Target
Glycogen synthase kinase-3 beta
Ligand
BDBM188515
Substrate
n/a
Meas. Tech.
Mobility Shift Microfluidics Assay
pH
7.5±n/a
Temperature
298.15±n/a K
IC50
5± 3 nM
Comments
extracted
Citation
 Wagner, FFBishop, JAGale, JPShi, XWalk, MKetterman, JPatnaik, DBarker, DWalpita, DCampbell, AJNguyen, SLewis, MRoss, LWeïwer, MAn, WFGermain, ARNag, PPMetkar, SKaya, TDandapani, SOlson, DEBarbe, ALLazzaro, FSacher, JRCheah, JHFei, DPerez, JMunoz, BPalmer, MStegmaier, KSchreiber, SLScolnick, EZhang, YLHaggarty, SJHolson, EBPan, JQ Inhibitors of Glycogen Synthase Kinase 3 with Exquisite Kinome-Wide Selectivity and Their Functional Effects. ACS Chem Biol 11:1952-63 (2016) [PubMed]  Article 
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:
BDBM188515
Synonyms:
(S)-3-cyclopropyl-4,7,7-trimethyl-4-phenyl-2,4,6,7,8,9-hexahydro-5H-pyrazolo[3,4-b]quinolin-5-one (BRD0209) | US10137122, Compound 114
Type:
Small organic molecule
Emp. Form.:
C22H25N3O
Mol. Mass.:
347.4534
SMILES:
CC1(C)CC(=O)C2=C(C1)Nc1n[nH]c(C3CC3)c1[C@]2(C)c1ccccc1 |r,c:6|
Structure:
Search PDB for entries with ligand similarity: