Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T63505 | Target Info | |||
Target Name | Tyrosine-protein kinase ABL1 (ABL) | ||||
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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Target Type | Successful Target | ||||
Gene Name | ABL1 | ||||
Biochemical Class | Kinase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Ponatinib | Drug Info | IC50 = 0.3 nM | Click to Show More | [1] | |
2 | KW-2449 | Drug Info | IC50 = 6.6 nM | [10] | ||
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) | Ponatinib | Drug Info | IC50 = 0.3 nM | [2] | ||
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) | Ponatinib | Drug Info | IC50 = 0.7 nM | [3] | ||
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
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Representative Drug(s) | SKI-758 | Drug Info | IC50 = 0.78 nM | Click to Show More | [4] | |
2 | Saracatinib | Drug Info | IC50 = 1 nM | [5] | ||
3 | Bosutinib | Drug Info | IC50 = 1 nM | [6] | ||
4 | Ponatinib | Drug Info | IC50 = 2.5 nM | [2] | ||
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) | Ponatinib | Drug Info | IC50 = 1.2 nM | [2] | ||
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) | Ponatinib | Drug Info | IC50 = 1.3 nM | [2] | ||
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) | Bosutinib | Drug Info | IC50 = 1.3 nM | Click to Show More | [6] | |
2 | Saracatinib | Drug Info | IC50 < 4 nM | [9] | ||
3 | SKI-758 | Drug Info | IC50 = 20 nM | [4] | ||
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) | Ponatinib | Drug Info | IC50 = 1.5 nM | Click to Show More | [7] | |
2 | SKI-758 | Drug Info | IC50 ~ 1000 nM | [4] | ||
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) | Ponatinib | Drug Info | IC50 = 1.7 nM | Click to Show More | [8] | |
2 | Bosutinib | Drug Info | IC50 = 32 nM | [6] | ||
3 | Saracatinib | Drug Info | IC50 = 200 nM | [9] | ||
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) | Bosutinib | Drug Info | IC50 = 1.8 nM | [6] | ||
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) | Bosutinib | Drug Info | IC50 = 2.5 nM | [6] | ||
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) | Ponatinib | Drug Info | IC50 = 2.6 nM | [2] | ||
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 | [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) | Bosutinib | Drug Info | IC50 = 27 nM | [6] | ||
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 | [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) | Bosutinib | Drug Info | IC50 = 53 nM | Click to Show More | [6] | |
2 | Saracatinib | Drug Info | IC50 = 66 nM | [11] | ||
3 | SKI-758 | Drug Info | IC50 = 230 nM | [4] | ||
4 | Ponatinib | Drug Info | IC50 ~ 1000 nM | [2] | ||
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 | [6] | ||
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) | Bosutinib | Drug Info | IC50 = 491 nM | [6] | ||
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 | [6] | ||
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 | [4] | ||
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) | Ponatinib | Drug Info | IC50 = 0.24 nM | Click to Show More | [7] | |
2 | Bosutinib | Drug Info | IC50 = 8 nM | [6] | ||
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 | [6] | |
2 | Saracatinib | Drug Info | IC50 = 0.7 nM | [12] | ||
3 | DCC-2036 | Drug Info | IC50 = 1.5 nM | [12] | ||
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 | [13] | ||
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) | Bosutinib | Drug Info | IC50 = 5.5 nM | [6] | ||
Co-Target Name | Fibroblast growth factor receptor 4 (FGFR4) | Clinical trial Target | ||||
UniProt ID | FGFR4_HUMAN | |||||
Gene Name | FGFR4 | |||||
Synonyms |
TKF; JTK2; FGFR-4; CD334
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 7.1 nM | [2] | ||
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) | Bosutinib | Drug Info | IC50 = 8.5 nM | [6] | ||
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) | Ponatinib | Drug Info | IC50 = 9.4 nM | [2] | ||
Co-Target Name | Receptor-interacting protein 1 (RIPK1) | Clinical trial Target | ||||
UniProt ID | RIPK1_HUMAN | |||||
Gene Name | RIPK1 | |||||
Synonyms |
Receptor-interacting serine/threonine-protein kinase 1; RIP1; RIP-1; RIP; Cell death protein RIP
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 12 nM | [14] | ||
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
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 20.9 nM | [2] | ||
Co-Target Name | P2Y purinoceptor 2 (P2RY2) | Clinical trial Target | ||||
UniProt ID | P2RY2_HUMAN | |||||
Gene Name | P2RY2 | |||||
Synonyms |
P2Y2; P2U1; P2U receptor; P2U purinoceptor 1; P2U nucleotide receptor; P2RY2; Adenosine P2Y2 receptor
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Representative Drug(s) | Adenosine triphosphate | Drug Info | EC50 = 30.1 nM | [15] | ||
Co-Target Name | P2X purinoceptor 3 (P2RX3) | Clinical trial Target | ||||
UniProt ID | P2RX3_HUMAN | |||||
Gene Name | P2RX3 | |||||
Synonyms |
P2X3 receptor; P2X3; P2RX3; ATP-gated ion channel P2X(3)
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Representative Drug(s) | Adenosine triphosphate | Drug Info | EC50 = 340 nM | [16] | ||
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 | [6] | ||
