Co-Target(s) Information

Content Navigation (  All   None )                                      
Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T59328 Target Info
Target Name Epidermal growth factor receptor (EGFR)
Synonyms
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
    Click to Show/Hide
Target Type Successful Target
Gene Name EGFR
Biochemical Class Kinase
UniProt ID
EGFR_HUMAN
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
    Click to Show/Hide
Representative Drug(s) Drug Info Ki = 0.021 nM Click to Show More [1]
2 Vandetanib Drug Info IC50 = 9 nM [16]
3 VATALANIB Drug Info IC50 = 10 nM [18]
4 Gefitinib Drug Info IC50 = 48.5 nM [24]
5 Erlotinib Drug Info IC50 = 50.12 nM [18]
6 Drug Info IC50 = 849 nM [10]
7 HKI-272 Drug Info IC50 = 858.2 nM [38]
8 SKI-758 Drug Info IC50 ~ 1000 nM [2]
Co-Target Name Tyrosine-protein kinase ABL1 (ABL) Successful Target
UniProt ID ABL1_HUMAN
Gene Name ABL1
Synonyms
p150; Proto-oncogene tyrosine-protein kinase ABL1; Proto-oncogene c-Abl; JTK7; C-ABL; Abl; Abelson tyrosine-protein kinase 1; Abelson murine leukemia viral oncogene homolog 1
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 = 0.4 nM Click to Show More [2]
2 Drug Info IC50 = 80 nM [3]
3 Vandetanib Drug Info IC50 = 86 nM [30]
Co-Target Name Proto-oncogene c-Src (SRC) Successful Target
UniProt ID SRC_HUMAN
Gene Name SRC
Synonyms
pp60c-src; Tyrosine kinase (pp60(src)); Src tyrosine kinase; SRC1; Proto-oncogene tyrosine-protein kinase Src; Pp60(src); P60-Src; C-src TK; C-Src
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 = 0.78 nM Click to Show More [2]
2 Vandetanib Drug Info IC50 = 44 nM [23]
3 Dacomitinib Drug Info IC50 = 110 nM [29]
4 Drug Info IC50 = 390 nM [34]
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) Drug Info IC50 = 1 nM Click to Show More [3]
2 Erlotinib Drug Info IC50 = 60 nM [27]
Co-Target Name Erbb2 tyrosine kinase receptor (HER2) Successful Target
UniProt ID ERBB2_HUMAN
Gene Name ERBB2
Synonyms
p185erbB2; Tyrosine kinase-type cell surface receptor HER2; Receptor tyrosine-protein kinase erbB-2; Proto-oncogene c-ErbB-2; Proto-oncogene Neu; NGL; NEU; Metastatic lymph node gene 19 protein; MLN19; MLN 19; HER2; CD340
    Click to Show/Hide
Representative Drug(s) HKI-272 Drug Info IC50 = 1 nM Click to Show More [4]
2 BIBW 2992 Drug Info IC50 = 2 nM [4]
3 Varlitinib Drug Info IC50 = 2 nM [6]
4 Lapatinib Drug Info IC50 = 2.7 nM [7]
5 BIBX-1382 Drug Info IC50 = 3 nM [8]
6 Drug Info IC50 = 5 nM [12]
7 HM-78136B Drug Info IC50 = 5.3 nM [13]
8 Drug Info IC50 = 15.7 nM [19]
9 Drug Info IC50 = 22 nM [20]
10 Gefitinib Drug Info IC50 = 24 nM [21]
11 Dacomitinib Drug Info IC50 = 45.7 nM [9]
12 Erlotinib Drug Info IC50 = 64 nM [28]
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) Drug Info IC50 = 1.3 nM [5]
Co-Target Name Erbb4 tyrosine kinase receptor (Erbb-4) Successful Target
UniProt ID ERBB4_HUMAN
Gene Name ERBB4
Synonyms
Tyrosine kinase-type cell surface receptor HER4; Receptor tyrosine-protein kinase erbB-4; Proto-oncogene-like protein c-ErbB-4; P180erbB4; HER4
    Click to Show/Hide
Representative Drug(s) Varlitinib Drug Info IC50 = 4 nM Click to Show More [9]
2 Drug Info IC50 = 10 nM [12]
3 Dacomitinib Drug Info IC50 = 74 nM [29]
4 Drug Info IC50 = 190 nM [20]
5 Gefitinib Drug Info IC50 = 476 nM [29]
6 Lapatinib Drug Info IC50 ~ 1000 nM [40]
Co-Target Name Histone deacetylase (HDAC) Successful Target
UniProt ID HDAC1_HUMAN; HDAC2_HUMAN; HDAC3_HUMAN; HDAC4_HUMAN; HDAC5_HUMAN; HDAC6_HUMAN; HDAC7_HUMAN; HDAC8_HUMAN; HDAC9_HUMAN; HDA10_HUMAN; HDA11_HUMAN
Gene Name NO-GeName
Synonyms
Human histone deacetylase
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 4.4 nM [10]
Co-Target Name Histone deacetylase 1 (HDAC1) Successful Target
UniProt ID HDAC1_HUMAN
Gene Name HDAC1
Synonyms
RPD3L1; HD1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 4.5 nM [10]
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
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 4.63 nM [11]
Co-Target Name Proto-oncogene c-Ret (RET) Successful Target
UniProt ID RET_HUMAN
Gene Name RET
Synonyms
RET51; RET receptor tyrosine kinase; RET mutant Y791F; RET mutant V804M; RET mutant V804L; RET mutant S891A; RET mutant M918T; RET mutant G691S; Proto-oncogene tyrosine-protein kinase receptor Ret; PTC; Cadherin family member 12; CDHR16; CDHF12; C-ret
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 6 nM Click to Show More [14]
2 Vandetanib Drug Info IC50 = 49 nM [25]
Co-Target Name Inosine-5'-monophosphate dehydrogenase (IMPDH) Successful Target
UniProt ID IMDH1_HUMAN; IMDH2_HUMAN
Gene Name NO-GeName
Representative Drug(s) Drug Info IC50 = 7 nM [15]
Co-Target Name Inosine-5'-monophosphate dehydrogenase 2 (IMPDH2) Successful Target
UniProt ID IMDH2_HUMAN
Gene Name IMPDH2
Synonyms
IMPDH-II; IMPDH 2; IMPD2; IMPD 2; IMP dehydrogenase 2
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 10 nM [17]
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
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 10 nM Click to Show More [3]
2 Vandetanib Drug Info IC50 = 343 nM [30]
3 VATALANIB Drug Info IC50 = 730 nM [37]
Co-Target Name Platelet-derived growth factor receptor beta (PDGFRB) Successful Target
UniProt ID PGFRB_HUMAN
Gene Name PDGFRB
Synonyms
Platelet-derived growth factor receptor 1; PDGFR1; PDGFR-beta; PDGFR-1; PDGFR; PDGF-R-beta; CD140b antigen; CD140b; CD140 antigen-like family member B; Beta-type platelet-derived growth factor receptor; Beta-PDGFR; Beta platelet-derived growth factor receptor
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 10 nM Click to Show More [3]
2 Vandetanib Drug Info IC50 = 477 nM [30]
3 VATALANIB Drug Info IC50 = 490 nM [35]
Co-Target Name LCK tyrosine protein kinase (LCK) Successful Target
UniProt ID LCK_HUMAN
Gene Name LCK
Synonyms
p56-LCK; Tyrosine-protein kinase Lck; T cell-specific protein-tyrosine kinase; Proto-oncogene tyrosine-protein kinase LCK; Proto-oncogene Lck; Protein YT16; Lymphocyte cell-specific protein-tyrosine kinase; Leukocyte C-terminal Src kinase; LSK; LCK p59-Fyn; LCK Protooncogene Syn
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 = 20 nM Click to Show More [2]
2 Drug Info IC50 = 60 nM [3]
3 Dacomitinib Drug Info IC50 = 94 nM [29]
Co-Target Name Vascular endothelial growth factor receptor (VEGFR) Successful Target
UniProt ID VGFR1_HUMAN; VGFR2_HUMAN; VGFR3_HUMAN
Gene Name NO-GeName
Representative Drug(s) Vandetanib Drug Info IC50 = 25 nM Click to Show More [22]
2 VATALANIB Drug Info IC50 = 100 nM [16]
3 Erlotinib Drug Info IC50 = 250 nM [33]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
    Click to Show/Hide
Representative Drug(s) Drug Info Ki = 56 nM [26]
Co-Target Name ALK tyrosine kinase receptor (ALK) Successful Target
UniProt ID ALK_HUMAN
Gene Name ALK
Synonyms
CD246; Anaplastic lymphoma kinase
    Click to Show/Hide
Representative Drug(s) Osimertinib Drug Info IC50 = 177 nM [31]
Co-Target Name Tyrosine-protein kinase BTK (ATK) Successful Target
UniProt ID BTK_HUMAN
Gene Name BTK
Synonyms
