Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T62431 Target Info
Target Name Tyrosine-protein kinase SYK (SYK)
Synonyms
p72-Syk; Spleen tyrosine kinase
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Target Type Successful Target
Gene Name SYK
Biochemical Class Kinase
UniProt ID
KSYK_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) Drug Info IC50 = 1.1 nM [1]
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) Drug Info IC50 = 1.995 nM Click to Show More [2]
2 TAK-659 Drug Info IC50 = 45 nM [3]
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) TAK-659 Drug Info IC50 = 4.6 nM Click to Show More [3]
2 tamatinib Drug Info EC50 = 10 nM [7]
3 Drug Info IC50 = 131 nM [16]
4 GS-9973 Drug Info EC50 = 327 nM [7]
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) tamatinib Drug Info IC50 = 5 nM Click to Show More [4]
2 TAK-659 Drug Info IC50 = 8.4 nM [3]
3 GS-9973 Drug Info EC50 ~ 1000 nM [7]
Co-Target Name Janus kinase 2 (JAK-2) Successful Target
UniProt ID JAK2_HUMAN
Gene Name JAK2
Synonyms
Tyrosine-protein kinase JAK2
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Representative Drug(s) tamatinib Drug Info IC50 = 6 nM Click to Show More [5]
2 Cerdulatinib Drug Info IC50 = 6 nM [6]
3 GS-9973 Drug Info EC50 = 453 nM [7]
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
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Representative Drug(s) Cerdulatinib Drug Info IC50 = 8 nM Click to Show More [6]
2 TAK-659 Drug Info IC50 = 114 nM [3]
Co-Target Name Janus kinase 1 (JAK-1) Successful Target
UniProt ID JAK1_HUMAN
Gene Name JAK1
Synonyms
Tyrosine-protein kinase JAK1; JAK1B; JAK1A
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Representative Drug(s) Cerdulatinib Drug Info IC50 = 12 nM [6]
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) Drug Info Ki = 13 nM [8]
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) Drug Info IC50 = 16.4 nM [9]
Co-Target Name Carbonic anhydrase II (CA-II) Successful Target
UniProt ID CAH2_HUMAN
Gene Name CA2
Synonyms
Carbonic anhydrase C; Carbonic anhydrase 2; Carbonate dehydratase II; CAC
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Representative Drug(s) Drug Info Ki = 30.2 nM [10]
Co-Target Name Carbonic anhydrase I (CA-I) Successful Target
UniProt ID CAH1_HUMAN
Gene Name CA1
Synonyms
Carbonic anhydrase B; Carbonic anhydrase 1; Carbonate dehydratase I; CAB
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Representative Drug(s) Drug Info Ki = 31.9 nM [10]
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) tamatinib Drug Info EC50 = 36 nM Click to Show More [7]
2 TAK-659 Drug Info IC50 = 88 nM [3]
3 GS-9973 Drug Info EC50 ~ 1000 nM [7]
Co-Target Name Quinone reductase 2 (NQO2) Successful Target
UniProt ID NQO2_HUMAN
Gene Name NQO2
Synonyms
Quinone oxidoreductase 2; Qui reductase 2; QR2; NRH:quinone oxidoreductase 2; NRH:qui oxidoreductase 2; NQO2; NAD(P)H qui oxidoreductase 2
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Representative Drug(s) Drug Info Ki = 39 nM [11]
Co-Target Name Solute carrier family 47 member 1 (SLC47A1) Successful Target
UniProt ID S47A1_HUMAN
Gene Name SLC47A1
Synonyms
hMATE-1; Multidrug and toxin extrusion protein 1; MATE1; MATE-1
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Representative Drug(s) Drug Info IC50 = 40 nM [12]
Co-Target Name Platelet-derived growth factor receptor (PDGFR) Successful Target
UniProt ID PGFRA_HUMAN; PGFRB_HUMAN
Gene Name NO-GeName
Synonyms
Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R
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Representative Drug(s) Drug Info IC50 = 50 nM [13]
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) Drug Info IC50 = 72 nM [14]
Co-Target Name Protein kinase C alpha (PRKCA) Successful Target
UniProt ID KPCA_HUMAN
Gene Name PRKCA
Synonyms
Protein kinase C alpha type; PRKACA; PKCalpha; PKCA; PKC-alpha; PKC-A
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Representative Drug(s) PRT-062607 Drug Info IC50 = 90 nM [15]
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) Drug Info IC50 = 160 nM [17]
Co-Target Name Carbonic anhydrase VI (CA-VI) Successful Target
UniProt ID CAH6_HUMAN
Gene Name CA6
Synonyms
