Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T96144 | Target Info | |||
Target Name | DNA topoisomerase II (TOP2) | ||||
Synonyms |
TOP2; DNA topoisomerase 2
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Target Type | Successful Target | ||||
Gene Name | TOP2A; TOP2B | ||||
Biochemical Class | ATP-hydrolyzing DNA topoisomerase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Glucocorticoid receptor (NR3C1) | Successful Target | ||||
UniProt ID | GCR_HUMAN | |||||
Gene Name | NR3C1 | |||||
Synonyms |
Nuclear receptor subfamily 3 group C member 1; GRL; GR
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Representative Drug(s) | Podofilox | Drug Info | IC50 = 14 nM | [1] | ||
Co-Target Name | Histone deacetylase 1 (HDAC1) | Successful Target | ||||
UniProt ID | HDAC1_HUMAN | |||||
Gene Name | HDAC1 | |||||
Synonyms |
RPD3L1; HD1
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Representative Drug(s) | Etoposide | Drug Info | IC50 ~ 20 ug.mL-1 | [2] | ||
Co-Target Name | Multidrug resistance-associated protein 1 (ABCC1) | Successful Target | ||||
UniProt ID | MRP1_HUMAN | |||||
Gene Name | ABCC1 | |||||
Synonyms |
MRP1; MRP; Leukotriene C(4) transporter; LTC4 transporter; ATP-binding cassette sub-family C member 1
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Representative Drug(s) | Mitoxantrone | Drug Info | IC50 = 27.5 nM | [3] | ||
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) | Quinolones | Drug Info | Ki = 33 nM | [4] | ||
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) | Quinolones | Drug Info | Ki = 36 nM | [4] | ||
Co-Target Name | DNA topoisomerase II beta (TOP2B) | Successful Target | ||||
UniProt ID | TOP2B_HUMAN | |||||
Gene Name | TOP2B | |||||
Synonyms |
Topo IIbeta; TOP2beta; TOP2B
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Representative Drug(s) | Nalidixic Acid | Drug Info | IC50 = 52 ug.mL-1 | Click to Show More | [5] | |
2 | Etoposide | Drug Info | IC50 = 69.8 nM | [6] | ||
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) | Quinolones | Drug Info | Ki = 93 nM | [7] | ||
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) | Mitoxantrone | Drug Info | IC50 = 190 nM | [8] | ||
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) | Amsacrine | Drug Info | IC50 = 208.93 nM | Click to Show More | [9] | |
2 | GSK2140944 | Drug Info | IC50 = 588 ug.mL-1 | [11] | ||
Co-Target Name | Tubulin (TUB) | Successful Target | ||||
UniProt ID | TBA1A_HUMAN; TBA1B_HUMAN; TBA1C_HUMAN; TBA3C_HUMAN; TBA3E_HUMAN; TBA4A_HUMAN; TBB1_HUMAN; TBB2A_HUMAN; TBB2B_HUMAN; TBB3_HUMAN; TBB4A_HUMAN; TBB4B_HUMAN; TBB5_HUMAN; TBB6_HUMAN; TBB8_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
Human tubulin
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Representative Drug(s) | Podofilox | Drug Info | IC50 = 260 nM | [10] | ||
Co-Target Name | Carbonic anhydrase IV (CA-IV) | Successful Target | ||||
UniProt ID | CAH4_HUMAN | |||||
Gene Name | CA4 | |||||
Synonyms |
Carbonic anhydrase 4; Carbonate dehydratase IV; CAIV
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Representative Drug(s) | Quinolones | Drug Info | Ki = 360 nM | [4] | ||
Co-Target Name | ATP-binding cassette transporter G2 (ABCG2) | Successful Target | ||||
UniProt ID | ABCG2_HUMAN | |||||
Gene Name | ABCG2 | |||||
Synonyms |
Urate exporter; Placenta-specific ATP-binding cassette transporter; Mitoxantrone resistance-associated protein; MXR; CDw338; CD338; Breast cancer resistance protein; BCRP1; BCRP; ABCP
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Representative Drug(s) | Mitoxantrone | Drug Info | IC50 = 903.8 nM | [3] | ||
