General Information of the Protein
Protein ID
PT02436
Protein Name
G-protein coupled receptor 52
Gene Name
GPR52
Sequence
MNESRWTEWRILNMSSGIVNVSERHSCPLGFGHYSVVDVCIFETVVIVLLTFLIIAGNLTVIFVFHCAPLLHHYTTSYFIQTMAYADLFVGVSCLVPTLSLLHYSTGVHESLTCQVFGYIISVLKSVSMACLACISVDRYLAITKPLSYNQLVTPCRLRICIILIWIYSCLIFLPSFFGWGKPGYHGDIFEWCATSWLTSAYFTGFIVCLLYAPAAFVVCFTYFHIFKICRQHTKEINDRRARFPSHEVDSSRETGHSPDRRYAMVLFRITSVFYMLWLPYIIYFLLESSRVLDNPTLSFLTTWLAISNSFCNCVIYSLSNSVFRLGLRRLSETMCTSCMCVKDQEAQEPKPRKRANSCSI
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
Function
Gs-coupled receptor activated by antipsychotics reserpine leading to an increase in intracellular cAMP and its internalization (PubMed:24587241). May play a role in locomotor activity through modulation of dopamine, NMDA and ADORA2A-induced locomotor activity. These behavioral changes are accompanied by modulation of the dopamine receptor signaling pathway in striatum (PubMed:24587241). Modulates HTT level via cAMP-dependent but PKA independent mechanisms throught activation of RAB39B that translocates HTT to the endoplasmic reticulum, thus avoiding proteasome degradation (PubMed:25738228).
    Show/Hide
Uniprot ID
Primary ID:
Q9Y2T5

Secondarily ID:
O75654
Q4VBL6
Q6ISM0
    Show/Hide
HGNC ID
HGNC:4508
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
CP0416475
N-(2-hydroxyethyl)-3-methyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C23H20F3N3O2S
 1
1
EC50 = 5.2 nM
   TI
   LI
   LO
   TS
CP0476663
N-(2-methoxyethyl)-3-methyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C24H22F3N3O2S
 1
1
EC50 = 9.6 nM
   TI
   LI
   LO
   TS
CP0539172
4-[2-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C20H16F4N2OS
 1
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
CP0466025
N-(2-hydroxyethyl)-3,5-dimethyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C24H22F3N3O2S
 1
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
CP0511769
N-(2-methoxyethyl)-3,5-dimethyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C25H24F3N3O2S
 1
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0416474
N-(2-hydroxyethyl)-5-(hydroxymethyl)-3-methyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C24H22F3N3O3S
 1
1
EC50 = 21 nM
   TI
   LI
   LO
   TS
CP0419766
4-[5-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-2-methylpyrazol-3-yl]-2-methylbenzamide
   Show/Hide
C20H17F4N3O
 1
1
EC50 = 23 nM
   TI
   LI
   LO
   TS
CP0419767
4-[2-[(3-chloro-5-fluorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C19H16ClFN2OS
 1
1
EC50 = 25 nM
   TI
   LI
   LO
   TS
CP0398813
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzofuran-4-yl]benzamide
   Show/Hide
C25H20F3NO3
 1
1
EC50 = 28.18 nM
   TI
   LI
   LO
   TS
CP0334329
3-[2-[(3-chloro-5-fluorophenyl)methyl]-1-benzothiophen-7-yl]-N-(2-methoxyethyl)benzamide
   Show/Hide
C25H21ClFNO2S
 1
1
EC50 = 29.51 nM
   TI
   LI
   LO
   TS
CP0523051
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzofuran-7-yl]benzamide
   Show/Hide
C25H20F3NO3
 1
1
EC50 = 34.67 nM
   TI
   LI
   LO
   TS
CP0532168
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]benzamide
   Show/Hide
C25H20F3NO2S
 1
1
EC50 = 37.15 nM
   TI
   LI
   LO
   TS
CP0555255
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-4-yl]benzamide
   Show/Hide
C25H20F3NO2S
 1
1
EC50 = 38.02 nM
   TI
   LI
   LO
   TS
CP0555256
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]indazol-4-yl]benzamide
   Show/Hide
C24H20F3N3O2
 1
1
EC50 = 38.9 nM
   TI
   LI
   LO
   TS
CP0475963
N-(2-methoxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]benzamide
   Show/Hide
C26H22F3NO2S
 1
1
EC50 = 42.66 nM
   TI
   LI
   LO
   TS
CP0466024
N-(2-hydroxyethyl)-2-methyl-5-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-3-carboxamide
   Show/Hide
C23H20F3N3O2S
 1
1
EC50 = 45 nM
   TI
   LI
   LO
   TS
CP0398817
N-(2-amino-2-oxoethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]benzamide
   Show/Hide
C25H19F3N2O2S
 1
1
EC50 = 54.95 nM
   TI
   LI
   LO
   TS
CP0407281
4-[4-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-2-methylimidazol-1-yl]-2-methylbenzamide
   Show/Hide
C20H17F4N3O
 1
1
EC50 = 59 nM
   TI
   LI
   LO
   TS
CP0547139
N-(2-methoxyethyl)-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C23H20F3N3O2S
 1
1
EC50 = 62 nM
   TI
   LI
   LO
   TS
CP0578013
N-(2-methoxyethyl)-5-methyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C24H22F3N3O2S
