Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T23003 Target Info
Target Name MAPK/ERK kinase kinase (MAP3K)
Target Type Successful Target
Gene Name NO-GeName
Biochemical Class Kinase
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name Serine/threonine-protein kinase B-raf (BRAF) Successful Target
UniProt ID BRAF_HUMAN
Gene Name BRAF
Synonyms
V-Raf murine sarcoma viral oncogene homolog B1; RAFB1; Proto-oncogene B-Raf; P94; BRAF1; BRAF(V599E); BRAF serine/threonine kinase; B-raf protein; B-Raf
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Representative Drug(s) Cotellic Drug Info IC50 = 1.8 nM Click to Show More [1]
2 PD-0325901 Drug Info IC50 = 6 nM [3]
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) E6201 Drug Info IC50 = 5 nM [2]
Co-Target Name Multidrug resistance protein 1 (ABCB1) Clinical trial Target
UniProt ID MDR1_HUMAN
Gene Name ABCB1
Synonyms
PGY1; P-glycoprotein 1; MDR1; CD243 antigen; CD243; ATP-binding cassette sub-family B member 1
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Representative Drug(s) Drug Info EC50 = 247 nM [4]
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) Drug Info IC50 = 0.7 nM Click to Show More [5]
2 Cotellic Drug Info IC50 = 0.9 nM [6]
3 TAK-733 Drug Info IC50 = 1.79 nM [8]
4 MSC1936369B Drug Info IC50 = 1.81 nM [8]
5 PD-0325901 Drug Info IC50 = 7 nM [9]
6 Drug Info IC50 = 9 nM [10]
7 E6201 Drug Info IC50 = 50 nM [2]
8 RO-5126766 Drug Info IC50 = 160 nM [12]
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) Drug Info IC50 = 1.6 nM Click to Show More [7]
2 PD-0325901 Drug Info IC50 = 110 nM [13]
Co-Target Name Extracellular signal-regulated kinase 2 (ERK2) Clinical trial Target
UniProt ID MK01_HUMAN
Gene Name MAPK1
Synonyms
PRKM2; PRKM1; P42-MAPK; P42 Mitogen-activated protein kinase; Mitogen-activated protein kinase 2; Mitogen-activated protein kinase 1; MAPK 2; MAPK 1; MAP kinase isoform p42; MAP kinase 2; MAP kinase 1; ERT1; ERK-2
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Representative Drug(s) PD-0325901 Drug Info IC50 = 25 nM [11]
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) RO-5126766 Drug Info IC50 = 56 nM [12]
References  Top
REF 1 Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions. Drug Metab Dispos. 2012 May;40(5):919-27.
REF 2 Dual FLT3 inhibitors: Against the drug resistance of acute myeloid leukemia in recent decade. Eur J Med Chem. 2019 Sep 15;178:468-483.
REF 3 Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents. Bioorg Med Chem. 2016 Aug 15;24(16):3472-82.
REF 4 Novel chalcone and flavone derivatives as selective and dual inhibitors of the transport proteins ABCB1 and ABCG2. Eur J Med Chem. 2019 Feb 15;164:193-213.
REF 5 Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors. Eur J Med Chem. 2019 Apr 15;168:315-329.
REF 6 Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973). ACS Med Chem Lett. 2012 Apr 9;3(5):416-21.
REF 7 The effect of a thieno[2,3-b]pyridine PLC-gamma inhibitor on the proliferation, morphology, migration and cell cycle of breast cancer cells. Medchemcomm. 2014;5:99-106.
REF 8 Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2555-9.
REF 9 Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2384-90.
REF 10 Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold. Bioorg Med Chem. 2018 Feb 1;26(3):581-9.
REF 11 Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase. J Med Chem. 2014 Nov 13;57(21):8817-26.
REF 12 Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning. ACS Med Chem Lett. 2014 Jan 22;5(4):309-14.
REF 13 Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911.

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