General Information of the Protein
Protein ID
PT05721
Protein Name
Substance-P receptor
Secondarily
Protein Name
NK-1 receptor
Tachykinin receptor 1
Gene Name
TACR1
Sequence
MDNVLPGDSDLFPNISTNSSESNQFVQPAWQIVLWAAAYTVIVVTSVVGNVVVMWIILAHKRMRTVTNYFLVNLAFAEASMAAFNTVVNFTYAVHNEWYYGLFYCKFHNFFPIAAVFASIYSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPGRVVCMIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQVSAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYVKKFIQQVYLAIMWLAMSSTMYNPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQGSVYKVSRLETTISTVVGAHEDEAEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
    Show/Hide
Organism
Meriones unguiculatus, Mongolian jird, Gerbillus unguiculatus
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Neurokinin receptor
Function
This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system (By similarity).
    Show/Hide
Uniprot ID
Q5DUB1
Ensembl ID
ENSG00000115353
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
CP0528880
(2S,3S)-3-[[2-methoxy-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl]methoxy]-2-phenylpiperidine
   Show/Hide
C21H22F3N5O2
 1
1
IC50 = 0.03 nM
   TI
   LI
   LO
   TS
CP0443583
(2S,3S)-3-[[2-methoxy-5-(5-methyltetrazol-1-yl)phenyl]methoxy]-2-phenylpiperidine
   Show/Hide
C21H25N5O2
 1
1
IC50 = 0.05 nM
   TI
   LI
   LO
   TS
CP0559365
(2S,3S)-3-[[2-methoxy-5-(tetrazol-1-yl)phenyl]methoxy]-2-phenylpiperidine
   Show/Hide
C20H23N5O2
 1
1
IC50 = 0.05 nM
   TI
   LI
   LO
   TS
CP0107813
3-[2-{1-[3,5-di(trifluoromethyl)phenyl]ethoxy}-3-(4-fluorophenyl)-1,4-oxazinan-4-ylmethyl]-4,5-dihydro-1H-1,2,4-triazol-5-one
   Show/Hide
C23H21F7N4O3
 1
1
IC50 = 0.09 nM
   TI
   LI
   LO
   TS
CP0463077
4-[3-[(1-ethyl-4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C29H29F3N2O
 1
1
IC50 = 0.25 nM
   TI
   LI
   LO
   TS
CP0504467
4-[3-[(1-methyl-4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C28H27F3N2O
 1
1
IC50 = 0.29 nM
   TI
   LI
   LO
   TS
CP0447811
2,6-difluoro-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H23F5N2O
 1
1
IC50 = 0.32 nM
   TI
   LI
   LO
   TS
CP0463078
4-[3-[(4-phenyl-1-propan-2-ylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C30H31F3N2O
 1
1
IC50 = 0.39 nM
   TI
   LI
   LO
   TS
CP0447810
4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H25F3N2O
 1
1
IC50 = 0.45 nM
   TI
   LI
   LO
   TS
CP0463073
2,5-difluoro-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H23F5N2O
 1
1
IC50 = 0.91 nM
   TI
   LI
   LO
   TS
CP0407872
4-[[3-(4-methoxyphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H28F3NO2
 1
1
IC50 = 0.93 nM
   TI
   LI
   LO
   TS
CP0528874
2-fluoro-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H24F4N2O
 1
1
IC50 = 1.1 nM
   TI
   LI
   LO
   TS
CP0528875
2-chloro-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H24ClF3N2O
 1
1
IC50 = 1.1 nM
   TI
   LI
   LO
   TS
CP0443710
2-methyl-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C28H27F3N2O
 1
1
IC50 = 1.2 nM
   TI
   LI
   LO
   TS
CP0385768
4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]pyridine
   Show/Hide
C25H25F3N2O
 1
1
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
CP0452645
4-[3-[(1-cyclopropyl-4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C30H29F3N2O
 1
1
IC50 = 1.8 nM
   TI
   LI
   LO
   TS
CP0559362
5-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]pyridine-2-carbonitrile
   Show/Hide
C26H24F3N3O
 1
1
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0504468
4-[3-[(1-benzyl-4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C34H31F3N2O
 1
1
IC50 = 2 nM
   TI
   LI
   LO
   TS
CP0504472
4-[[3-(4-fluorophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F4NO
 1
1
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0382160
4-[[3-(4-chlorophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25ClF3NO
 1
1
IC50 = 2.8 nM
   TI
   LI
   LO
   TS
CP0463080
4-[[3-(4-ethoxyphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C28H30F3NO2
 1
1
IC50 = 3.4 nM
   TI
   LI
   LO
   TS
CP0407870
4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]phenol
   Show/Hide
C26H26F3NO2
 1
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
CP0504473
4-[[3-(4-nitrophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F3N2O3
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0547787
2,3,5,6-tetrafluoro-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H21F7N2O
 1
1
