Co-Target(s) Information
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 |
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
Click to Show/Hide
|
|||||
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
Click to Show/Hide
|
|||||
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
Click to Show/Hide
|
|||||
Representative Drug(s) | Trametinib | 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
Click to Show/Hide
|
|||||
Representative Drug(s) | Trametinib | 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 | Selumetinib | 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
Click to Show/Hide
|
|||||
Representative Drug(s) | Trametinib | 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
Click to Show/Hide
|
|||||
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
Click to Show/Hide
|
|||||
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. |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.