GPR132

Summary

GPR132 (G protein-coupled receptor 132, HGNC:17482) is a protein-coding gene on chromosome 14q32.33, encoding Probable G-protein coupled receptor 132 (Q9UNW8). May be a receptor for oxidized free fatty acids derived from linoleic and arachidonic acids such as 9-hydroxyoctadecadienoic acid (9-HODE).

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. The receptors are seven-pass transmembrane proteins that respond to extracellular cues and activate intracellular signal transduction pathways. This protein was reported to be a receptor for lysophosphatidylcholine action, but PubMedID: 15653487 retracts this finding and instead suggests this protein to be an effector of lysophosphatidylcholine action. This protein may have proton-sensing activity and may be a receptor for oxidized free fatty acids. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 29933 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 76 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_013345

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17482
Approved symbol	GPR132
Name	G protein-coupled receptor 132
Location	14q32.33
Locus type	gene with protein product
Status	Approved
Aliases	G2A
Ensembl gene	ENSG00000183484
Ensembl biotype	protein_coding
OMIM	606167
Entrez	29933

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 6 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000329797, ENST00000392585, ENST00000539291, ENST00000546679, ENST00000549990, ENST00000551869, ENST00000943828, ENST00000943829

RefSeq mRNA: 4 — MANE Select: NM_013345 NM_001278694, NM_001278695, NM_001278696, NM_013345

CCDS: CCDS61567, CCDS9997

Canonical transcript exons

ENST00000329797 — 4 exons

Exon	Start	End
ENSE00001297887	105055387	105056166
ENSE00001370377	105065379	105065430
ENSE00001512438	105049395	105052102
ENSE00003641654	105057167	105057280

Expression profiles

Bgee: expression breadth ubiquitous, 159 present calls, max score 86.50.

FANTOM5 (CAGE): breadth broad, TPM avg 5.9326 / max 310.5099, expressed in 466 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
145165	5.7908	462
207388	0.1417	85

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	86.50	gold quality
leukocyte	CL:0000738	83.91	gold quality
monocyte	CL:0000576	83.60	gold quality
blood	UBERON:0000178	82.23	gold quality
bone marrow cell	CL:0002092	78.12	gold quality
spleen	UBERON:0002106	76.16	gold quality
right uterine tube	UBERON:0001302	75.72	gold quality
lymph node	UBERON:0000029	75.70	gold quality
vermiform appendix	UBERON:0001154	73.55	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	72.31	gold quality
metanephros cortex	UBERON:0010533	70.99	gold quality
bone marrow	UBERON:0002371	69.93	gold quality
buccal mucosa cell	CL:0002336	69.87	silver quality
small intestine Peyer’s patch	UBERON:0003454	68.38	gold quality
caecum	UBERON:0001153	68.16	gold quality
upper lobe of left lung	UBERON:0008952	67.26	gold quality
skin of leg	UBERON:0001511	67.21	gold quality
small intestine	UBERON:0002108	66.46	gold quality
gall bladder	UBERON:0002110	66.43	gold quality
upper lobe of lung	UBERON:0008948	66.15	gold quality
omental fat pad	UBERON:0010414	65.83	gold quality
peritoneum	UBERON:0002358	65.76	gold quality
thyroid gland	UBERON:0002046	65.71	gold quality
right coronary artery	UBERON:0001625	65.69	gold quality
right lung	UBERON:0002167	65.24	gold quality
adipose tissue of abdominal region	UBERON:0007808	64.54	gold quality
right lobe of thyroid gland	UBERON:0001119	64.42	gold quality
left lobe of thyroid gland	UBERON:0001120	64.42	gold quality
skin of abdomen	UBERON:0001416	64.20	gold quality
mucosa of transverse colon	UBERON:0004991	64.10	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	9.46
E-MTAB-7381	no	847.12

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): TBX21

miRNA regulators (miRDB)

