General Information of DTT (ID: TTRSMW9)

DTT Name Glycogen synthase kinase-3 beta (GSK-3B) DTT Info
Gene Name GSK3B

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Clinical Trial Drug(s)
Patented Agent(s)
Investigative Drug(s)
6 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMO-02 DMJRU3A Myotonic dystrophy 8C71.0 Phase 2/3 [1]
9-ING-41 DM57TY3 Myelofibrosis 2A20.2 Phase 2 [2]
Lithium DMZ3OU6 Bipolar disorder 6A60 Phase 2 [3]
LY2090314 DMTBFE4 Acute myeloid leukaemia 2A60 Phase 2 [4]
Tideglusib DME4LA1 Alzheimer disease 8A20 Phase 2 [5]
Neu-120 DMXKOUC Parkinson disease 8A00.0 Phase 1/2 [6]
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⏷ Show the Full List of 6 Clinical Trial Drug(s)
5 Patented Agent(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AR-A014418 DMUPN01 Ovarian cancer 2C73 Patented [7]
CHIR-99021 DMB8MNU Allergic inflammation 4A80-4A85 Patented [8]
KENPAULLONE DMAGVXW Discovery agent N.A. Patented [9]
PMID26161698-Compound-18 DM6JVR5 N. A. N. A. Patented [10]
TDZD-8 DMG6Q45 Malignant glioma 2A00.0 Patented [11]
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3 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
AZD-1080 DMIM9N1 Alzheimer disease 8A20 Discontinued in Phase 1 [12]
RO-320432 DMFZ1YW N. A. N. A. Terminated [13]
SAN-61 DMGUA9Y Alzheimer disease 8A20 Terminated [14]
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74 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
(2'Z,3'E)-7-Azaindirubin-3'-oxime DMUIOAP Discovery agent N.A. Investigative [15]
(E)-N-(6-(prop-1-enyl)-1H-indazol-3-yl)butyramide DMHKXPM Discovery agent N.A. Investigative [16]
12,13-DEHYDRO-8-O-ACETYLMANZAMINE A DMVP39I Discovery agent N.A. Investigative [17]
12,13-DEHYDROMANZAMINE A DM8XAWU Discovery agent N.A. Investigative [17]
3-(6-(phenylamino)-9H-purin-8-yl)benzonitrile DM8WL21 Discovery agent N.A. Investigative [18]
3-phenyl-4-(phenylamino)-1H-pyrrole-2,5-dione DM6T5K4 Discovery agent N.A. Investigative [19]
4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole DMN9YOB Discovery agent N.A. Investigative [20]
4-(5-bromo-1H-indol-3-yl)pyrimidin-2-amine DMJKUQI Discovery agent N.A. Investigative [7]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol DMSKJ1X Discovery agent N.A. Investigative [21]
6-deoxymanzamine X DMKPWN0 Discovery agent N.A. Investigative [17]
8-O-(4-bromobenzenesulfonyl)manzamine F DMDRPLA Discovery agent N.A. Investigative [17]
8-O-(4-chlorobenzenesulfonyl)manzamine F DM48JMC Discovery agent N.A. Investigative [17]
8-O-(4-toluenesulfonyl)manzamine A DM249GI Discovery agent N.A. Investigative [17]
8-OH-MANZAMINE A DM4QYEF Discovery agent N.A. Investigative [22]
9-N-ETHYL-8-ETHOXY-MANZAMINE A DMPXLEU Discovery agent N.A. Investigative [17]
9-N-METHYL-8-METHOXY-MANZAMINE A DM1YUBX Discovery agent N.A. Investigative [17]
alsterpaullone 2-cyanoethyl DMDI2KH Discovery agent N.A. Investigative [23]
AMP-PNP DMTOK1D Discovery agent N.A. Investigative [24]
AS-601245 DMQ95EB Discovery agent N.A. Investigative [25]
AZAKENPAULLONE DM61H07 Discovery agent N.A. Investigative [9]
Bisindolylmaleimide-I DMOQJZC Discovery agent N.A. Investigative [26]
BX-795 DMRIMLJ Discovery agent N.A. Investigative [27]
BX-912 DMZA45C Discovery agent N.A. Investigative [27]
CHIR-98014 DMVEBT6 Discovery agent N.A. Investigative [8]
CHIR-98023 DMFBW1H Discovery agent N.A. Investigative [7]
CI-1040 DMF3DZX Discovery agent N.A. Investigative [26]
CP-70949 DMBQTZG Diabetic complication 5A2Y Investigative [28]
CT-98024 DM6F8DM Discovery agent N.A. Investigative [13]
DM-204 DMSXI6W Solid tumour/cancer 2A00-2F9Z Investigative [28]
