Target
Glycogen synthase kinase-3 alpha
Ligand
BDBM345143
Substrate
n/a
Meas. Tech.
Enzyme Inhibition
IC50
244±n/a nM
Citation
 Fyfe, MCMeghani, PThom, SM Kinase inhibitors US Patent  US9783556 Publication Date 10/10/2017 
Target
Name:
Glycogen synthase kinase-3 alpha
Synonyms:
GSK-3 alpha | GSK3A | GSK3A_HUMAN | Glycogen synthase kinase 3 alpha (GSKalpha) | Glycogen synthase kinase-3 | Glycogen synthase kinase-3 alpha | Glycogen synthase kinase-3 alpha (GSK3 Alpha) | Glycogen synthase kinase-3 alpha (GSK3A) | Glycogen synthase kinase-3 alpha (GSK3alpha)
Type:
Enzyme
Mol. Mass.:
50991.79
Organism:
Homo sapiens (Human)
Description:
P49840
Residue:
483
Sequence:
MSGGGPSGGGPGGSGRARTSSFAEPGGGGGGGGGGPGGSASGPGGTGGGKASVGAMGGGVGASSSGGGPGGSGGGGSGGPGAGTSFPPPGVKLGRDSGKVTTVVATLGQGPERSQEVAYTDIKVIGNGSFGVVYQARLAETRELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDELYLNLVLEYVPETVYRVARHFTKAKLTIPILYVKVYMYQLFRSLAYIHSQGVCHRDIKPQNLLVDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFKSRTPPEAIALCSSLLEYTPSSRLSPLEACAHSFFDELRCLGTQLPNNRPLPPLFNFSAGELSIQPSLNAILIPPHLRSPAGTTTLTPSSQALTETPTSSDWQSTDATPTLTNSS
  
Inhibitor
Name:
BDBM345143
Synonyms:
1-(4-((2-((7-Methyl-1H-indazol-5-yl)amino)pyrimidin-4-yl)oxy)naphthalen-1-yl)-3-(1-(4-(2-morpholinoethoxy)phenyl)-3-(trimethylsilyl)-1H-pyrazol-5-yl)urea | US9783556, Example 15
Type:
Small organic molecule
Emp. Form.:
C41H44N10O4Si
Mol. Mass.:
768.9382
SMILES:
Cc1cc(Nc2nccc(Oc3ccc(NC(=O)Nc4cc(nn4-c4ccc(OCCN5CCOCC5)cc4)[Si](C)(C)C)c4ccccc34)n2)cc2cn[nH]c12
Structure:
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