Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T85943 Target Info
Target Name Proto-oncogene c-Src (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
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Target Type Successful Target
Gene Name SRC
Biochemical Class Kinase
UniProt ID
SRC_HUMAN
Co-Targets of This Target  Top
Co-Target Name Fusion protein Bcr-Abl (Bcr-Abl) Successful Target
UniProt ID BCR_HUMAN-ABL1_HUMAN
Gene Name BCR-ABL1
Synonyms
BCR-ABL fusion protein; BCR-ABL
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Representative Drug(s) Dasatinib Drug Info EC50 = 0.04 nM Click to Show More [1]
2 Bosutinib Drug Info IC50 = 20 nM [15]
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) CP-868596 Drug Info IC50 = 0.06 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
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.17 nM Click to Show More [3]
2 SKI-758 Drug Info IC50 = 0.4 nM [5]
3 Bosutinib Drug Info IC50 = 0.5 nM [7]
4 Saracatinib Drug Info IC50 = 30 nM [16]
Co-Target Name Fyn tyrosine protein kinase (FYN) Successful Target
UniProt ID FYN_HUMAN
Gene Name FYN
Synonyms
Tyrosine-protein kinase Fyn; Src-like kinase; SLK; Proto-oncogene tyrosine-protein kinase Fyn; Proto-oncogene c-Fyn; Proto-oncogene Syn; Fyn p59-Fyn; Fyn Protooncogene Syn
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.2 nM Click to Show More [4]
2 Bosutinib Drug Info IC50 = 1.8 nM [7]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.4 nM Click to Show More [6]
2 Bosutinib Drug Info IC50 = 1.3 nM [7]
3 Saracatinib Drug Info IC50 < 4 nM [9]
4 SKI-758 Drug Info IC50 = 20 nM [5]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 1.3 nM Click to Show More [8]
2 Bosutinib Drug Info IC50 = 2.5 nM [7]
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) Dasatinib Drug Info IC50 = 1.5 nM Click to Show More [7]
2 Bosutinib Drug Info IC50 = 32 nM [7]
3 Saracatinib Drug Info IC50 = 200 nM [9]
Co-Target Name Fibroblast growth factor receptor 2 (FGFR2) Successful Target
UniProt ID FGFR2_HUMAN
Gene Name FGFR2
Synonyms
Keratinocyte growth factor receptor 2; Keratinocyte growth factor receptor; KSAM; KGFR; K-sam; FGFR-2; FGF-2 receptor; CD332; BEK
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Representative Drug(s) PD173074 Drug Info IC50 = 5 nM [10]
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) Dasatinib Drug Info IC50 = 9.9 nM [11]
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
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Representative Drug(s) Dasatinib Drug Info Ki < 10 nM [12]
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) PD173074 Drug Info IC50 = 19 nM Click to Show More [13]
2 Dasatinib Drug Info IC50 = 880 nM [6]
Co-Target Name Epidermal growth factor receptor (EGFR) Successful Target
UniProt ID EGFR_HUMAN
Gene Name EGFR
Synonyms
Receptor tyrosine-protein kinase erbB-1; Proto-oncogene c-ErbB-1; HER1; ERBB1; ERBB
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Representative Drug(s) Dasatinib Drug Info IC50 = 20 nM Click to Show More [14]
2 Bosutinib Drug Info IC50 = 53 nM [7]
3 Saracatinib Drug Info IC50 = 66 nM [17]
4 SKI-758 Drug Info IC50 = 230 nM [5]
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) Bosutinib Drug Info IC50 = 22 nM [7]
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) Bosutinib Drug Info IC50 = 27 nM [7]
Co-Target Name Tyrosine-protein kinase SYK (SYK) Successful Target
UniProt ID KSYK_HUMAN
Gene Name SYK
Synonyms
p72-Syk; Spleen tyrosine kinase
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Representative Drug(s) Bosutinib Drug Info IC50 = 52 nM [7]
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) PD173074 Drug Info IC50 = 100 nM Click to Show More [18]