46 targeting GPR132, 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-4673	100.00	66.64	1490
HSA-MIR-3689D	100.00	66.14	1181
HSA-MIR-6851-5P	100.00	65.63	1294
HSA-MIR-4500	99.99	72.72	2367
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790
HSA-LET-7E-5P	99.98	72.29	1790
HSA-LET-7F-5P	99.98	72.56	1784
HSA-LET-7G-5P	99.98	72.37	1784
HSA-LET-7I-5P	99.98	72.37	1788
HSA-MIR-98-5P	99.98	72.33	1787
HSA-MIR-4645-5P	99.98	65.81	1284
HSA-MIR-8075	99.97	67.20	962
HSA-LET-7D-5P	99.96	71.76	1632
HSA-MIR-4458	99.96	71.64	1650
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-218-5P	99.93	72.22	2103
HSA-MIR-22-3P	99.93	68.13	917
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-378G	99.71	64.90	1106
HSA-MIR-18A-3P	99.56	65.68	1092
HSA-MIR-4437	99.52	65.29	1266
HSA-MIR-4708-3P	99.51	67.99	870
HSA-MIR-6727-3P	99.49	65.92	1333
HSA-MIR-4687-3P	99.48	66.41	968
HSA-MIR-766-3P	99.47	65.24	1811
HSA-MIR-4722-3P	99.35	65.22	1099
HSA-MIR-520F-5P	99.34	70.40	1632
HSA-MIR-4505	99.27	67.81	2678

Literature-anchored findings (GeneRIF, showing 17)

• G2A is a negative modifier of lymphoid leukemogenesis initiated by the BCR-ABL oncogene (PMID:12086852)
• In atherosclerotic plaques of human coronary arterial specimens, G2A is expressed by macrophages within the lipid-rich plaques, whereas no immunoreactivity of G2A is observed in fibrous plaques where macrophages do not exist. (PMID:12482833)
• G2A can activate a specific combination of G proteins, and G2A/LPC-induced apoptosis involves both G alpha(13)- and G alpha(s)-mediated pathways (PMID:12586833)
• G2A was not detected in either brain or skin vascular endothelial cell type. (PMID:12805023)
• G2A is a proton-sensing G-protein-coupled receptor antagonized by lysophosphatidylcholine (PMID:15280385)
• Activity of the human G2A receptor is less sensitive to pH fluctuations as measured by inositol phosphate and cAMP accumulation. (PMID:15665078)
• results indicate that G protein-coupled receptor G2A is a receptor for 9-hydroxyoctadecadienoic acid (9-HODE) and other oxidized free fatty acids and is activated by oxidized free fatty acids (PMID:16236715)
• G2A latent within neutrophil secretory vesicles may facilitate signaling through lysophospholipids for neutrophil activation and calcium flux. (PMID:17475884)
• 9-HODE-G2A signaling plays proinflammatory roles in skin under oxidative conditions (PMID:18034171)
• the G-protein-coupled receptor G2A, unlike its relative GPR4, is involved in the chemotaxis of monocytic cells. (PMID:18089568)
• we found an additional novel G2A variant (G2A-b) that is the major transcript with functional response to ligand stimulation as well as G2A-a, and succeeded in discriminating proton-sensing and oxidized fatty acid-sensing activities of G2A. (PMID:19855098)
• coexpression of OGR1- and G2A-enhanced proton sensitivity and proton-induced calcium signals. This alteration is attributed to oligomerization of OGR1 and G2A. The oligomeric potential locates receptors at a specific site, which leads to enhanced (PMID:27049592)
• High GPR132 expression is associated with acute lymphoblastic leukemia. (PMID:27588474)
• G protein-coupled receptor 132 (Gpr132) functions as a key macrophage sensor of the rising lactate in the acidic tumor milieu to mediate the reciprocal interaction between cancer cells and macrophages during breast cancer metastasis. Lactate activates macrophage Gpr132 to promote the alternatively activated macrophage (M2)-like phenotype, which, in turn, facilitates cancer cell adhesion, migration, and invasion. (PMID:28049847)
• Expression profiles of proton-sensing G-protein coupled receptors in common skin tumors. (PMID:32948783)
• Lipid Receptor G2A-Mediated Signal Pathway Plays a Critical Role in Inflammatory Response by Promoting Classical Macrophage Activation. (PMID:33941654)
• Activation of orphan receptor GPR132 induces cell differentiation in acute myeloid leukemia. (PMID:36437247)

