LPAR5

Summary

LPAR5 (lysophosphatidic acid receptor 5, HGNC:13307) is a protein-coding gene on chromosome 12p13.31, encoding Lysophosphatidic acid receptor 5 (Q9H1C0). Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities.

This gene encodes a member of the rhodopsin class of G protein-coupled transmembrane receptors. This protein transmits extracellular signals from lysophosphatidic acid to cells through heterotrimeric G proteins and mediates numerous cellular processes. Many G protein receptors serve as targets for pharmaceutical drugs. Transcript variants of this gene have been described.

Source: NCBI Gene 57121 — RefSeq curated summary.

At a glance

• GWAS associations: 6
• Clinical variants (ClinVar): 63 total
• Druggable target: yes
• MANE Select transcript: NM_020400

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:13307
Approved symbol	LPAR5
Name	lysophosphatidic acid receptor 5
Location	12p13.31
Locus type	gene with protein product
Status	Approved
Aliases	KPG_010, LPA5
Ensembl gene	ENSG00000184574
Ensembl biotype	protein_coding
OMIM	606926
Entrez	57121

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 8 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000329858, ENST00000431922, ENST00000540335, ENST00000889787, ENST00000889789, ENST00000889791, ENST00000889792, ENST00000889794, ENST00000960206

RefSeq mRNA: 2 — MANE Select: NM_020400 NM_001142961, NM_020400

CCDS: CCDS8553

Canonical transcript exons

ENST00000329858 — 2 exons

Exon	Start	End
ENSE00001297856	6618835	6621464
ENSE00001402010	6635907	6635959

Expression profiles

Bgee: expression breadth ubiquitous, 218 present calls, max score 90.30.

FANTOM5 (CAGE): breadth broad, TPM avg 5.1575 / max 225.6890, expressed in 681 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
129140	4.0160	601
129139	0.6513	218
129142	0.2326	125
129143	0.1384	70
129138	0.0596	34
129141	0.0357	15
129135	0.0239	10

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
gingival epithelium	UBERON:0001949	90.30	gold quality
gingiva	UBERON:0001828	89.24	gold quality
esophagus squamous epithelium	UBERON:0006920	89.12	gold quality
ileal mucosa	UBERON:0000331	88.58	gold quality
oral cavity	UBERON:0000167	88.05	gold quality
colonic mucosa	UBERON:0000317	87.02	gold quality
mucosa of sigmoid colon	UBERON:0004993	86.73	gold quality
mucosa of transverse colon	UBERON:0004991	86.37	gold quality
esophagus mucosa	UBERON:0002469	85.98	gold quality
palpebral conjunctiva	UBERON:0001812	85.09	gold quality
jejunal mucosa	UBERON:0000399	85.04	gold quality
amniotic fluid	UBERON:0000173	84.64	gold quality
lower esophagus mucosa	UBERON:0035834	84.02	gold quality
endothelial cell	CL:0000115	84.00	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.23	gold quality
granulocyte	CL:0000094	80.50	gold quality
duodenum	UBERON:0002114	80.34	gold quality
blood	UBERON:0000178	79.56	gold quality
germinal epithelium of ovary	UBERON:0001304	79.24	gold quality
rectum	UBERON:0001052	78.98	gold quality
spleen	UBERON:0002106	78.68	gold quality
inferior vagus X ganglion	UBERON:0005363	77.50	gold quality
vagina	UBERON:0000996	77.39	gold quality
leukocyte	CL:0000738	77.22	gold quality
lymph node	UBERON:0000029	77.09	gold quality
monocyte	CL:0000576	76.70	gold quality
transverse colon	UBERON:0001157	76.68	gold quality
epithelium of nasopharynx	UBERON:0001951	76.56	gold quality
tonsil	UBERON:0002372	76.45	gold quality
small intestine Peyer’s patch	UBERON:0003454	75.87	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.11

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

60 targeting LPAR5, 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-4768-5P	100.00	69.49	2861
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-4715-3P	99.98	66.03	670
HSA-MIR-8062	99.88	68.43	995
HSA-MIR-3133	99.81	70.92	3506
HSA-MIR-4639-5P	99.81	67.37	1028
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-4306	99.72	70.50	3630
HSA-MIR-4516	99.61	67.78	3390
HSA-MIR-6073	99.60	70.36	793
HSA-MIR-18A-3P	99.56	65.68	1092
HSA-MIR-365A-3P	99.43	70.02	836
HSA-MIR-365B-3P	99.43	70.02	836
HSA-MIR-4480	99.42	66.02	735
HSA-MIR-4644	99.35	69.12	2514
HSA-MIR-185-5P	99.35	68.60	2497
HSA-MIR-6731-5P	99.28	67.42	2375
HSA-MIR-8085	99.28	67.56	2362
HSA-MIR-223-5P	99.24	68.82	1206
HSA-MIR-4784	99.15	67.41	1733
HSA-MIR-323B-3P	99.14	68.89	725
HSA-MIR-4764-5P	98.88	65.53	894
HSA-MIR-3150B-3P	98.81	67.21	1728
HSA-MIR-5000-3P	98.79	65.63	1251
HSA-MIR-1183	98.75	67.10	1116