2 SKI-758 Drug Info IC50 ~ 1000 nM [5]
Co-Target Name Tyrosine-protein kinase UFO (AXL) Successful Target
UniProt ID UFO_HUMAN
Gene Name AXL
Synonyms
UFO; Tyrosine-protein kinase receptor UFO; AXL oncogene
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Representative Drug(s) Bosutinib Drug Info IC50 = 174 nM [7]
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) PD173074 Drug Info IC50 = 190 nM [13]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 433 nM [11]
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
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Representative Drug(s) Bosutinib Drug Info IC50 = 491 nM [7]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 710 nM [4]
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
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Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [5]
Co-Target Name Yes tyrosine kinase (YES) Clinical trial Target
UniProt ID YES_HUMAN
Gene Name YES1
Synonyms
p61-Yes; Yes p59-Fyn; Yes Protooncogene Syn; Tyrosine-protein kinase Yes; Proto-oncogene c-Yes
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Representative Drug(s) Bosutinib Drug Info IC50 = 0.4 nM Click to Show More [7]
2 Dasatinib Drug Info IC50 < 0.5 nM [11]
3 Saracatinib Drug Info IC50 = 0.7 nM [19]
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
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Representative Drug(s) Dasatinib Drug Info IC50 < 1 nM Click to Show More [14]
2 Bosutinib Drug Info IC50 = 5.5 nM [7]
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) Bosutinib Drug Info IC50 = 1 nM [20]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 1.2 nM Click to Show More [21]
2 Bosutinib Drug Info IC50 = 8 nM [7]
Co-Target Name Ephrin type-B receptor 2 (EPHB2) Clinical trial Target
UniProt ID EPHB2_HUMAN
Gene Name EPHB2
Synonyms
hEK5; Tyrosine-protein kinase receptor EPH-3; Tyrosine-protein kinase TYRO5; TYRO5; Renal carcinoma antigen NY-REN-47; Receptor protein-tyrosine kinase HEK5; EphB2 receptor tyrosine kinase; EphB2; EPTH3; EPHT3; EPH-like kinase 5; EPH tyrosine kinase 3; ELK-related tyrosine kinase; EK5; Developmentally-regulated Eph-related tyrosine kinase; DRT
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Representative Drug(s) Dasatinib Drug Info IC50 = 4.4 nM Click to Show More [7]
2 Bosutinib Drug Info IC50 = 8.5 nM [7]
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) Dasatinib Drug Info IC50 = 5.012 nM [22]
Co-Target Name Tyrosine-protein kinase BRK (PTK6) Clinical trial Target
UniProt ID PTK6_HUMAN
Gene Name PTK6
Synonyms
Protein-tyrosine kinase 6; Breast tumor kinase; BRK
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Representative Drug(s) Dasatinib Drug Info IC50 = 5.3 nM [21]
Co-Target Name Fibroblast growth factor receptor (FGFR) Clinical trial Target
UniProt ID FGFR1_HUMAN; FGFR2_HUMAN; FGFR3_HUMAN; FGFR4_HUMAN
Gene Name NO-GeName
Synonyms
FGF receptor
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Representative Drug(s) PD173074 Drug Info IC50 = 7 nM [13]
Co-Target Name Fibroblast growth factor receptor 3 (FGFR3) Clinical trial Target
UniProt ID FGFR3_HUMAN
Gene Name FGFR3
Synonyms
JTK4; FGFR-3; CD333
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Representative Drug(s) PD173074 Drug Info EC50 = 30 nM [16]
Co-Target Name Stress-activated protein kinase (p38) Clinical trial Target
UniProt ID MK11_HUMAN; MK12_HUMAN; MK13_HUMAN; MK14_HUMAN
Gene Name NO-GeName
Synonyms
p38) Stress-activated protein kinase; P38 MAPK; P38 MAP kinase; Mitogen-activated protein kinase p38
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Representative Drug(s) Dasatinib Drug Info IC50 = 100 nM [6]
Co-Target Name Ephrin type-A receptor 2 (EPHA2) Clinical trial Target
