General Information of the Protein
Protein ID
PT06171
Protein Name
G-protein coupled receptor homolog US28
Secondarily
Protein Name
HHRF3
Gene Name
US28
Sequence
MTPTTTTAELTTEFDYDEDATPCVFTDVLNQSKPVTLFLYGVVFLFGSIGNFLVIFTITWRRRIQCSGDVYFINLAAADLLFVCTLPLWMQYLLDHNSLASVPCTLLTACFYVAMFASLCFITEIALDRYYAIVYMRYRPVKQACLFSIFWWIFAVIIAIPHFMVVTKKDNQCMTDYDYLEVSYPIILNVELMLGAFVIPLSVISYCYYRISRIVAVSQSRHKGRIVRVLIAVVLVFIIFWLPYHLTLFVDTLKLLKWISSSCEFERSLKRALILTESLAFCHCCLNPLLYVFVGTKFRQELHCLLAEFRQRLFSRDVSWYHSMSFSRRSSPSRRETSSDTLSDEVCRVSQIIP
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Organism
Human cytomegalovirus (strain AD169), HHV-5, Human herpesvirus 5
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Chemokine receptor
>
CC chemokine receptor
Function
Binds to a great number of different CC-chemokines including CCL5/RANTES, CCL2/MCP-1, CCL3/MIP-1-alpha as well as CX3CL1/Fractalkine (PubMed:7961796, PubMed:25745166, PubMed:7540006). Transduces signals resulting in the activation of MAP kinase signaling pathways and augmentation of intracellular calcium ion levels, leading to alterations in chemotactic behavior of vascular smooth muscle cells and macrophages. The US28 receptor also exhibits high levels of agonist-independent signaling activity and agonist-independent endocytosis (PubMed:11050102, PubMed:25745166). Interacts with the host Gi complex without activating it, thereby probably interfering with the chemokine-Gi signaling (PubMed:35061538). May also function as a G protein sink to sequester G protein from the cell surface via internalization (PubMed:35061538). Interacts with endogenous Gaq/11 subunits and thereby constitutively activates phospholipase C (PubMed:11050102).
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Uniprot ID
Primary ID:
P69332

Secondarily ID:
P09704
P32952
Q7M6H3
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Subcellular Location
Host 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: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0149004
5-(4-(4-chlorophenyl)-4-hydroxy-piperidin-1-yl)-2,2-diphenylpentanenitrile
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C28H29ClN2O
 2
1
EC50 = 3200 nM
   TI
   LI
   LO
   TS
2
IC50 = 9300 nM
   TI
   LI
   LO
   TS
CP0436101
4-(4-Chloro-phenyl)-1-(4,4-diphenyl-butyl)-piperidin-4-ol
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C27H30ClNO
 2
1
EC50 = 4200 nM
   TI
   LI
   LO
   TS
2
IC50 = 6500 nM
   TI
   LI
   LO
   TS
CP0455657
4-(4-Chloro-phenyl)-1-(4-phenyl-4-o-tolyl-butyl)-piperidin-4-ol
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C28H32ClNO
 2
1
EC50 = 9800 nM
   TI
   LI
   LO
   TS
2
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0515626
4-(4-Chloro-phenyl)-1-(4-phenyl-4-p-tolyl-butyl)-piperidin-4-ol
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C28H32ClNO
 2
1
EC50 = 11500 nM
   TI
   LI
   LO
   TS
2
IC50 = 30900 nM
   TI
   LI
   LO
   TS
CP0490729
5-[4-(4-Chloro-phenyl)-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
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C28H29ClN2
 2
1
EC50 = 13800 nM
   TI
   LI
   LO
   TS
2
IC50 = 10500 nM
   TI
   LI
   LO
   TS
CP0428273
5-(4-Hydroxy-4-phenyl-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C28H30N2O
 2
1
EC50 = 28200 nM
   TI
   LI
   LO
   TS
2
IC50 = 35500 nM
   TI
   LI
   LO
   TS
CP0389170
5-[4-Hydroxy-4-(4-methoxy-phenyl)-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
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C29H32N2O2
 2
1
EC50 = 28800 nM
   TI
   LI
   LO
   TS
2
IC50 = 72400 nM
   TI
   LI
   LO
   TS
CP0378237
1-(4-Cyano-4,4-diphenyl-butyl)-piperidine-4-carboxylic acid ethyl ester
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C25H30N2O2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 = 34700 nM
   TI
   LI
   LO
   TS
CP0378238
5-(4-Benzhydrylidene-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C35H34N2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0392112
5-[4-(4-Chloro-phenyl)-piperazin-1-yl]-2,2-diphenyl-pentanenitrile
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C27H28ClN3
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0392113
