Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T09826 | Target Info | |||
Target Name | DNA topoisomerase I (TOP1) | ||||
Synonyms |
DNA topoisomerase I
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Target Type | Successful Target | ||||
Gene Name | TOP1 | ||||
Biochemical Class | Topoisomerase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Prostaglandin G/H synthase 2 (COX-2) | Successful Target | ||||
UniProt ID | PGH2_HUMAN | |||||
Gene Name | PTGS2 | |||||
Synonyms |
Prostaglandin-endoperoxide synthase 2; Prostaglandin H2 synthase 2; PHS II; PGHS-2; PGH synthase 2; Cyclooxygenase-2; COX2; COX-2
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 2.5 ug.mL-1 | [1] | ||
Co-Target Name | Influenza Neuraminidase (Influ NA) | Successful Target | ||||
UniProt ID | NRAM_I33A0 | |||||
Gene Name | Influ NA | |||||
Synonyms |
STNA; NEU1; NANase; N-acylneuraminate glycohydrolase; Influ Sialidase
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 9.65 ug.mL-1 | [2] | ||
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) | B-Lactams | Drug Info | IC50 = 10 ug.mL-1 | [3] | ||
Co-Target Name | Acetylcholinesterase (AChE) | Successful Target | ||||
UniProt ID | ACES_HUMAN | |||||
Gene Name | ACHE | |||||
Synonyms |
YT; N-ACHE; ARACHE
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Representative Drug(s) | Irinotecan | Drug Info | Ki = 50.5 nM | [4] | ||
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) | B-Lactams | Drug Info | Ki = 60.3 nM | [5] | ||
Co-Target Name | Indoleamine 2,3-dioxygenase 1 (IDO1) | Successful Target | ||||
UniProt ID | I23O1_HUMAN | |||||
Gene Name | IDO1 | |||||
Synonyms |
Indoleamine-pyrrole 2,3-dioxygenase; INDO; IDO-1; IDO
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Representative Drug(s) | Drug Info | Ki = 100 nM | [6] | |||
Co-Target Name | Dipeptidyl peptidase 4 (DPP-4) | Successful Target | ||||
UniProt ID | DPP4_HUMAN | |||||
Gene Name | DPP4 | |||||
Synonyms |
Tcell activation antigen CD26; TP103; T-cell activation antigen CD26; Dipeptidyl peptidase IV; Dipeptidyl peptidase 4 soluble form; DPP-IV; DPP IV; DPP 4; CD26; Adenosine deaminase complexing protein-2; Adenosine deaminase complexing protein 2; ADCP2; ADCP-2; ADABP
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 120 nM | [7] | ||
Co-Target Name | Human immunodeficiency virus Reverse transcriptase (HIV RT) | Successful Target | ||||
UniProt ID | POL_HV1B1 | |||||
Gene Name | HIV RT | |||||
Synonyms |
HIV p66 RT; HIV Exoribonuclease H
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Representative Drug(s) | Camptothecin | Drug Info | IC50 ~ 200 ug.mL-1 | [8] | ||
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) | B-Lactams | Drug Info | Ki = 293 nM | [5] | ||
Co-Target Name | Human immunodeficiency virus Protease (HIV PR) | Successful Target | ||||
UniProt ID | POL_HV1B1 | |||||
Gene Name | HIV PR | |||||
Synonyms |
HIV Retropepsin; HIV PR
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 450 nM | [9] | ||
Co-Target Name | DNA topoisomerase II (TOP2) | Successful Target | ||||
UniProt ID | TOP2A_HUMAN; TOP2B_HUMAN | |||||
Gene Name | TOP2A; TOP2B | |||||
Synonyms |
TOP2; DNA topoisomerase 2
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Representative Drug(s) | Topotecan | Drug Info | IC50 = 480 nM | [10] | ||
Co-Target Name | Xanthine dehydrogenase/oxidase (XDH) | Successful Target | ||||
UniProt ID | XDH_HUMAN | |||||
Gene Name | XDH | |||||
Synonyms |
Xanthine oxidase; Xanthine dehydrogenase; XDHA
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 550 nM | [11] | ||
Co-Target Name | Aldose reductase (AKR1B1) | Successful Target | ||||
UniProt ID | ALDR_HUMAN | |||||
Gene Name | AKR1B1 | |||||
Synonyms |
Aldehyde reductase; AKR1B1
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 600 nM | [12] | ||
Co-Target Name | Glycogen synthase kinase-3 alpha (GSK-3A) | Successful Target | ||||
UniProt ID | GSK3A_HUMAN | |||||
Gene Name | GSK3A | |||||
Synonyms |
Serine/threonineprotein kinase GSK3A; Serine/threonine-protein kinase GSK3A; Glycogen synthase kinase3 alpha; Glycogen synthase kinase 3; GSK3 alpha; GSK-3 alpha; GSK-3
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 800 nM | [13] | ||
