General Information of the Protein
Protein ID
PT05121
Protein Name
G-protein coupled receptor 39
Gene Name
GPR39
Sequence
MASSSGSNHICSRVIDHSHVPEFEVATWIKITLILVYLIIFVVGILGNSVTIRVTQVLQKKGYLQKEVTDHMVSLACSDILVFLIGMPMEFYSIIWNPLTTPSYALSCKLHTFLFETCSYATLLHVLTLSFERYIAICHPFKYKAVSGPRQVKLLIGFVWVTSALVALPLLFAMGIEYPLVNVPTHKGLNCNLSRTRHHDEPGNSNMSICTNLSNRWEVFQSSIFGAFAVYLVVLASVAFMCWNMMKVLMKSKQGTLAGTGPQLQLRKSESEESRTARRQTIIFLRLIVVTLAVCWMPNQIRRIMAAAKPKHDWTRTYFRAYMILLPFSDTFFYLSSVVNPLLYNVSSQQFRKVFWQVLCCRLTLQHANQEKRQRARFISTKDSTSSARSPLIFLASRRSNSSSRRTNKVFLSTFQTEAKPGEAKPQPLSPESPQTGSETKPAGSTTENSLQEQEV
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Organism
Mus musculus, Mouse
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:17030183, 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 (By similarity). 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 (PubMed:31346193). Regulates adipose tissue metabolism, especially lipolysis, and regulates the function of lipases, such as hormone-sensitive lipase and adipose triglyceride lipase (PubMed:21784784). 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. 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 (By similarity).
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Uniprot ID
Primary ID:
Q5U431

Secondarily ID:
Q80UC7
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Ensembl ID
ENSG00000183840
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0492475
4-N-[(2,4-dichlorophenyl)methyl]-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C17H15Cl2N5
 1
1
EC50 = 0.5 nM
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CP0418268
4-N-[(4-chlorophenyl)methyl]-6-pyridin-2-yl-2-N-(2,2,2-trifluoroethyl)pyrimidine-2,4-diamine
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C18H15ClF3N5
 1
1
EC50 = 1 nM
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CP0386379
N-[4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]acetamide
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C19H20N6O
 1
1
EC50 = 2 nM
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CP0077262
4-[(6-fluoro-4H-1,3-benzodioxin-8-yl)methoxy]-3-methyl-1-(7H-purin-6-yl)-5,7-dihydro-4H-pyrazolo[3,4-b]pyridin-6-one
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C21H18FN7O4
 1
1
EC50 = 2.6 nM
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CP0463104
4-N-[(4-chlorophenyl)methyl]-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C17H16ClN5
 1
1
EC50 = 3 nM
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CP0107678
4-(2-chloro-4-fluorophenyl)-3-methyl-1-(7H-purin-6-yl)-5,7-dihydro-4H-pyrazolo[3,4-b]pyridin-6-one
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C18H13ClFN7O
 2
1
EC50 = 5 nM
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2
EC50 = 180 nM
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CP0519169
2-N-methyl-6-pyridin-2-yl-4-N-[[4-(trifluoromethoxy)phenyl]methyl]pyrimidine-2,4-diamine
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C18H16F3N5O
 1
1
EC50 = 7 nM
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CP0459579
N-[4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]methanesulfonamide
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C18H20N6O2S
 1
1
EC50 = 8 nM
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CP0515155
N-methyl-4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]benzamide
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C19H20N6O
 1
1
EC50 = 8 nM
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CP0448155
4-N-(cyclohexylmethyl)-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C17H23N5
 1
1
EC50 = 10 nM
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CP0481891
N-[(4-chlorophenyl)methyl]-2-methyl-6-pyridin-2-ylpyrimidin-4-amine
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C17H15ClN4
 1
1
EC50 = 17 nM
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CP0549616
4-N-(cyclopropylmethyl)-6-pyridin-2-yl-2-N-[[4-(trifluoromethoxy)phenyl]methyl]pyrimidine-2,4-diamine
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C21H20F3N5O
 1
1
EC50 = 22 nM
   TI
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CP0492476
4-N-[1-(4-chlorophenyl)cyclobutyl]-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C20H20ClN5
 1
1
EC50 = 34 nM
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CP0418306
4-N-(cyclopropylmethyl)-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C14H17N5
 1
1
EC50 = 115 nM
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CP0481892
2-N-methyl-4-N-[(4-methylsulfonylphenyl)methyl]-6-pyridin-2-ylpyrimidine-2,4-diamine
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C18H19N5O2S
 1
1
EC50 = 185 nM
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CP0519167
2-N-methyl-6-pyridin-2-yl-4-N-(pyridin-4-ylmethyl)pyrimidine-2,4-diamine
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C16H16N6
 1
1
EC50 = 304 nM
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CP0481890
4-N-(2,2-dimethylpropyl)-2-N-methyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C15H21N5
 1
1
EC50 = 365 nM
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CP0402780
3-methyl-4-(4-propan-2-yloxyphenyl)-1-(7H-purin-6-yl)-5,7-dihydro-4H-pyrazolo[3,4-b]pyridin-6-one
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C21H21N7O2
 1
1
EC50 = 380 nM
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CP0418305
4-N-(cyclopropylmethyl)-2-N-(2,2-dimethylpropyl)-6-pyridin-2-ylpyrimidine-2,4-diamine
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C18H25N5
 1
1
EC50 = 1500 nM
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CP0398850
N-methyl-N-[4-[[[2-(methylamino)-6-pyridin-2-ylpyrimidin-4-yl]amino]methyl]phenyl]acetamide
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C20H22N6O
 1
1
EC50 = 2612 nM
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CP0386399
4-N-(cyclopropylmethyl)-2-N,2-N-dimethyl-6-pyridin-2-ylpyrimidine-2,4-diamine
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C15H19N5
 1
1
EC50 = 6716 nM
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CP0519168
4-N-(cyclopropylmethyl)-2-N-(2-methoxyethyl)-6-pyridin-2-ylpyrimidine-2,4-diamine
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C16H21N5O
 1
1
EC50 = 10000 nM
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CP0549615
N-(cyclopropylmethyl)-6-pyridin-2-ylpyrimidin-4-amine
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C13H14N4
 1
1
EC50 = 10000 nM
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