Co-Target Name | P2X purinoceptor 4 (P2RX4) | Clinical trial Target | ||||
UniProt ID | P2RX4_HUMAN | |||||
Gene Name | P2RX4 | |||||
Synonyms |
P2X4; P2RX4
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Representative Drug(s) | Adenosine triphosphate | Drug Info | EC50 = 500 nM | [16] | ||
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 | [6] | ||
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 | [6] | ||
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 | [4] | ||
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 | [4] | ||
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 | [13] | ||
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 | [6] | ||
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) | Bosutinib | Drug Info | IC50 = 3.2 nM | [6] | ||
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 | [6] | ||
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) | Bosutinib | Drug Info | IC50 = 63 nM | Click to Show More | [6] | |
2 | Saracatinib | Drug Info | IC50 = 840 nM | [9] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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) | Bosutinib | Drug Info | Ki = 12.7 nM | Click to Show More | [17] | |
2 | Saracatinib | Drug Info | Ki = 39.8 nM | [17] | ||
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) | Bosutinib | Drug Info | IC50 = 40 nM | [6] | ||
Co-Target Name | P2X purinoceptor 1 (P2RX1) | Literature-reported Target | ||||
UniProt ID | P2RX1_HUMAN | |||||
Gene Name | P2RX1 | |||||
Synonyms |
Purinergic receptor 1; P2X1
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Representative Drug(s) | Adenosine triphosphate | Drug Info | EC50 = 56 nM | [16] | ||
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 | [6] | ||
Co-Target Name | P2Y purinoceptor 1 (P2RY1) | Literature-reported Target | ||||
UniProt ID | P2RY1_HUMAN | |||||
Gene Name | P2RY1 | |||||
Synonyms |
P2Y1; P2Y(1) receptor; P2RY1; Adenosine P2Y1 receptor
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Representative Drug(s) | Adenosine triphosphate | Drug Info | EC50 = 150 nM | [18] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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) | Ponatinib | Drug Info | IC50 = 1 nM | [14] | ||
Co-Target Name | Receptor-interacting serine/threonine-protein kinase 3 (RIPK3) | Co-Target | ||||
UniProt ID | RIPK3_HUMAN | |||||
Gene Name | RIPK3 | |||||
Synonyms |
RIP-like protein kinase 3; Receptor-interacting protein 3; RIP-3
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Representative Drug(s) | Ponatinib | Drug Info | IC50 = 1.6 nM | [14] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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 | [6] | ||
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 | [19] | ||
Co-Target Name | Coiled coil domain containing protein 6-Proto oncogene c Ret complex (CCDC6-RET) | Co-Target | ||||
UniProt ID | CCDC6_HUMAN-RET_HUMAN | |||||
Gene Name | CCDC6-RET | |||||
Representative Drug(s) | Ponatinib | Drug Info | IC50 = 180.4 nM | [20] | ||
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 | [6] |
References | Top | ||||
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REF 1 | Inhibitors of Stat5 protein signalling. Medchemcomm. 2012;3:22-7. | ||||
REF 2 | Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. Eur J Med Chem. 2017 Jan 27;126:122-32. | ||||
REF 3 | Novel benzothiazinones (BTOs) as allosteric modulator or substrate competitive inhibitor of glycogen synthase kinase 3beta (GSK-3beta) with cellular activity of promoting glucose uptake. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5639-43. | ||||
REF 4 | 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 5 | 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 6 | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85. | ||||
REF 7 | 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 8 | Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15. | ||||
REF 9 | Emerging targets in osteoporosis disease modification. J Med Chem. 2010 Jun 10;53(11):4332-53. | ||||
REF 10 | 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 11 | 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 12 | Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4398-403. | ||||
REF 13 | AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem. 2016 Apr 28;59(8):3593-608. | ||||
REF 14 | Small-Molecule Inhibitors of Necroptosis: Current Status and Perspectives. J Med Chem. 2020 Feb 27;63(4):1490-1510. | ||||
REF 15 | Key determinants of nucleotide-activated G protein-coupled P2Y(2) receptor function revealed by chemical and pharmacological experiments, mutagenesis and homology modeling. J Med Chem. 2009 May 14;52(9):2762-75. | ||||
REF 16 | Purine and pyrimidine (P2) receptors as drug targets. J Med Chem. 2002 Sep 12;45(19):4057-93. | ||||
REF 17 | 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 18 | Diadenosine 5',5''-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors. J Med Chem. 2010 Dec 23;53(24):8485-97. | ||||
REF 19 | 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 20 | Discovery of 4-chloro-3-(5-(pyridin-3-yl)-1,2,4-oxadiazole-3-yl)benzamides as novel RET kinase inhibitors. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5679-5684. |
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