General Information of the Protein
Protein ID
PT03925
Protein Name
Lysophosphatidic acid receptor 1
Secondarily
Protein Name
Lysophosphatidic acid receptor Edg-2
Gene Name
LPAR1
Secondarily
Gene Name
EDG2
LPA1
Sequence
MAAISTSIPVISQPQFTAMNEPQCFYNESIAFFYNRSGKHLATEWNTVSKLVMGLGITVCIFIMLANLLVMVAIYVNRRFHFPIYYLMANLAAADFFAGLAYFYLMFNTGPNTRRLTVSTWLLRQGLIDTSLTASVANLLAIAIERHITVFRMQLHTRMSNRRVVVVIVVIWTMAIVMGAIPSVGWNCICDIENCSNMAPLYSDSYLVFWAIFNLVTFVVMVVLYAHIFGYVRQRTMRMSRHSSGPRRNRDTMMSLLKTVVIVLGAFIICWTPGLVLLLLDVCCPQCDVLAYEKFFLLLAEFNSAMNPIIYSYRDKEMSATFRQILCCQRSENPTGPTEGSDRSASSLNHTILAGVHSNDHSVV
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Lipid-like ligand receptor (family A GPCR)
>
EDG receptor
Function
Receptor for lysophosphatidic acid (LPA) (PubMed:9070858, PubMed:19306925, PubMed:25025571, PubMed:26091040). Plays a role in the reorganization of the actin cytoskeleton, cell migration, differentiation and proliferation, and thereby contributes to the responses to tissue damage and infectious agents. Activates downstream signaling cascades via the G(i)/G(o), G(12)/G(13), and G(q) families of heteromeric G proteins. Signaling inhibits adenylyl cyclase activity and decreases cellular cAMP levels (PubMed:26091040). Signaling triggers an increase of cytoplasmic Ca(2+) levels (PubMed:19656035, PubMed:19733258, PubMed:26091040). Activates RALA; this leads to the activation of phospholipase C (PLC) and the formation of inositol 1,4,5-trisphosphate (PubMed:19306925). Signaling mediates activation of down-stream MAP kinases (By similarity). Contributes to the regulation of cell shape. Promotes Rho-dependent reorganization of the actin cytoskeleton in neuronal cells and neurite retraction (PubMed:26091040). Promotes the activation of Rho and the formation of actin stress fibers (PubMed:26091040). Promotes formation of lamellipodia at the leading edge of migrating cells via activation of RAC1 (By similarity). Through its function as LPA receptor, plays a role in chemotaxis and cell migration, including responses to injury and wounding (PubMed:18066075, PubMed:19656035, PubMed:19733258). Plays a role in triggering inflammation in response to bacterial lipopolysaccharide (LPS) via its interaction with CD14. Promotes cell proliferation in response to LPA (By similarity). Inhibits the intracellular ciliogenesis pathway in response to LPA and through AKT1 activation (PubMed:31204173). Required for normal skeleton development. May play a role in osteoblast differentiation. Required for normal brain development. Required for normal proliferation, survival and maturation of newly formed neurons in the adult dentate gyrus. Plays a role in pain perception and in the initiation of neuropathic pain (By similarity).