Literature-anchored findings (GeneRIF, showing 28)

• GPR92 is proposed as a fifth LPA receptor, LPA5, which likely has distinct physiological functions in view of its expression pattern. (PMID:16774927)
• FPP and NAG play a role in the sensory nervous system through activation of GPR92 (PMID:18499677)
• Four residues involved in ligand recognition in LPA(5) were identified as follows: R2.60N mutant abolished receptor activation, whereas H4.64E, R6.62A, and R7.32A greatly reduced receptor activation. (PMID:19366702)
• 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)
• LPA5 is a bona fide LPA receptor on human mast cells responsible for the majority of LPA induced MIP-1beta release. (PMID:21464938)
• It was shown that lysophosphatidic acid 5 receptor transactivated the epidermal growth factor receptor and that inhibition of epidermal growth factor receptor blocked lysophosphatidic acid 5 receptor-dependent activation of NHE3. (PMID:21832242)
• These results suggest that LPA5 may act as a negative regulator of cellular responses in mouse fibroblast 3T3 cells, similar to the case for LPA1. (PMID:24632199)
• MMP-2 and MMP-9 were found in HT1080L5 cells, in comparison with control cells. These results suggest that LPA signaling via LPA5 negatively regulates the cell motile and invasive activities of human sarcoma cells. (PMID:24676544)
• Down-regulation of LPA receptor 5 contributes to aberrant LPA signalling in EBV-associated nasopharyngeal carcinoma. (PMID:25294670)
• 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)
• These results suggest that the cell motile activity is regulated through the induction of LPA5 by phorbol ester and anticancer drug treatments in A375cells. (PMID:29309788)
• It signaling may play a key role in the mechanisms underlying neuropathic pain following demyelination in the brain. (PMID:29409686)
• LPAR2 and LPAR5 regulate cellular functions during tumor progression in fibrosarcoma HT1080 cells. (PMID:30093116)
• LPA5 Is an Inhibitory Receptor That Suppresses CD8 T-Cell Cytotoxic Function via Disruption of Early TCR Signaling. (PMID:31231367)
• LPAR5 expression was elevated in A375cells treated with anticancer drugs. The high cell survival of highly migratory A375cells is associated with the low LPAR5 expression. The cell survival of A375cells treated with anticancer drugs was increased by LPA5 knockdown. (PMID:31362892)
• Downregulation of LPAR5 expression can inhibit the physiological process of PTC, and this phenomenon is related to the PI3K/AKT pathway and EMT. (PMID:31902939)
• Lysophosphatidic acid receptor 5 transactivation of TGFBR1 stimulates the mRNA expression of proteoglycan synthesizing genes XYLT1 and CHST3. (PMID:32920014)
• LPAR5 stimulates the malignant progression of non-small-cell lung carcinoma by upregulating MLLT11. (PMID:32964980)
• Lysophosphatidic acid mediates the pathogenesis of psoriasis by activating keratinocytes through LPAR5. (PMID:33452232)
• LPAR5 promotes thyroid carcinoma cell proliferation and migration by activating class IA PI3K catalytic subunit p110beta. (PMID:33540491)
• Control of Intestinal Epithelial Permeability by Lysophosphatidic Acid Receptor 5. (PMID:33975030)
• Interference with lysophosphatidic acid receptor 5 ameliorates oxidized low-density lipoprotein-induced human umbilical vein endothelial cell injury by inactivating NOD-like receptor family, pyrin domain containing 3 inflammasome signaling. (PMID:34662522)
• LPAR5 confers radioresistance to cancer cells associated with EMT activation via the ERK/Snail pathway. (PMID:36199069)
• Infiltration of LPAR5[+] macrophages in osteosarcoma tumor microenvironment predicts better outcomes. (PMID:36591220)
• Potential role of LPAR5 gene in prognosis and immunity of thyroid papillary carcinoma and pan-cancer. (PMID:37037831)
• Emerging roles of lysophosphatidic acid receptor subtype 5 (LPAR5) in inflammatory diseases and cancer. (PMID:37061203)
• Crosstalk between cannabinoid receptor 2 and lysophosphatidic acid receptor 5. (PMID:37187093)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	lpar5a	ENSDARG00000010384
danio_rerio	lpar5b	ENSDARG00000068638
mus_musculus	Lpar5	ENSMUSG00000067714
rattus_norvegicus	Lpar5	ENSRNOG00000021401

