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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM188512
Substrate
n/a
Meas. Tech.
ADP Glo Assay Protocol
IC50
<100±n/a nM
Citation
Wagner, FF; Pan, JQ; Dandapani, S; Germain, A; Holson, E; Munoz, B; Nag, PP; Lewis, MC; Haggarty, SJ; Bishop, JA; Stegmaier, K; Weiwer, M; Banerji, V Kinase inhibitors and methods of use thereof US Patent US10137122 Publication Date 11/27/2018
More Info.:
Target
Name:
Glycogen synthase kinase-3 beta
Synonyms:
GSK-3 beta | GSK-3, beta | GSK3B | GSK3B_HUMAN | Glycogen synthase kinase 3 beta (GSK3B) | Glycogen synthase kinase 3-beta (GSK3B) | Glycogen synthase kinase-3 beta (GSK-3B) | Glycogen synthase kinase-3 beta (GSK3 Beta) | Glycogen synthase kinase-3 beta (GSK3B) | Glycogen synthase kinase-3B (GSK-3B) | Glycogen synthase kinase-3beta (GSK3B) | Serine/threonine-protein kinase GSK3B
Type:
Enzyme
Mol. Mass.:
46756.38
Organism:
Homo sapiens (Human)
Description:
P49841
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST
Inhibitor
Name:
BDBM188512
Synonyms:
(R)-4-(2-methoxyphenyl)-7,7-dimethyl-3-(trifluoromethyl)-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one (BRD1172) | US10137122, Compound 54
Type:
Small organic molecule
Emp. Form.:
C20H20F3N3O2
Mol. Mass.:
391.3869
SMILES:
COc1ccccc1[C@H]1c2c(NC3=C1C(=O)CC(C)(C)C3)n[nH]c2C(F)(F)F |r,c:13|