Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T62449 Target Info
Target Name Checkpoint kinase-1 (CHK1)
Synonyms
Serine/threonine-protein kinase Chk1; Chk1; Cell cycle checkpoint kinase; CHK1 checkpoint homolog
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Target Type Clinical trial Target
Gene Name CHEK1
Biochemical Class Kinase
UniProt ID
CHK1_HUMAN
Co-Targets of This Target  Top
Co-Target Name Fms-like tyrosine kinase 3 (FLT-3) Successful Target
UniProt ID FLT3_HUMAN
Gene Name FLT3
Synonyms
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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Representative Drug(s) LY2606368 Drug Info IC50 = 385.98 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 Serine/threonine-protein kinase Chk2 (RAD53) Clinical trial Target
UniProt ID CHK2_HUMAN
Gene Name CHEK2
Synonyms
hCds1; Hucds1; Checkpoint kinase 2; Cds1 homolog; Cds1; CHK2 checkpoint homolog; CHK2
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Representative Drug(s) AZD7762 Drug Info IC50 < 10 nM Click to Show More [3]
2 LY2606368 Drug Info IC50 = 32.57 nM [1]
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 [4]
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 [5]
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 [6]
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 [6]
Co-Target Name AMP-activated protein kinase (AMPK) Clinical trial Target
UniProt ID AAPK1_HUMAN; AAKB1_HUMAN; AAKG1_HUMAN
Gene Name PRKAA1; PRKAB1; PRKAG1
Synonyms
AMPK; 5'-AMP-activated protein kinase
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Representative Drug(s) LY2606368 Drug Info IC50 = 101.62 nM [1]
Co-Target Name Ribosomal protein S6 kinase beta-1 (S6K1) Clinical trial Target
UniProt ID KS6B1_HUMAN
Gene Name RPS6KB1
Synonyms
p70-S6K 1; p70 ribosomal S6 kinase alpha; p70 S6KA; p70 S6K-alpha; p70 S6 kinase alpha; Serine/threonine-protein kinase 14A; STK14A; S6K-beta-1; S6K; Ribosomal protein S6 kinase I; P70S6K1; P70-S6K; 70 kDa ribosomal protein S6 kinase 1
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Representative Drug(s) LY2606368 Drug Info IC50 = 382.18 nM [1]
References  Top
REF 1 Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies. Eur J Med Chem. 2019 Jul 1;173:44-62.
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 Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas. J Med Chem. 2012 Jun 14;55(11):5130-42.
REF 4 Pharmacophore identification of Raf-1 kinase inhibitors. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2346-50.
REF 5 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 6 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.

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