Paralogs (1): GPR68 (ENSG00000119714)

Protein

Protein identifiers

Lysophosphatidic acid receptor 5 — Q9H1C0 (reviewed: Q9H1C0)

Alternative names: G-protein coupled receptor 92, G-protein coupled receptor 93

All UniProt accessions (2): Q9H1C0, Q5KU18

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for lysophosphatidic acid (LPA), a mediator of diverse cellular activities.

Subcellular location. Cell membrane.

Tissue specificity. Not expressed in frontal cortex, basal forebrain, caudate putamen, thalamus, or hippocampus.

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

RefSeq proteins (2): NP_001136433, NP_065133* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (22 total): topological domain 8, transmembrane region 7, compositionally biased region 2, glycosylation site 2, chain 1, region of interest 1, disulfide bond 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H1C0-F1	84.71	0.66

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): 94–175

Glycosylation sites (2): 4, 9

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

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

MSigDB gene sets: 82 (showing top): GOBP_BEHAVIOR, GOBP_MULTICELLULAR_ORGANISMAL_RESPONSE_TO_STRESS, RICKMAN_TUMOR_DIFFERENTIATED_WELL_VS_POORLY_DN, GOBP_BEHAVIORAL_RESPONSE_TO_PAIN, GOBP_RESPONSE_TO_PAIN, SENESE_HDAC3_TARGETS_DN, REACTOME_CLASS_A_1_RHODOPSIN_LIKE_RECEPTORS, REACTOME_G_ALPHA_Q_SIGNALLING_EVENTS, GOMF_TRANSMEMBRANE_SIGNALING_RECEPTOR_ACTIVITY, DODD_NASOPHARYNGEAL_CARCINOMA_DN, CHENG_IMPRINTED_BY_ESTRADIOL, GOMF_G_PROTEIN_COUPLED_RECEPTOR_ACTIVITY, GOBP_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, ANDERSEN_CHOLANGIOCARCINOMA_CLASS2, ZHOU_INFLAMMATORY_RESPONSE_FIMA_DN

GO Biological Process (3): behavioral response to pain (GO:0048266), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186)

GO Molecular Function (1): G protein-coupled receptor activity (GO:0004930)

GO Cellular Component (2): plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
behavior	1
response to pain	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
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
membrane	1
cell periphery	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1880 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
LPAR5	GNAQ	P50148	919
LPAR5	LPAR2	Q9HBW0	886
LPAR5	LPAR1	P78351	878
LPAR5	LPAR3	Q9UBY5	877
LPAR5	GNA12	Q03113	811
LPAR5	ENPP2	Q13822	719
LPAR5	FFAR4	Q5NUL3	631
LPAR5	NHERF2	Q15599	618
LPAR5	GDPD1	Q8N9F7	614
LPAR5	FGF23	Q9GZV9	608
LPAR5	GDPD3	Q7L5L3	602
LPAR5	GPRC6A	Q5T6X5	598
LPAR5	TAS1R1	Q7RTX1	592
LPAR5	S1PR4	O95977	547
LPAR5	TRPV1	Q8NER1	547

IntAct

2 interactions, top by confidence:

A	B	Type	Score
LPAR5	PIK3CB	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (4): LPAR5 (Affinity Capture-MS), LPAR5 (Phenotypic Enhancement), LPAR5 (Affinity Capture-RNA), LPAR5 (Affinity Capture-RNA)

ESM2 similar proteins: A0A0R4IM31, A0A0R4IP11, E9QJ73, F8VQN3, O00270, O00421, O15218, O35457, O97663, P31392, P32302, P34997, P43142, P49685, Q04683, Q0II78, Q0VDU3, Q149R9, Q16570, Q3ZC80, Q67ES2, Q6XKD3, Q75ZH0, Q7TMA4, Q7TQA9, Q7TQP4, Q7TSN5, Q7TSN6, Q863H8, Q8BZR0, Q8TDV2, Q95LF2, Q95LF3, Q95LF4, Q95LF5, Q95LF7, Q95LF9, Q95LG5, Q96CH1, Q96G91

Diamond homologs: A0A4W3GG95, A0A6I8PUB9, A6QLE7, D4A7K7, E7FEL0, E9QJ73, O00254, O08675, O46685, P0C0W8, P0C5J4, P32246, P32249, P32250, P34996, P35366, P35383, P41231, P41232, P46093, P47900, P48042, P49650, P49651, P49652, P50132, P56482, P58826, P59902, P79928, P97266, Q149R9, Q15743, Q1JQB3, Q2Y2P0, Q3U6B2, Q3ZC80, Q4G072, Q4KLH9, Q5E9H8

SIGNOR signaling

7 interactions.