UniProt ID EPHA2_HUMAN
Gene Name EPHA2
Synonyms
Tyrosine-protein kinase receptor ECK; Epithelial cell kinase; EphA2receptor; ECK
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Representative Drug(s) Dasatinib Drug Info IC50 = 137 nM [23]
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) Dasatinib Drug Info IC50 = 164 nM [7]
Co-Target Name T-cell-specific kinase (ITK) Clinical trial Target
UniProt ID ITK_HUMAN
Gene Name ITK
Synonyms
Tyrosine kinase ITK; Inducible T cell kinase; EMT
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Representative Drug(s) Dasatinib Drug Info IC50 = 228 nM [8]
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
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Representative Drug(s) Dasatinib Drug Info EC50 = 470 nM [24]
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
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Representative Drug(s) Bosutinib Drug Info IC50 = 491 nM [7]
Co-Target Name Focal adhesion kinase 1 (FAK) Clinical trial Target
UniProt ID FAK1_HUMAN
Gene Name PTK2
Synonyms
pp125FAK; p125FAK; Protein-tyrosine kinase 2; Protein phosphatase 1 regulatory subunit 71; PPP1R71; Focal adhesion kinase-related nonkinase; FRNK; FAK1; FADK 1; FADK
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Representative Drug(s) Bosutinib Drug Info IC50 = 538 nM [7]
Co-Target Name Renal carcinoma antigen NY-REN-64 (IRAK-4) Clinical trial Target
UniProt ID IRAK4_HUMAN
Gene Name IRAK4
Synonyms
Interleukin-1 receptor-associated kinase 4; IRAK-4
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Representative Drug(s) Bosutinib Drug Info IC50 = 574 nM [7]
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
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Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [5]
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
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Representative Drug(s) SKI-758 Drug Info IC50 ~ 1000 nM [5]
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
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.4 nM [25]
Co-Target Name Epithelial discoidin domain receptor 1 (DDR1) Patented-recorded Target
UniProt ID DDR1_HUMAN
Gene Name DDR1
Synonyms
Tyrosine-protein kinase CAK; Tyrosine kinase DDR; TRKE; TRK E; RTK6; Protein-tyrosine kinase RTK-6; Protein-tyrosine kinase 3A; PTK3A; NTRK4; NEP; Mammary carcinoma kinase 10; MCK-10; HGK2; Epithelial discoidin domain-containing receptor 1; EDDR1; Discoidin receptor tyrosine kinase; Cell adhesion kinase; CD167a; CD167 antigen-like family member A
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.5 nM [26]
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
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Representative Drug(s) Bosutinib Drug Info IC50 = 1 nM [20]
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
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Representative Drug(s) Dasatinib Drug Info IC50 < 1 nM [14]
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
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Representative Drug(s) Dasatinib Drug Info IC50 < 1 nM Click to Show More [14]
2 Bosutinib Drug Info IC50 = 3.2 nM [7]
Co-Target Name Tyrosine-protein kinase CSK (CSK) Patented-recorded Target
UniProt ID CSK_HUMAN
Gene Name CSK
Synonyms
Protein-tyrosine kinase CYL; C-Src kinase
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Representative Drug(s) Dasatinib Drug Info IC50 = 1.3 nM Click to Show More [21]
2 Bosutinib Drug Info IC50 = 63 nM [7]
3 Saracatinib Drug Info IC50 = 840 nM [9]
Co-Target Name Activated CDC42 kinase 1 (ACK-1) Patented-recorded Target
UniProt ID ACK1_HUMAN
Gene Name TNK2
Synonyms