Bruton's tyrosine kinase; Bruton tyrosine kinase; BPK; B-cell progenitor kinase; B cell progenitor kinase; Agammaglobulinemia tyrosine kinase; Agammaglobulinaemia tyrosine kinase; AGMX1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 185 nM [32]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name HTR2C
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
    Click to Show/Hide
Representative Drug(s) Drug Info Ki = 417 nM [26]
Co-Target Name Voltage-gated potassium channel Kv11.1 (KCNH2) Successful Target
UniProt ID KCNH2_HUMAN
Gene Name KCNH2
Synonyms
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
    Click to Show/Hide
Representative Drug(s) Osimertinib Drug Info IC50 = 570 nM Click to Show More [36]
2 Lapatinib Drug Info IC50 = 1000 nM [41]
Co-Target Name Insulin receptor (INSR) Successful Target
UniProt ID INSR_HUMAN
Gene Name INSR
Synonyms
IR; CD220 antigen; CD220
    Click to Show/Hide
Representative Drug(s) Osimertinib Drug Info IC50 = 912 nM [39]
Co-Target Name Cyclin-dependent kinase 4 (CDK4) Successful Target
UniProt ID CDK4_HUMAN
Gene Name CDK4
Synonyms
PSK-J3; Cell division protein kinase 4
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [2]
Co-Target Name Janus kinase 3 (JAK-3) Successful Target
UniProt ID JAK3_HUMAN
Gene Name JAK3
Synonyms
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
    Click to Show/Hide
Representative Drug(s) Gefitinib Drug Info IC50 ~ 1000 nM [29]
Co-Target Name Ephrin type-B receptor 4 (EPHB4) Clinical trial Target
UniProt ID EPHB4_HUMAN
Gene Name EPHB4
Synonyms
Tyrosine-protein kinase TYRO11; TYRO11; MYK1; Hepatoma transmembrane kinase; HTK
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 0.2 nM Click to Show More [42]
2 Gefitinib Drug Info IC50 = 1000 nM [34]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name TEK
Synonyms
hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 0.39 nM Click to Show More [43]
2 Vandetanib Drug Info IC50 = 567 nM [30]
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) Drug Info IC50 = 1 nM [3]
Co-Target Name Erbb3 tyrosine kinase receptor (Erbb-3) Clinical trial Target
UniProt ID ERBB3_HUMAN
Gene Name ERBB3
Synonyms
Tyrosine kinase-type cell surface receptor HER3; Receptor tyrosine-protein kinase erbB-3; Proto-oncogene-like protein c-ErbB-3; HER3; C-erbB3; C-erbB-3 protein
    Click to Show/Hide
Representative Drug(s) Osimertinib Drug Info IC50 = 2.1 nM Click to Show More [44]
2 Erlotinib Drug Info IC50 = 10 nM [46]
3 CO-1686 Drug Info IC50 = 46 nM [46]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 3 nM Click to Show More [45]
2 VATALANIB Drug Info IC50 = 195 nM [51]
3 Vandetanib Drug Info IC50 = 233 nM [30]
Co-Target Name Histone deacetylase 6 (HDAC6) Clinical trial Target
UniProt ID HDAC6_HUMAN
Gene Name HDAC6
Synonyms
KIAA0901; JM21; HD6
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 5.1 nM [10]
Co-Target Name Histone deacetylase 3 (HDAC3) Clinical trial Target
UniProt ID HDAC3_HUMAN
Gene Name HDAC3
Synonyms
SMAP45; RPD32; RPD3-2; HD3
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 9.1 nM [10]
Co-Target Name Soluble epoxide hydrolase (EPHX2) Clinical trial Target
UniProt ID HYES_HUMAN
Gene Name EPHX2
Synonyms
Bifunctional epoxide hydrolase 2
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 12 nM [47]
Co-Target Name Histone deacetylase 2 (HDAC2) Clinical trial Target
UniProt ID HDAC2_HUMAN
Gene Name HDAC2
Synonyms
HD2
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 12.6 nM [10]
Co-Target Name Histone deacetylase 4 (HDAC4) Clinical trial Target