A	Effect	B	Mechanism
LPAR5	“up-regulates activity”	GNAI1	binding
LPAR5	“up-regulates activity”	GNAI3	binding
LPAR5	“up-regulates activity”	GNAO1	binding
LPAR5	“up-regulates activity”	GNAZ	binding
LPAR5	“up-regulates activity”	GNA12	binding
LPAR5	“up-regulates activity”	GNA13	binding
“lysophosphatidic acid”	“up-regulates activity”	LPAR5	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	62
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

333 predictions. Top by Δscore:

Variant	Effect	Δscore
12:6621461:AGACC:A	acceptor_loss	0.9900
12:6621463:ACCT:A	acceptor_loss	0.9900
12:6621464:CCT:C	acceptor_loss	0.9900
12:6621465:CT:C	acceptor_loss	0.9900
12:6621466:T:A	acceptor_loss	0.9900
12:6624015:CG:C	donor_gain	0.9900
12:6624015:CGCA:C	donor_gain	0.9900
12:6626475:T:C	acceptor_gain	0.9900
12:6621465:C:CC	acceptor_gain	0.9800
12:6623786:T:TA	donor_gain	0.9800
12:6624014:A:AC	donor_gain	0.9800
12:6624015:C:CC	donor_gain	0.9800
12:6631579:ACTT:A	donor_loss	0.9800
12:6631580:CTTA:C	donor_loss	0.9800
12:6631581:TTACC:T	donor_loss	0.9800
12:6631582:TACCT:T	donor_loss	0.9800
12:6631583:A:AC	donor_gain	0.9800
12:6631584:C:CA	donor_loss	0.9800
12:6631584:C:CC	donor_gain	0.9800
12:6631584:CCT:C	donor_gain	0.9800
12:6621470:A:AC	acceptor_gain	0.9700
12:6624015:CGCAT:C	donor_gain	0.9700
12:6631583:ACCT:A	donor_gain	0.9700
12:6631584:CCTC:C	donor_gain	0.9700
12:6623986:C:CA	donor_gain	0.9600
12:6626475:T:TC	acceptor_gain	0.9600
12:6621460:GAGAC:G	acceptor_gain	0.9500
12:6621462:GAC:G	acceptor_gain	0.9500
12:6624019:T:C	donor_gain	0.9400
12:6631583:ACCTC:A	donor_gain	0.9400

AlphaMissense

2341 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:6620925:G:C	S108R	0.993
12:6620925:G:T	S108R	0.993
12:6620927:T:G	S108R	0.993
12:6620968:C:G	C94S	0.993
12:6620969:A:T	C94S	0.993
12:6620697:C:A	W184C	0.992
12:6620697:C:G	W184C	0.992
12:6621048:G:C	S67R	0.991
12:6621048:G:T	S67R	0.991
12:6621050:T:G	S67R	0.991
12:6621060:G:C	N63K	0.990
12:6621060:G:T	N63K	0.990
12:6620508:G:C	F247L	0.989
12:6620508:G:T	F247L	0.989
12:6620510:A:G	F247L	0.989
12:6621046:T:G	D68A	0.989
12:6620813:A:G	W146R	0.988
12:6620813:A:T	W146R	0.988
12:6620968:C:T	C94Y	0.988
12:6620988:C:A	W87C	0.988
12:6620988:C:G	W87C	0.988
12:6621046:T:A	D68V	0.988
12:6620513:A:G	C246R	0.986
12:6620649:G:C	F200L	0.985
12:6620649:G:T	F200L	0.985
12:6620651:A:G	F200L	0.985
12:6620725:C:G	C175S	0.984
12:6620726:A:T	C175S	0.984
12:6620937:G:C	N104K	0.984
12:6620937:G:T	N104K	0.984

dbSNP variants (sampled 300 via entrez): RS1000091978 (12:6622764 T>A), RS1000112868 (12:6635084 C>G,T), RS1000220212 (12:6628606 G>A), RS1000323201 (12:6626422 T>C), RS1000340413 (12:6632361 A>G), RS1000396133 (12:6634608 AGAC>A), RS1000430524 (12:6632097 G>A), RS1000525453 (12:6625576 A>C), RS1000555437 (12:6627568 G>A), RS1000607977 (12:6627825 C>A,T), RS1000733433 (12:6633249 TC>T), RS1000784997 (12:6637171 G>T), RS1000958042 (12:6627277 G>A), RS1001062705 (12:6625293 C>T), RS1001279585 (12:6637012 G>A,C)