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) | B-Lactams | Drug Info | IC50 = 830 nM | [14] | ||
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) | Camptothecin | Drug Info | EC50 = 2.1 nM | [15] | ||
Co-Target Name | Somatostatin receptor (SSTR) | Clinical trial Target | ||||
UniProt ID | SSR1_HUMAN; SSR2_HUMAN; SSR3_HUMAN; SSR4_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Camptothecin | Drug Info | IC50 = 2.21 nM | [16] | ||
Co-Target Name | Lysosomal alpha-glucosidase (GAA) | Successful Target | ||||
UniProt ID | LYAG_HUMAN | |||||
Gene Name | GAA | |||||
Synonyms |
GAA; Aglucosidase alfa; Acid maltase
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 5.96 ug.mL-1 | [17] | ||
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) | Topotecan | Drug Info | EC50 = 12 nM | Click to Show More | [18] | |
2 | Topotecan | Drug Info | EC50 = 71.3 nM | [20] | ||
Co-Target Name | Cytochrome P450 1B1 (CYP1B1) | Clinical trial Target | ||||
UniProt ID | CP1B1_HUMAN | |||||
Gene Name | CYP1B1 | |||||
Synonyms |
CYPIB1
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Representative Drug(s) | B-Lactams | Drug Info | Ki = 56 nM | [19] | ||
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) | Topotecan | Drug Info | EC50 = 71.3 nM | [20] | ||
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) | B-Lactams | Drug Info | IC50 = 500 nM | Click to Show More | [21] | |
2 | B-Lactams | Drug Info | IC50 < 1000 nM | [25] | ||
Co-Target Name | Glycogen synthase kinase-3 beta (GSK-3B) | Clinical trial Target | ||||
UniProt ID | GSK3B_HUMAN | |||||
Gene Name | GSK3B | |||||
Synonyms |
Serine/threonine-protein kinase GSK3B; GSK-3 beta
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 800 nM | [13] | ||
Co-Target Name | Plasmodium Oxoacyl-[acyl-carrier protein] reductase (Malaria fabG) | Clinical trial Target | ||||
UniProt ID | Q965D6_PLAFA | |||||
Gene Name | Malaria fabG | |||||
Synonyms |
3-oxoacyl-acyl-carrier protein reductase
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Representative Drug(s) | B-Lactams | Drug Info | Ki = 800 nM | [22] | ||
Co-Target Name | NADPH oxidase 4 (NOX4) | Clinical trial Target | ||||
UniProt ID | NOX4_HUMAN | |||||
Gene Name | NOX4 | |||||
Synonyms |
Renal NAD(P)Hoxidase; Renal NAD(P)H-oxidase; RENOX; Kidney superoxideproducing NADPH oxidase; Kidney superoxide-producing NADPH oxidase; Kidney oxidase1; Kidney oxidase-1; KOX1; KOX-1
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 850 nM | [23] | ||
Co-Target Name | Matrix metalloproteinase-12 (MMP-12) | Clinical trial Target | ||||
UniProt ID | MMP12_HUMAN | |||||
Gene Name | MMP12 | |||||
Synonyms |
Macrophage metalloelastase; Macrophage elastase; MME; ME; HME
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Representative Drug(s) | B-Lactams | Drug Info | IC50 = 980 nM | [24] | ||
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) | B-Lactams | Drug Info | Ki = 4.7 nM | [5] | ||
Co-Target Name | Tyrosyl-DNA phosphodiesterase 2 (TDP2) | Literature-reported Target | ||||
UniProt ID | TYDP2_HUMAN | |||||
Gene Name | TDP2 | |||||
Synonyms |
hTDP2; VPg unlinkase; Tyrosyl-RNA phosphodiesterase; Tyr-DNA phosphodiesterase 2; TRAF and TNF receptor-associated protein; TDP2; ETS1-associated protein II; ETS1-associated protein 2; EAPII; 5'-tyrosyl-DNA phosphodiesterase; 5'-Tyr-DNA phosphodiesterase
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Representative Drug(s) | Drug Info | IC50 = 970 nM | [26] | |||
Co-Target Name | Carboxylesterase 2 (CES2) | Co-Target | ||||
UniProt ID | EST2_HUMAN | |||||
Gene Name | CES2 | |||||
Synonyms |
Cocaine esterase; CE-2; hCE-2; Methylumbelliferyl-acetate deacetylase 2
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Representative Drug(s) | Drug Info | Ki = 109 nM | [27] | |||
Co-Target Name | Thiosulfate sulfurtransferase (TST) | Co-Target | ||||
UniProt ID | THTR_HUMAN | |||||
Gene Name | TST | |||||
Synonyms |
Rhodanese
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Representative Drug(s) | Drug Info | IC50 = 120 nM | [28] | |||
Co-Target Name | Cytochrome P450 1A1 (CYP1A1) | Co-Target | ||||
UniProt ID | CP1A1_HUMAN | |||||
Gene Name | CYP1A1 | |||||
Synonyms |
