General Information of the Protein
Protein ID
PT05857
Protein Name
Neuropeptide S receptor
Secondarily
Protein Name
G-protein coupled receptor 154
G-protein coupled receptor PGR14
G-protein coupled receptor for asthma susceptibility
Gene Name
NPSR1
Secondarily
Gene Name
GPR154
GPRA
PGR14
Sequence
MPANFTEGSFDSSGTGQTLDSSPVACTETVTFTEVVEGKEWGSFYYSFKTEQLITLWVLFVFTIVGNSVVLFSTWRRKKKSRMTFFVTQLAITDSFTGLVNILTDINWRFTGDFTAPDLVCRVVRYLQVVLLYASTYVLVSLSIDRYHAIVYPMKFLQGEKQARVLIVIAWSLSFLFSIPTLIIFGKRTLSNGEVQCWALWPDDSYWTPYMTIVAFLVYFIPLTIISIMYGIVIRTIWIKSKTYETVISNCSDGKLCSSYNRGLISKAKIKAIKYSIIIILAFICCWSPYFLFDILDNFNLLPDTQERFYASVIIQNLPALNSAINPLIYCVFSSSISFPCREQRSQDSRMTFRERTERHEMQILSKPEFI
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Neuropeptide receptor
Function
G-protein coupled receptor for neuropeptide S (NPS) (PubMed:16790440). Promotes mobilization of intracellular Ca(2+) stores (PubMed:16790440). Inhibits cell growth in response to NPS binding (PubMed:15947423). Involved in pathogenesis of asthma and other IgE-mediated diseases.
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Uniprot ID
Primary ID:
Q6W5P4

Secondarily ID:
A2RTZ4
Q2XP58
Q56H76
Q56H77
Q56H78
Q6JSL4
Q6JSL5
Q6JSL6
Q6JSL7
Q6JSL8
Q6W5P3
Q6ZMB8
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HGNC ID
HGNC:23631
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
CP0505881
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-(3-methyl-1-piperidin-1-ylpentan-3-yl)cyclohexanecarboxamide
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C29H43N3O2
 1
1
IC50 = 7 nM
   TI
   LI
   LO
   TS
CP0377181
N-[1-(4-fluoropiperidin-1-yl)-3-methylpentan-3-yl]-N-[(1-methyl-2-oxoquinolin-3-yl)methyl]cyclohexanecarboxamide
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C29H42FN3O2
 1
1
IC50 = 14 nM
   TI
   LI
   LO
   TS
CP0489449
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-[[1-(4-methylpiperazin-1-yl)cyclohexyl]methyl]cyclohexanecarboxamide
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C30H44N4O2
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0490896
N-[1-(4,4-difluoropiperidin-1-yl)-3-methylpentan-3-yl]-N-[(1-methyl-2-oxoquinolin-3-yl)methyl]cyclohexanecarboxamide
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C29H41F2N3O2
 1
1
IC50 = 22 nM
   TI
   LI
   LO
   TS
CP0470702
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-(2-methyl-4-piperidin-1-ylbutan-2-yl)cyclohexanecarboxamide
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C28H41N3O2
 1
1
IC50 = 31 nM
   TI
   LI
   LO
   TS
CP0262580
3-[5-(4-chlorophenyl)-6-methoxyimidazo[1,2-b]isoindol-5-yl]-N,N-diethylpropanamide
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C24H26ClN3O2
 1
1
IC50 = 43 nM
   TI
   LI
   LO
   TS
CP0501177
5-(4-chlorophenyl)-6-methoxy-5-(oxan-4-ylmethyl)imidazo[2,1-a]isoindole
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C23H23ClN2O2
 1
1
IC50 = 46 nM
   TI
   LI
   LO
   TS
CP0397254
3-[5-(4-chlorophenyl)-7-methoxyimidazo[1,2-b]isoindol-5-yl]-1-[(2S,5R)-2,5-dimethylpyrrolidin-1-yl]propan-1-one
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C26H28ClN3O2
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0087277
5-(4-chlorophenyl)-7-methoxy-5-(oxan-4-ylmethyl)imidazo[2,1-a]isoindole
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C23H23ClN2O2
 1
1
IC50 = 82 nM
   TI
   LI
   LO
   TS
CP0501176
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-N,N-diethylpropanamide
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C23H24ClN3O
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0378255
5-(4-bromophenyl)-5-(oxan-4-ylmethyl)imidazo[2,1-a]isoindole