Secreted carbonic anhydrase; Salivary carbonic anhydrase; Carbonic anhydrase 6; Carbonate dehydratase VI
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Representative Drug(s) Drug Info Ki = 392 nM [10]
Co-Target Name Carbonic anhydrase XIV (CA-XIV) Successful Target
UniProt ID CAH14_HUMAN
Gene Name CA14
Synonyms
UNQ690/PRO1335; Carbonic anhydrase 14; Carbonate dehydratase XIV
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Representative Drug(s) Drug Info Ki = 468 nM [10]
Co-Target Name Carbonic anhydrase XII (CA-XII) Successful Target
UniProt ID CAH12_HUMAN
Gene Name CA12
Synonyms
Tumor antigen HOM-RCC-3.1.3; Carbonic anhydrase 12; Carbonate dehydratase XII
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Representative Drug(s) Drug Info Ki = 980 nM [10]
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
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Representative Drug(s) Drug Info IC50 ~ 1000 nM [18]
Co-Target Name Stress-activated protein kinase JNK1 (JNK1) Clinical trial Target
UniProt ID MK08_HUMAN
Gene Name MAPK8
Synonyms
Stress-activated protein kinase 1c; SAPK1c; PRKM8; Mitogen-activated protein kinase 8; MAPK 8; MAP kinase 8; JNK-46; C-Jun N-terminal kinase 1
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Representative Drug(s) tamatinib Drug Info EC50 = 10 nM [4]
Co-Target Name Checkpoint kinase-1 (CHK1) Clinical trial Target
UniProt ID CHK1_HUMAN
Gene Name CHEK1
Synonyms
Serine/threonine-protein kinase Chk1; Chk1; Cell cycle checkpoint kinase; CHK1 checkpoint homolog
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Representative Drug(s) TAK-659 Drug Info IC50 = 50 nM [3]
Co-Target Name Carbonic anhydrase IX (CA-IX) Clinical trial Target
UniProt ID CAH9_HUMAN
Gene Name CA9
Synonyms
Renal cell carcinoma-associated antigen G250; RCC-associated antigen G250; PMW1; P54/58N; Membrane antigen MN; MN; G250 antigen (MN/CA IX/G250); G250; Carbonic anhydrase 9; Carbonate dehydratase IX; CAIX
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Representative Drug(s) Drug Info Ki = 75.7 nM [10]
Co-Target Name PAK-4 protein kinase (PAK4) Clinical trial Target
UniProt ID PAK4_HUMAN
Gene Name PAK4
Synonyms
p21-activated kinase 4; Serine/threonine-protein kinase PAK 4; PAK-4; KIAA1142
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Representative Drug(s) TAK-659 Drug Info IC50 = 76 nM [3]
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) Drug Info IC50 = 220 nM Click to Show More [19]
2 PRT-062607 Drug Info IC50 = 238 nM [5]
3 tamatinib Drug Info IC50 = 732 nM [5]
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) Drug Info IC50 = 291 nM [14]
Co-Target Name Stress-activated protein kinase JNK2 (JNK2) Patented-recorded Target
UniProt ID MK09_HUMAN
Gene Name MAPK9
Synonyms
Stress-activated protein kinase 1a; SAPK1a; PRKM9; Mitogen-activated protein kinase 9; Mitogen-activated protein kinase 8-interacting protein 2; MAPK 9; MAP kinase 9; Jun-N-terminal kinase 2; JNK-interacting protein 2; JNK-55; JNK MAP kinase scaffold protein 2; JIP-2; Islet-brain-2; IB-2; C-jun-amino-terminal kinase interacting protein 2; C-Jun N-terminal kinase 2
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Representative Drug(s) tamatinib Drug Info EC50 = 10 nM [4]
Co-Target Name Tyrosine-protein kinase ZAP-70 (ZAP-70) Patented-recorded Target
UniProt ID ZAP70_HUMAN
Gene Name ZAP70
Synonyms
Syk-related tyrosine kinase; SRK; 70 kDa zeta-chain associated protein
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Representative Drug(s) tamatinib Drug Info IC50 = 42 nM Click to Show More [5]
2 PRT-062607 Drug Info IC50 = 60 nM [5]
3 TAK-659 Drug Info IC50 = 75 nM [3]
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) Drug Info IC50 = 43 nM [14]
Co-Target Name Carbonic anhydrase VII (CA-VII) Patented-recorded Target
UniProt ID CAH7_HUMAN
Gene Name CA7
Synonyms
Carbonic anhydrase 7; Carbonate dehydratase VII
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Representative Drug(s) Drug Info Ki = 109 nM [10]
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) Drug Info IC50 = 141 nM [14]
Co-Target Name Ephrin type-A receptor 1 (EPHA1) Literature-reported Target
UniProt ID EPHA1_HUMAN
Gene Name EPHA1
Synonyms