Disease associations

OMIM: gene MIM:606926 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

6 associations (top):

Study	Trait	p-value
GCST010241_399	Apolipoprotein A1 levels	1.000000e-10
GCST010242_20	HDL cholesterol levels	1.000000e-16
GCST010244_301	Triglyceride levels	4.000000e-12
GCST90002392_371	Mean corpuscular volume	7.000000e-09
GCST90002396_515	Mean reticulocyte volume	2.000000e-11
GCST90002404_131	Red cell distribution width	5.000000e-13

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004614	apolipoprotein A 1 measurement
EFO:0004612	high density lipoprotein cholesterol measurement
EFO:0004530	triglyceride measurement
EFO:0010701	mean reticulocyte volume
EFO:0009188	Red cell distribution width

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5700 (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 (10 total), top 10:

Ligand	Action	Affinity	Parameter
alkyl glycerol phosphate 18:1	Full agonist	8.7	pEC50
LPA	Agonist	7.9	pEC50
compound 66 [PMID: 36126387]	Antagonist	7.5	pIC50
AS2717638	Antagonist	7.42	pIC50
farnesyl monophosphate	Agonist	7.31	pEC50
compound 65 [PMID: 36126387]	Antagonist	7.2	pIC50
farnesyl diphosphate	Partial agonist	6.54	pEC50
TCLPA5	Antagonist	6.1	pIC50
octyl thiophosphatidic acid	Partial agonist	5.68	pEC50
N-arachidonoylglycine	Partial agonist	4.3	pEC50

Binding affinities (BindingDB)

83 measured of 83 human assays (83 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[[3-(3-fluorophenyl)propyl-[4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	0.3 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[3-(3-fluorophenyl)propyl]amino]methyl]benzoic acid	IC50	0.4 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[3-(2-fluorophenyl)propyl]amino]methyl]benzoic acid	IC50	1 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(2-phenylcyclopropyl)methyl]amino]methyl]benzoic acid	IC50	1 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(4-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	2 nM	US-9464060: Compounds
4-[[[4-(2-methoxyphenoxy)benzoyl]-(3-phenylpropyl)amino]methyl]benzoic acid	IC50	2 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(3-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	4 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	4 nM	US-9464060: Compounds
4-[[[4-(2-methoxyphenoxy)benzoyl]-(2,2,2-trifluoroethyl)amino]methyl]benzoic acid	IC50	4 nM	US-9464060: Compounds
4-[[[4-(2-methoxyphenoxy)benzoyl]-propylamino]methyl]benzoic acid	IC50	5 nM	US-9464060: Compounds
methyl 4-[[butyl-[4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoate	IC50	5 nM	US-9464060: Compounds
4-[[benzyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	6 nM	US-9464060: Compounds
2-fluoro-4-[[[4-(2-fluorophenoxy)benzoyl]-[(3-methoxyphenyl)methyl]amino]methyl]benzoic acid	IC50	6 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(2S)-2-hydroxy-3-phenylpropyl]amino]methyl]benzoic acid	IC50	7 nM	US-9464060: Compounds
4-[[[4-(2-chlorophenoxy)benzoyl]-(cyclopropylmethyl)amino]methyl]benzoic acid	IC50	7 nM	US-9464060: Compounds
4-[[2,2-difluoropropyl-[4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	7 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[2-fluoro-4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	7 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(2-fluoro-6-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	7 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(2-fluorophenyl)methyl]amino]methyl]benzoic acid	IC50	9 nM	US-9464060: Compounds
4-[[[4-(2-methoxyphenoxy)benzoyl]-(3,3,3-trifluoropropyl)amino]methyl]benzoic acid	IC50	9 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-(4-phenylbutyl)amino]methyl]benzoic acid	IC50	11 nM	US-9464060: Compounds
4-[[benzyl-[4-(2-methylphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	11 nM	US-9464060: Compounds
4-[[benzyl-[4-(2,6-difluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	11 nM	US-9464060: Compounds
4-[[benzyl-[4-(2-chloro-6-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	11 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(2R)-2-hydroxy-3-phenylpropyl]amino]methyl]benzoic acid	IC50	12 nM	US-9464060: Compounds
4-[[[4-(2-methoxyphenoxy)benzoyl]-(2-methylpropyl)amino]methyl]benzoic acid	IC50	12 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[5-(2-methoxyphenoxy)pyridine-2-carbonyl]amino]methyl]benzoic acid	IC50	12 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(4-fluoro-2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	13 nM	US-9464060: Compounds
4-[[[4-(2-methylphenoxy)benzoyl]-(2-phenylethyl)amino]methyl]benzoic acid	IC50	14 nM	US-9464060: Compounds
4-[[2-cyclopropylethyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	15 nM	US-9464060: Compounds
4-[[[4-(2-chloro-6-fluorophenoxy)benzoyl]-(cyclopropylmethyl)amino]methyl]benzoic acid	IC50	17 nM	US-9464060: Compounds
4-[[3-(3-fluorophenyl)propyl-[4-(2-methoxyphenoxy)cyclohexanecarbonyl]amino]methyl]benzoic acid	IC50	17 nM	US-9464060: Compounds
4-[[benzyl-[4-(2,6-dimethylphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	19 nM	US-9464060: Compounds
4-[[[4-(2,6-dimethylphenoxy)benzoyl]-(2-phenylethyl)amino]methyl]benzoic acid	IC50	22 nM	US-9464060: Compounds
4-[[cyclobutylmethyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	24 nM	US-9464060: Compounds
4-[[[4-(2-chlorophenoxy)benzoyl]-(2-phenylethyl)amino]methyl]benzoic acid	IC50	24 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(2,6-difluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	25 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[2-fluoro-4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	27 nM	US-9464060: Compounds
4-[[[4-(2-chlorophenoxy)benzoyl]-(2,2,2-trifluoroethyl)amino]methyl]benzoic acid	IC50	29 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(2-methylphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	30 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-[(3-methoxycyclobutyl)methyl]amino]methyl]benzoic acid	IC50	31 nM	US-9464060: Compounds
4-[[butyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	31 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-propylamino]methyl]benzoic acid	IC50	33 nM	US-9464060: Compounds
4-[[2,2-difluoroethyl-[4-(2-methoxyphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	34 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-(2,2,2-trifluoroethyl)amino]methyl]benzoic acid	IC50	35 nM	US-9464060: Compounds
4-[[2-cyclopropylethyl-[4-(2,6-difluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	36 nM	US-9464060: Compounds
4-[[2,2-difluoropropyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	40 nM	US-9464060: Compounds
4-[[cyclobutylmethyl-[4-(2-methylphenoxy)benzoyl]amino]methyl]benzoic acid	IC50	44 nM	US-9464060: Compounds
4-[[cyclopropylmethyl-[4-(2-fluorophenoxy)benzoyl]amino]methyl]benzoic acid	IC50	46 nM	US-9464060: Compounds
4-[[[4-(2-fluorophenoxy)benzoyl]-(3-methylbutyl)amino]methyl]benzoic acid	IC50	46 nM	US-9464060: Compounds

ChEMBL bioactivities

176 potent at pChembl≥5 of 176 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.59	EC50	0.26	nM	CHEMBL2335049
9.59	EC50	0.257	nM	CHEMBL2335049
9.40	IC50	0.4	nM	CHEMBL3936755
9.40	IC50	0.4	nM	CHEMBL3966526
9.08	EC50	0.83	nM	CHEMBL2335052
9.08	EC50	0.8318	nM	CHEMBL2335052
9.00	IC50	1	nM	CHEMBL3972698
9.00	IC50	1	nM	CHEMBL3943133
8.74	EC50	1.81	nM	CHEMBL2335051
8.74	EC50	1.82	nM	CHEMBL2335051
8.70	IC50	2	nM	CHEMBL3911605
8.70	IC50	2	nM	CHEMBL3980736
8.52	EC50	3	nM	CHEMBL2335050
8.52	EC50	3.02	nM	CHEMBL2335050
8.52	IC50	3	nM	CHEMBL3900559
8.47	EC50	3.4	nM	CHEMBL2335047
8.47	EC50	3.388	nM	CHEMBL2335047
8.40	IC50	4	nM	CHEMBL3920849
8.30	EC50	5.012	nM	CHEMBL357053
8.30	IC50	5	nM	CHEMBL3945517
8.30	IC50	5	nM	CHEMBL3910049
8.30	IC50	5	nM	CHEMBL3980174
8.29	EC50	5.1	nM	CHEMBL357053
8.22	IC50	6	nM	CHEMBL3891550
8.22	IC50	6	nM	CHEMBL3920145
8.21	EC50	6.1	nM	CHEMBL2335048
8.21	EC50	6.166	nM	CHEMBL2335048
8.20	EC50	6.3	nM	CHEMBL2017139
8.20	EC50	6.31	nM	CHEMBL2017139
8.15	IC50	7	nM	CHEMBL3942894
8.15	IC50	7	nM	CHEMBL3951978
8.15	IC50	7	nM	CHEMBL3987061
8.10	IC50	8	nM	CHEMBL3901720
8.10	IC50	8	nM	CHEMBL3985179
8.09	EC50	8.2	nM	CHEMBL153043
8.09	EC50	8.128	nM	CHEMBL153043
8.05	IC50	9	nM	CHEMBL3910281
8.05	IC50	9	nM	CHEMBL3955284
8.05	IC50	9	nM	CHEMBL3961765
8.00	IC50	10	nM	CHEMBL3892760
8.00	IC50	10	nM	CHEMBL3918970
7.96	IC50	11	nM	CHEMBL3956413
7.96	IC50	11	nM	CHEMBL3918468
7.96	IC50	11	nM	CHEMBL3914963
7.96	IC50	11	nM	CHEMBL3911962
7.92	IC50	12	nM	CHEMBL3942192
7.92	EC50	12	nM	LYSOPHOSPHATIDIC ACID
7.82	IC50	15	nM	CHEMBL3914942
7.82	EC50	15	nM	CHEMBL5416462
7.80	IC50	16	nM	CHEMBL3986752

