Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T70977 Target Info
Target Name Glycogen synthase kinase-3 beta (GSK-3B)
Synonyms
Serine/threonine-protein kinase GSK3B; GSK-3 beta
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Target Type Clinical trial Target
Gene Name GSK3B
Biochemical Class Kinase
UniProt ID
GSK3B_HUMAN
Co-Targets of This Target  Top
Co-Target Name Glycogen synthase kinase-3 alpha (GSK-3A) Successful Target
UniProt ID GSK3A_HUMAN
Gene Name GSK3A
Synonyms
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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Representative Drug(s) Drug Info IC50 = 1.02 nM [1]
Co-Target Name ERK activator kinase 1 (MEK1) Clinical trial Target
UniProt ID MP2K1_HUMAN
Gene Name MAP2K1
Synonyms
PRKMK1; Mitogen-activated protein kinase kinase 1; MKK1; MEK 1; MAPKK 1; MAPK/ERKkinase 1; MAPK/ERK kinase 1; MAP kinase kinase 1; Dual specificity mitogen-activated protein kinase kinase 1
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Representative Drug(s) CI-1040 Drug Info IC50 = 2 nM [2]
Co-Target Name Proto-oncogene c-RAF (c-RAF) Clinical trial Target
UniProt ID RAF1_HUMAN
Gene Name RAF1
Synonyms
cRaf; Raf-1; RAF proto-oncogene serine/threonine-protein kinase; RAF
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Representative Drug(s) CI-1040 Drug Info IC50 = 12 nM [3]
Co-Target Name ERK activator kinase 2 (MEK2) Clinical trial Target
UniProt ID MP2K2_HUMAN
Gene Name MAP2K2
Synonyms
PRKMK2; MKK2; MEK 2; MAPKK 2; MAPK/ERK kinase 2; MAP kinase kinase 2; Dual specificity mitogenactivated protein kinase kinase 2; Dual specificity mitogen-activated protein kinase kinase 2
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Representative Drug(s) CI-1040 Drug Info IC50 = 16 nM [4]
Co-Target Name Casein kinase II alpha (CSNK2A1) Clinical trial Target
UniProt ID CSK21_HUMAN
Gene Name CSNK2A1
Synonyms
Protein kinase CK2; Casein kinase II subunit alpha; CK2A1; CK II alpha; CK II
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Representative Drug(s) CI-1040 Drug Info IC50 = 17 nM [5]
Co-Target Name Casein kinase II (CSNK2) Clinical trial Target
UniProt ID CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN
Gene Name NO-GeName
Representative Drug(s) CI-1040 Drug Info EC50 = 100 nM [5]
Co-Target Name Protein kinase C beta (PRKCB) Clinical trial Target
UniProt ID KPCB_HUMAN
Gene Name PRKCB
Synonyms
Protein kinase C beta type; PRKCB1; PKCB; PKC-beta; PKC-B
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Representative Drug(s) Drug Info IC50 = 420 nM [6]
References  Top
REF 1 Discovery of novel glycogen synthase kinase-3alpha inhibitors: Structure-based virtual screening, preliminary SAR and biological evaluation for treatment of acute myeloid leukemia. Eur J Med Chem. 2019 Jun 1;171:221-234.
REF 2 Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3031-4.
REF 3 Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50.
REF 4 4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase. J Med Chem. 2007 Oct 18;50(21):5090-102.
REF 5 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. J Med Chem. 2019 Feb 28;62(4):1817-1836.
REF 6 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. 2004 Jul 29;47(16):3934-7.

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