General Information of the Protein
Protein ID
PT06274
Protein Name
Succinate receptor 1
Secondarily
Protein Name
G-protein coupled receptor 91
P2Y purinoceptor 1-like
Gene Name
SUCNR1
Secondarily
Gene Name
GPR91
Sequence
MLGIMAWNATCKNWLAAEAALEKYYLSIFYGIEFVVGVLGNTIVVYGYIFSLKNWNSSNIYLFNLSVSDLAFLCTLPMLIRSYANGNWIYGDVLCISNRYVLHANLYTSILFLTFISIDRYLIIKYPFREHLLQKKEFAILISLAIWVLVTLELLPILPLINPVITDNGTTCNDFASSGDPNYNLIYSMCLTLLGFLIPLFVMCFFYYKIALFLKQRNRQVATALPLEKPLNLVIMAVVIFSVLFTPYHVMRNVRIASRLGSWKQYQCTQVVINSFYIVTRPLAFLNSVINPVFYFLLGDHFRDMLMNQLRHNFKSLTSFSRWAHELLLSFREK
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Small molecule receptor (family A GPCR)
>
Carboxylic acid receptor
>
Succinate receptor
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 (By similarity) (PubMed:15141213, PubMed:34133934, PubMed:23770096). Succinate-SUCNR1 signaling serves as a link between metabolic stress, inflammation and energy homeostasis (PubMed:18820681, PubMed:34133934). 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 (By similarity). Hyperpolarizes M2 macrophages versus M1 phenotype through Gq signaling by regulating the transcription of genes involoved in immune function (PubMed:34133934). In activated M1 macrophages, plays a pro-inflammatory role in response to LPS (By similarity). 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 (PubMed:18820681). In the small intestine, mediates the activation of tuft cells by dietary succinate and triggers type 2 immunity (By similarity). 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 (By similarity). 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 (By similarity). 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 (By similarity).
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Uniprot ID
Primary ID:
Q9BXA5

Secondarily ID:
A8K305
Q8TDQ8
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Ensembl ID
ENSG00000198829
HGNC ID
HGNC:4542
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0481690
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C31H23F4N3O
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0446824
N-[(1S)-1-[4-(3-chlorophenyl)phenyl]ethyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H24ClN3O
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0453891
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-methyl-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide
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C33H27F4N3O
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0381392
4-(1,8-naphthyridin-2-yl)-N-[1-[4-[3-(trifluoromethyl)phenyl]phenyl]ethyl]butanamide
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C27H24F3N3O
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0517994
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
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C32H22F7N3O2
 1
1
IC50 = 16 nM
   TI
   LI
   LO
   TS
CP0508186
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-methyl-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide
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C32H25F4N3O
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0534545
N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-hydroxy-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C31H23F4N3O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0499875
2,2-difluoro-N-[(1S)-1-[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]ethyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C31H21F6N3O
 1
1
IC50 = 19 nM
   TI
   LI
   LO
   TS
CP0512222
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H21F4N3O
 1
1
IC50 = 22 nM
   TI
   LI
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   TS
CP0455192
N-[[4-(3-methylphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H25N3O
 1
1
IC50 = 30 nM
   TI
   LI
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   TS
CP0516152
N-[[4-(3-chloro-4-fluorophenyl)phenyl]methyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C29H21ClFN3O
 1
1
IC50 = 31 nM
   TI
   LI
   LO
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CP0413768
3,3,3-trifluoro-N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-hydroxy-2-[4-(1,8-naphthyridin-2-yl)phenyl]propanamide
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C31H20F7N3O2
 1
1
IC50 = 34 nM
   TI
   LI
   LO
   TS
CP0498295
N-[[3-[4-fluoro-3-(trifluoromethyl)phenyl]-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C23H18F4N4O2
 1
1
IC50 = 35 nM
   TI
   LI
   LO
   TS
CP0507080
N-[[4-(3-chloro-4-fluorophenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C25H21ClFN3O
 1
1
IC50 = 38 nM
   TI
   LI
   LO
   TS
CP0381391
N-[[4-(3-chlorophenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C25H22ClN3O
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0456687
2-[4-(3-chlorophenyl)phenyl]-5-[3-(1,8-naphthyridin-2-yl)propyl]-1,3,4-oxadiazole
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C25H19ClN4O
 1
1
IC50 = 40 nM
   TI
   LI
   LO
   TS
CP0512223
N-[[2-fluoro-4-[3-(trifluoromethyl)phenyl]phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H21F4N3O
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0435902
N-[[2-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidin-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C24H19F4N5O
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0449448
N-[[3-(3-chlorophenyl)-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H19ClN4O2
 1
1
IC50 = 65 nM
   TI
   LI
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CP0525082
N-[[4-(3-ethylphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C27H27N3O
 1
1
IC50 = 65 nM
   TI
   LI
   LO
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CP0535905