PubChem BioAssay actives

93 with measured affinity, of 337 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
sodium (2-hexadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0003	uM
dihydroxy-(2-methoxy-3-octadecoxypropoxy)-sulfanylidene-lambda5-phosphane	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0008	uM
sodium [1-[hydroxy(oxido)phosphinothioyl]oxy-3-methoxypropan-2-yl] octadecanoate	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0018	uM
sodium (2-heptadecoxy-3-methoxypropoxy)-hydroxy-oxido-sulfanylidene-lambda5-phosphane	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0030	uM
dihydroxy-[(2S)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0034	uM
[(2S)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0050	uM
dihydroxy-[(2R)-2-methoxy-3-octadecoxypropoxy]-sulfanylidene-lambda5-phosphane	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0061	uM
(3-dihydroxyphosphinothioyloxy-2-methoxypropyl) octadecanoate	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0063	uM
[(2R)-3-dihydroxyphosphinothioyloxy-2-methoxypropyl] octadecanoate	733688: Agonist activity at human LPA5 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] (Z)-octadec-9-enoate	457518: Agonist activity at LPA5 expressed in human chem1 cells assessed as intracellular calcium mobilization by FLIPR assay	ec50	0.0120	uM
[(2R)-3-hexadecoxy-2-hydroxypropyl] dihydrogen phosphate	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ec50	0.0150	uM
4-[[[2-[[1-(2,4-dichlorophenyl)-4-methyl-5-[4-(trifluoromethyl)phenyl]pyrazol-3-yl]methoxy]-2-methylpropanoyl]amino]methyl]benzoic acid	1938510: Antagonist activity at human LPA5 receptor by FLIPR analysis	ic50	0.0300	uM
4-(4-ethynylpiperidine-1-carbonyl)-6,7-dimethoxy-2-(3-methyl-1-benzothiophen-5-yl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0320	uM
6,7-dimethoxy-2-(3-methyl-1-benzothiophen-5-yl)-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0320	uM
6,7-dimethoxy-2-(5-methyl-1,2-benzoxazol-3-yl)-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0360	uM
2-[3-(dimethylamino)phenyl]-4-(4-ethynylpiperidine-1-carbonyl)-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0460	uM
6,7-dimethoxy-2-(3-methyl-1-benzofuran-5-yl)-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0480	uM
2-(1-ethyl-2,3-dihydroindol-6-yl)-4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0580	uM
6,7-dimethoxy-4-(piperidine-1-carbonyl)-2-(3-propan-2-ylphenyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0630	uM
6,7-dimethoxy-2-(1-methylindol-6-yl)-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0640	uM
[(2R)-2-hydroxy-3-phosphonooxypropyl] hexadecanoate	733688: Agonist activity at human LPA5 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay in presence of Ki16425	ec50	0.0676	uM
4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxy-2-(3-methyl-1-benzothiophen-5-yl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0690	uM
2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0790	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0870	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(4-prop-1-ynylpiperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.0910	uM
1-[2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-1-oxoisoquinoline-4-carbonyl]piperidine-4-carbonitrile	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.1020	uM
(2-hydroxy-3-phosphonooxypropyl) (Z)-octadec-9-enoate	1431881: Agonist activity at FLAG-tagged LPA5 receptor (unknown origin) expressed in rat B103 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	0.1400	uM
4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxy-2-(3-methyl-1-benzofuran-5-yl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.1440	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(4-methylpiperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.1600	uM
2-(3-tert-butylphenyl)-6,7-dimethoxy-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.1730	uM
4-(4-fluoropiperidine-1-carbonyl)-6,7-dimethoxy-2-(3-propan-2-ylphenyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.2000	uM
6,7-dimethoxy-2-(8-methylnaphthalen-2-yl)-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.2100	uM
2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxy-6-pentoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.2300	uM
4-(8-azabicyclo[3.2.1]octane-8-carbonyl)-2-[3-(dimethylamino)phenyl]-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.2300	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(3-methylpiperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.2600	uM
