Target
Neuromedin-K receptor
Ligand
BDBM362842
Substrate
n/a
Meas. Tech.
Binding Competition Assay
Ki
52.0±n/a nM
Citation
 Hoveyda, HDutheuil, GFraser, G N-acyl-(3-substituted)-(8-methyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a] pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders US Patent  US9840508 Publication Date 12/12/2017 
Target
Name:
Neuromedin-K receptor
Synonyms:
NK-3 receptor | NK-3R | NK3R | NK3R_HUMAN | NKR | Neurokinin 3 receptor | Neurokinin B receptor | Neurokinin-3 (NK-3) | Neuromedin-3 receptor (NK-3R) | Neuromedin-3 receptor (NK3) | Neuromedin-K receptor | Neuromedin-K receptor (NK-3 receptor) | Neuromedin-K receptor (NK3) | Neuromedin-K receptor(NK3R) | TAC3R | TACR3 | Tachykinin receptor 3 | Tachykinin receptor 3 (NK3)
Type:
Enzyme
Mol. Mass.:
52221.96
Organism:
Homo sapiens (Human)
Description:
P29371
Residue:
465
Sequence:
MATLPAAETWIDGGGGVGADAVNLTASLAAGAATGAVETGWLQLLDQAGNLSSSPSALGLPVASPAPSQPWANLTNQFVQPSWRIALWSLAYGVVVAVAVLGNLIVIWIILAHKRMRTVTNYFLVNLAFSDASMAAFNTLVNFIYALHSEWYFGANYCRFQNFFPITAVFASIYSMTAIAVDRYMAIIDPLKPRLSATATKIVIGSIWILAFLLAFPQCLYSKTKVMPGRTLCFVQWPEGPKQHFTYHIIVIILVYCFPLLIMGITYTIVGITLWGGEIPGDTCDKYHEQLKAKRKVVKMMIIVVMTFAICWLPYHIYFILTAIYQQLNRWKYIQQVYLASFWLAMSSTMYNPIIYCCLNKRFRAGFKRAFRWCPFIKVSSYDELELKTTRFHPNRQSSMYTVTRMESMTVVFDPNDADTTRSSRKKRATPRDPSFNGCSRRNSKSASATSSFISSPYTSVDEYS
  
Inhibitor
Name:
BDBM362842
Synonyms:
(R)-(8-methyl-3-(5- methylfuran-2-yl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl)(2,3,4,5- tetrafluorophenyl)methanone | US9840508, Compound 4
Type:
Small organic molecule
Emp. Form.:
C18H14F4N4O2
Mol. Mass.:
394.323
SMILES:
C[C@H]1N(CCn2c1nnc2-c1ccc(C)o1)C(=O)c1cc(F)c(F)c(F)c1F |r|
Structure:
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