IC50 = 4.8 nM
   TI
   LI
   LO
   TS
CP0443714
4-[[3-(3-fluorophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F4NO
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0443716
4-[[3-(3-nitrophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F3N2O3
 1
1
IC50 = 5.2 nM
   TI
   LI
   LO
   TS
CP0550090
4-phenyl-4-[[3-phenyl-5-(trifluoromethyl)phenyl]methoxymethyl]piperidine
   Show/Hide
C26H26F3NO
 1
1
IC50 = 6.3 nM
   TI
   LI
   LO
   TS
CP0385763
4-[[3-(2-nitrophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F3N2O3
 1
1
IC50 = 6.5 nM
   TI
   LI
   LO
   TS
CP0542712
4-[[3-(1,3-benzodioxol-5-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H26F3NO3
 1
1
IC50 = 7.1 nM
   TI
   LI
   LO
   TS
CP0404467
6-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]pyridine-3-carbonitrile
   Show/Hide
C26H24F3N3O
 1
1
IC50 = 8.1 nM
   TI
   LI
   LO
   TS
CP0443719
4-[[3-(4-methylphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H28F3NO
 1
1
IC50 = 8.4 nM
   TI
   LI
   LO
   TS
CP0504471
3-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]phenol
   Show/Hide
C26H26F3NO2
 1
1
IC50 = 13 nM
   TI
   LI
   LO
   TS
CP0463079
methyl 4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzoate
   Show/Hide
C28H28F3NO3
 1
1
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0452647
N,N-dimethyl-4-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]aniline
   Show/Hide
C28H31F3N2O
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0404469
4-[[3-(2-fluorophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25F4NO
 1
1
IC50 = 23 nM
   TI
   LI
   LO
   TS
CP0542708
4-[[3-(3-methylphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H28F3NO
 1
1
IC50 = 24 nM
   TI
   LI
   LO
   TS
CP0504470
3-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]aniline
   Show/Hide
C26H27F3N2O
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0443718
4-phenyl-4-[[3-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]phenyl]methoxymethyl]piperidine
   Show/Hide
C27H25F6NO
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0528878
4-[[3-(2-methyltetrazol-5-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C22H24F3N5O
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0528877
2-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]pyridine
   Show/Hide
C25H25F3N2O
 1
1
IC50 = 41 nM
   TI
   LI
   LO
   TS
CP0382162
4-[[3-(furan-2-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C24H24F3NO2
 1
1
IC50 = 47 nM
   TI
   LI
   LO
   TS
CP0559364
3-[3-[(4-phenylpiperidin-4-yl)methoxymethyl]-5-(trifluoromethyl)phenyl]benzonitrile
   Show/Hide
C27H25F3N2O
 1
1
IC50 = 49 nM
   TI
   LI
   LO
   TS
CP0528876
4-[[3-(2-methoxyphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H28F3NO2
 1
1
IC50 = 54 nM
   TI
   LI
   LO
   TS
CP0443581
4-[[3-(1-methyltetrazol-5-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C22H24F3N5O
 1
1
IC50 = 65 nM
   TI
   LI
   LO
   TS
CP0447812
4-[[3-(2-chlorophenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C26H25ClF3NO
 1
1
IC50 = 68 nM
   TI
   LI
   LO
   TS
CP0882061
2-(3-(((4-phenylpiperidin-4-yl)methoxy)methyl)-5-(trifluoromethyl)phenyl)thiazole
   Show/Hide
C23H23F3N2OS
 1
1
IC50 = 70 nM
   TI
   LI
   LO
   TS
CP0443582
4-[[2-methoxy-5-(5-methyltetrazol-1-yl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C22H27N5O2
 1
1
IC50 = 87 nM
   TI
   LI
   LO
   TS
CP0504469
4-[[3-naphthalen-2-yl-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C30H28F3NO
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0404470
4-[[3-(2-methylphenyl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C27H28F3NO
 1
1
IC50 = 130 nM
   TI
   LI
   LO
   TS
CP0463082
4-[[3-(5-methyltetrazol-1-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C22H24F3N5O
 1
1
IC50 = 180 nM
   TI
   LI
   LO
   TS
CP0528879
4-phenyl-4-[[3-(2H-tetrazol-5-yl)-5-(trifluoromethyl)phenyl]methoxymethyl]piperidine
   Show/Hide
C21H22F3N5O
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0404468
4-[[3-naphthalen-1-yl-5-(trifluoromethyl)phenyl]methoxymethyl]-4-phenylpiperidine
   Show/Hide
C30H28F3NO
 1
1
IC50 = 540 nM
   TI
   LI
   LO
   TS
CP0382163
4-phenyl-4-[[3-(trifluoromethyl)-5-[5-(trifluoromethyl)tetrazol-1-yl]phenyl]methoxymethyl]piperidine
   Show/Hide
C22H21F6N5O
 1
1
IC50 = 700 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT02240 Substance-P receptor Rattus norvegicus, Rat