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Target
Glycogen synthase kinase-3 beta
Ligand
BDBM50150698
Substrate
n/a
Meas. Tech.
ChEMBL_305251 (CHEMBL833508)
IC50
1.3±n/a nM
Citation
Engler, TA; Henry, JR; Malhotra, S; Cunningham, B; Furness, K; Brozinick, J; Burkholder, TP; Clay, MP; Clayton, J; Diefenbacher, C; Hawkins, E; Iversen, PW; Li, Y; Lindstrom, TD; Marquart, AL; McLean, J; Mendel, D; Misener, E; Briere, D; O'Toole, JC; Porter, WJ; Queener, S; Reel, JK; Owens, RA; Brier, RA; Eessalu, TE; Wagner, JR; Campbell, RM; Vaughn, R Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. J Med Chem 47:3934-7 (2004) [PubMed] Article
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:
Human
Description:
P49841
Residue:
420
Sequence:
MSGRPRTTSFAESCKPVQQPSAFGSMKVSRDKDGSKVTTVVATPGQGPDRPQEVSYTDTKVIGNGSFGVVYQAKLCDSGELVAIKKVLQDKRFKNRELQIMRKLDHCNIVRLRYFFYSSGEKKDEVYLNLVLDYVPETVYRVARHYSRAKQTLPVIYVKLYMYQLFRSLAYIHSFGICHRDIKPQNLLLDPDTAVLKLCDFGSAKQLVRGEPNVSYICSRYYRAPELIFGATDYTSSIDVWSAGCVLAELLLGQPIFPGDSGVDQLVEIIKVLGTPTREQIREMNPNYTEFKFPQIKAHPWTKVFRPRTPPEAIALCSRLLEYTPTARLTPLEACAHSFFDELRDPNVKLPNGRDTPALFNFTTQELSSNPPLATILIPPHARIQAAASTPTNATAASDANTGDRGQTNNAASASASNST
Inhibitor
Name:
BDBM50150698
Synonyms:
3-(imidazo[1,2-a]pyridin-3-yl)-4-(2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-1H-pyrrole-2,5-dione | 3-Imidazo[1,2-a]pyridin-3-yl-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl]-pyrrole-2,5-dione | CHEMBL178737
Type:
Small organic molecule
Emp. Form.:
C27H24N6O4
Mol. Mass.:
496.5173
SMILES:
O=C(N1CCOCC1)N1CCn2cc(C3=C(C(=O)NC3=O)c3cnc4ccccn34)c3cccc(C1)c23 |t:15|