2-[3-(4-nitrophenoxy)phenyl]-1,3-dioxoisoindole-5-carboxylic acid	454070: Binding affinity to LPA5	ki	0.2920	uM
4-(azocane-1-carbonyl)-2-[3-(dimethylamino)phenyl]-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.3010	uM
2-[3-(dimethylamino)phenyl]-N,6,7-trimethoxy-N-methyl-1-oxoisoquinoline-4-carboxamide	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.3200	uM
2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxy-6-propan-2-yloxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.3690	uM
2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxy-6-propoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.4800	uM
6-cyclohexyloxy-2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.5100	uM
6,7-dimethoxy-4-(piperidine-1-carbonyl)-2-(3-propan-2-yloxyphenyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.6300	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(4-methoxypiperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.6400	uM
2-(1-benzothiophen-5-yl)-6,7-dimethoxy-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.6400	uM
5-(3-chloro-4-cyclohexylphenyl)-1-(3-methoxyphenyl)pyrazole-3-carboxylic acid	2120490: Antagonist activity at LPA5 (unknown origin)	ic50	0.8000	uM
6-cyclopentyloxy-2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.8900	uM
2-[3-(dimethylamino)phenyl]-6,7-dimethoxy-4-(2-methylpiperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	0.9900	uM
2-[3-(dimethylamino)phenyl]-4-(4-fluoropiperidine-1-carbonyl)-7-methoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	1.0600	uM
2-[3-(dimethylamino)phenyl]-4-(4,4-dimethylpiperidine-1-carbonyl)-6,7-dimethoxyisoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	1.1000	uM
2-(1-benzofuran-5-yl)-6,7-dimethoxy-4-(piperidine-1-carbonyl)isoquinolin-1-one	2000970: Antagonist activity at human LPA5 receptor expressed in RH7777 cells assessed as inhibition of EC80 concentration of hexadecyl LPA-induced calcium mobilization incubated for 15 mins by FLIPR method	ic50	1.1000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases methylation, affects cotreatment, increases expression	5
Benzo(a)pyrene	affects methylation, decreases methylation	2
triphenyl phosphate	affects expression	1
quercitrin	increases expression	1
beta-lapachone	increases expression	1
sodium arsenite	increases expression	1
benzo(e)pyrene	increases methylation	1
lysophosphatidic acid	decreases reaction, increases activity, affects binding	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression, affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
2-palmitoylglycerol	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
2,2’,4,4’,5-brominated diphenyl ether	increases expression	1
abrine	decreases expression	1
ormosil	affects binding, decreases expression	1
dorsomorphin	affects cotreatment, increases expression	1
asparanin A	increases expression	1
Leflunomide	increases expression	1
Vehicle Emissions	decreases methylation	1
Chelating Agents	affects binding, increases expression	1
Copper	affects binding, increases expression	1
Diethylhexyl Phthalate	increases expression	1
Doxorubicin	decreases expression	1
Estradiol	affects cotreatment, increases expression	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression, affects cotreatment	1
Methapyrilene	increases methylation	1
Polyethylene Glycols	affects binding, decreases expression	1
Silicon Dioxide	decreases expression	1
Tobacco Smoke Pollution	affects expression	1
Urethane	increases expression	1

ChEMBL screening assays

38 unique, capped per target: 29 functional, 9 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1064666	Functional	Antagonist activity at LPA5 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium response	Structure-based drug design identifies novel LPA3 antagonists. — Bioorg Med Chem
CHEMBL1064671	Binding	Binding affinity to LPA5	Structure-based drug design identifies novel LPA3 antagonists. — Bioorg Med Chem

Cellosaurus cell lines

5 cell lines: 4 cancer cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D7TS	Ubigene A-549 LPAR5 KO	Cancer cell line	Male
CVCL_D8PE	Ubigene HCT 116 LPAR5 KO	Cancer cell line	Male
CVCL_E0GN	Ubigene HeLa LPAR5 KO	Cancer cell line	Female
CVCL_KX78	PathHunter CHO-K1 GPR92 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_ZK35	Tango GPR92-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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