hEpha1; Tyrosine-protein kinase receptor EPH; Erythropoietin-producing hepatoma receptor; EPHT1; EPHT; EPH tyrosine kinase 1; EPH tyrosine kinase; EPH
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Representative Drug(s) TAK-659 Drug Info IC50 = 31 nM [3]
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) TAK-659 Drug Info IC50 = 51 nM [3]
Co-Target Name Phosphorylase kinase testis gamma 2 (PHKG2) Literature-reported Target
UniProt ID PHKG2_HUMAN
Gene Name PHKG2
Synonyms
Phosphorylase kinase subunit gamma-2; Phosphorylase b kinase gamma catalytic chain, liver/testis isoform; PSK-C3; PHK-gamma-T; PHK-gamma-LT
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Representative Drug(s) TAK-659 Drug Info IC50 = 226 nM [3]
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) Drug Info IC50 = 272 nM [11]
Co-Target Name Multidrug and toxin extrusion protein 2 (MATE2) Literature-reported Target
UniProt ID S47A2_HUMAN
Gene Name SLC47A2
Synonyms
hMATE-2; Solute carrier family 47 member 2; MATE2; MATE-2; Kidney-specific H(+)/organic cation antiporter
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Representative Drug(s) Drug Info IC50 = 350 nM [12]
Co-Target Name Mitogen-activated protein kinase 1 (MAPK1) Co-Target
UniProt ID MK01_HUMAN
Gene Name MAPK1
Synonyms
MAP kinase 1; MAPK 1; ERT1; Extracellular signal-regulated kinase 2; ERK-2; MAP kinase isoform p42; p42-MAPK; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2
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Representative Drug(s) tamatinib Drug Info EC50 = 10 nM [4]
Co-Target Name Mitogen-activated protein kinase 3 (MAPK3) Co-Target
UniProt ID MK03_HUMAN
Gene Name MAPK3
Synonyms
MAP kinase 3; MAPK 3; ERT2; Extracellular signal-regulated kinase 1; ERK-1; Insulin-stimulated MAP2 kinase; MAP kinase isoform p44; p44-MAPK; Microtubule-associated protein 2 kinase; p44-ERK1
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Representative Drug(s) tamatinib Drug Info EC50 = 10 nM [4]
Co-Target Name Carbonic anhydrase III (CA3) Co-Target
UniProt ID CAH3_HUMAN
Gene Name CA3
Synonyms
Carbonic anhydrase 3; Carbonate dehydratase III; CA-III
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Representative Drug(s) Drug Info Ki = 528 nM [10]
References  Top
REF 1 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 2 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 3 Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-50.
REF 4 Discovery and development of spleen tyrosine kinase (SYK) inhibitors. J Med Chem. 2012 Apr 26;55(8):3614-43.
REF 5 Syk inhibitors with high potency in presence of blood. Bioorg Med Chem Lett. 2014 May 15;24(10):2278-82.
REF 6 Fibrogenic Disorders in Human Diseases: From Inflammation to Organ Dysfunction. J Med Chem. 2018 Nov 21;61(22):9811-40.
REF 7 Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase. J Med Chem. 2014 May 8;57(9):3856-73.
REF 8 Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. Eur J Med Chem. 2008 Dec;43(12):2665-76.
REF 9 Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15.
REF 10 The protein tyrosine kinase inhibitors imatinib and nilotinib strongly inhibit several mammalian alpha-carbonic anhydrase isoforms. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4102-6.
REF 11 Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40.
REF 12 Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling. J Med Chem. 2013 Feb 14;56(3):781-795.
REF 13 Designed multiple ligands. An emerging drug discovery paradigm. J Med Chem. 2005 Oct 20;48(21):6523-43.
REF 14 Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib. Bioorg Med Chem. 2010 Oct 1;18(19):6977-86.
REF 15 Discovery and profiling of a selective and efficacious Syk inhibitor. J Med Chem. 2015 Feb 26;58(4):1950-63.
REF 16 Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia. J Med Chem. 2019 Dec 26;62(24):11135-11150.
REF 17 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. J Med Chem. 2009 Aug 13;52(15):4743-56.
REF 18 Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors. J Med Chem. 2013 Feb 28;56(4):1677-92.
REF 19 Structural factors contributing to the Abl/Lyn dual inhibitory activity of 3-substituted benzamide derivatives. Bioorg Med Chem Lett. 2007 May 15;17(10):2712-7.

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