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Uniprot ID
Primary ID:
Q92633

Secondarily ID:
B4DK36
O00656
O00722
P78351
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HGNC ID
HGNC:3166
Subcellular Location
Cell surface
Cell membrane
Endosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0461724
2-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)phenethylthio)acetic acid
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C22H21ClN2O5S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0510616
3-(4-(4-((1-(2-chlorocyclopent-1-enyl)ethoxy)carbonyl)isoxazol-3-yl)benzylthio)propanoic acid
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C21H23ClN2O5S
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0467202
4-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)phenylamino)-4-oxobutanoic acid
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C22H20ClN3O6
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0461725
3-(4-(4-((1-(2-chlorocyclohex-1-enyl)ethoxy)carbonyl)isoxazol-3-yl)benzylthio)propanoic acid
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C22H25ClN2O5S
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0458400
5-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)phenyl)pentanoic acid
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C23H23ClN2O5
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0444706
3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)benzylthio)propanoic acid
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C22H21ClN2O5S
 1
1
IC50 = 220 nM
   TI
   LI
   LO
   TS
CP0458399
3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-5-yl)benzylthio)propanoic acid
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C22H21ClN2O5S
 1
1
IC50 = 260 nM
   TI
   LI
   LO
   TS
CP0457570
3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)benzylsulfonyl)propanoic acid
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C22H21ClN2O7S
 1
1
IC50 = 280 nM
   TI
   LI
   LO
   TS
CP0542188
5-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)phenyl)-3,3-dimethylpentanoic acid
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C25H27ClN2O5
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0458398
2-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)isoxazol-3-yl)benzylthio)ethanesulfonic acid
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C21H21ClN2O6S2
 1
1
IC50 = 430 nM
   TI
   LI
   LO
   TS
CP0233368
3-(4-(4-((1-(2-chlorophenyl)ethoxy)carbonyl)-3-methylisoxazol-5-yl)benzylthio)propanoic acid
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C23H23ClN2O5S
 1
1
IC50 = 510 nM
   TI
   LI
   LO
   TS
CP0464284
3-{2'-[1-(2-chloro-phenyl)-ethoxycarbonylamino]-biphenyl-4-ylmethylsulfanyl}-propionic acid
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C25H24ClNO4S
 1
1
IC50 > 40000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0307182
3-[[(Z)-octadec-9-enoyl]amino]propanoylphosphonic acid
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C21H40NO5P
 1
1 EC50 = 221 nM
CP0169579
1-[4-[3-fluoro-4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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C28H25FN4O4
 1
1 IC50 = 18 nM
CP0212474
1-[4-[4-[1-methyl-5-[[(1R)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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C29H25F3N4O4
 1
1 IC50 = 18 nM
CP0238378
1-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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C28H26N4O4
 1
1 IC50 = 18 nM
CP0097125
[(1R)-1-phenylethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate
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C29H29N5O5S
 1
1 IC50 = 18.8 nM
CP0169580
[(1R)-1-[3-(trifluoromethyl)phenyl]ethyl] N-[3-methyl-5-[4-[4-[1-(methylsulfonylcarbamoyl)cyclopropyl]phenyl]phenyl]triazol-4-yl]carbamate
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C30H28F3N5O5S
 1
1 IC50 = 24.5 nM
CP0323007
2-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]acetic acid
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C26H24N4O4
 1
1 IC50 = 48 nM
CP0212475
2-[4-[4-[1-methyl-5-[[(1R)-1-phenylethoxy]carbonylamino]triazol-4-yl]phenyl]cyclohexyl]acetic acid
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C26H30N4O4
 1
1 IC50 = 58 nM
CP0193813
1-[4-[4-[1-methyl-5-[[(2R)-3-methylbutan-2-yl]oxycarbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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C25H28N4O4
 1
1 IC50 = 70 nM
CP0166826
[(2R)-2-[[(Z)-octadec-9-enoyl]amino]-3-[4-(pyridin-2-ylmethoxy)phenyl]propyl] dihydrogen phosphate
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C33H51N2O6P
 2
1 IC50 = 109 nM
2 Ki = 18 nM
CP0099061
[(2S)-2-[[(Z)-octadec-9-enoyl]amino]-3-[4-(pyridin-2-ylmethoxy)phenyl]propyl] dihydrogen phosphate
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C33H51N2O6P
 2
1 IC50 = 604 nM
2 Ki = 156 nM
CP0241461
1-[4-[4-[1-methyl-5-[[(1S)-1-[3-(trifluoromethyl)phenyl]ethoxy]carbonylamino]triazol-4-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid
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C29H25F3N4O4
 1
1 IC50 = 2660 nM
CP0128457
2-(3-(4-nitrophenoxy)phenyl)-1,3-dioxoisoindoline-5-carboxylic acid
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C21H12N2O7
 1
1 Ki = 48 nM
CP0151570
2-(1,3-dioxo-5-(p-tolyloxy)isoindolin-2-yl)acetic acid
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C17H13NO5
 1
1 Ki = 311 nM
Clinical Information about the Protein
Target 1 ( Lysophosphatidic acid receptor 1 (LPAR1) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Pulmonary fibrosis [ICD-11: CB03.4]
2 Scleroderma [ICD-11: 4A42]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 BMS-986278 Phase 2
Pulmonary fibrosis
2 BMS-986020 Phase 2
Scleroderma