Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T57700 Target Info
Target Name Tyrosine-protein kinase Kit (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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Target Type Successful Target
Gene Name KIT
Biochemical Class Kinase
UniProt ID
KIT_HUMAN
Co-Targets of This Target  Top
Co-Target Name Vascular endothelial growth factor receptor 2 (KDR) Successful Target
UniProt ID VGFR2_HUMAN
Gene Name KDR
Synonyms
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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Representative Drug(s) Drug Info Ki = 0.021 nM Click to Show More [1]
2 Ponatinib Drug Info IC50 = 1.5 nM [11]
3 Drug Info IC50 = 2 nM [13]
4 Regorafenib Drug Info IC50 = 4.2 nM [15]
5 OSI-930 Drug Info IC50 = 5 nM [17]
6 Romiplostim Drug Info IC50 = 12.9 nM [19]
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) Ponatinib Drug Info EC50 = 0.05 nM Click to Show More [2]
2 Drug Info IC50 = 1.1 nM [8]
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 [3]
2 Drug Info IC50 = 1.3 nM [9]
3 Pexidartinib Drug Info IC50 = 5 nM [16]
4 Regorafenib Drug Info IC50 = 82 nM [29]
5 Drug Info IC50 = 131 nM [29]
6 Romiplostim Drug Info IC50 = 160 nM [30]
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 Click to Show More [4]
2 Drug Info IC50 = 6 nM [18]
3 Romiplostim Drug Info IC50 = 170 nM [30]
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) Ponatinib Drug Info IC50 = 0.32 nM Click to Show More [5]
2 Drug Info Ki = 13 nM [20]
3 Drug Info IC50 = 80 nM [7]
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 Click to Show More [6]
2 Regorafenib Drug Info IC50 = 1.5 nM [10]
3 Drug Info IC50 = 4.63 nM [14]
Co-Target Name Serine/threonine-protein kinase B-raf (BRAF) Successful Target
UniProt ID BRAF_HUMAN
Gene Name BRAF
Synonyms
V-Raf murine sarcoma viral oncogene homolog B1; RAFB1; Proto-oncogene B-Raf; P94; BRAF1; BRAF(V599E); BRAF serine/threonine kinase; B-raf protein; B-Raf
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Representative Drug(s) Drug Info IC50 = 1 nM Click to Show More [7]
2 Regorafenib Drug Info IC50 = 1.5 nM [10]
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 Click to Show More [4]
2 Regorafenib Drug Info IC50 = 1.5 nM [10]
3 Drug Info IC50 = 4 nM [13]
4 Drug Info IC50 = 10 nM [7]
5 Romiplostim Drug Info IC50 = 68 nM [27]
6 Drug Info IC50 = 72 nM [28]
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 [4]
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 [12]
2 Ponatinib Drug Info IC50 = 2.6 nM [4]
3 Romiplostim Drug Info IC50 = 200 nM [32]
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) Ponatinib Drug Info IC50 = 2.5 nM Click to Show More [4]
2 Drug Info IC50 = 390 nM [33]
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) Drug Info IC50 = 2.96 nM Click to Show More [14]
2 Ponatinib Drug Info IC50 ~ 1000 nM [4]
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) OSI-930 Drug Info IC50 = 22 nM Click to Show More [21]
2 Drug Info IC50 = 60 nM [7]
3 Drug Info IC50 = 160 nM [31]
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 [22]
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 [22]
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 [23]
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 [24]
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 [25]
Co-Target Name 5-HT 2B receptor (HTR2B) Successful Target
UniProt ID 5HT2B_HUMAN
Gene Name HTR2B
Synonyms
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) Drug Info Ki = 56 nM [26]
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 [22]
Co-Target Name 5-HT 2C receptor (HTR2C) Successful Target
UniProt ID 5HT2C_HUMAN
Gene Name HTR2C
Synonyms
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) Drug Info Ki = 417 nM [26]
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 [22]
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 [22]
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) MP470 Drug Info IC50 < 1000 nM [34]
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) Drug Info IC50 = 0.2 nM [35]
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 [11]
2 Drug Info IC50 = 220 nM [45]
Co-Target Name Angiopoietin 1 receptor (TEK) Clinical trial Target
UniProt ID TIE2_HUMAN
Gene Name TEK
Synonyms
hTIE2; VMCM1; VMCM; Tyrosine-protein kinase receptor TIE-2; Tyrosine-protein kinase receptor TEK; Tyrosine kinase with Ig and EGF homology domains-2; Tunica interna endothelial cell kinase; TIE2; P140 TEK; Endothelial tyrosine kinase; Endothelial Cell-Specific Receptor TIE-2; CD202b antigen; CD202b
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Representative Drug(s) Drug Info IC50 = 0.39 nM Click to Show More [36]
2 Regorafenib Drug Info IC50 = 1.5 nM [10]
Co-Target Name Soluble epoxide hydrolase (EPHX2) Clinical trial Target
UniProt ID HYES_HUMAN
Gene Name EPHX2
Synonyms
Bifunctional epoxide hydrolase 2
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Representative Drug(s) Regorafenib Drug Info IC50 = 0.5 nM Click to Show More [37]
2 Drug Info IC50 = 12 nM [37]
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) Drug Info IC50 = 1 nM Click to Show More [7]
2 Regorafenib Drug Info IC50 = 1.5 nM [10]
3 OSI-930 Drug Info IC50 = 41 nM [21]
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) Regorafenib Drug Info IC50 = 1.5 nM Click to Show More [10]
2 Romiplostim Drug Info IC50 = 8 nM [39]
3 Drug Info IC50 = 18 nM [42]
4 Ponatinib Drug Info IC50 = 20.9 nM [4]
Co-Target Name Vascular endothelial growth factor receptor 3 (FLT-4) Clinical trial Target
UniProt ID VGFR3_HUMAN
Gene Name FLT4
Synonyms
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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Representative Drug(s) Drug Info IC50 = 3 nM Click to Show More [38]
2 Romiplostim Drug Info IC50 = 50 nM [44]
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 [4]
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 [4]
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) Pexidartinib Drug Info IC50 = 10.8 nM Click to Show More [40]
2 Drug Info IC50 = 19 nM [7]
3 Romiplostim Drug Info IC50 = 84 nM [44]
4 Drug Info IC50 = 291 nM [28]
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 [41]
Co-Target Name Extracellular signal-regulated kinase 1 (ERK1) Clinical trial Target
UniProt ID MK03_HUMAN
Gene Name MAPK3
Synonyms
PRKM3; P44-MAPK; P44-ERK1; P44 Mitogen-activated protein kinase; Mitogen-activated protein kinase 3; Microtubule-associated protein-2 kinase; Microtubule-associated protein 2 kinase; MAPK 3; MAP kinase isoform p44; MAP kinase 3; Insulin-stimulated MAP2 kinase; ERT2; ERK-1
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Representative Drug(s) Drug Info IC50 = 18.1 nM [43]
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) Drug Info IC50 = 37.4 nM [43]
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 [22]
Co-Target Name Extracellular signal-regulated kinase 2 (ERK2) Clinical trial Target
UniProt ID MK01_HUMAN
Gene Name MAPK1
Synonyms
PRKM2; PRKM1; P42-MAPK; P42 Mitogen-activated protein kinase; Mitogen-activated protein kinase 2; Mitogen-activated protein kinase 1; MAPK 2; MAPK 1; MAP kinase isoform p42; MAP kinase 2; MAP kinase 1; ERT1; ERK-2
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Representative Drug(s) Drug Info IC50 = 109.5 nM [43]
Co-Target Name MAP kinase signal-integrating kinase 2 (MKNK2) Clinical trial Target
UniProt ID MKNK2_HUMAN
Gene Name MKNK2
Synonyms
Mnk2; MAPK signal-integrating kinase 2
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Representative Drug(s) Drug Info IC50 = 262 nM [46]
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 = 7 nM Click to Show More [47]
2 Drug Info IC50 = 141 nM [28]
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 [28]
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 [22]
Co-Target Name Cyclin-dependent kinase 8 (CDK8) Patented-recorded Target
UniProt ID CDK8_HUMAN
Gene Name CDK8
Synonyms
Protein kinase K35; Mediator of RNA polymerase II transcription subunit CDK8; Mediator complex subunit CDK8; Cell division protein kinase 8
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Representative Drug(s) Drug Info IC50 = 199 nM [48]
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) Drug Info IC50 = 250 nM [33]
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) Drug Info IC50 = 530 nM [33]
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 [23]
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 [24]
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 [41]
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 [41]
Co-Target Name Serine/threonine-protein kinase A-Raf (ARAF) Co-Target
UniProt ID ARAF_HUMAN
Gene Name ARAF
Synonyms
Proto-oncogene A-Raf; Proto-oncogene A-Raf-1; Proto-oncogene Pks
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Representative Drug(s) Drug Info IC50 = 7.1 nM [49]
Co-Target Name Cyclin dependent kinase 8-Cyclin C complex (CDK8-CCNC) Co-Target
UniProt ID CDK8_HUMAN-CCNC_HUMAN
Gene Name CDK8-CCNC
Representative Drug(s) Drug Info IC50 = 32.5 nM [50]
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 [51]
Co-Target Name Cyclin-dependent kinase 19 (CDK19) Co-Target
UniProt ID CDK19_HUMAN
Gene Name CDK19
Synonyms
CDC2-related protein kinase 6; Cell division cycle 2-like protein kinase 6; Cell division protein kinase 19; Cyclin-dependent kinase 11; Death-preventing kinase
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Representative Drug(s) Drug Info IC50 = 206 nM [48]
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 [22]
References  Top
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REF 2 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 3 Inhibitors of Stat5 protein signalling. Medchemcomm. 2012;3:22-7.
REF 4 Discovery of novel Ponatinib analogues for reducing KDR activity as potent FGFRs inhibitors. Eur J Med Chem. 2017 Jan 27;126:122-32.
REF 5 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 6 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 7 Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors. J Med Chem. 2008 Nov 27;51(22):7049-52.
REF 8 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 9 Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model. Eur J Med Chem. 2019 Aug 15;176:248-267.
REF 10 Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors. Eur J Med Chem. 2019 Oct 1;179:707-722.
REF 11 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 12 Selectivity data: assessment, predictions, concordance, and implications. J Med Chem. 2013 Sep 12;56(17):6991-7002.
REF 13 Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives. J Med Chem. 2010 Nov 25;53(22):8140-9.
REF 14 Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors. Bioorg Med Chem. 2016 Feb 15;24(4):750-8.
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