Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T78874 Target Info
Target Name Protein kinase (PK)
Target Type Clinical trial Target
Gene Name NO-GeName
Biochemical Class Kinase
UniProt ID
NOUNIPROTAC
Co-Targets of This Target  Top
Co-Target Name Vascular endothelial growth factor receptor 2 (KDR) Successful Target
UniProt ID VGFR2_HUMAN
Gene Name KDR
Synonyms
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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Representative Drug(s) MGCD265 Drug Info IC50 = 1 nM Click to Show More [1]
2 MGCD516 Drug Info IC50 = 5 nM [2]
3 ENMD-2076 Drug Info IC50 = 10 nM [3]
Co-Target Name Proto-oncogene c-Met (MET) Successful Target
UniProt ID MET_HUMAN
Gene Name MET
Synonyms
Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase
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Representative Drug(s) MGCD265 Drug Info IC50 = 1 nM Click to Show More [1]
2 LY2801653 Drug Info IC50 = 4.7 nM [2]
3 MGCD516 Drug Info IC50 = 20 nM [4]
Co-Target Name Tropomyosin-related kinase A (TrkA) Successful Target
UniProt ID NTRK1_HUMAN
Gene Name NTRK1
Synonyms
gp140trk; Tyrosine kinase receptor A; Tyrosine kinase receptor; Trk-A; TRKA; TRK1-transforming tyrosine kinase protein; TRK1 transforming tyrosinekinase protein; TRK; P140-TrkA; Neurotrophic tyrosine kinase receptor type 1; NGF-trk receptor type A; MTC; High affinity nerve growth factor receptor
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Representative Drug(s) MGCD516 Drug Info IC50 = 5 nM [2]
Co-Target Name Tyrosine-protein kinase Kit (KIT) Successful Target
UniProt ID KIT_HUMAN
Gene Name KIT
Synonyms
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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Representative Drug(s) MGCD516 Drug Info IC50 = 6 nM Click to Show More [2]
2 ENMD-2076 Drug Info IC50 = 120 nM [6]
Co-Target Name BDNF/NT-3 growth factors receptor (TrkB) Successful Target
UniProt ID NTRK2_HUMAN
Gene Name NTRK2
Synonyms
Tropomyosin-related kinase B; TrkB tyrosine kinase; Trk-B; TRKB; Neurotrophic tyrosine kinase receptor type 2; GP145-TrkB
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Representative Drug(s) MGCD516 Drug Info IC50 = 9 nM [2]
Co-Target Name Platelet-derived growth factor receptor alpha (PDGFRA) Successful Target
UniProt ID PGFRA_HUMAN
Gene Name PDGFRA
Synonyms
RHEPDGFRA; Platelet-derived growth factor receptor 2; Platelet-derived growth factor alpha receptor; PDGFR2; PDGFR-alpha; PDGFR-2; PDGF-R-alpha; CD140a antigen; CD140a; CD140 antigen-like family member A; Alpha-type platelet-derived growth factor receptor; Alpha platelet-derived growth factor receptor
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Representative Drug(s) ENMD-2076 Drug Info IC50 = 10 nM [3]
Co-Target Name Smoothened homolog (SMO) Successful Target
UniProt ID SMO_HUMAN
Gene Name SMO
Synonyms
Smo-D473H; SMOH; Protein Gx
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Representative Drug(s) MGCD265 Drug Info Ki = 41.7 nM [5]
Co-Target Name Fibroblast growth factor receptor 1 (FGFR1) Successful Target
UniProt ID FGFR1_HUMAN
Gene Name FGFR1
Synonyms
c-fgr; bFGF-R-1; bFGF-R; N-sam; HBGFR; Fms-like tyrosine kinase 2; FLT2; FLT-2; FLG; FGFR-1; FGFBR; CEK; CD331 antigen; CD331; Basic fibroblast growth factor receptor 1; BFGFR
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Representative Drug(s) ENMD-2076 Drug Info IC50 = 93 nM [6]
