SUCNR1

Summary

SUCNR1 (succinate receptor 1, HGNC:4542) is a protein-coding gene on chromosome 3q25.1, encoding Succinate receptor 1 (Q9BXA5). G protein-coupled receptor for succinate able to mediate signaling through Gq/GNAQ or Gi/GNAI second messengers depending on the cell type and the processes regulated.

This gene encodes a G-protein-coupled receptor for succinate, an intermediate molecule of the citric acid cycle. It is involved in the promotion of hematopoietic progenitor cell development, and it has a potential role in renovascular hypertension which has known correlations to renal failure, diabetes and atherosclerosis.

Source: NCBI Gene 56670 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_033050

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:4542
Approved symbol	SUCNR1
Name	succinate receptor 1
Location	3q25.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000198829
Ensembl biotype	protein_coding
OMIM	606381
Entrez	56670

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000362032, ENST00000875328, ENST00000943239

RefSeq mRNA: 1 — MANE Select: NM_033050 NM_033050

CCDS: CCDS3162

Canonical transcript exons

ENST00000362032 — 3 exons

Exon	Start	End
ENSE00001131718	151880559	151884619
ENSE00001677218	151879852	151879907
ENSE00001710822	151873643	151873706

Expression profiles

Bgee: expression breadth ubiquitous, 144 present calls, max score 98.86.

FANTOM5 (CAGE): breadth broad, TPM avg 7.7670 / max 504.3291, expressed in 423 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
39246	7.7670	423

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
kidney epithelium	UBERON:0004819	98.86	gold quality
trabecular bone tissue	UBERON:0002483	84.93	gold quality
bone marrow	UBERON:0002371	82.93	gold quality
adult mammalian kidney	UBERON:0000082	80.82	gold quality
kidney	UBERON:0002113	78.97	gold quality
renal medulla	UBERON:0000362	78.75	gold quality
thyroid gland	UBERON:0002046	76.76	gold quality
left lobe of thyroid gland	UBERON:0001120	76.54	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	75.27	gold quality
right lobe of thyroid gland	UBERON:0001119	74.01	gold quality
bone marrow cell	CL:0002092	72.52	gold quality
cortex of kidney	UBERON:0001225	71.88	gold quality
vena cava	UBERON:0004087	69.75	silver quality
buccal mucosa cell	CL:0002336	69.06	gold quality
spleen	UBERON:0002106	68.86	gold quality
skin of hip	UBERON:0001554	68.20	gold quality
adult organism	UBERON:0007023	67.62	gold quality
monocyte	CL:0000576	67.41	gold quality
leukocyte	CL:0000738	66.95	gold quality
metanephros cortex	UBERON:0010533	66.52	gold quality
lymph node	UBERON:0000029	66.40	gold quality
parietal pleura	UBERON:0002400	65.51	gold quality
omental fat pad	UBERON:0010414	65.34	gold quality
peritoneum	UBERON:0002358	65.28	gold quality
adipose tissue of abdominal region	UBERON:0007808	64.55	gold quality
vermiform appendix	UBERON:0001154	64.21	gold quality
amniotic fluid	UBERON:0000173	63.29	gold quality
liver	UBERON:0002107	63.09	gold quality
islet of Langerhans	UBERON:0000006	62.97	gold quality
right lobe of liver	UBERON:0001114	62.44	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-CURD-114	yes	11.55
E-ANND-3	no	3.34

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

186 targeting SUCNR1, 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-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-6758-5P	100.00	66.21	1470
HSA-MIR-6856-5P	100.00	65.47	1298
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-LET-7A-3P	100.00	74.03	3932
HSA-LET-7B-3P	100.00	74.08	3913
HSA-LET-7F-1-3P	100.00	74.02	3928
HSA-MIR-98-3P	100.00	74.08	3907
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-507	99.97	70.11	1915
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-4725-3P	99.96	69.53	2520
HSA-MIR-6780B-5P	99.96	69.60	2562
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-557	99.96	70.01	1640
HSA-MIR-559	99.95	72.28	3609

Literature-anchored findings (GeneRIF, showing 29)

