abundance | 1 |
| Cannabinoids | affects methylation, increases abundance | 1 |
| Bucladesine | affects cotreatment, increases expression | 1 |
| Estradiol | increases expression, affects cotreatment | 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)
Via MONDO — disease-level, not drug-specific.
Predicted chemistry — Sugi Predict
The predicted patent-compound landscape for LPAR3 across ~30M SureChEMBL compounds — explore on Sugi Predict.
Related Atlas pages
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): dental caries, type 1 diabetes mellitus