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TargetGonadotropin-releasing hormone receptor
LigandBDBM50161500
Substrate/Competitorn/a
Meas. Tech.ChEMBL_302845 (CHEMBL827890)
Ki 2.3±n/a nM
Citation Tucci, FCZhu, YFStruthers, RSGuo, ZGross, TDRowbottom, MWAcevedo, OGao, YSaunders, JXie, QReinhart, GJLiu, XJLing, NBonneville, AKChen, TBozigian, HChen, C 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization. J Med Chem48:1169-78 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Gonadotropin-releasing hormone receptor
Name:Gonadotropin-releasing hormone receptor
Synonyms:GNRHR | GNRHR_HUMAN | GRHR | GnRH receptor | GnRH-R | Gonadotropin releasing hormone 1 (GnRHR1) | Gonadotropin-releasing hormone receptor | Gonadotropin-releasing hormone receptor (GnRH)
Type:Enzyme
Mol. Mass.:37749.45
Organism:Homo sapiens (Human)
Description:P30968
Residue:328
Sequence:
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKL
QKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYL
KLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRM
IHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTR
VLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRL
SDPVNHFFFLFAFLNPCFDPLIYGYFSL
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  Blast E-value cutoff:
BDBM50161500
n/a
NameBDBM50161500
Synonyms:(R)-1-(2,6-difluorobenzyl)-3-(2-amino-2-phenylethyl)-5-(3-methoxyphenyl)-6-methylpyrimidine-2,4(1H,3H)-dione | 3-((R)-2-Amino-2-phenyl-ethyl)-1-(2,6-difluoro-benzyl)-5-(3-methoxy-phenyl)-6-methyl-1H-pyrimidine-2,4-dione | CHEMBL359894
TypeSmall organic molecule
Emp. Form.C27H25F2N3O3
Mol. Mass.477.5025
SMILESCOc1cccc(c1)-c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O |r|
Structure
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