• GPR91 is a receptor for succinate and mediates succinate-induced hypertension. (PMID:15141213)
• This paper describes function in another species. (PMID:15141213)
• Succinate stimulates cell proliferation through GPR91 and requires activation of the Erk MAPK pathway. (PMID:19204147)
• A review of how neuron-derived factors, GPR91 and Semaphorin 3A, guide retinal vascularization and are major contributors to the pathogenesis of retinopathy of prematurity . (PMID:22497252)
• results show that GPR91 when expressed in HEK293s cells couples exclusively through the Galphai pathway and acts through Galphai not only to inhibit cAMP production but also to increase intracellular Ca(2+) (PMID:23770096)
• These findings suggest that deficiency in SUCNR1 is a possible contributing factor to the pathogenesis of dry age-related macular degeneration. (PMID:23833031)
• These results show for the first time that succinate plays an important role in cardiomyocyte hypertrophy through GPR91 activation and extend our understanding of how ischemia can induce hypertrophic cardiomyopathy (PMID:25539979)
• results show that succinate plays an important role in HSC activation through GPR91 induction, and suggest that succinate and GPR91 may represent new therapeutic targets for modulating hepatic fibrosis (PMID:26051274)
• Through GPR91, succinate is involved in functions such as regulation of blood pressure, inhibition of lipolysis in white adipose tissue, development of retinal vascularization and cardiac hypertrophy. [review] (PMID:26759054)
• We give an exhaustive overview of the known and hypothetical signaling partners of SUCNR1 in different in vitro and in vivo systems and also discuss the link between SUCNR1 intracellular pathways and its pathophysiological roles. (PMID:26808164)
• The findings indicate that succinate-GPR91 signaling may be involved in right ventricular hypertrophy via PI3K/Akt signaling in vivo and in vitro. (PMID:26824665)
• Succinate is abundant in synovial fluids from rheumatoid arthritis (RA) patients, and these fluids elicit IL-1beta release from macrophages in a GPR91-dependent manner. (PMID:27481132)
• This study reports the expression of GPR91 on mouse and human mast cells and reveals a hyperactive behavior of mouse Sucnr1-/- mast cells in a mechanistic in vivo model of skin inflammation. (PMID:27527650)
• Data show that succinate upregulates vascular endothelial growth factor (VEGF) expression by activation of signal transducer and activator of transcription 3 (STAT3) and extracellular regulated kinase (ERK)1/2 via its receptor G-protein coupled receptor 91 (GPR91). (PMID:28061458)
• activation of SUCNR1 in macrophages is important for both infiltration and inflammation of adipose tissue in obesity (PMID:28382382)
• succinate promotes DRP1-mediated mitochondrial fission via GPR91, consequently stimulating the hMSC migration through mtROS-induced F-actin formation. (PMID:28974722)
• This study shows that metformin can attenuate activation of HSCs by activating the AMPK pathway and inhibiting the succinate-GPR91 pathway. Metformin has therapeutic potential for treating steatohepatitis and liver fibrosis. (PMID:29278707)
• Study demonstrates that the T allele of rs13079080 in SUCNR1 disrupts a binding site for miRNA-4470, potentially increasing SUCNR1 expression and consequently increasing the capacity of sensing and dealing with oxidative stress. Also, genotyping rs13079080 in an AMD case-control cohort revealed a protective effect of the TT genotype on age-related macular degeneration (AMD) compared to the CC genotype. (PMID:31304868)
• These effects are mediated by SUCNR1-triggered PI3K-hypoxia-inducible factor 1alpha (HIF-1alpha) axis. (PMID:31735641)
• Inhibition of GPR91 Reduces Inflammatory Mediators Involved in Active Labor in Myometrium. (PMID:32377163)
• pH-Gated Succinate Secretion Regulates Muscle Remodeling in Response to Exercise. (PMID:32946811)
• GPR91 Receptor Mediates Protection against Doxorubicin-Induced Cardiotoxicity without Altering Its Anticancer Efficacy. An In Vitro Study on H9C2 Cardiomyoblasts and Breast Cancer-Derived MCF-7 Cells. (PMID:32992522)
• Associations of SUCNR1, GRK4, CAMK1D gene polymorphisms and the susceptibility of type 2 diabetes mellitus and essential hypertension in a northern Chinese Han population. (PMID:33127268)
• Succinate Mediates Tumorigenic Effects via Succinate Receptor 1: Potential for New Targeted Treatment Strategies in Succinate Dehydrogenase Deficient Paragangliomas. (PMID:33776908)
• Extracellular succinate hyperpolarizes M2 macrophages through SUCNR1/GPR91-mediated Gq signaling. (PMID:34133934)
• SUCNR1 Is Expressed in Human Placenta and Mediates Angiogenesis: Significance in Gestational Diabetes. (PMID:34769478)
• Succinate receptor 1 inhibits mitochondrial respiration in cancer cells addicted to glutamine. (PMID:34813893)
• Human umbilical cord mesenchymal stem cell-derived exosomes carrying miR-1827 downregulate SUCNR1 to inhibit macrophage M2 polarization and prevent colorectal liver metastasis. (PMID:36652132)
• Protective effects of the succinate/SUCNR1 axis on damaged hepatocytes in NAFLD. (PMID:37315889)