ELLAGIC ACID DMX8BS5 Discovery agent N.A. Investigative [29]
GSK-3beta inhibitor II DMQR7TZ Discovery agent N.A. Investigative [30]
GSK-3beta inhibitor XI DM734QB Discovery agent N.A. Investigative [31]
I-5 DM1TQ7N Discovery agent N.A. Investigative [32]
IM-12 DM58DGY Discovery agent N.A. Investigative [33]
indirubin deriv. 8a DMYLVQF Discovery agent N.A. Investigative [34]
K00244 DM2BKU8 Discovery agent N.A. Investigative [35]
L-779450 DM51B74 Discovery agent N.A. Investigative [36]
LEUCETTAMINE B DMFQEWM Discovery agent N.A. Investigative [37]
MANZAMINE A DMB3GNC Discovery agent N.A. Investigative [38]
Manzamine E DMOI9RT Discovery agent N.A. Investigative [22]
Manzamine Y DMC7ADZ N. A. N. A. Investigative [22]
N,8-diphenyl-9H-purin-6-amine DMZXF36 Discovery agent N.A. Investigative [18]
N-(6-(2-chlorophenyl)-1H-indazol-3-yl)butyramide DMDCX5O Discovery agent N.A. Investigative [16]
N-(6-(3-hydroxyphenyl)-1H-indazol-3-yl)butyramide DMKGBZA Discovery agent N.A. Investigative [16]
N-(6-(4-aminophenyl)-1H-indazol-3-yl)butyramide DMDQEZG Discovery agent N.A. Investigative [16]
N-(6-(4-fluorophenyl)-1H-indazol-3-yl)butyramide DM4M12J Discovery agent N.A. Investigative [16]
N-(6-(4-hydroxyphenyl)-1H-indazol-3-yl)butyramide DM8JLR4 Discovery agent N.A. Investigative [16]
N-(6-(furan-3-yl)-1H-indazol-3-yl)butyramide DMRGQTM Discovery agent N.A. Investigative [16]
N-(6-(pyridin-3-yl)-1H-indazol-3-yl)butyramide DM3FOKL Discovery agent N.A. Investigative [39]
N-(6-(pyridin-4-yl)-1H-indazol-3-yl)butyramide DM4GRK8 Discovery agent N.A. Investigative [16]
N-(6-(thiophen-3-yl)-1H-indazol-3-yl)butyramide DMNRSYP Discovery agent N.A. Investigative [16]
N-(6-(trifluoromethyl)-1H-indazol-3-yl)butyramide DMMHD9Z Discovery agent N.A. Investigative [16]
N-(6-benzyl-1H-indazol-3-yl)butyramide DM0OCLU Discovery agent N.A. Investigative [16]
N-(6-bromo-1H-indazol-3-yl)butyramide DMJPL7E Discovery agent N.A. Investigative [16]
N-(6-chloro-1H-indazol-3-yl)butyramide DMHGXPY Discovery agent N.A. Investigative [16]
N-(6-chloro-5-p-tolyl-1H-indazol-3-yl)butyramide DMIN128 Discovery agent N.A. Investigative [16]
N-(6-chloro-5-phenyl-1H-indazol-3-yl)butyramide DMJV3UO Discovery agent N.A. Investigative [39]
N-(6-phenethyl-1H-indazol-3-yl)butyramide DM9K4WP Discovery agent N.A. Investigative [16]
N-(6-phenyl-1H-indazol-3-yl)butyramide DMVCPLU Discovery agent N.A. Investigative [39]
N-(8-(3-cyanophenyl)-9H-purin-6-yl)pentanamide DMHFPE3 Discovery agent N.A. Investigative [18]
Neo-kauluamine DM6D0JC Discovery agent N.A. Investigative [22]
NU-6102 DMMOFKD Discovery agent N.A. Investigative [40]
PAULLONE DMQA8N3 Discovery agent N.A. Investigative [13]
PF-228 DM32FKD Discovery agent N.A. Investigative [41]
PMID19115845C89S DMB9F2L Discovery agent N.A. Investigative [42]
PYRAZOLOPYRIDAZINE 1 DMKTB5U Discovery agent N.A. Investigative [43]
PYRAZOLOPYRIDAZINE 2 DMI7AUJ Discovery agent N.A. Investigative [43]
Quinoxaline1 DMRWXH4 Discovery agent N.A. Investigative [23]
RGB-286147 DMP08BY Discovery agent N.A. Investigative [23]
Ro31-8220 DMDJLF0 Discovery agent N.A. Investigative [26]
SB-415286 DMMAL3I Discovery agent N.A. Investigative [7]
STAUROSPORINONE DMU2H4K Discovery agent N.A. Investigative [26]
Thieno analogue of kenpaullone DMIOTHG Discovery agent N.A. Investigative [9]
TWS-119 DMS29M4 Discovery agent N.A. Investigative [44]
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⏷ Show the Full List of 74 Investigative Drug(s)
Molecule Interaction Atlas

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer. Sci Rep. 2019 Dec 27;9(1):19977.