Cross-species orthologs

1 orthologs

Organism	Symbol	Gene ID
rattus_norvegicus	Gpr132	ENSRNOG00000013914

Paralogs (7): GPR174 (ENSG00000147138), GPR146 (ENSG00000164849), GPR183 (ENSG00000169508), GPR151 (ENSG00000173250), RXFP3 (ENSG00000182631), GPR141 (ENSG00000187037), P2RY11 (ENSG00000244165)

Protein

Protein identifiers

Probable G-protein coupled receptor 132 — Q9UNW8 (reviewed: Q9UNW8)

Alternative names: G2 accumulation protein

All UniProt accessions (3): A0A0G2JL29, F8VRH8, Q9UNW8

UniProt curated annotations — full annotation on UniProt →

Function. May be a receptor for oxidized free fatty acids derived from linoleic and arachidonic acids such as 9-hydroxyoctadecadienoic acid (9-HODE). Activates a G alpha protein, most likely G alpha(q). May be involved in apoptosis. Functions at the G2/M checkpoint to delay mitosis. May function as a sensor that monitors the oxidative states and mediates appropriate cellular responses such as secretion of paracrine signals and attenuation of proliferation. May mediate ths accumulation of intracellular inositol phosphates at acidic pH through proton-sensing activity.

Subcellular location. Cell membrane.

Tissue specificity. Highly expressed in macrophages and hematopoietic tissues rich in lymphocytes, like spleen and thymus. Weakly expressed in heart and lung. In atherosclerotic plaques, expression is observed around the lipid core and at the shoulder region.

Induction. By stress and DNA-damaging agents.

Miscellaneous. More abundant than isoform 1 in leukocytes by approximately 3-fold.

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

Isoforms (3)

UniProt ID	Names	Canonical?
Q9UNW8-1	1, G2A-a	yes
Q9UNW8-2	2
Q9UNW8-3	3, G2A-b

RefSeq proteins (4): NP_001265623, NP_001265624, NP_001265625, NP_037477* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR005388	G2A_lysphc_rcpt	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (38 total): helix 12, topological domain 8, transmembrane region 7, mutagenesis site 3, splice variant 2, turn 2, chain 1, glycosylation site 1, disulfide bond 1, strand 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
8HQM	ELECTRON MICROSCOPY	2.95
8HQE	ELECTRON MICROSCOPY	2.97
8HQN	ELECTRON MICROSCOPY	3
8HVI	ELECTRON MICROSCOPY	3.04

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9UNW8-F1	79.86	0.48

Antibody-complex structures (SAbDab): 4 — 8HQE, 8HQM, 8HQN, 8HVI

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): 115–186

Glycosylation sites (1): 35

Mutagenesis-validated functional residues (3):

Position	Phenotype
7	no change in basal activity.
31	decreased ip1 accumulation at any ph.
42	decreased basal activity at alkaline ph and loss of proton-sensing activity at low ph.

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-416476	G alpha (q) signalling events

MSigDB gene sets: 161 (showing top): GOBP_CELL_CYCLE_PHASE_TRANSITION, GOBP_REGULATION_OF_CELL_CYCLE_G2_M_PHASE_TRANSITION, GOBP_NEGATIVE_REGULATION_OF_CELL_CYCLE_PROCESS, GOBP_NEGATIVE_REGULATION_OF_CELL_CYCLE, GOBP_REGULATION_OF_CELL_CYCLE, GOBP_CELL_CYCLE_G1_S_PHASE_TRANSITION, GOBP_NEGATIVE_REGULATION_OF_MITOTIC_CELL_CYCLE, GOBP_MITOTIC_CELL_CYCLE, GOBP_CELL_CYCLE_G2_M_PHASE_TRANSITION, GOBP_NEGATIVE_REGULATION_OF_CELL_CYCLE_G2_M_PHASE_TRANSITION, RYTTCCTG_ETS2_B, EGR1_01, GOBP_REGULATION_OF_CELL_CYCLE_PHASE_TRANSITION, GOBP_REGULATION_OF_CELL_CYCLE_PROCESS, DANG_BOUND_BY_MYC

GO Biological Process (4): G1/S transition of mitotic cell cycle (GO:0000082), negative regulation of G2/M transition of mitotic cell cycle (GO:0010972), 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-2 pathways:

Category	Pathways
GPCR ligand binding	1
GPCR downstream signalling	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
mitotic cell cycle	1
mitotic cell cycle phase transition	1
cell cycle G1/S phase transition	1
G2/M transition of mitotic cell cycle	1
regulation of G2/M transition of mitotic cell cycle	1
negative regulation of mitotic cell cycle phase transition	1
negative regulation of cell cycle G2/M phase transition	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

916 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
GPR132	MAP3K4	Q9Y6R4	761
GPR132	ABL1	P00519	588
GPR132	GPR68	Q15743	544
GPR132	TIMD4	Q96H15	523
GPR132	ASIC3	Q9UHC3	497
GPR132	CX3CL1	P78423	481
GPR132	GPR151	Q8TDV0	465
GPR132	GPR142	Q7Z601	451
GPR132	LPCAT3	Q6P1A2	447
GPR132	GPR4	P46093	446
GPR132	KRTAP1-1	Q07627	439
GPR132	CD274	Q9NZQ7	437
GPR132	NMT1	P30419	434
GPR132	GPR119	Q8TDV5	430
GPR132	ADGRB1	O14514	420

IntAct

0 interactions, top by confidence:

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

9 interactions.

A	Effect	B	Mechanism
GPR132	“up-regulates activity”	GNAS	binding
GPR132	“up-regulates activity”	GNAL	binding
GPR132	“up-regulates activity”	GNAI3	binding
GPR132	“up-regulates activity”	GNAO1	binding
GPR132	“up-regulates activity”	GNAZ	binding
GPR132	“up-regulates activity”	GNAQ	binding
GPR132	“up-regulates activity”	GNA14	binding
GPR132	“up-regulates activity”	GNA15	binding
9-HODE	“up-regulates activity”	GPR132	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	57
Likely benign	9
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

669 predictions. Top by Δscore:

Variant	Effect	Δscore
14:105052099:TTTC:T	acceptor_gain	1.0000
14:105052100:TTC:T	acceptor_gain	1.0000
14:105052101:TC:T	acceptor_gain	1.0000
14:105052101:TCC:T	acceptor_loss	1.0000
14:105052102:CC:C	acceptor_gain	1.0000
14:105052103:C:CC	acceptor_gain	1.0000
14:105052103:C:CG	acceptor_loss	1.0000
14:105052104:T:A	acceptor_loss	1.0000
14:105052098:GTTTC:G	acceptor_gain	0.9900
14:105057279:ACCT:A	acceptor_loss	0.9900
14:105057281:CTGGA:C	acceptor_loss	0.9900
14:105057129:T:TA	donor_gain	0.9800
14:105057162:CTCA:C	donor_loss	0.9800
14:105057164:CACCT:C	donor_loss	0.9800
14:105057165:ACCT:A	donor_loss	0.9800
14:105065377:A:AC	donor_gain	0.9800
14:105065377:AC:A	donor_gain	0.9800
14:105065378:C:CC	donor_gain	0.9800
14:105065378:CC:C	donor_gain	0.9800
14:105052111:C:CT	acceptor_gain	0.9700
14:105057277:TGAC:T	acceptor_gain	0.9700
14:105065374:CTTA:C	donor_loss	0.9600
14:105065375:TTACC:T	donor_loss	0.9600
14:105065376:TA:T	donor_loss	0.9600
14:105065378:C:A	donor_loss	0.9600
14:105054020:T:TA	donor_gain	0.9500
14:105054021:C:A	donor_gain	0.9500
14:105065372:GACTT:G	donor_loss	0.9500
14:105065373:ACTTA:A	donor_loss	0.9500
14:105055389:TTGTA:T	donor_gain	0.9400