Cross-species orthologs

2 orthologs

Organism	Symbol	Gene ID
mus_musculus	Sucnr1	ENSMUSG00000027762
rattus_norvegicus	Sucnr1	ENSRNOG00000014039

Paralogs (15): GPR31 (ENSG00000120436), GPR42 (ENSG00000126251), FFAR2 (ENSG00000126262), FFAR1 (ENSG00000126266), OXER1 (ENSG00000162881), OXGR1 (ENSG00000165621), P2RY1 (ENSG00000169860), P2RY6 (ENSG00000171631), GPR82 (ENSG00000171657), P2RY2 (ENSG00000175591), HCAR2 (ENSG00000182782), FFAR3 (ENSG00000185897), P2RY4 (ENSG00000186912), HCAR1 (ENSG00000196917), HCAR3 (ENSG00000255398)

Protein

Protein identifiers

Succinate receptor 1 — Q9BXA5 (reviewed: Q9BXA5)

Alternative names: G-protein coupled receptor 91, P2Y purinoceptor 1-like

All UniProt accessions (1): Q9BXA5

UniProt curated annotations — full annotation on UniProt →

Function. G protein-coupled receptor for succinate able to mediate signaling through Gq/GNAQ or Gi/GNAI second messengers depending on the cell type and the processes regulated. Succinate-SUCNR1 signaling serves as a link between metabolic stress, inflammation and energy homeostasis. In macrophages, plays a range of immune-regulatory roles. During inflammation, succinate-SUCNR1 signaling may act as an anti-inflammatory mediator or boost inflammation depending on the inflammatory status of cells. Hyperpolarizes M2 macrophages versus M1 phenotype through Gq signaling by regulating the transcription of genes involved in immune function. In activated M1 macrophages, plays a pro-inflammatory role in response to LPS. Expressed in dendritic cells, where it is involved in the sensing of immunological danger and enhances immunity. Mediates succinate triggered intracelleular calcium mobilization, induces migratory responses and acts in synergy with Toll-like receptor ligands for the production of proinflammatory cytokines as well as an enhancement of antigen-specific activation of helper T cells. In the small intestine, mediates the activation of tuft cells by dietary succinate and triggers type 2 immunity. In adipocytes, plays an important role in the control of energy metabolism. In response to succinate, controls leptin expression in an AMPK-JNK-CEBPA-dependent as well as circadian clock-regulated manner. In muscle tissue, is expressed in non-muscle cells and coordinates muscle remodeling in response to the succinate produced during exercise training in a paracrine manner. In retina, acts as a mediator of vessel growth during retinal development. In response to succinate, regulates the production of angiogenic factors, including VEGF, by retinal ganglion neurons.

Subcellular location. Cell membrane.

Tissue specificity. Expressed specifically in kidney. Highly expressed in immature dendritic cells, expression rapidly downregulates after maturation. Also expressed in macrophages.

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

RefSeq proteins (1): NP_149039* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (47 total): helix 13, topological domain 8, transmembrane region 7, mutagenesis site 7, strand 5, turn 3, glycosylation site 2, chain 1, disulfide bond 1

Structure

Experimental structures (PDB)

7 structures.

PDB	Method	Resolution (Å)
8YKV	ELECTRON MICROSCOPY	2.48
8YKX	ELECTRON MICROSCOPY	2.69
8YKW	ELECTRON MICROSCOPY	2.75
8JPN	ELECTRON MICROSCOPY	2.9
8WOG	ELECTRON MICROSCOPY	2.97
8WP1	ELECTRON MICROSCOPY	3.15
8JPP	ELECTRON MICROSCOPY	3.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9BXA5-F1	87.70	0.57

Antibody-complex structures (SAbDab): 4 — 8JPN, 8YKV, 8YKW, 8YKX

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): 95–172

Glycosylation sites (2): 8, 168

Mutagenesis-validated functional residues (7):

Position	Phenotype
99	abolishes activation by succinate.
103	abolishes activation by succinate.
107	no effect on receptor function.
249	no effect on receptor function.
252	abolishes activation by succinate.
255	no effect on receptor function.
281	abolishes activation by succinate.