5-[4-(4-Chloro-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-2,2-diphenyl-pentanenitrile
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C28H27ClN2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0436103
1-[4-Biphenyl-4-yl-4-(4-chloro-phenyl)-butyl]-4-(4-chloro-phenyl)-piperidin-4-ol
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C33H33Cl2NO
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0442708
1-(4-Cyano-4,4-diphenyl-butyl)-4-phenyl-piperidine-4-carbonitrile
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C29H29N3
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0442709
4-(4-Chloro-phenyl)-1-(4-hydroxy-4-phenyl-butyl)-piperidin-4-ol
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C21H26ClNO2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0445792
5-(4-Butyl-4-hydroxy-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C26H34N2O
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0446390
5-(4-Hydroxy-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C22H26N2O
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0446391
4-(4-Chloro-phenyl)-1-(4-cyano-4,4-diphenyl-butyl)-4-hydroxy-1-methyl-piperidinium
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C29H32ClN2O+
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0493099
1-(4-Cyano-4,4-diphenyl-butyl)-piperidine-4-carboxylic acid amide
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C23H27N3O
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0540279
5-(4-Hydroxy-4-methyl-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C23H28N2O
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0541527
1-(4-Cyano-4,4-diphenyl-butyl)-piperidine-4-carboxylic acid
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C23H26N2O2
 2
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
2
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0486612
4-(4-Chloro-phenyl)-1-(4-phenyl-4-m-tolyl-butyl)-piperidin-4-ol
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C28H32ClNO
 1
1
IC50 = 11500 nM
   TI
   LI
   LO
   TS
CP0476709
4-(4-Chloro-phenyl)-1-(4-phenyl-butyl)-piperidin-4-ol
   Show/Hide
C21H26ClNO
 1
1
IC50 = 14800 nM
   TI
   LI
   LO
   TS
CP0403411
4-(4-Chloro-phenyl)-1-[4-(4-methoxy-phenyl)-4-phenyl-butyl]-piperidin-4-ol
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C28H32ClNO2
 1
1
IC50 = 15500 nM
   TI
   LI
   LO
   TS
CP0378239
4-(4-Chloro-phenyl)-1-[4-(3,4-dichloro-phenyl)-4-phenyl-butyl]-piperidin-4-ol
   Show/Hide
C27H28Cl3NO
 1
1
IC50 = 15800 nM
   TI
   LI
   LO
   TS
CP0436102
4-(4-Chloro-phenyl)-1-[4-(4-chloro-phenyl)-4-phenyl-butyl]-piperidin-4-ol
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C27H29Cl2NO
 1
1
IC50 = 17000 nM
   TI
   LI
   LO
   TS
CP0486611
1-[4,4-Bis-(4-chloro-phenyl)-butyl]-4-(4-chloro-phenyl)-piperidin-4-ol
   Show/Hide
C27H28Cl3NO
 1
1
IC50 = 17400 nM
   TI
   LI
   LO
   TS
CP0403418
5-[4-(4-Bromo-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
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C28H29BrN2O
 1
1
IC50 = 19500 nM
   TI
   LI
   LO
   TS
CP0392092
5-[4-(3,4-Dichloro-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
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C28H28Cl2N2O
 1
1
IC50 = 38000 nM
   TI
   LI
   LO
   TS
CP0495173
5-[4-(4-Chloro-3-trifluoromethyl-phenyl)-4-hydroxy-piperidin-1-yl]-2,2-diphenyl-pentanenitrile
   Show/Hide
C29H28ClF3N2O
 1
1
IC50 = 45700 nM
   TI
   LI
   LO
   TS
CP0485050
5-(4-Hydroxy-4-p-tolyl-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C29H32N2O
 1
1
IC50 = 60300 nM
   TI
   LI
   LO
   TS
CP0392114
4-(4-Chloro-phenyl)-1-(3-phenoxy-propyl)-piperidin-4-ol
   Show/Hide
C20H24ClNO2
 1
1
IC50 = 61700 nM
   TI
   LI
   LO
   TS
CP0442707
5-(4-Benzyl-4-hydroxy-piperidin-1-yl)-2,2-diphenyl-pentanenitrile
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C29H32N2O
 1
1
IC50 = 63100 nM
   TI
   LI
   LO
   TS
CP0421011
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-phenyl-butan-1-one
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C21H24ClNO2
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS