Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T52624 Target Info
Target Name Platelet-derived growth factor receptor (PDGFR)
Synonyms
Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R
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Target Type Successful Target
Gene Name NO-GeName
UniProt ID
NOUNIPROTAC
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 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) BAY-57-9352 Drug Info IC50 = 6 nM Click to Show More [2]
2 Rosiglitazone + metformin Drug Info IC50 = 135 nM [9]
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 [3]
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 [4]
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 [5]
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 [5]
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 [6]
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 [7]
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) Drug Info IC50 = 131 nM [8]
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 [10]
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 [5]
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 [5]
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 [5]
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) BAY-57-9352 Drug Info IC50 = 4 nM [11]
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) Rosiglitazone + metformin Drug Info IC50 = 28 nM [9]
Co-Target Name Aurora kinase B (AURKB) Clinical trial Target
UniProt ID AURKB_HUMAN
Gene Name AURKB
Synonyms
Serine/threonine-protein kinase aurora-B; Serine/threonine-protein kinase 5; Serine/threonine-protein kinase 12; Serine/threonine protein kinase 12; STK5; STK12; Aurora/IPL1-related kinase 2; Aurora-related kinase 2; Aurora-B; Aurora-2 kinase; Aurora-2; Aurora- and Ipl1-like midbody-associated protein 1; Aurora 1; ARK2; ARK-2; AIRK2; AIM1; AIM-1; AIK2
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Representative Drug(s) Rosiglitazone + metformin Drug Info IC50 = 35 nM [12]
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 [5]
Co-Target Name Aurora kinase C (AURKC) Clinical trial Target
UniProt ID AURKC_HUMAN
Gene Name AURKC
Synonyms
Serine/threonine-protein kinase aurora-C; STK13; Aurora/Ipl1/Eg2 protein 2; Aurora/Ipl1-related kinase 3; Aurora-related kinase 3; Aurora-C; Aurora 3; ARK3; ARK-3; AIRK3; AIK3; AIE2
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Representative Drug(s) Rosiglitazone + metformin Drug Info IC50 = 210 nM [12]
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 [13]
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 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 [5]
Co-Target Name Discoidin domain-containing receptor 2 (DDR2) Patented-recorded Target
UniProt ID DDR2_HUMAN
Gene Name DDR2
Synonyms
Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B
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Representative Drug(s) Drug Info IC50 = 141 nM [14]
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 [6]
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 [7]
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 [5]
References  Top
REF 1 Selectively nonselective kinase inhibition: striking the right balance. J Med Chem. 2010 Feb 25;53(4):1413-37.
REF 2 Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors. Eur J Med Chem. 2010 Nov;45(11):5420-7.
REF 3 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 4 Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT. J Med Chem. 2017 Nov 9;60(21):8801-15.
REF 5 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 6 Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40.
REF 7 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 8 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 9 The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
REF 10 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 11 Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem. 2012 Dec 27;55(24):10797-822.
REF 12 The selectivity of protein kinase inhibitors: a further update. Biochem J. 2007 Dec 15;408(3):297-315.
REF 13 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.
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.

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