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

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

MSigDB gene sets: 156 (showing top): GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE_BY_CIRCULATORY_RENIN_ANGIOTENSIN, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_CIRCULATORY_SYSTEM_PROCESS, GOBP_INFLAMMATORY_RESPONSE, GOBP_MACROPHAGE_ACTIVATION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_REGULATION_OF_SYSTEMIC_ARTERIAL_BLOOD_PRESSURE, GOBP_CELL_CELL_SIGNALING, GOBP_RESPONSE_TO_METAL_ION, GOBP_CELL_ACTIVATION_INVOLVED_IN_IMMUNE_RESPONSE, GOBP_POSITIVE_REGULATION_OF_RESPONSE_TO_EXTERNAL_STIMULUS, GOBP_TAXIS, GOBP_MYELOID_LEUKOCYTE_ACTIVATION, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, GOBP_MACROPHAGE_ACTIVATION, GOBP_SECRETION

GO Biological Process (10): renin secretion into blood stream (GO:0002001), macrophage activation involved in immune response (GO:0002281), G protein-coupled receptor signaling pathway (GO:0007186), glucose homeostasis (GO:0042593), positive regulation of inflammatory response (GO:0050729), positive regulation of chemotaxis (GO:0050921), response to calcium ion (GO:0051592), regulation of angiotensin metabolic process (GO:0060177), energy homeostasis (GO:0097009), signal transduction (GO:0007165)

GO Molecular Function (3): G protein-coupled receptor activity (GO:0004930), signaling receptor activity (GO:0038023), protein binding (GO:0005515)

GO Cellular Component (3): plasma membrane (GO:0005886), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Signaling by GPCR	2
GPCR ligand binding	1
GPCR downstream signalling	1
Signal Transduction	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
positive regulation of response to external stimulus	2
renal response to blood flow involved in circulatory renin-angiotensin regulation of systemic arterial blood pressure	1
protein secretion	1
signal release	1
myeloid cell activation involved in immune response	1
leukocyte activation involved in immune response	1
immune response	1
macrophage activation	1
G protein-coupled receptor activity	1
signal transduction	1
carbohydrate homeostasis	1
inflammatory response	1
positive regulation of defense response	1
regulation of inflammatory response	1
chemotaxis	1
positive regulation of locomotion	1
regulation of chemotaxis	1
response to metal ion	1
regulation of protein metabolic process	1
multicellular organismal-level homeostasis	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
transmembrane signaling receptor activity	1
G protein-coupled receptor signaling pathway	1
molecular transducer activity	1
binding	1
membrane	1
cell periphery	1
extracellular vesicle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

724 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SUCNR1	REN	P00797	710
SUCNR1	ALDH18A1	P54886	541
SUCNR1	HIF1A	Q16665	507
SUCNR1	AKT1	P31749	492
SUCNR1	TRPM5	Q9NZQ8	471
SUCNR1	FFAR3	O14843	454
SUCNR1	ACOD1	A6NK06	446
SUCNR1	FFAR2	O15552	425
SUCNR1	HCAR2	Q8TDS4	419
SUCNR1	TAS1R1	Q7RTX1	416
SUCNR1	POU2F3	Q9UKI9	406
SUCNR1	TAS1R3	Q7RTX0	398
SUCNR1	SLC13A3	Q8WWT9	395
SUCNR1	ALDH3B1	P43353	387
SUCNR1	GORAB	Q5T7V8	385

IntAct

13 interactions, top by confidence:

A	B	Type	Score
SUCNR1	TMEM14B	psi-mi:“MI:0915”(physical association)	0.560
SUCNR1	LAMP2	psi-mi:“MI:0915”(physical association)	0.560
SUCNR1	SH3GLB1	psi-mi:“MI:0915”(physical association)	0.560
SUCNR1	PRMT8	psi-mi:“MI:0915”(physical association)	0.400
RAMP1	SUCNR1	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	SUCNR1	psi-mi:“MI:0915”(physical association)	0.400
SUCNR1	TMEM14B	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (3): MTCH2 (Affinity Capture-MS), SUCNR1 (Two-hybrid), PRMT8 (Affinity Capture-MS)