Tyrosine kinase non-receptor protein 2; ACK1; ACK-1
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Representative Drug(s) Bosutinib Drug Info IC50 = 2.7 nM Click to Show More [7]
2 Dasatinib Drug Info Ki < 10 nM [12]
Co-Target Name MEK kinase kinase 2 (MAP4K2) Patented-recorded Target
UniProt ID M4K2_HUMAN
Gene Name MAP4K2
Synonyms
Rab8-interacting protein; RAB8IP; Mitogen-activated protein kinase kinase kinase kinase 2; MEKKK 2; MAPK/ERK kinase kinase kinase 2; Germinal center kinase; GCK; GC kinase; B lymphocyte serine/threonine-protein kinase
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Representative Drug(s) Bosutinib Drug Info IC50 = 9.9 nM [7]
Co-Target Name Tyrosine-protein kinase Tec (PSCTK4) Patented-recorded Target
UniProt ID TEC_HUMAN
Gene Name TEC
Synonyms
Tec protein tyrosine kinase
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Representative Drug(s) Bosutinib Drug Info IC50 = 282 nM Click to Show More [7]
2 Dasatinib Drug Info IC50 = 297 nM [8]
Co-Target Name NF-kappa-B-activating kinase (TBK1) Patented-recorded Target
UniProt ID TBK1_HUMAN
Gene Name TBK1
Synonyms
TANK-binding kinase 1; T2K; Serine/threonine-protein kinase TBK1; NAK
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Representative Drug(s) Bosutinib Drug Info IC50 = 471 nM [7]
Co-Target Name Tyrosine-protein kinase TXK (TXK) Literature-reported Target
UniProt ID TXK_HUMAN
Gene Name TXK
Synonyms
Resting lymphocyte kinase; RLK; Protein-tyrosine kinase 4; PTK4
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Representative Drug(s) Dasatinib Drug Info IC50 = 0.3 nM Click to Show More [7]
2 Bosutinib Drug Info IC50 = 40 nM [7]
Co-Target Name Tyrosine-protein kinase ABL2 (ABL2) Literature-reported Target
UniProt ID ABL2_HUMAN
Gene Name ABL2
Synonyms
Tyrosine-protein kinase ARG; Abelson-related gene protein; Abelson tyrosine-protein kinase 2; Abelson murine leukemia viral oncogene homolog 2; ARG; ABLL
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Representative Drug(s) Bosutinib Drug Info IC50 = 0.5 nM [7]
Co-Target Name Membrane-associated kinase (PKMYT1) Literature-reported Target
UniProt ID PMYT1_HUMAN
Gene Name PKMYT1
Synonyms
Myt1 kinase; Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase; MYT1
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Representative Drug(s) Dasatinib Drug Info Ki = 0.5 nM Click to Show More [27]
2 Bosutinib Drug Info Ki = 12.7 nM [27]
3 Saracatinib Drug Info Ki = 39.8 nM [27]
Co-Target Name Tyrosine-protein kinase Fgr (FGR) Literature-reported Target
UniProt ID FGR_HUMAN
Gene Name FGR
Synonyms
p58c-Fgr; p58-Fgr; p55-Fgr; SRC2; Proto-oncogene c-Fgr; Gardner-Rasheed feline sarcoma viral (v-fgr) oncogene homolog
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Representative Drug(s) Bosutinib Drug Info IC50 = 1.1 nM [7]
Co-Target Name Salt-inducible kinase 1 (SIK1) Literature-reported Target
UniProt ID SIK1_HUMAN
Gene Name SIK1
Synonyms
Serine/threonine-protein kinase SNF1LK; Serine/threonine-protein kinase SNF1-like kinase 1; Serine/threonine-protein kinase SIK1; SNF1LK; SIK-1; SIK
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Representative Drug(s) Dasatinib Drug Info Ki < 10 nM [12]
Co-Target Name LIM domain kinase-1 (LIMK-1) Literature-reported Target
UniProt ID LIMK1_HUMAN
Gene Name LIMK1
Synonyms
LIMK-1; LIMK
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Representative Drug(s) Dasatinib Drug Info IC50 = 114 nM [7]
Co-Target Name Focal adhesion kinase 2 (PTK2B) Literature-reported Target
UniProt ID FAK2_HUMAN
Gene Name PTK2B
Synonyms
Related adhesion focal tyrosine kinase; RAFTK; Protein-tyrosine kinase 2-beta; Proline-rich tyrosine kinase 2; PYK2; FAK2; FADK 2; Cell adhesion kinase beta; Calcium-regulated non-receptor proline-rich tyrosine kinase; Calcium-dependent tyrosine kinase; CAKB; CAK-beta; CADTK
