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TargetGonadotropin-releasing hormone receptor
LigandBDBM50162019
Substrate/Competitorn/a
Meas. Tech.ChEMBL_302845 (CHEMBL827890)
Ki 53±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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BDBM50162019
n/a
NameBDBM50162019
Synonyms:3-((R)-2-Amino-2-phenyl-ethyl)-1-benzyl-5-(2-fluoro-phenyl)-6-methyl-1H-pyrimidine-2,4-dione | CHEMBL434906
TypeSmall organic molecule
Emp. Form.C26H24FN3O2
Mol. Mass.429.4861
SMILESCc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 |wD:14.15,(3.95,-1.61,;2.61,-.84,;2.61,.7,;3.95,1.47,;5.27,.69,;6.61,1.46,;6.61,3,;5.27,3.77,;3.95,3,;2.61,3.77,;1.28,1.49,;1.28,3.03,;-.04,.7,;-1.38,1.47,;-2.7,.69,;-2.7,-.85,;-4.05,1.46,;-5.37,.69,;-6.71,1.45,;-6.71,3,;-5.38,3.77,;-4.05,3,;-.04,-.84,;-1.38,-1.61,;1.28,-1.59,;1.28,-3.13,;-.04,-3.9,;-1.38,-3.13,;-2.72,-3.9,;-2.72,-5.44,;-1.37,-6.21,;-.04,-5.44,)|
Structure
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