ESM2 similar proteins: A1A5S3, A5PLE7, B0UXR0, B5X337, F5HDK1, F5HF62, F8VQN3, O00421, O18982, O97663, P09703, P32249, P35351, P35374, P46002, P49685, P50052, P51676, P56412, P69332, P69333, Q01035, Q0II78, Q0VDU3, Q14330, Q1RMI1, Q28929, Q3T0E9, Q3U507, Q4R613, Q6IYF9, Q75ZH0, Q83207, Q89609, Q8BZR0, Q8IYL9, Q8K1Z6, Q95N03, Q96P67, Q98146

Diamond homologs: A0T2N3, A5PLE7, B0UXR0, B5X337, O00155, O00254, O00398, O08675, O18951, O35811, O88410, O93361, P26824, P28646, P30872, P30873, P30937, P31391, P32250, P32300, P32302, P32303, P33533, P33534, P33535, P34975, P34996, P34997, P35346, P35372, P35373, P35383, P41231, P41232, P42866, P43657, P47749, P47900, P48042, P49650

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

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

Top pathogenic / likely-pathogenic (0)

SpliceAI

479 predictions. Top by Δscore:

Variant	Effect	Δscore
3:151873702:GAATG:G	donor_gain	1.0000
3:151879846:TTCTA:T	acceptor_loss	1.0000
3:151879847:TCTA:T	acceptor_loss	1.0000
3:151879848:CTA:C	acceptor_loss	1.0000
3:151879850:A:AG	acceptor_gain	1.0000
3:151879851:G:A	acceptor_loss	1.0000
3:151879851:G:GG	acceptor_gain	1.0000
3:151880713:GCA:G	donor_gain	1.0000
3:151873707:G:GG	donor_gain	0.9900
3:151873707:G:T	donor_loss	0.9900
3:151873708:T:TC	donor_loss	0.9900
3:151879851:GGTT:G	acceptor_gain	0.9900
3:151879906:TGGT:T	donor_loss	0.9900
3:151879907:GGTAT:G	donor_loss	0.9900
3:151879908:G:GG	donor_gain	0.9900
3:151879909:T:G	donor_loss	0.9900
3:151880553:CTTTA:C	acceptor_loss	0.9900
3:151880554:TTTA:T	acceptor_loss	0.9900
3:151880555:TTAG:T	acceptor_loss	0.9900
3:151880556:TAGG:T	acceptor_loss	0.9900
3:151880557:A:AG	acceptor_gain	0.9900
3:151880557:AGG:A	acceptor_loss	0.9900
3:151880558:G:A	acceptor_loss	0.9900
3:151880558:G:GG	acceptor_gain	0.9900
3:151880558:GGC:G	acceptor_gain	0.9900
3:151880558:GGCAT:G	acceptor_gain	0.9900
3:151880716:G:GG	donor_gain	0.9900
3:151879851:GGTTA:G	acceptor_gain	0.9700
3:151879932:A:G	donor_gain	0.9600
3:151880557:AG:A	acceptor_gain	0.9600

AlphaMissense

2206 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:151880892:A:C	S117R	0.998
3:151880894:C:A	S117R	0.998
3:151880894:C:G	S117R	0.998
3:151880902:G:C	R120P	0.997
3:151881298:G:C	R252P	0.997
3:151880868:A:C	S109R	0.996
3:151880870:C:A	S109R	0.996
3:151880870:C:G	S109R	0.996
3:151880737:T:C	L65P	0.994
3:151880982:T:A	W147R	0.994
3:151880982:T:C	W147R	0.994
3:151880652:G:A	G37R	0.993
3:151880652:G:C	G37R	0.993
3:151880839:G:C	R99P	0.993
3:151881105:A:C	S188R	0.993
3:151881107:C:A	S188R	0.993
3:151881107:C:G	S188R	0.993
3:151881405:A:C	S288R	0.993
3:151881407:T:A	S288R	0.993
3:151881407:T:G	S288R	0.993
3:151880653:G:A	G37E	0.992
3:151880735:C:A	N64K	0.992
3:151880735:C:G	N64K	0.992
3:151881057:T:A	C172S	0.992
3:151881058:G:C	C172S	0.992
3:151881129:T:C	F196L	0.991
3:151881131:C:A	F196L	0.991
3:151881131:C:G	F196L	0.991
3:151881264:T:C	F241L	0.991
3:151881266:C:A	F241L	0.991

dbSNP variants (sampled 300 via entrez): RS1000034320 (3:151879511 C>T), RS1000490987 (3:151879787 T>A,C), RS1001095406 (3:151878505 GA>G,GAA), RS1001127932 (3:151875595 A>G), RS1001160294 (3:151879222 G>A), RS1001443378 (3:151878132 G>C), RS1001655536 (3:151882336 G>A), RS1001707758 (3:151871681 A>G), RS1001765584 (3:151875362 C>T), RS1001784682 (3:151882824 T>C,G), RS1002021768 (3:151881135 A>G), RS1002113759 (3:151873420 G>T), RS1002156252 (3:151877318 G>C), RS1002803326 (3:151884450 A>T), RS1002816053 (3:151873860 A>G)