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C22H21BrN2O
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0505139
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-1-[(2S,5R)-2,5-dimethylpyrrolidin-1-yl]propan-1-one
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C25H26ClN3O
 1
1
IC50 = 92 nM
   TI
   LI
   LO
   TS
CP0505138
1-(8-azabicyclo[3.2.1]octan-8-yl)-3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]propan-1-one
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C26H26ClN3O
 1
1
IC50 = 95 nM
   TI
   LI
   LO
   TS
CP0501175
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-N,N-di(propan-2-yl)propanamide
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C25H28ClN3O
 1
1
IC50 = 96 nM
   TI
   LI
   LO
   TS
CP0487865
N-(3-ethyl-1-morpholin-4-ylpentan-3-yl)-N-[(1-methyl-2-oxoquinolin-3-yl)methyl]cyclohexanecarboxamide
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C29H43N3O3
 1
1
IC50 = 103 nM
   TI
   LI
   LO
   TS
CP0499927
4-[5-(cyclohexylmethyl)imidazo[1,2-b]isoindol-5-yl]benzonitrile
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C24H23N3
 1
1
IC50 = 114 nM
   TI
   LI
   LO
   TS
CP0474007
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-1-[4-(1-pyrrolidin-1-ylethyl)piperidin-1-yl]propan-1-one
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C30H35ClN4O
 1
1
IC50 = 126 nM
   TI
   LI
   LO
   TS
CP0378254
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-1-(2-ethylpiperidin-1-yl)propan-1-one
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C26H28ClN3O
 1
1
IC50 = 131 nM
   TI
   LI
   LO
   TS
CP0505140
5-(4-chlorophenyl)-5-(oxan-4-ylmethyl)imidazo[2,1-a]isoindole
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C22H21ClN2O
 1
1
IC50 = 134 nM
   TI
   LI
   LO
   TS
CP0522097
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-N-ethyl-N-propan-2-ylpropanamide
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C24H26ClN3O
 1
1
IC50 = 138 nM
   TI
   LI
   LO
   TS
CP0377180
N-(2-methyl-4-morpholin-4-ylbutan-2-yl)-N-[(1-methyl-2-oxoquinolin-3-yl)methyl]cyclohexanecarboxamide
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C27H39N3O3
 1
1
IC50 = 144 nM
   TI
   LI
   LO
   TS
CP0503444
4-[5-(cyclopentylmethyl)imidazo[1,2-b]isoindol-5-yl]benzonitrile
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C23H21N3
 1
1
IC50 = 145 nM
   TI
   LI
   LO
   TS
CP0489756
5-(4-bromophenyl)-5-[2-(oxan-4-yl)ethyl]imidazo[2,1-a]isoindole
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C23H23BrN2O
 1
1
IC50 = 154 nM
   TI
   LI
   LO
   TS
CP0397253
3-[5-(4-chlorophenyl)imidazo[1,2-b]isoindol-5-yl]-1-[4-[1-(3,3-difluoropyrrolidin-1-yl)ethyl]piperidin-1-yl]propan-1-one
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C30H33ClF2N4O
 1
1
IC50 = 239 nM
   TI
   LI
   LO
   TS
CP0503443
5-(4-bromophenyl)-5-(cyclohexylmethyl)imidazo[2,1-a]isoindole
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C23H23BrN2
 1
1
IC50 = 254 nM
   TI
   LI
   LO
   TS
CP0493932
5-(4-bromophenyl)-5-(cyclopentylmethyl)imidazo[2,1-a]isoindole
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C22H21BrN2
 1
1
IC50 = 321 nM
   TI
   LI
   LO
   TS
CP0509771
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-(2-methyl-4-pyrrolidin-1-ylbutan-2-yl)cyclohexanecarboxamide
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C27H39N3O2
 1
1
IC50 = 326 nM
   TI
   LI
   LO
   TS
CP0493933
5-benzyl-5-(4-fluorophenyl)imidazo[2,1-a]isoindole
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C23H17FN2
 1
1
IC50 = 336 nM
   TI
   LI
   LO
   TS
CP0499926
5-(4-bromophenyl)-5-(pyridin-3-ylmethyl)imidazo[2,1-a]isoindole