UniProt ID HDAC4_HUMAN
Gene Name HDAC4
Synonyms
KIAA0288; HD4
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 13.2 nM [10]
Co-Target Name Vascular endothelial growth factor receptor 1 (FLT-1) Clinical trial Target
UniProt ID VGFR1_HUMAN
Gene Name FLT1
Synonyms
Vascular permeability factor receptor; VEGFR1; VEGFR-1; VEGF-1 receptor; Tyrosine-protein kinase receptor FLT; Tyrosine-protein kinase FRT; Fms-like tyrosine kinase 1; FRT; FLT
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 18 nM Click to Show More [48]
2 Vandetanib Drug Info IC50 = 22 nM [50]
3 VATALANIB Drug Info IC50 = 54 nM [50]
4 Erlotinib Drug Info IC50 ~ 1000 nM [54]
Co-Target Name Extracellular signal-regulated kinase 1 (ERK1) Clinical trial Target
UniProt ID MK03_HUMAN
Gene Name MAPK3
Synonyms
PRKM3; P44-MAPK; P44-ERK1; P44 Mitogen-activated protein kinase; Mitogen-activated protein kinase 3; Microtubule-associated protein-2 kinase; Microtubule-associated protein 2 kinase; MAPK 3; MAP kinase isoform p44; MAP kinase 3; Insulin-stimulated MAP2 kinase; ERT2; ERK-1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 18.1 nM [49]
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
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 19 nM [3]
Co-Target Name Stress-activated protein kinase 2a (p38 alpha) Clinical trial Target
UniProt ID MK14_HUMAN
Gene Name MAPK14
Synonyms
SAPK2A; P38 mitogen activatedprotein kinase; P38 Mitogen-activatedprotein kinase alpha; Mitogen-activated protein kinase p38 alpha; Mitogen-activated protein kinase 14; MXI2; MAX-interacting protein 2; MAPK 14; MAP kinase p38alpha; MAP kinase p38 alpha; MAP kinase MXI2; MAP kinase 14; Cytokine suppressive anti-inflammatory drug-binding protein; Cytokine suppressive anti-inflammatory drug binding protein; CSPB1; CSBP2; CSBP1; CSBP; CSAID-binding protein; CSAID binding protein; CRK1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 37.4 nM [49]
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) Drug Info IC50 = 109.5 nM [49]
Co-Target Name MAP kinase signal-integrating kinase 2 (MKNK2) Clinical trial Target
UniProt ID MKNK2_HUMAN
Gene Name MKNK2
Synonyms
Mnk2; MAPK signal-integrating kinase 2
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 262 nM [52]
Co-Target Name HUMAN cyclin G-associated kinase (GAK) Clinical trial Target
UniProt ID GAK_HUMAN
Gene Name GAK
Synonyms
cyclin G associated kinase
    Click to Show/Hide
Representative Drug(s) Gefitinib Drug Info IC50 = 420 nM Click to Show More [53]
2 Erlotinib Drug Info IC50 = 910 nM [53]
Co-Target Name Tyrosine-protein kinase Lyn (JTK8) Clinical trial Target
UniProt ID LYN_HUMAN
Gene Name LYN
Synonyms
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 840 nM [10]
Co-Target Name RAC-alpha serine/threonine-protein kinase (AKT1) Clinical trial Target
UniProt ID AKT1_HUMAN
Gene Name AKT1
Synonyms
RAC-PK-alpha; RAC; Proto-oncogene c-Akt; Protein kinase B alpha; PKB alpha
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [2]
Co-Target Name Phosphoinositide dependent protein kinase-1 (PDPK1) Clinical trial Target
UniProt ID PDPK1_HUMAN
Gene Name PDPK1
Synonyms
PDK1; HPDK1; 3-phosphoinositide-dependent protein kinase 1; 3-Phosphoinositide-dependent kinase-1; 3'-phosphoinositide dependent kinase 1
    Click to Show/Hide
Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [2]
Co-Target Name Discoidin domain-containing receptor 2 (DDR2) Patented-recorded Target
UniProt ID DDR2_HUMAN
Gene Name DDR2
Synonyms
Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 7 nM [55]
Co-Target Name Histone deacetylase 5 (HDAC5) Patented-recorded Target
UniProt ID HDAC5_HUMAN
Gene Name HDAC5
Synonyms
KIAA0600; HD5; Antigen NY-CO-9
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 11.4 nM [10]
Co-Target Name Histone deacetylase 10 (HDAC10) Patented-recorded Target
UniProt ID HDA10_HUMAN
Gene Name HDAC10
Synonyms
Polyamine deacetylase HDAC10; HD10
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 26.1 nM [10]
Co-Target Name B lymphocyte kinase (BLK) Patented-recorded Target
UniProt ID BLK_HUMAN
Gene Name BLK
Synonyms
p55-Blk; Tyrosine-protein kinase Blk
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 29 nM [32]
Co-Target Name Tyrosine-protein kinase BMX (BMX) Patented-recorded Target
UniProt ID BMX_HUMAN
Gene Name BMX
Synonyms
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 62 nM [32]
Co-Target Name Histone deacetylase 9 (HDAC9) Patented-recorded Target
UniProt ID HDAC9_HUMAN
Gene Name HDAC9
Synonyms
MITR; MEF2-interacting transcription repressor MITR; KIAA0744; Histone deacetylase-related protein; Histone deacetylase 7B; HDRP; HDAC7B; HDAC7; HD9; HD7b
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 67.2 nM [10]
Co-Target Name Histone deacetylase 8 (HDAC8) Patented-recorded Target
UniProt ID HDAC8_HUMAN
Gene Name HDAC8
Synonyms
Histone deacetylase-8; HDACL1; HD8; CDA07
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 79.8 nM [10]
Co-Target Name Hematopoietic cell kinase (HCK) Patented-recorded Target
UniProt ID HCK_HUMAN
Gene Name HCK
Synonyms
p61Hck; p59Hck; p59-HCK/p60-HCK; Tyrosine-protein kinase HCK; Hemopoietic cell kinase
    Click to Show/Hide
Representative Drug(s) Gefitinib Drug Info IC50 = 110 nM Click to Show More [34]
2 Drug Info IC50 = 530 nM [34]
Co-Target Name Cyclin-dependent kinase 8 (CDK8) Patented-recorded Target
UniProt ID CDK8_HUMAN
Gene Name CDK8
Synonyms
Protein kinase K35; Mediator of RNA polymerase II transcription subunit CDK8; Mediator complex subunit CDK8; Cell division protein kinase 8
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 199 nM [56]
Co-Target Name Casein kinase I alpha (CSNK1A1) Patented-recorded Target
UniProt ID KC1A_HUMAN
Gene Name CSNK1A1
Synonyms
Casein kinase I isoform alpha; CKI-alpha; CK1
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 250 nM [34]
Co-Target Name Histone deacetylase 7 (HDAC7) Patented-recorded Target
UniProt ID HDAC7_HUMAN
Gene Name HDAC7
Synonyms
Histone deacetylase 7A; HDAC7A; HD7a; HD7
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 373 nM [10]
Co-Target Name NIMA-related kinase 2 (NEK2) Literature-reported Target
UniProt ID NEK2_HUMAN
Gene Name NEK2
Synonyms
Serine/threonine-protein kinase Nek2; NimA-related protein kinase 2; NimA-like protein kinase 1; Never in mitosis A-related kinase 2; NLK1; NEK2A; HSPK 21
    Click to Show/Hide
Representative Drug(s) HKI-272 Drug Info IC50 = 274 nM Click to Show More [57]
2 Pelitinib Drug Info IC50 = 661 nM [57]
Co-Target Name Organic anion transporter B (SLCO2B1) Literature-reported Target
UniProt ID SO2B1_HUMAN
Gene Name SLCO2B1
Synonyms
Solute carrier organic anion transporter family member 2B1; Solute carrier family 21 member 9; SLC21A9; Organic anion transporter polypeptide-related protein 2; OATPRP2; OATPB; OATP2B1; OATP-RP2; OATP-B; KIAA0880
    Click to Show/Hide
Representative Drug(s) Erlotinib Drug Info Ki = 530 nM [58]
Co-Target Name Serine/threonine-protein kinase A-Raf (ARAF) Co-Target
UniProt ID ARAF_HUMAN
Gene Name ARAF
Synonyms
Proto-oncogene A-Raf; Proto-oncogene A-Raf-1; Proto-oncogene Pks
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 7.1 nM [59]
Co-Target Name Cyclin dependent kinase 8-Cyclin C complex (CDK8-CCNC) Co-Target
UniProt ID CDK8_HUMAN-CCNC_HUMAN
Gene Name CDK8-CCNC
Representative Drug(s) Drug Info IC50 = 32.5 nM [60]
Co-Target Name Cyclin-dependent kinase 19 (CDK19) Co-Target
UniProt ID CDK19_HUMAN
Gene Name CDK19
Synonyms
CDC2-related protein kinase 6; Cell division cycle 2-like protein kinase 6; Cell division protein kinase 19; Cyclin-dependent kinase 11; Death-preventing kinase
    Click to Show/Hide
Representative Drug(s) Drug Info IC50 = 206 nM [56]
Co-Target Name Kinesin 1 heavy chain-Tyrosine protein kinase receptor RET (KIF5B-RET) Co-Target
UniProt ID KINH_HUMAN-RET_HUMAN
Gene Name KIF5B-RET
Representative Drug(s) Vandetanib Drug Info IC50 = 400 nM [25]
References  Top
REF 1 Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: comparison of binding to non-phosphorylated and phosphorylated VEGFR2. Bioorg Med Chem. 2011 Sep 15;19(18):5342-51.
REF 2 Synthesis and Src kinase inhibitory activity of a series of 4-[(2,4-dichloro-5-methoxyphenyl)amino]-7-furyl-3-quinolinecarbonitriles. J Med Chem. 2006 Dec 28;49(26):7868-76.
REF 3 Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors. J Med Chem. 2008 Nov 27;51(22):7049-52.
REF 4 Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):21-6.
REF 5 Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model. Eur J Med Chem. 2019 Aug 15;176:248-267.
REF 6 Synthesis and investigation of novel 6-(1,2,3-triazol-4-yl)-4-aminoquinazolin derivatives possessing hydroxamic acid moiety for cancer therapy. Bioorg Med Chem. 2017 Jan 1;25(1):27-37.
REF 7 Design and synthesis of Lapatinib derivatives containing a branched side chain as HER1/HER2 targeting antitumor drug candidates. Eur J Med Chem. 2014 Nov 24;87:631-42.
REF 8 A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci U S A. 2007 Dec 18;104(51):20523-8.
REF 9 Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry. Eur J Med Chem. 2019 May 15;170:55-72.
REF 10 Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer. J Med Chem. 2010 Mar 11;53(5):2000-9.
REF 11 Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors. Bioorg Med Chem. 2016 Feb 15;24(4):750-8.
REF 12 Irreversible protein kinase inhibitors: balancing the benefits and risks. J Med Chem. 2012 Jul 26;55(14):6243-62.
REF 13 How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors. Eur J Med Chem. 2017 Dec 15;142:131-51.
REF 14 Progress in Discovery of KIF5B-RET Kinase Inhibitors for the Treatment of Non-Small-Cell Lung Cancer. J Med Chem. 2015 May 14;58(9):3672-81.
REF 15 New dermatological agents for the treatment of psoriasis. J Med Chem. 2001 Feb 1;44(3):281-97.
REF 16 Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. J Med Chem. 2005 Mar 10;48(5):1610-9.
REF 17 Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity. J Med Chem. 2002 May 23;45(11):2127-30.
REF 18 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 19 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 20 Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases. J Med Chem. 2009 Nov 12;52(21):6527-30.
REF 21 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors. Eur J Med Chem. 2017 Jan 27;126:853-869.
REF 22 Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. J Med Chem. 2002 Mar 14;45(6):1300-12.
REF 23 Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors. J Med Chem. 2014 Jun 12;57(11):4598-605.