Disease associations

OMIM: gene MIM:606381 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST000763_8	Immunoglobulin A	3.000000e-06
GCST003983_10	Male-pattern baldness	5.000000e-19
GCST006661_125	Male-pattern baldness	3.000000e-15
GCST006661_292	Male-pattern baldness	1.000000e-10
GCST008460_10	Gout vs. Hyperuricemia	1.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004747	protein measurement
EFO:0009104	hyperuricemia

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2150838 (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: 1,121,639 (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
CHEMBL576	SUCCINIC ACID	3	1,121,639

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Succinate receptor

Most potent curated ligand interactions (12 total), top 12:

Ligand	Action	Affinity	Parameter
compound 31 [PMID: 29968758]	Partial agonist	7.64	pEC50
compound 4c [PMID: 21571530]	Antagonist	7.52	pIC50
NF-56-EJ40	Antagonist	7.48	pKd
compound 5g [PMID: 21571530]	Antagonist	7.46	pIC50
compound 7e [PMID: 21571530]	Antagonist	6.74	pIC50
compound 130 [PMID: 29157600]	Partial agonist	5.65	pEC50
cis-epoxysuccinic acid	Full agonist	5.57	pEC50
succinic acid	Full agonist	4.7	pEC50
cis-1,2-cyclopropanedicarboxylic acid	Full agonist	4.31	pEC50
maleic acid	Agonist	4.2	pEC50
(S)-chlorosuccinic acid	Full agonist	4.14	pEC50
methylmalonic acid	Full agonist	3.55	pEC50

ChEMBL bioactivities

118 potent at pChembl≥5 of 126 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.15	IC50	7	nM	CHEMBL2153461
7.96	IC50	11	nM	CHEMBL2153446
7.85	IC50	14	nM	CHEMBL2153465
7.80	IC50	16	nM	CHEMBL2153445
7.80	IC50	16	nM	CHEMBL2153468
7.80	Ki	15.85	nM	CHEMBL4781545
7.77	IC50	17	nM	CHEMBL2153462
7.75	IC50	18	nM	CHEMBL2153467
7.72	IC50	19	nM	CHEMBL2153466
7.66	IC50	22	nM	CHEMBL2153441
7.60	IC50	25	nM	CHEMBL4790324
7.60	Ki	25.12	nM	CHEMBL4781545
7.52	IC50	30	nM	CHEMBL2153439
7.51	IC50	31	nM	CHEMBL2153459
7.50	Ki	31.62	nM	CHEMBL5432512
7.48	IC50	33.11	nM	CHEMBL5432512
7.47	IC50	34	nM	CHEMBL2153463
7.46	IC50	35	nM	CHEMBL2153581
7.44	EC50	36.31	nM	CHEMBL5412414
7.43	EC50	37.15	nM	CHEMBL5430997
7.42	IC50	38	nM	CHEMBL2153442
7.40	IC50	40	nM	CHEMBL2153440
7.40	IC50	40	nM	CHEMBL2153586
7.40	Ki	39.81	nM	CHEMBL4790324
7.40	Ki	39.81	nM	CHEMBL5432512
7.40	Ki	39.81	nM	CHEMBL5426854
7.39	IC50	41	nM	CHEMBL2153443
7.31	IC50	49	nM	CHEMBL2153469
7.30	Ki	50.12	nM	CHEMBL5426854
7.26	IC50	54.95	nM	CHEMBL5426854
7.26	IC50	54.95	nM	CHEMBL5399663
7.24	IC50	57.54	nM	CHEMBL5403855
7.21	IC50	61.66	nM	CHEMBL5422075
7.19	IC50	65	nM	CHEMBL2153444
7.19	IC50	65	nM	CHEMBL2153579
7.12	IC50	75	nM	CHEMBL2153460
7.12	IC50	76	nM	CHEMBL4763307
7.10	Ki	79.43	nM	CHEMBL4790324
7.07	IC50	85.11	nM	CHEMBL4790324
7.06	IC50	88	nM	CHEMBL4751488
7.05	IC50	90	nM	CHEMBL2153580
7.05	IC50	90	nM	CHEMBL4757124
7.04	IC50	92	nM	CHEMBL4752851
7.02	EC50	95.5	nM	CHEMBL5399023
7.02	IC50	95.5	nM	CHEMBL5426931
7.00	IC50	100	nM	CHEMBL2153587
6.97	EC50	107.2	nM	CHEMBL5425930
6.96	EC50	109.7	nM	CHEMBL5405388
6.91	IC50	123	nM	CHEMBL5404924
6.85	IC50	140	nM	CHEMBL4791540

