General Information of the Protein
Protein ID
PT04126
Protein Name
Neuromedin-K receptor
Secondarily
Protein Name
NK-3 receptor
Neurokinin B receptor
Tachykinin receptor 3
Gene Name
TACR3
Secondarily
Gene Name
Tac3r
Sequence
MASVPRGENWTDGTVEVGTHTGNLSSALGVTEWLALQAGNFSSALGLPATTQAPSQVRANLTNQFVQPSWRIALWSLAYGLVVAVAVFGNLIVIWIILAHKRMRTVTNYFLVNLAFSDASVAAFNTLINFIYGLHSEWYFGANYCRFQNFFPITAVFASIYSMTAIAVDRYMAIIDPLKPRLSATATKIVIGSIWILAFLLAFPQCLYSKIKVMPGRTLCYVQWPEGPKQHFTYHIIVIILVYCFPLLIMGVTYTIVGITLWGGEIPGDTCDKYHEQLKAKRKVVKMMIIVVVTFAICWLPYHVYFILTAIYQQLNRWKYIQQVYLASFWLAMSSTMYNPIIYCCLNKRFRAGFKRAFRWCPFIQVSSYDELELKTTRFHPTRQSSLYTVSRMESVTVLFDPNDGDPTKSSRKKRAVPRDPSANGCSHRGSKSASTTSSFISSPYTSVDEYS
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Organism
Rattus norvegicus, Rat
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 neuromedin-K (neurokinin B). It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: neuromedin-K > substance K > substance P.
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Uniprot ID
P16177
Ensembl ID
ENSG00000169836
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
CP0751077
(S)-4-((S)-1-{[(S)-1-({[(S)-1-((S)-1-Carbamoyl-3-methylsulfanyl-propylcarbamoyl)-3-methyl-butylcarbamoyl]-methyl}-carbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-phenyl-ethylcarbamoyl)-4-(oxalyl-amino)-butyric acid
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C39H53N7O11S
 1
1
EC50 = 0.013 nM
   TI
   LI
   LO
   TS
CP0088817
(S)-N-((S)-1-{[(S)-1-({[(S)-1-((S)-1-Carbamoyl-3-methylsulfanyl-propylcarbamoyl)-3-methyl-butylcarbamoyl]-methyl}-carbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-phenyl-ethyl)-3-(3-carboxy-propionylamino)-succinamic acid
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C40H55N7O11S
 2
1
EC50 = 0.023 nM
   TI
   LI
   LO
   TS
2
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0402314
[(1S)-2-methyl-1-phenylpropyl] N-[(2R)-1-[7-(carbamoylamino)heptylamino]-3-(2,3-difluorophenyl)-2-methyl-1-oxopropan-2-yl]carbamate
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C29H40F2N4O4
 1
1
IC50 = 30 nM
   TI
   LI
   LO
   TS
CP0373658
[(1S)-2-methyl-1-phenylpropyl] N-[(2R)-1-[7-(carbamoylamino)heptylamino]-3-(2-fluorophenyl)-2-methyl-1-oxopropan-2-yl]carbamate
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C29H41FN4O4
 1
1
IC50 = 83 nM
   TI
   LI
   LO
   TS
CP0409470
tert-butyl N-[(2S)-1-[[(2R)-1-[7-(carbamoylamino)heptylamino]-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate
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C32H47N5O5
 1
1
IC50 = 1730 nM
   TI
   LI
   LO
   TS
CP0507580
tert-butyl N-[(2S)-1-[[(2R)-1-(8-hydroxyoctylamino)-2-methyl-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate
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C32H47N3O5
 1
1
IC50 = 2790 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0088817
(S)-N-((S)-1-{[(S)-1-({[(S)-1-((S)-1-Carbamoyl-3-methylsulfanyl-propylcarbamoyl)-3-methyl-butylcarbamoyl]-methyl}-carbamoyl)-2-phenyl-ethyl]-methyl-carbamoyl}-2-phenyl-ethyl)-3-(3-carboxy-propionylamino)-succinamic acid
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C40H55N7O11S
 1
1 EC50 = 13 nM
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01199 Neuromedin-K receptor Homo sapiens, Human