 1
1
EC50 = 62 nM
   TI
   LI
   LO
   TS
CP0398815
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]indazol-7-yl]benzamide
   Show/Hide
C24H20F3N3O2
 1
1
EC50 = 64.57 nM
   TI
   LI
   LO
   TS
CP0414086
2-methyl-4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C20H17F3N2OS
 1
1
EC50 = 73 nM
   TI
   LI
   LO
   TS
CP0033447
4-[3-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-5-methyl-1,2,4-triazol-1-yl]-2-methylbenzamide
   Show/Hide
C19H16F4N4O
 1
1
EC50 = 75 nM
   TI
   LI
   LO
   TS
CP0398814
N-(2-hydroxyethyl)-3-[3-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzofuran-7-yl]benzamide
   Show/Hide
C26H22F3NO3
 1
1
EC50 = 81.28 nM
   TI
   LI
   LO
   TS
CP0510805
2-ethyl-4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C21H19F3N2OS
 1
1
EC50 = 83 nM
   TI
   LI
   LO
   TS
CP0448356
N-(2-amino-2-oxoethyl)-3-[4-fluoro-2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]benzamide
   Show/Hide
C25H18F4N2O2S
 1
1
EC50 = 83.18 nM
   TI
   LI
   LO
   TS
CP0519760
N-(2-hydroxyethyl)-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C22H18F3N3O2S
 1
1
EC50 = 87 nM
   TI
   LI
   LO
   TS
CP0547944
4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]-2-(trifluoromethyl)benzamide
   Show/Hide
C20H14F6N2OS
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0543059
4-[2-[(3-chlorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C19H17ClN2OS
 1
1
EC50 = 130 nM
   TI
   LI
   LO
   TS
CP0519759
N-(2-hydroxyethyl)-3-(hydroxymethyl)-5-methyl-1-[2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzothiophen-7-yl]pyrazole-4-carboxamide
   Show/Hide
C24H22F3N3O3S
 1
1
EC50 = 146 nM
   TI
   LI
   LO
   TS
CP0402870
4-[2-[(3-methoxyphenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C20H20N2O2S
 1
1
EC50 = 160 nM
   TI
   LI
   LO
   TS
CP0407282
2-methoxy-4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C20H17F3N2O2S
 1
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
CP0523053
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-2,3-dihydro-1-benzofuran-7-yl]benzamide
   Show/Hide
C25H22F3NO3
 1
1
EC50 = 208.93 nM
   TI
   LI
   LO
   TS
CP0432823
4-[2-[(4-chlorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C19H17ClN2OS
 1
1
EC50 = 210 nM
   TI
   LI
   LO
   TS
CP0447332
4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C19H15F3N2OS
 1
1
EC50 = 220 nM
   TI
   LI
   LO
   TS
CP0539173
4-[2-[(3-fluorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C19H17FN2OS
 1
1
EC50 = 260 nM
   TI
   LI
   LO
   TS
CP0419769
4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]-2-propan-2-ylbenzamide
   Show/Hide
C22H21F3N2OS
 1
1
EC50 = 370 nM
   TI
   LI
   LO
   TS
CP0543061
2-fluoro-4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C19H14F4N2OS
 1
1
EC50 = 380 nM
   TI
   LI
   LO
   TS
CP0565934
6-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]pyridine-3-carboxamide
   Show/Hide
C18H14F3N3OS
 1
1
EC50 = 400 nM
   TI
   LI
   LO
   TS
CP0523052
N-(2-hydroxyethyl)-3-[2-[[3-(trifluoromethyl)phenyl]methyl]-2,3-dihydro-1-benzofuran-4-yl]benzamide
   Show/Hide
C25H22F3NO3
 1
1
EC50 = 645.65 nM
   TI
   LI
   LO
   TS
CP0558689
4-[2-[[3-(dimethylamino)phenyl]methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C21H23N3OS
 1
1
EC50 = 690 nM
   TI
   LI
   LO
   TS
CP0432830
3-methyl-4-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]benzamide
   Show/Hide
C20H17F3N2OS
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0419768
4-[2-[(2-chlorophenyl)methyl]-4-methyl-1,3-thiazol-5-yl]-2-methylbenzamide
   Show/Hide
C19H17ClN2OS
 1
1
EC50 = 3900 nM
   TI
   LI
   LO
   TS
CP0489437
N-(2-hydroxyethyl)-3-[3-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1-benzofuran-4-yl]benzamide
   Show/Hide
C26H22F3NO3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0865725
N-(3,4-dimethoxyphenethyl)-4-(4-methoxyphenyl)pyrimidin-2-amine
   Show/Hide
C21H23N3O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0030334
5-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]pyridine-2-carboxamide
   Show/Hide
C18H14F3N3OS
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0033447
4-[3-[[3-fluoro-5-(trifluoromethyl)phenyl]methyl]-5-methyl-1,2,4-triazol-1-yl]-2-methylbenzamide
   Show/Hide
C19H16F4N4O
 1
1 EC50 = 93 nM
CP0030334
5-[4-methyl-2-[[3-(trifluoromethyl)phenyl]methyl]-1,3-thiazol-5-yl]pyridine-2-carboxamide
   Show/Hide
C18H14F3N3OS
 1
1 EC50 > 1000 nM