PubChem BioAssay actives

118 with measured affinity, of 184 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
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0070	uM
N-[(1S)-1-[4-(3-chlorophenyl)phenyl]ethyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0110	uM
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-methyl-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0140	uM
2-[2-[[3-(4-chlorophenyl)benzoyl]amino]phenyl]acetic acid	1981504: Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ki	0.0158	uM
4-(1,8-naphthyridin-2-yl)-N-[1-[4-[3-(trifluoromethyl)phenyl]phenyl]ethyl]butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0160	uM
3,3,3-trifluoro-N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-hydroxy-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0160	uM
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-methyl-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0170	uM
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-hydroxy-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0180	uM
2,2-difluoro-N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0190	uM
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0220	uM
2-[2-[[3-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]benzoyl]amino]phenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.0250	uM
N-[[4-(3-methylphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0300	uM
N-[[4-(3-chloro-4-fluorophenyl)phenyl]methyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0310	uM
2-[2-[[3-(4-chloro-2-methylphenyl)benzoyl]amino]phenyl]acetic acid	1981507: Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2465 by BRET assay	ki	0.0316	uM
3,3,3-trifluoro-N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-hydroxy-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0340	uM
N-[[3-[4-fluoro-3-(trifluoromethyl)phenyl]-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0350	uM
(2S)-2-[[5-[4-(6-aminohexoxy)phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.0363	uM
(2S)-2-[[6-[4-(trifluoromethoxy)phenyl]pyridine-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.0372	uM
N-[[4-(3-chloro-4-fluorophenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0380	uM
2-[2-[[3-[2-methyl-4-[(4-methylpiperazin-1-yl)methyl]phenyl]benzoyl]amino]phenyl]acetic acid	1981504: Competitive binding affinity to N-terminal Nluc-tagged human succinate receptor 1 expressed in Flp-In-T-REx-293 cells assessed as inhibition constant incubated for 5 mins in the presence of TUG-2384 by BRET assay	ki	0.0398	uM
2-[4-(3-chlorophenyl)phenyl]-5-[3-(1,8-naphthyridin-2-yl)propyl]-1,3,4-oxadiazole	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0400	uM
N-[[4-(3-chlorophenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0400	uM
N-[[2-fluoro-4-[3-(trifluoromethyl)phenyl]phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0410	uM
N-[[2-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidin-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0490	uM
2-[2-[[3-[2-methyl-4-[[4-[2-[(4-nitro-4,7-dihydro-2,1,3-benzoxadiazol-7-yl)amino]ethyl]piperazin-1-yl]methyl]phenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.0549	uM
2-[2-[[3-[4-(3-aminopropoxy)-2-methylphenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.0575	uM
2-[2-[[3-[4-(5-aminopentoxy)-2-methylphenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.0617	uM
N-[[3-(3-chlorophenyl)-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0650	uM
N-[[4-(3-ethylphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0650	uM
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0750	uM
2-[2-[[3-[4-chloro-2-fluoro-3-[(3R)-piperidin-3-yl]oxyphenyl]benzoyl]amino]phenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.0760	uM
2-[2-[[3-[4-chloro-2-fluoro-5-[(3R)-piperidin-3-yl]oxyphenyl]-2-fluorobenzoyl]amino]-5-fluorophenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.0880	uM
2-[2-[[3-[4-chloro-2-fluoro-5-[(3R)-piperidin-3-yl]oxyphenyl]benzoyl]amino]-5-fluorophenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.0900	uM
N-[[3-(3-chloro-4-fluorophenyl)-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.0900	uM
2-[2-[[3-[4-chloro-2-fluoro-3-[(3R)-piperidin-3-yl]oxyphenyl]benzoyl]amino]-5-fluorophenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.0920	uM
(2S)-2-[[5-[4-(3-aminopropoxy)phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.0955	uM
2-[2-[[3-[2-methyl-4-[[4-[2-[(2-methylpropan-2-yl)oxycarbonylamino]ethyl]piperazin-1-yl]methyl]phenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.0955	uM
2-[4-(3-chloro-4-fluorophenyl)phenyl]-5-[3-(1,8-naphthyridin-2-yl)propyl]-1,3,4-oxadiazole	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.1000	uM
(2S)-2-[[5-[4-[6-[2-[(2-methylpropan-2-yl)oxycarbonylamino]ethylamino]hexoxy]phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.1071	uM
(2S)-2-[[5-[4-(4-aminobutoxy)phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.1096	uM
2-[2-[[3-[4-(6-aminohexoxy)phenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.1230	uM
2-[2-[[3-(4-chloro-3-piperidin-4-yloxyphenyl)benzoyl]amino]phenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.1400	uM
2-[2-[[3-(4-chloro-3-pyrrolidin-3-yloxyphenyl)benzoyl]amino]phenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.1400	uM
2-[2-[[3-[3-(azetidin-3-yloxy)-4-chlorophenyl]benzoyl]amino]phenyl]acetic acid	1724287: Antagonist activity at human SUCNR1 expressed in human CHEM1 cells incubated for 60 mins in presence of [35S]GTPgammaS by scintillation proximity assay	ic50	0.1400	uM
(2S)-2-[[5-[4-[6-[2-[(4-nitro-2,1,3-benzoxadiazol-7-yl)amino]ethylamino]hexoxy]phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.1445	uM
(2S)-2-[[5-[4-(5-aminopentoxy)phenyl]furan-2-carbonyl]amino]butanedioic acid	1981471: Agonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of forskolin-induced cAMP production incubated for 30 mins by TR-FRET analysis	ec50	0.1479	uM
2-[2-[[3-[4-[[4-[2-[(2-methylpropan-2-yl)oxycarbonylamino]ethyl]piperazin-1-yl]methyl]phenyl]benzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.1514	uM
2-[4-chloro-3-(trifluoromethyl)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.1600	uM
2-[2-[[3-(4-chlorophenyl)-4-methylbenzoyl]amino]phenyl]acetic acid	1981475: Antagonist activity at human succinate receptor 1 expressed in human Flp-In-T-REx-293 cells assessed as inhibition of succinate response by cAMP assay	ic50	0.1660	uM
2-[3,4-bis(trifluoromethyl)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole	692076: Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay	ic50	0.1700	uM