REF 24 Discovery and optimization of tetrahydropyrido[4,3-d]pyrimidine derivatives as novel ATX and EGFR dual inhibitors. Bioorg Med Chem. 2018 May 1;26(8):1784-96.
REF 25 The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem. 2016 Apr 13;112:20-32.
REF 26 Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors. J Med Chem. 2012 Jun 28;55(12):5749-59.
REF 27 Design, synthesis and anticancer evaluation of novel spirobenzo[h]chromene and spirochromane derivatives with dual EGFR and B-RAF inhibitory activities. Eur J Med Chem. 2018 Apr 25;150:567-78.
REF 28 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 29 Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. J Med Chem. 2016 Sep 8;59(17):8103-24.
REF 30 Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93.
REF 31 Discovery of a potent dual ALK and EGFR T790M inhibitor. Eur J Med Chem. 2017 Aug 18;136:497-510.
REF 32 Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5916-9.
REF 33 Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity. Eur J Med Chem. 2018 Aug 5;156:918-32.
REF 34 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
REF 35 Chemical modulation of receptor signaling inhibits regenerative angiogenesis in adult zebrafish. Nat Chem Biol. 2006 May;2(5):265-73.
REF 36 Design, synthesis, SAR discussion, in vitro and in vivo evaluation of novel selective EGFR modulator to inhibit L858R/T790M double mutants. Eur J Med Chem. 2017 Jul 28;135:12-23.
REF 37 Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching. Bioorg Med Chem Lett. 2003 Sep 15;13(18):2967-71.
REF 38 Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cyst... Bioorg Med Chem. 2007 Jun 1;15(11):3635-48.
REF 39 Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.
REF 40 Synthesis and biological evaluation of pyrimidine-based dual inhibitors of human epidermal growth factor receptor 1 (HER-1) and HER-2 tyrosine kinases. J Med Chem. 2012 Mar 22;55(6):2846-57.
REF 41 Prediction of Thorough QT study results using action potential simulations based on ion channel screens. J Pharmacol Toxicol Methods. Nov-Dec 2014;70(3):246-54.
REF 42 Discovery of novel anti-angiogenesis agents. Part 6: Multi-targeted RTK inhibitors. Eur J Med Chem. 2017 Feb 15;127:275-85.
REF 43 Discovery of novel anti-angiogenesis agents. Part 10: Multi-target inhibitors of VEGFR-2, Tie-2 and EphB4 incorporated with 1,2,3-triazol. Eur J Med Chem. 2019 Feb 1;163:1-9.
REF 44 Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors. Bioorg Med Chem. 2018 May 1;26(8):2173-85.
REF 45 Synthesis and structure-activity relationship of 6-arylureido-3-pyrrol-2-ylmethylideneindolin-2-one derivatives as potent receptor tyrosine kinase inhibitors. Bioorg Med Chem. 2010 Jul 1;18(13):4674-86.
REF 46 Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR. J Med Chem. 2017 Apr 13;60(7):3002-3019.
REF 47 Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3732-7.
REF 48 Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3). Bioorg Med Chem. 2011 Jul 15;19(14):4173-82.
REF 49 Design and synthesis of potent 1,2,4-trisubstituted imidazolinone derivatives with dual p38alphaMAPK and ERK1/2 inhibitory activity. Eur J Med Chem. 2015 Apr 13;94:397-404.
REF 50 ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1369-75.
REF 51 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822.
REF 52 Design and synthesis of novel 6-hydroxy-4-methoxy-3-methylbenzofuran-7-carboxamide derivatives as potent Mnks inhibitors by fragment-based drug design. Bioorg Med Chem. 2018 Sep 1;26(16):4602-14.
REF 53 Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma. J Med Chem. 2019 May 9;62(9):4772-4778.
REF 54 Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines. Medchemcomm. 2010;1:282-6.
REF 55 Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62.
REF 56 Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?. J Med Chem. 2018 Jun 28;61(12):5073-92.
REF 57 Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition. J Med Chem. 2014 Jul 24;57(14):5835-44.
REF 58 Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. J Med Chem. 2012 May 24;55(10):4740-63.
REF 59 Discovery of potent Pan-Raf inhibitors with increased solubility to overcome drug resistance. Eur J Med Chem. 2019 Feb 1;163:243-255.
REF 60 Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. ACS Med Chem Lett. 2016 Apr 5;7(6):595-600.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.