General Information of the Protein
Protein ID
PT03123
Protein Name
G-protein coupled receptor 39
Gene Name
GPR39
Sequence
MASPSLPGSDCSQIIDHSHVPEFEVATWIKITLILVYLIIFVMGLLGNSATIRVTQVLQKKGYLQKEVTDHMVSLACSDILVFLIGMPMEFYSIIWNPLTTSSYTLSCKLHTFLFEACSYATLLHVLTLSFERYIAICHPFRYKAVSGPCQVKLLIGFVWVTSALVALPLLFAMGTEYPLVNVPSHRGLTCNRSSTRHHEQPETSNMSICTNLSSRWTVFQSSIFGAFVVYLVVLLSVAFMCWNMMQVLMKSQKGSLAGGTRPPQLRKSESEESRTARRQTIIFLRLIVVTLAVCWMPNQIRRIMAAAKPKHDWTRSYFRAYMILLPFSETFFYLSSVINPLLYTVSSQQFRRVFVQVLCCRLSLQHANHEKRLRVHAHSTTDSARFVQRPLLFASRRQSSARRTEKIFLSTFQSEAEPQSKSQSLSLESLEPNSGAKPANSAAENGFQEHEV
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
Function
Zinc-sensing receptor that can sense changes in extracellular Zn(2+), mediate Zn(2+) signal transmission, and participates in the regulation of numerous physiological processes including glucose homeostasis regulation, gastrointestinal mobility, hormone secretion and cell death (PubMed:18180304). Activation by Zn(2+) in keratinocytes increases the intracellular concentration of Ca(2+) and activates the ERK/MAPK and PI3K/AKT signaling pathways leading to epithelial repair (PubMed:20522546). Plays an essential role in normal wound healing by inducing the production of cytokines including the major inflammatory cytokine IL6 via the PKC/MAPK/CEBPB pathway (By similarity). Regulates adipose tissue metabolism, especially lipolysis, and regulates the function of lipases, such as hormone-sensitive lipase and adipose triglyceride lipase (By similarity). Plays a role in the inhibition of cell death and protects against oxidative, endoplasmic reticulum and mitochondrial stress by inducing secretion of the cytoprotective pigment epithelium-derived growth factor (PEDF) and probably other protective transcripts in a GNA13/RHOA/SRE-dependent manner (PubMed:18180304). Forms dynamic heteroreceptor complexes with HTR1A and GALR1 depending on cell type or specific physiological states, resulting in signaling diversity: HTR1A-GPR39 shows additive increase in signaling along the serum response element (SRE) and NF-kappa-B pathways while GALR1 acts as an antagonist blocking SRE (PubMed:26365466).
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Uniprot ID
Primary ID:
O43194

Secondarily ID:
B2RC12
B6V9G4
Q08AS2
Q53R01
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Ensembl ID
ENSG00000183840
HGNC ID
HGNC:4496
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0567871
4-N-[(2-chlorophenyl)methyl]-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C17H16ClN5
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0067898
N-[3-chloro-4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
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C18H19ClN6O2S
 2
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0544591
N-[(4-fluorophenyl)methyl]-5-methyl-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidin-7-amine
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C19H16FN5
 2
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0544592
4-N-cyclohexyl-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C16H21N5
 2
1
EC50 = 16 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0572896
5-methyl-7-(2-phenylpyrrolidin-1-yl)-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidine
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C22H21N5
 2
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0542984
N-methyl-4-phenoxy-6-pyridin-2-ylpyrimidin-2-amine
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C16H14N4O
 2
1
EC50 = 23 nM
   TI
   LI
   LO
   TS
2
EC50 = 481 nM
   TI
   LI
   LO
   TS
CP0569067
N-[2-(4-fluorophenyl)propan-2-yl]-5-methyl-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidin-7-amine
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C21H20FN5
 2
1
EC50 = 63 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0545070
2-(4-fluorophenyl)-N-methyl-2-[(5-methyl-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidin-7-yl)amino]acetamide
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C21H19FN6O
 2
1
EC50 = 78 nM
   TI
   LI
   LO
   TS
2
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0965297
2-(1-amino-2-(1H-imidazol-5-yl)ethyl)-6-phenylquinazolin-4(3H)-one
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C19H17N5O
 2
1
EC50 = 251 nM
   TI
   LI
   LO
   TS
2
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0576719
2-N-cyclohexyl-4-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C16H21N5
 2
1
EC50 = 487 nM
   TI
   LI
   LO
   TS
2
EC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0968151
2-(1-amino-3-(benzyloxy)propyl)-6-(1-methyl-1H-pyrazol-4-yl)quinazolin-4(3H)-one
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C22H23N5O2
 2
1
EC50 = 641 nM
   TI
   LI
   LO
   TS
2
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0569877
2-[3-(cyclobutylmethyl)-4-oxophthalazin-1-yl]-N-(pyridin-2-ylmethyl)acetamide
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C21H22N4O2
 2
1
EC50 = 4040 nM
   TI
   LI
   LO
   TS
2
EC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0055399
6-[4-[(6-chloroimidazo[1,2-a]pyridin-2-yl)methyl]piperazin-1-yl]pyridine-3-carbonitrile
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C18H17ClN6
 1
1
EC50 = 6250 nM
   TI
   LI
   LO
   TS
CP0550002
5-methyl-7-(3-phenylpyrrolidin-1-yl)-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidine
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C22H21N5
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0568569
5-methyl-3-pyridin-2-yl-7-(2-pyridin-3-ylpyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidine
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C21H20N6
 1
1
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0571680
N-[1-(4-fluorophenyl)ethyl]-5-methyl-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidin-7-amine
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C20H18FN5
 1
1
EC50 > 27100 nM
   TI
   LI
   LO
   TS
CP0577232
1-(5-methyl-3-pyridin-2-ylpyrazolo[1,5-a]pyrimidin-7-yl)-5-phenylpyrrolidin-2-one
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C22H19N5O
 2
1
EC50 > 27100 nM
   TI
   LI
   LO
   TS
2
EC50 > 31600 nM
   TI
   LI
   LO
   TS
CP0006743
4-methoxy-N-(2,4,6-trimethylphenyl)benzenesulfonamide
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C16H19NO3S
 1
1
EC50 > 50118.72 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0067898
N-[3-chloro-4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
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C18H19ClN6O2S
 1
1 EC50 = 0.8 nM
Clinical Information about the Protein
Target 1 ( G-protein coupled receptor 39 (GPR39) )
Target Type Literature-reported Target