CTD chemical–gene interactions

27 total (human), top 27 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, increases expression	3
GSK-J4	increases expression	1
lasiocarpine	decreases expression	1
methyleugenol	decreases expression	1
propionaldehyde	increases expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
trichostatin A	increases expression	1
mono-(2-ethylhexyl)phthalate	increases abundance, increases methylation	1
sulforaphane	increases expression	1
S-(1,2-dichlorovinyl)cysteine	affects cotreatment, decreases expression, affects response to substance, increases expression	1
pentanal	increases expression	1
gardiquimod	decreases reaction, increases expression	1
PCI 5002	affects cotreatment, increases expression	1
Zoledronic Acid	decreases expression	1
Benzo(a)pyrene	decreases expression	1
Carbamazepine	affects expression	1
Cisplatin	increases expression	1
Diethylhexyl Phthalate	increases abundance, increases methylation	1
Lipopolysaccharides	decreases expression, affects response to substance, increases expression, affects cotreatment	1
Nickel	increases expression	1
Silicon Dioxide	affects expression	1
Tretinoin	increases expression	1
Zinc	increases expression, affects cotreatment	1
Aflatoxin B1	decreases expression	1
Okadaic Acid	decreases expression	1
Copper Sulfate	decreases expression	1
Protein Kinase Inhibitors	decreases reaction, increases expression	1

ChEMBL screening assays

23 unique, capped per target: 12 binding, 11 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2155422	Functional	Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level at 10 uM by FLIPR assay	Discovery of a potent and selective small molecule hGPR91 antagonist. — Bioorg Med Chem Lett
CHEMBL4883603	Binding	PRESTO-Tango GPCRome screening (SUCNR1)	Data for DCP probe UCSF924

Cellosaurus cell lines

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

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

Cellosaurus	Name	Category	Sex
CVCL_D8WP	Ubigene HCT 116 SUCNR1 KO	Cancer cell line	Male
CVCL_H504	CHO-K1/SUCNR1/Galpha15	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

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