CYPIA1; Hydroperoxy icosatetraenoate dehydratase; Cytochrome P450 form 6; Cytochrome P450-C; Cytochrome P450-P1
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Representative Drug(s) | B-Lactams | Drug Info | Ki = 890 nM | [19] |
References | Top | ||||
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REF 1 | Screening of ubiquitous plant constituents for COX-2 inhibition with a scintillation proximity based assay. J Nat Prod. 2002 Nov;65(11):1517-21. | ||||
REF 2 | QSAR study of flavonoids and biflavonoids as influenza H1N1 virus neuraminidase inhibitors. Eur J Med Chem. 2010 May;45(5):1724-30. | ||||
REF 3 | Protein-tyrosine kinase inhibition: mechanism-based discovery of antitumor agents. J Nat Prod. 1992 Nov;55(11):1529-60. | ||||
REF 4 | Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely... J Med Chem. 2008 Jun 12;51(11):3154-70. | ||||
REF 5 | New natural product carbonic anhydrase inhibitors incorporating phenol moieties. Bioorg Med Chem. 2015 Nov 15;23(22):7219-25. | ||||
REF 6 | Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors. J Med Chem. 2015 Dec 24;58(24):9421-37. | ||||
REF 7 | Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus. Eur J Med Chem. 2018 May 10;151:145-157. | ||||
REF 8 | Evaluation of natural products as inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. J Nat Prod. 1991 Jan-Feb;54(1):143-54. | ||||
REF 9 | Design and discovery of flavonoid-based HIV-1 integrase inhibitors targeting both the active site and the interaction with LEDGF/p75. Bioorg Med Chem. 2014 Jun 15;22(12):3146-58. | ||||
REF 10 | Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives. Bioorg Med Chem. 2019 Oct 1;27(19):115026. | ||||
REF 11 | Structure-activity relationship and classification of flavonoids as inhibitors of xanthine oxidase and superoxide scavengers. J Nat Prod. 1998 Jan;61(1):71-6. | ||||
REF 12 | Synthesis of organic nitrates of luteolin as a novel class of potent aldose reductase inhibitors. Bioorg Med Chem. 2013 Jul 15;21(14):4301-10. | ||||
REF 13 | Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43. | ||||
REF 14 | Flavonoids as receptor tyrosine kinase FLT3 inhibitors. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1768-70. | ||||
REF 15 | Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem. 2007 Apr 1;15(7):2759-67. | ||||
REF 16 | An adjustable release rate linking strategy for cytotoxin-peptide conjugates. Bioorg Med Chem Lett. 2003 Mar 10;13(5):799-803. | ||||
REF 17 | Antioxidant and alpha-glucosidase inhibitory compounds from Pimpinella candolleana Wight et Arn. Med Chem Res. 2012 Jan 18;21:4324-9. | ||||
REF 18 | Tetracycline analogues with a selective inhibitory effect on HIF-1alpha. Medchemcomm. 2014;5:923-6. | ||||
REF 19 | Comparative CYP1A1 and CYP1B1 substrate and inhibitor profile of dietary flavonoids. Bioorg Med Chem. 2011 May 1;19(9):2842-9. | ||||
REF 20 | Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells. J Nat Prod. 2004 Dec;67(12):2002-7. | ||||
REF 21 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. Bioorg Med Chem. 2019 Mar 1;27(5):677-685. | ||||
REF 22 | Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids. J Med Chem. 2006 Jun 1;49(11):3345-53. | ||||
REF 23 | Small-molecule inhibitors of NADPH oxidase 4. J Med Chem. 2010 Sep 23;53(18):6758-62. | ||||
REF 24 | Natural products as a gold mine for selective matrix metalloproteinases inhibitors. Bioorg Med Chem. 2012 Jul 1;20(13):4164-71. | ||||
REF 25 | Structural Insight into the Interactions between Death-Associated Protein Kinase 1 and Natural Flavonoids. J Med Chem. 2015 Sep 24;58(18):7400-8. | ||||
REF 26 | Toxoflavins and deazaflavins as the first reported selective small molecule inhibitors of tyrosyl-DNA phosphodiesterase II. J Med Chem. 2013 Aug 22;56(16):6352-70. | ||||
REF 27 | Selective Inhibitors of Human Liver Carboxylesterase Based on a beta-Lapachone Scaffold: Novel Reagents for Reaction Profiling. J Med Chem. 2017 Feb 23;60(4):1568-1579. | ||||
REF 28 | HSP60/10 chaperonin systems are inhibited by a variety of approved drugs, natural products, and known bioactive molecules. Bioorg Med Chem Lett. 2019 May 1;29(9):1106-1112. |
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