Co-Target Name Debrisoquine 4-hydroxylase (CYP2D6) Successful Target
UniProt ID CP2D6_HUMAN
Gene Name CYP2D6
Synonyms
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) TG02 Drug Info IC50 = 950 nM [7]
Co-Target Name Macrophage-stimulating protein receptor (RON) Clinical trial Target
UniProt ID RON_HUMAN
Gene Name MST1R
Synonyms
p185Ron; Proteintyrosine kinase 8; Macrophagestimulating protein receptor beta chain; Macrophagestimulating protein receptor; MST1R; MSP receptor; CDw136; CD136
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Representative Drug(s) LY2801653 Drug Info IC50 = 1.2 nM [2]
Co-Target Name Macrophage colony-stimulating factor 1 receptor (CSF1R) Clinical trial Target
UniProt ID CSF1R_HUMAN
Gene Name CSF1R
Synonyms
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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Representative Drug(s) ENMD-2076 Drug Info IC50 = 10 nM [3]
Co-Target Name Cyclin dependent kinase 9-Cyclin H complex (CDK9-CCNH) Co-Target
UniProt ID CDK9_HUMAN-CCNH_HUMAN
Gene Name CDK9-CCNH
Representative Drug(s) TG02 Drug Info IC50 = 3 nM Click to Show More [8]
2 TG02 Drug Info IC50 = 3 nM [8]
Co-Target Name Cyclin dependent kinase 3-G1/Sspecific cyclin E1 complex (CDK3-CCNE1) Co-Target
UniProt ID CDK3_HUMAN-CCNE1_HUMAN
Gene Name CDK3-CCNE1
Representative Drug(s) TG02 Drug Info IC50 = 3 nM [9]
Co-Target Name CDK7-Cyclin H-CDK activating kinase assembly factor MAT1 complex (CDK7-CCNH-MNAT1) Co-Target
UniProt ID CDK7_HUMAN-CCNH_HUMAN-MAT1_HUMAN
Gene Name CDK7-CCNH-MNAT1
Representative Drug(s) TG02 Drug Info IC50 = 3 nM [9]
Co-Target Name Cyclin dependent kinase 5-CDK5 activator 1 complex (CDK5-CDK5R1) Co-Target
UniProt ID CDK5_HUMAN-CD5R1_HUMAN
Gene Name CDK5-CDK5R1
Representative Drug(s) TG02 Drug Info IC50 = 4 nM [8]
Co-Target Name Cyclin dependent kinase 2-G1/S specific cyclin E1 complex (CDK2-CCNE1) Co-Target
UniProt ID CDK2_HUMAN-CCNE1_HUMAN
Gene Name CDK2-CCNE1
Representative Drug(s) TG02 Drug Info IC50 = 5 nM [8]
Co-Target Name Cyclin dependent kinase 1-G2/mitotic specific cyclin B1 complex (CDK1-CCNB1) Co-Target
UniProt ID CDK1_HUMAN-CCNB1_HUMAN
Gene Name CDK1-CCNB1
Representative Drug(s) TG02 Drug Info IC50 = 9 nM [8]
Co-Target Name Cyclin dependent kinase 2-Cyclin A complex (CDK2-CCNA2) Co-Target
UniProt ID CDK2_HUMAN-CCNA1_HUMAN/CCNA2_HUMAN
Gene Name CDK2-CCNA1/CCNA2
Representative Drug(s) TG02 Drug Info IC50 = 13 nM [7]
References  Top
REF 1 AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608.
REF 2 Insights into Current Tropomyosin Receptor Kinase (TRK) Inhibitors: Development and Clinical Application. J Med Chem. 2019 Feb 28;62(4):1731-1760.
REF 3 Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases. Eur J Med Chem. 2019 Dec 15;184:111710.
REF 4 Exploration of novel pyrrolo[2,1-f][1,2,4]triazine derivatives with improved anticancer efficacy as dual inhibitors of c-Met/VEGFR-2. Eur J Med Chem. 2018 Oct 5;158:814-31.
REF 5 Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-58.
REF 6 Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem. 2009 May 14;52(9):2629-51.
REF 7 Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012 Jan 12;55(1):169-96.
REF 8 Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update. J Med Chem. 2019 May 9;62(9):4233-4251.
REF 9 Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. J Med Chem. 2016 Oct 13;59(19):8667-84.

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