N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C30H21F4N3O
 1
1
IC50 = 75 nM
   TI
   LI
   LO
   TS
CP0517995
N-[[3-(3-chloro-4-fluorophenyl)-1,2-oxazol-5-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H18ClFN4O2
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0553492
2-[4-(3-chloro-4-fluorophenyl)phenyl]-5-[3-(1,8-naphthyridin-2-yl)propyl]-1,3,4-oxadiazole
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C25H18ClFN4O
 1
1
IC50 = 100 nM
   TI
   LI
   LO
   TS
CP0446345
2-[4-chloro-3-(trifluoromethyl)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C21H16ClF3N4O
 1
1
IC50 = 160 nM
   TI
   LI
   LO
   TS
CP0517996
2-[3,4-bis(trifluoromethyl)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C22H16F6N4O
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0426059
2-[3-chloro-4-(trifluoromethoxy)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C21H16ClF3N4O2
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0426058
2-[3-(1,8-naphthyridin-2-yl)propyl]-5-[4-[3-(trifluoromethyl)phenyl]phenyl]-1,3,4-oxadiazole
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C26H19F3N4O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0499479
N-[[5-[4-fluoro-3-(trifluoromethyl)phenyl]pyrimidin-2-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C24H19F4N5O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0449447
N-[[1-[4-fluoro-3-(trifluoromethyl)phenyl]pyrazol-4-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C23H19F4N5O
 1
1
IC50 = 210 nM
   TI
   LI
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CP0462857
N-[[5-[4-fluoro-3-(trifluoromethyl)phenyl]-1,3,4-thiadiazol-2-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H17F4N5OS
 1
1
IC50 = 270 nM
   TI
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CP0486967
N-[[4-(4-chloro-3-methylphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H24ClN3O
 1
1
IC50 = 300 nM
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   LI
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CP0513868
N-[[4-(3-chlorophenyl)-1,3-thiazol-2-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H19ClN4OS
 1
1
IC50 = 300 nM
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CP0534544
2-amino-N-[[4-[4-fluoro-3-(trifluoromethyl)phenyl]phenyl]methyl]-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
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C30H22F4N4O
 1
1
IC50 = 330 nM
   TI
   LI
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CP0535904
4-(1,8-naphthyridin-2-yl)-N-[[4-[3-(trifluoromethoxy)phenyl]phenyl]methyl]butanamide
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C26H22F3N3O2
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0515722
N-[[2-(3-chlorophenyl)-1,3-thiazol-4-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H19ClN4OS
 1
1
IC50 = 700 nM
   TI
   LI
   LO
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CP0435903
N-[[6-[4-fluoro-3-(trifluoromethyl)phenyl]pyridazin-3-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C24H19F4N5O
 1
1
IC50 = 720 nM
   TI
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CP0493491
methyl 2-fluoro-6-[3-fluoro-4-[[4-(1,8-naphthyridin-2-yl)butanoylamino]methyl]phenyl]benzoate
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C27H23F2N3O3
 1
1
IC50 = 800 nM
   TI
   LI
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CP0446825
4-(1,8-naphthyridin-2-yl)-N-[(4-phenylphenyl)methyl]butanamide
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C25H23N3O
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
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CP0493492
N-[[4-(3-methoxyphenyl)phenyl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C26H25N3O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0523642
N-[[5-[4-fluoro-3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]methyl]-4-(1,8-naphthyridin-2-yl)butanamide
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C22H17F4N5O2
 1
1
IC50 = 1000 nM
   TI
   LI
   LO
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CP0523643
2-[3-[3-[4-(3-chloro-4-fluorophenyl)phenyl]-1H-1,2,4-triazol-5-yl]propyl]-1,8-naphthyridine
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C25H19ClFN5
 1
1
IC50 = 1000 nM
   TI
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   LO
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CP0553493
2-[4-fluoro-3-(trifluoromethyl)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C21H16F4N4O
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
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CP0435904
2-[4-(3-chlorophenyl)phenyl]-5-[3-(1,8-naphthyridin-2-yl)propyl]-1,3,4-thiadiazole
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C25H19ClN4S
 1
1
IC50 = 3000 nM
   TI
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CP0446344
2-[4-(1,8-naphthyridin-2-yl)butyl]-5-[4-(trifluoromethoxy)phenyl]-1,3,4-oxadiazole
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C21H17F3N4O2
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0523644
2-[4-(1,8-naphthyridin-2-yl)butyl]-5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazole
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C21H17F3N4O
 1
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
CP0523645
2-[4-fluoro-3-(trifluoromethoxy)phenyl]-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C21H16F4N4O2
 1
1
IC50 = 4000 nM
   TI
   LI
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CP0514015
2-(4-chlorophenyl)-5-[4-(1,8-naphthyridin-2-yl)butyl]-1,3,4-oxadiazole
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C20H17ClN4O
 1
1
IC50 > 3000 nM
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Clinical Information about the Protein
Target 1 ( Succinate receptor (SUCNR1) )
Target Type Literature-reported Target