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Representative Drug(s) Bosutinib Drug Info IC50 = 134 nM [7]
Co-Target Name MST-1 protein kinase (STK4) Literature-reported Target
UniProt ID STK4_HUMAN
Gene Name STK4
Synonyms
Serine/threonine-protein kinase Krs-2; Serine/threonine-protein kinase 4 18kDa subunit; Serine/threonine-protein kinase 4; STE20-like kinase MST1; Mammalian STE20-like protein kinase 1; MST1/N; MST1/C; MST1; MST-1; KRS2
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Representative Drug(s) Bosutinib Drug Info IC50 = 191 nM [7]
Co-Target Name Proto-oncogene c-Fes (FES) Literature-reported Target
UniProt ID FES_HUMAN
Gene Name FES
Synonyms
p93c-fes; Tyrosine-protein kinase Fes/Fps; Proto-oncogene c-Fps; Feline sarcoma/Fujinami avian sarcoma oncogene homolog; FPS
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Representative Drug(s) Bosutinib Drug Info IC50 = 358 nM [7]
Co-Target Name Proto-oncogene c-Fer (FER) Literature-reported Target
UniProt ID FER_HUMAN
Gene Name FER
Synonyms
p94-Fer; Tyrosine-protein kinase Fer; Tyrosine kinase 3; TYK3; Fujinami poultry sarcoma/Feline sarcoma-related protein Fer; Feline encephalitis virus-related kinase FER
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Representative Drug(s) Bosutinib Drug Info IC50 = 490 nM [7]
Co-Target Name Mitogen-activated protein kinase kinase kinase kinase 5 (MAP4K5) Co-Target
UniProt ID M4K5_HUMAN
Gene Name MAP4K5
Synonyms
Kinase homologous to SPS1/STE20; KHS; MAPK/ERK kinase kinase kinase 5; MEK kinase kinase 5; MEKKK 5
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Representative Drug(s) Bosutinib Drug Info IC50 = 0.3 nM [7]
Co-Target Name Tyrosine-protein kinase FRK (FRK) Co-Target
UniProt ID FRK_HUMAN
Gene Name FRK
Synonyms
FYN-related kinase; Nuclear tyrosine protein kinase RAK; Protein-tyrosine kinase 5
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Representative Drug(s) Bosutinib Drug Info IC50 = 2.2 nM [7]
Co-Target Name Serine/threonine-protein kinase 24 (STK24) Co-Target
UniProt ID STK24_HUMAN
Gene Name STK24
Synonyms
Mammalian STE20-like protein kinase 3; MST-3; STE20-like kinase MST3
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Representative Drug(s) Bosutinib Drug Info IC50 = 3.9 nM [7]
Co-Target Name Serine/threonine-protein kinase RIPK2 (RIPK2) Co-Target
UniProt ID RIPK2_HUMAN
Gene Name RIPK2
Synonyms
Receptor-interacting serine/threonine-protein kinase 2; CARD-containing interleukin-1 beta-converting enzyme-associated kinase; CARD-containing IL-1 beta ICE-kinase; RIP-like-interacting CLARP kinase; Receptor-interacting protein 2; RIP-2; Tyrosine-protein kinase RIPK2
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Representative Drug(s) Dasatinib Drug Info Ki < 10 nM [12]
Co-Target Name Misshapen-like kinase 1 (MINK1) Co-Target
UniProt ID MINK1_HUMAN
Gene Name MINK1
Synonyms
GCK family kinase MiNK; MAPK/ERK kinase kinase kinase 6; MEK kinase kinase 6; MEKKK 6; Misshapen/NIK-related kinase; Mitogen-activated protein kinase kinase kinase kinase 6
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Representative Drug(s) Bosutinib Drug Info IC50 = 22 nM [7]
Co-Target Name Serine/threonine-protein kinase 10 (STK10) Co-Target
UniProt ID STK10_HUMAN
Gene Name STK10
Synonyms
Lymphocyte-oriented kinase
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Representative Drug(s) Bosutinib Drug Info IC50 = 52 nM [7]
Co-Target Name Myelin transcription factor 1 (MYT1) Co-Target
UniProt ID MYT1_HUMAN
Gene Name MYT1
Synonyms
MyT1; Myelin transcription factor I; MyTI; PLPB1; Proteolipid protein-binding protein
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Representative Drug(s) Dasatinib Drug Info IC50 = 63 nM [28]
Co-Target Name CaM kinase I delta (CAMK1D) Co-Target
UniProt ID KCC1D_HUMAN
Gene Name CAMK1D
Synonyms
Calcium/calmodulin-dependent protein kinase type 1D; CaM kinase ID; CaM-KI delta; CaMKI delta; CaMKID; CaMKI-like protein kinase; CKLiK
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Representative Drug(s) Bosutinib Drug Info IC50 = 92 nM [7]
Co-Target Name Nucleophosmin-ALK tyrosine kinase receptor fusion protein (NPM-ALK) Co-Target
UniProt ID NPM_HUMAN-ALK_HUMAN
Gene Name NPM1-ALK
Representative Drug(s) Bosutinib Drug Info IC50 = 150 nM [15]
Co-Target Name CaM kinase II gamma (CAMK2G) Co-Target
UniProt ID KCC2G_HUMAN
Gene Name CAMK2G
Synonyms
Calcium/calmodulin-dependent protein kinase type II subunit gamma; CaM kinase II subunit gamma; CaMK-II subunit gamma
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Representative Drug(s) Bosutinib Drug Info IC50 = 184 nM [7]
References  Top
REF 1 Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors. J Med Chem. 2016 Apr 28;59(8):3886-905.
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 Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem. 2013 Feb 14;56(3):879-94.
REF 4 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor. J Med Chem. 2006 Nov 16;49(23):6819-32.
REF 5 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 6 Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J Med Chem. 2004 Dec 30;47(27):6658-61.
REF 7 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85.
REF 8 The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci U S A. 2007 Aug 14;104(33):13283-8.
REF 9 Emerging targets in osteoporosis disease modification. J Med Chem. 2010 Jun 10;53(11):4332-53.
REF 10 An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors. Eur J Med Chem. 2017 Jan 27;126:476-90.
REF 11 Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710.
REF 12 Controlling cellular distribution of drugs with permeability modifying moieties. Med. Chem. Commun. 2019;10:974-984.
REF 13 Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. J Med Chem. 2005 Jul 14;48(14):4628-53.
REF 14 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
REF 15 Structural insights into the ATP binding pocket of the anaplastic lymphoma kinase by site-directed mutagenesis, inhibitor binding analysis, and hom... J Med Chem. 2006 Sep 21;49(19):5759-68.
REF 16 Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19936-41.
REF 17 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 18 Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. ACS Med Chem Lett. 2016 Apr 20;7(6):629-34.
REF 19 Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403.
REF 20 AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608.
REF 21 The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series. Eur J Med Chem. 2019 Feb 1;163:610-625.
REF 22 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 23 c-Src protein kinase inhibitors block assembly and maturation of dengue virus. Proc Natl Acad Sci U S A. 2007 Feb 27;104(9):3520-5.
REF 24 Discovery of a potent p38alpha/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies. Eur J Med Chem. 2019 Dec 1;183:111684.
REF 25 Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62.
REF 26 Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. J Med Chem. 2015 Apr 23;58(8):3287-301.
REF 27 Identification of PKMYT1 inhibitors by screening the GSK published protein kinase inhibitor set I and II. Bioorg Med Chem. 2018 Aug 7;26(14):4014-4024.
REF 28 Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay. Eur J Med Chem. 2013 Mar;61:41-8.

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