AlphaMissense

2463 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:105051813:C:A	W108C	0.991
14:105051813:C:G	W108C	0.991
14:105051513:A:C	F208L	0.986
14:105051513:A:T	F208L	0.986
14:105051515:A:G	F208L	0.986
14:105051815:A:G	W108R	0.985
14:105051815:A:T	W108R	0.985
14:105051372:G:C	F255L	0.982
14:105051372:G:T	F255L	0.982
14:105051374:A:G	F255L	0.982
14:105051987:G:C	S50R	0.977
14:105051987:G:T	S50R	0.977
14:105051989:T:G	S50R	0.977
14:105051750:G:C	S129R	0.973
14:105051750:G:T	S129R	0.973
14:105051752:T:G	S129R	0.973
14:105051384:G:C	F251L	0.967
14:105051384:G:T	F251L	0.967
14:105051386:A:G	F251L	0.967
14:105051505:G:C	P211R	0.964
14:105051367:G:T	P257Q	0.959
14:105051525:G:C	F204L	0.959
14:105051525:G:T	F204L	0.959
14:105051527:A:G	F204L	0.959
14:105051367:G:C	P257R	0.956
14:105051370:G:T	A256D	0.956
14:105051737:A:G	C134R	0.955
14:105051505:G:T	P211H	0.954
14:105051626:C:G	G171R	0.954
14:105051626:C:T	G171R	0.954

dbSNP variants (sampled 300 via entrez): RS1000080371 (14:105052134 G>C), RS1000124188 (14:105049186 G>T), RS1000167216 (14:105063671 C>T), RS1000264162 (14:105057252 A>G), RS1000404832 (14:105062415 G>A), RS1000420872 (14:105062180 G>A), RS1000695557 (14:105056076 G>A,T), RS1000730664 (14:105058522 G>A), RS1000752849 (14:105061174 G>A), RS1000917320 (14:105066414 T>C), RS1001015470 (14:105056740 C>T), RS1001361962 (14:105066594 G>A,C), RS1001547803 (14:105061879 C>T), RS1001641059 (14:105061689 G>A), RS1001807368 (14:105066975 G>A,T)

Disease associations

OMIM: gene MIM:606167 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3085618 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 819 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL4297310	DORDAVIPRONE	3	819

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Class A Orphans with emerging pharmacology

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
NOX-6-18	Antagonist	7.77	pIC50
NOX-6-7	Agonist	7.3	pEC50
ONC212	Agonist	6.39	pEC50
9-hydroxyoctadecadienoic acid	Full agonist	5.7	pEC50

ChEMBL bioactivities

27 potent at pChembl≥5 of 64 total, top 26 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.09	EC50	820	nM	CHEMBL5315640
6.09	EC50	812.8	nM	CHEMBL5315640
5.76	EC50	1740	nM	CHEMBL5549824
5.71	EC50	1960	nM	CHEMBL5542713
5.71	EC50	1950	nM	CHEMBL5542713
5.60	EC50	2512	nM	CHEMBL5549824
5.54	EC50	2920	nM	CHEMBL5558575
5.54	EC50	2870	nM	CHEMBL5505872
5.54	EC50	2884	nM	CHEMBL5558575
5.54	EC50	2884	nM	CHEMBL5505872
5.48	EC50	3340	nM	CHEMBL5532567
5.48	EC50	3311	nM	CHEMBL5532567
5.41	EC50	3920	nM	CHEMBL5287669
5.21	EC50	6200	nM	CHEMBL5558112
5.21	EC50	6166	nM	CHEMBL5558112
5.16	EC50	6870	nM	CHEMBL5555854
5.16	EC50	6918	nM	CHEMBL5555854
5.14	EC50	7244	nM	CHEMBL5558868
5.13	EC50	7330	nM	CHEMBL5558868
5.13	EC50	7413	nM	CHEMBL5505940
5.12	EC50	7530	nM	CHEMBL5512528
5.12	EC50	7500	nM	CHEMBL5505940
5.12	EC50	7500	nM	CHEMBL1077284
5.12	EC50	7586	nM	CHEMBL5512528
5.11	EC50	7700	nM	CHEMBL5315640
5.06	EC50	8710	nM	CHEMBL5556971

