Co-Target(s) Information
Target General Information | Top | ||||
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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 |
Co-Targets of This Target | Top | |||||
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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) | LY2090314 | 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) | LY2090314 | Drug Info | IC50 = 420 nM | [6] |
References | Top | ||||
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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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