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Target
Gonadotropin-releasing hormone receptor
Ligand
BDBM405266
Substrate
n/a
Meas. Tech.
Activity Assay
IC50
1.46±n/a nM
Citation
 Lu, H; Sun, P; Gui, B; Dong, Q Pyrazolopyrimidone or Pyrrolotriazone derivatives, method of preparing same, and pharmaceutical applications thereof US Patent  US10344034 Publication Date 7/9/2019 
Target
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:
MANSASPEQNQNHCSAINNSIPLMQGNLPTLTLSGKIRVTVTFFLFLLSATFNASFLLKLQKWTQKKEKGKKLSRMKLLLKHLTLANLLETLIVMPLDGMWNITVQWYAGELLCKVLSYLKLFSMYAPAFMMVVISLDRSLAITRPLALKSNSKVGQSMVGLAWILSSVFAGPQLYIFRMIHLADSSGQTKVFSQCVTHCSFSQWWHQAFYNFFTFSCLFIIPLFIMLICNAKIIFTLTRVLHQDPHELQLNQSKNNIPRARLKTLKMTVAFATSFTVCWTPYYVLGIWYWFDPEMLNRLSDPVNHFFFLFAFLNPCFDPLIYGYFSL
  
Inhibitor
Name:
BDBM405266
Synonyms:
1-(4-(7-(2,6-difluorobenzyl)-3-((dimethylamino)methyl)-5-(2-fluoro-3-methoxyphenyl)-4,6-dioxo-4,5,6,7-tetrahydro-2H-pyrazolo[3,4-d]pyrimidin-2-yl)phenyl)-3-methoxyurea | US10344034, Example 2 | US10633388, Example 2
Type:
Small organic molecule
Emp. Form.:
C30H28F3N7O5
Mol. Mass.:
623.5824
SMILES:
CONC(=O)Nc1ccc(cc1)-n1nc2n(Cc3c(F)cccc3F)c(=O)n(-c3cccc(OC)c3F)c(=O)c2c1CN(C)C |(-10.58,-1.9,;-9.04,-1.9,;-8.27,-.56,;-6.73,-.56,;-5.96,-1.9,;-5.96,.77,;-4.42,.77,;-3.65,-.56,;-2.11,-.56,;-1.34,.77,;-2.11,2.1,;-3.65,2.1,;.2,.77,;1.11,-.48,;2.57,0,;3.91,-.77,;3.91,-2.31,;5.24,-3.08,;6.57,-2.31,;7.91,-1.54,;7.91,-3.08,;7.91,-4.62,;6.57,-5.39,;5.24,-4.62,;3.91,-5.39,;5.24,0,;6.57,-.77,;5.24,1.54,;6.57,2.31,;6.57,3.85,;7.91,4.62,;9.24,3.85,;9.24,2.31,;10.58,1.54,;10.58,0,;7.91,1.54,;7.91,0,;3.91,2.31,;3.91,3.85,;2.57,1.54,;1.11,2.02,;.71,3.5,;-.78,3.9,;-1.18,5.39,;-1.87,2.81,)|
Structure:
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