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) | Mitoxantrone | Drug Info | IC50 = 1000 nM | [12] | ||
Co-Target Name | Aurora kinase A (AURKA) | Clinical trial Target | ||||
UniProt ID | AURKA_HUMAN | |||||
Gene Name | AURKA | |||||
Synonyms |
hARK1; Serine/threonine-protein kinase aurora-A; Serine/threonine-protein kinase 6; Serine/threonine-protein kinase 15; Serine/threonine kinase 15; STK6; STK15; IAK1; Breast tumor-amplified kinase; BTAK; Aurora/IPL1-related kinase 1; Aurora-related kinase 1; Aurora-A; Aurora 2; AYK1; AURA; ARK1; ARK-1; AIRK1; AIK
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Representative Drug(s) | Doxorubicin | Drug Info | IC50 = 40 nM | [13] | ||
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) | Quinolones | Drug Info | Ki = 82 nM | [4] | ||
Co-Target Name | Hypoxia-inducible factor 2 alpha (HIF-2A) | Successful Target | ||||
UniProt ID | EPAS1_HUMAN | |||||
Gene Name | EPAS1 | |||||
Synonyms |
bHLHe73; PASD2; PAS domain-containing protein 2; Member of PAS protein 2; MOP2; Hypoxia-inducible factor 2-alpha; HLF; HIF2A; HIF2-alpha; HIF-2-alpha; HIF-1-alpha-like factor; Endothelial PAS domain-containing protein 1; EPAS-1; Class E basic helix-loop-helix protein 73; Basic-helix-loop-helix-PAS protein MOP2
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Representative Drug(s) | Doxorubicin | Drug Info | EC50 = 120 nM | [14] | ||
Co-Target Name | Hypoxia-inducible factor 1 alpha (HIF-1A) | Clinical trial Target | ||||
UniProt ID | HIF1A_HUMAN | |||||
Gene Name | HIF1A | |||||
Synonyms |
bHLHe78; Transcription factor HIF-1; PASD8; PAS domain-containing protein 8; Member of PAS protein 1; MOP1; Hypoxia-inducible transcription factor (HIF)-1; Hypoxia-inducible factor 1-alpha; Hypoxia-inducible factor 1 A; Hypoxia inducible factor 1; HIF1-alpha; HIF1 alpha; HIF-1alpha; HIF-1-alpha; HIF-1 alpha; Class E basic helix-loop-helix protein 78; Basic-helix-loop-helix-PAS protein MOP1; ARNT-interacting protein; ARNT interacting protein
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Representative Drug(s) | Doxorubicin | Drug Info | EC50 = 120 nM | [14] | ||
Co-Target Name | DNA topoisomerase II alpha (TOP2A) | Clinical trial Target | ||||
UniProt ID | TOP2A_HUMAN | |||||
Gene Name | TOP2A | |||||
Synonyms |
DNA topoisomerase II, alpha isozyme; DNA topoisomerase 2alpha; DNA topoisomerase 2-alpha
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Representative Drug(s) | Doxorubicin | Drug Info | IC50 = 600 nM | [15] | ||
Co-Target Name | Casein kinase II (CSNK2) | Clinical trial Target | ||||
UniProt ID | CSK21_HUMAN; CSK22_HUMAN; CSK23_HUMAN; CSK2B_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Mitoxantrone | Drug Info | IC50 = 660 nM | [12] | ||
Co-Target Name | Caspase-3 (CASP3) | Clinical trial Target | ||||
UniProt ID | CASP3_HUMAN | |||||
Gene Name | CASP3 | |||||
Synonyms |
Yama protein; SREBP cleavage activity 1; SCA-1; Protein Yama; Cysteine protease CPP32; Caspase 3; CPP32; CPP-32; CASP-3; Apopain
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Representative Drug(s) | Etoposide | Drug Info | IC50 < 1000 nM | [16] | ||
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) | Quinolones | Drug Info | Ki = 420 nM | [4] | ||
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) | Mitoxantrone | Drug Info | IC50 = 530 nM | [8] | ||
Co-Target Name | Carbonic anhydrase XIII (CA13) | Co-Target | ||||
UniProt ID | CAH13_HUMAN | |||||
Gene Name | CA13 | |||||
Synonyms |
Carbonic anhydrase 13; Carbonate dehydratase XIII; CA-XIII