PubChem BioAssay actives

27 with measured affinity, of 119 total; 14 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
(2R)-3-phenyl-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	0.8128	uM
3-phenyl-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	1.7400	uM
3-(4-fluorophenyl)-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	1.9498	uM
3-phenyl-2-[[3-(pyridin-4-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	2.8700	uM
(2S)-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]pentanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	2.8840	uM
2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]-3-[4-(trifluoromethoxy)phenyl]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	3.3113	uM
11-benzyl-7-[[4-(trifluoromethyl)phenyl]methyl]-2,5,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),5-dien-8-one	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	3.9200	uM
2-phenyl-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	6.1659	uM
2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]pentanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	6.8700	uM
(2S)-3-methyl-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]butanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	7.2444	uM
3-phenyl-2-[(3-phenylmethoxybenzoyl)amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	7.4131	uM
(10E,12Z)-9-hydroxyoctadeca-10,12-dienoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	7.5000	uM
(2R)-3-(4-chlorophenyl)-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	7.5300	uM
(2R)-2-[[3-(pyridin-3-ylmethoxy)benzoyl]amino]-3-[4-(trifluoromethyl)phenyl]propanoic acid	2066327: Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	ec50	8.7096	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Estradiol	affects cotreatment, increases expression	2
aristolochic acid I	increases expression	1
3-((6-(2-methoxyphenyl)pyrimidin-4-yl)amino)phenyl)methane sulfonamide	decreases expression	1
GSK-J4	decreases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression	1
lead acetate	affects cotreatment, decreases expression	1
beta-lapachone	increases expression	1
zinc protoporphyrin	affects cotreatment, decreases expression	1
sodium arsenite	increases expression	1
butyraldehyde	decreases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression	1
di-n-butylphosphoric acid	affects expression	1
jinfukang	decreases expression	1
Air Pollutants, Occupational	increases expression	1
Benzene	affects expression	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Camptothecin	increases expression	1
Cisplatin	increases expression	1
Demecolcine	increases expression	1
Ethyl Methanesulfonate	increases expression	1
Fluorouracil	increases expression	1
Formaldehyde	increases expression	1
Lipopolysaccharides	increases expression, affects response to substance	1
Methyl Methanesulfonate	increases expression	1
Nickel	increases expression	1
Silicon Dioxide	decreases expression	1
Tobacco Smoke Pollution	decreases expression	1
Tretinoin	increases expression	1
Valproic Acid	increases methylation	1

ChEMBL screening assays

12 unique, capped per target: 7 binding, 5 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3089343	Binding	Agonist activity at GPR132 (unknown origin) expressed in CHO-K1 cells at 10 uM after 90 to 180 mins by beta-arrestin assay relative to control	Identification of CB1/CB2 ligands from Zanthoxylum bungeanum. — J Nat Prod
CHEMBL5505148	Functional	Agonist activity at human G2A expressed in CHO-K1 cells co-expressing human GNA11 assessed as accumulation of IP-1 incubated for 90 mins by HTRF based FRET assay	Development of a Potent and Selective G2A (GPR132) Agonist. — J Med Chem

Cellosaurus cell lines

5 cell lines: 3 cancer cell line, 1 spontaneously immortalized cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B7XI	Abcam Raji GPR132 KO	Cancer cell line	Male
CVCL_B9Y7	Abcam THP-1 GPR132 KO	Cancer cell line	Male
CVCL_C7A1	Abcam PC-3 GPR132 KO	Cancer cell line	Male
CVCL_KX29	PathHunter CHO-K1 GPR132 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_XA27	GeneBLAzer T-REx-G2A-NFAT-bla FreeStyle 293F	Transformed cell line	Female

Clinical trials (associated diseases)

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