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C22H16BrN3
 1
1
IC50 = 351 nM
   TI
   LI
   LO
   TS
CP0493934
5-benzyl-5-(4-chlorophenyl)imidazo[2,1-a]isoindole
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C23H17ClN2
 1
1
IC50 = 358 nM
   TI
   LI
   LO
   TS
CP0493953
2-[[5-(4-bromophenyl)imidazo[1,2-b]isoindol-5-yl]methyl]benzonitrile
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C24H16BrN3
 1
1
IC50 = 369 nM
   TI
   LI
   LO
   TS
CP0397250
4-(5-benzylimidazo[1,2-b]isoindol-5-yl)benzonitrile
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C24H17N3
 1
1
IC50 = 387 nM
   TI
   LI
   LO
   TS
CP0487866
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-[1-(2-morpholin-4-ylethyl)cyclohexyl]cyclohexanecarboxamide
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C30H43N3O3
 1
1
IC50 = 398 nM
   TI
   LI
   LO
   TS
CP0503112
4-[5-(oxan-4-ylmethyl)imidazo[1,2-b]isoindol-5-yl]benzonitrile
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C23H21N3O
 1
1
IC50 = 635 nM
   TI
   LI
   LO
   TS
CP0526617
5-(4-fluorophenyl)-5-(oxan-4-ylmethyl)imidazo[2,1-a]isoindole
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C22H21FN2O
 1
1
IC50 = 660 nM
   TI
   LI
   LO
   TS
CP0496044
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-(4-morpholin-4-ylbutan-2-yl)cyclohexanecarboxamide
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C26H37N3O3
 1
1
IC50 = 725 nM
   TI
   LI
   LO
   TS
CP0397252
5-(6-bromopyridin-3-yl)-5-(cyclopentylmethyl)imidazo[2,1-a]isoindole
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C21H20BrN3
 1
1
IC50 = 851 nM
   TI
   LI
   LO
   TS
CP0397249
5-benzyl-5-(4-methylphenyl)imidazo[2,1-a]isoindole
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C24H20N2
 1
1
IC50 = 1325 nM
   TI
   LI
   LO
   TS
CP0498343
7-benzyl-7-(4-bromophenyl)-3,6,12-triazatricyclo[6.4.0.02,6]dodeca-1(8),2,4,9,11-pentaene
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C22H16BrN3
 1
1
IC50 = 1458 nM
   TI
   LI
   LO
   TS
CP0526616
5-benzyl-5-(6-bromopyridin-3-yl)imidazo[2,1-a]isoindole
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C22H16BrN3
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0475419
N-[(1-methyl-2-oxoquinolin-3-yl)methyl]-N-(4-pyrrolidin-1-ylbutan-2-yl)cyclohexanecarboxamide
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C26H37N3O2
 1
1
IC50 = 1577 nM
   TI
   LI
   LO
   TS
CP0501174
5-benzyl-5-(3-bromophenyl)imidazo[2,1-a]isoindole
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C23H17BrN2
 1
1
IC50 = 1725 nM
   TI
   LI
   LO
   TS
CP0397251
5-benzyl-5-(5-bromopyridin-2-yl)imidazo[2,1-a]isoindole
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C22H16BrN3
 1
1
IC50 = 2179 nM
   TI
   LI
   LO
   TS
CP0505084
3-(5-benzylimidazo[1,2-b]isoindol-5-yl)benzonitrile
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C24H17N3
 1
1
IC50 = 3166 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0321401
N-(3-methyl-1-morpholin-4-ylpentan-3-yl)-N-[(1-methyl-2-oxoquinolin-3-yl)methyl]cyclohexanecarboxamide
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C28H41N3O3
 1
1 IC50 = 1.3 nM
CP0334232
N-[(4-fluorophenyl)methyl]-3-oxo-1,1-diphenyl-5,6,8,8a-tetrahydro-[1,3]oxazolo[3,4-a]pyrazine-7-carboxamide
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C26H24FN3O3
 2
1 IC50 = 48 nM
2 Ki = 47.86 nM
CP0842124
3-(diphenylphosphorothioyl)-1,2-dimethylimidazo[1,2-a]pyridin-1-ium
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C21H20IN2PS
 1
1 IC50 = 84 nM
Clinical Information about the Protein
Target 1 ( Neuropeptide S receptor (NPSR) )
Target Type Patented-recorded Target