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Representative Drug(s) | Quinolones | Drug Info | Ki = 65 nM | [4] | ||
Co-Target Name | Carbonic anhydrase VA (CA5A) | Co-Target | ||||
UniProt ID | CAH5A_HUMAN | |||||
Gene Name | CA5A | |||||
Synonyms |
Carbonic anhydrase 5A, mitochondrial; Carbonate dehydratase VA; CA-VA
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Representative Drug(s) | Quinolones | Drug Info | Ki = 410 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) | Quinolones | Drug Info | Ki = 570 nM | [4] | ||
Co-Target Name | Carbonic anhydrase VB (CA5B) | Co-Target | ||||
UniProt ID | CAH5B_HUMAN | |||||
Gene Name | CA5B | |||||
Synonyms |
Carbonic anhydrase 5B, mitochondrial; Carbonate dehydratase VB; Carbonic anhydrase VB; CA-VB
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Representative Drug(s) | Quinolones | Drug Info | Ki = 750 nM | [4] |
References | Top | ||||
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REF 1 | Trypanothione reductase high-throughput screening campaign identifies novel classes of inhibitors with antiparasitic activity. Antimicrob Agents Chemother. 2009 Jul;53(7):2824-33. | ||||
REF 2 | The discovery and optimization of novel dual inhibitors of topoisomerase II and histone deacetylase. Bioorg Med Chem. 2013 Nov 15;21(22):6981-95. | ||||
REF 3 | Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors. J Med Chem. 2019 Sep 26;62(18):8578-8608. | ||||
REF 4 | New chemotypes acting as isozyme-selective carbonic anhydrase inhibitors with low affinity for the offtarget cytosolic isoform II. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2182-5. | ||||
REF 5 | DNA gyrase inhibitory and antimicrobial activities of some diphenic acid monohydroxamides. J Med Chem. 1997 Sep 26;40(20):3292-6. | ||||
REF 6 | Design, synthesis and screening of 1, 2, 4-triazinone derivatives as potential antitumor agents with apoptosis inducing activity on MCF-7 breast cancer cell line. Eur J Med Chem. 2018 Aug 5;156:563-79. | ||||
REF 7 | Heterocoumarins Are Selective Carbonic Anhydrase IX and XII Inhibitors with Cytotoxic Effects against Cancer Cells Lines. ACS Med Chem Lett. 2018 Aug 29;9(9):947-51. | ||||
REF 8 | 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 9 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. Eur J Med Chem. 2011 Feb;46(2):618-30. | ||||
REF 10 | Triazolopyridinyl-acrylonitrile derivatives as antimicrotubule agents: Synthesis, in vitro and in silico characterization of antiproliferative activity, inhibition of tubulin polymerization and binding thermodynamics. Eur J Med Chem. 2017 Dec 1;141:460-72. | ||||
REF 11 | Synthesis and anti-staphylococcal activity of novel bacterial topoisomerase inhibitors with a 5-amino-1,3-dioxane linker moiety. Bioorg Med Chem Lett. 2018 Aug 1;28(14):2477-80. | ||||
REF 12 | A new target for an old drug: identifying mitoxantrone as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling. J Med Chem. 2013 Mar 28;56(6):2619-29. | ||||
REF 13 | Single step synthesis of new fused pyrimidine derivatives and their evaluation as potent Aurora-A kinase inhibitors. Eur J Med Chem. 2011 Sep;46(9):3690-5. | ||||
REF 14 | Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii. J Nat Prod. 2009 May 22;72(5):805-12. | ||||
REF 15 | Design, Synthesis, and Biological Evaluation of Novel DNA Gyrase-Inhibiting Spiropyrimidinetriones as Potent Antibiotics for Treatment of Infections Caused by Multidrug-Resistant Gram-Positive Bacteria. J Med Chem. 2019 Mar 28;62(6):2950-2973. | ||||
REF 16 | Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50. |
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