Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T17980 Target Info
Target Name Fyn tyrosine protein kinase (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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Target Type Successful Target
Gene Name FYN
Biochemical Class Kinase
UniProt ID
FYN_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 [1]
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 [2]
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) Dasatinib Drug Info Ki = 0.295 nM [3]
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 [4]
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 [5]
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 [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) Dasatinib Drug Info IC50 = 9.9 nM [7]
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 [3]
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 [8]
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 [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 [9]
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) Dasatinib Drug Info IC50 = 880 nM [4]
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) Dasatinib Drug Info IC50 < 0.5 nM [7]
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 [8]
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 [10]
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 [6]
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 [11]
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 [10]
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 [4]
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 [12]
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 [6]
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 [5]
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 [13]
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 [14]
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 [15]
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 [8]
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 [8]
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 [10]
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) Dasatinib Drug Info Ki < 10 nM [3]
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) Dasatinib Drug Info IC50 = 297 nM [5]
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 [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) Dasatinib Drug Info Ki = 0.5 nM [16]
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 [3]
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 [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) Dasatinib Drug Info Ki < 10 nM [3]
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 [17]
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 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 3 Controlling cellular distribution of drugs with permeability modifying moieties. Med. Chem. Commun. 2019;10:974-984.
REF 4 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 5 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 6 Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. Leukemia. 2009 Mar;23(3):477-85.
REF 7 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 8 Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9.
REF 9 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 10 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 11 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 12 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 13 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 14 Identification of type II and III DDR2 inhibitors. J Med Chem. 2014 May 22;57(10):4252-62.
REF 15 Small molecule discoidin domain receptor kinase inhibitors and potential medical applications. J Med Chem. 2015 Apr 23;58(8):3287-301.
REF 16 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 17 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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