3 The GSK3 kinase inhibitor lithium produces unexpected hyperphosphorylation of -catenin, a GSK3 substrate, in human glioblastoma cells. Biol Open. 2018 Jan 26;7(1):bio030874.
4 Glycogen synthase kinase 3 (GSK-3) inhibitors: a patent update (2014-2015).Expert Opin Ther Pat. 2017 Jun;27(6):657-666.
5 Evidence for irreversible inhibition of glycogen synthase kinase-3beta by tideglusib. J Biol Chem. 2012 Jan 6;287(2):893-904.
6 Company report (Neurim Pharmaceuticals)
7 Fragment and knowledge-based design of selective GSK-3beta inhibitors using virtual screening models. Eur J Med Chem. 2009 Jun;44(6):2361-71.
8 Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.
9 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.
10 Cyclin-dependent kinase inhibitors for cancer therapy: a patent review (2009 - 2014).Expert Opin Ther Pat. 2015;25(9):953-70.
11 Identification of novel scaffold of benzothiazepinones as non-ATP competitive glycogen synthase kinase-3beta inhibitors through virtual screening. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7232-6.
12 AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.J Neurochem.2013 May;125(3):446-56.
13 Discovery of potent and bioavailable GSK-3beta inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1693-6.
14 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029796)
15 Synthesis and antiproliferative activity of 7-azaindirubin-3'-oxime, a 7-aza isostere of the natural indirubin pharmacophore. J Nat Prod. 2009 Dec;72(12):2199-202.
16 Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1985-9.
17 Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for ... J Nat Prod. 2007 Sep;70(9):1397-405.
18 Novel 8-arylated purines as inhibitors of glycogen synthase kinase. Eur J Med Chem. 2010 Aug;45(8):3389-93.
19 Novel GSK-3beta inhibitors from sequential virtual screening. Bioorg Med Chem. 2008 Jan 15;16(2):636-43.
20 Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. J Med Chem. 2004 Dec 2;47(25):6239-47.
21 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006 Nov 2;49(22):6500-9.
22 Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical p... J Nat Prod. 2006 Jul;69(7):1034-40.
23 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
24 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
25 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
26 Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105.
27 Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74.
28 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2030).
29 Identification of ellagic acid as potent inhibitor of protein kinase CK2: a successful example of a virtual screening application. J Med Chem. 2006 Apr 20;49(8):2363-6.
30 Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors. Bioorg Med Chem Lett. 2002 Jun 3;12(11):1525-8.
31 Design, synthesis, and biological evaluation of novel 7-azaindolyl-heteroaryl-maleimides as potent and selective glycogen synthase kinase-3beta (GSK-3beta) inhibitors. Bioorg Med Chem. 2004 Jun 15;12(12):3167-85.
32 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
33 Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. Bioorg Med Chem. 2010 Sep 15;18(18):6785-95.
34 Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. J Med Chem. 2004 Feb 12;47(4):935-46.
35 The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett. 2009 Jul 1;19(13):3586-92.
36 The identification of potent and selective imidazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2006 Jan 15;16(2):378-81.
37 Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors. Eur J Med Chem. 2010 Feb;45(2):805-10.
38 2-N-Methyl modifications and SAR studies of manzamine A. Bioorg Med Chem. 2008 Jul 15;16(14):6702-6.
39 Design of potent and selective GSK3beta inhibitors with acceptable safety profile and pharmacokinetics. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2344-9.
40 Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1353-7.
41 Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.
42 First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery. J Med Chem. 2009 Jan 22;52(2):293-307.
43 N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular effi... J Med Chem. 2004 Sep 9;47(19):4716-30.
44 Diversity-oriented synthesis: exploring the intersections between chemistry and biology. Nat Chem Biol. 2005 Jul;1(2):74-84.