Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T60529 | Target Info | |||
Target Name | Prostaglandin G/H synthase 1 (COX-1) | ||||
Synonyms |
Prostaglandin-endoperoxide synthase 1; Prostaglandin H2 synthase 1; PHS 1; PGHS-1; PGH synthase 1; Cyclooxygenase-1; COX1; COX-1
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Target Type | Successful Target | ||||
Gene Name | PTGS1 | ||||
Biochemical Class | Paired donor oxygen oxidoreductase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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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) | Drug Info | IC50 = 0.6 nM | [1] | |||
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) | Flufenamic Acid | Drug Info | IC50 = 16 nM | Click to Show More | [2] | |
2 | Drug Info | IC50 = 750 nM | [9] | |||
3 | Naproxen | Drug Info | IC50 = 900 nM | [5] | ||
Co-Target Name | Aromatase (CYP19A1) | Successful Target | ||||
UniProt ID | CP19A_HUMAN | |||||
Gene Name | CYP19A1 | |||||
Synonyms |
P-450AROM; Estrogen synthetase; Estrogen synthase; Cytochrome P450 19A1; Cytochrome P-450AROM; CYPXIX; CYP19; CYAR; ARO1
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Representative Drug(s) | Drug Info | IC50 ~ 40 ug.mL-1 | [3] | |||
Co-Target Name | Dihydrodiol dehydrogenase type I (AKR1C3) | Successful Target | ||||
UniProt ID | AK1C3_HUMAN | |||||
Gene Name | AKR1C3 | |||||
Synonyms |
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase; Testosterone 17-beta-dehydrogenase 5; Prostaglandin F synthase; PGFS; KIAA0119; Indanol dehydrogenase; HSD17B5; HA1753; Dihydrodiol dehydrogenase 3; DDH1; DD3; DD-3; Chlordecone reductase homolog HAKRb; Aldo-keto reductase family 1 member C3; 3-alpha-hydroxysteroid dehydrogenase type 2; 3-alpha-HSD type II, brain; 3-alpha-HSD type 2; 17-beta-hydroxysteroid dehydrogenase type 5; 17-beta-HSD 5
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Representative Drug(s) | Flufenamic Acid | Drug Info | IC50 = 50 nM | Click to Show More | [2] | |
2 | Naproxen | Drug Info | IC50 = 180 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 = 88 nM | [4] | |||
Co-Target Name | PI3-kinase alpha (PIK3CA) | Successful Target | ||||
UniProt ID | PK3CA_HUMAN | |||||
Gene Name | PIK3CA | |||||
Synonyms |
p110alpha; Serine/threonine protein kinase PIK3CA; PtdIns3kinase subunit p110alpha; PtdIns3kinase subunit alpha; PtdIns-3-kinase subunit p110-alpha; PtdIns-3-kinase subunit alpha; Phosphoinositide3kinase catalytic alpha polypeptide; Phosphoinositide-3-kinase catalytic alpha polypeptide; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalytic subunit alpha; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; PI3kinase subunit alpha; PI3Kalpha; PI3K-alpha; PI3-kinase subunit alpha
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Representative Drug(s) | Drug Info | IC50 = 250 nM | [6] | |||
Co-Target Name | Amyloid beta A4 protein (APP) | Successful Target | ||||
UniProt ID | A4_HUMAN | |||||
Gene Name | APP | |||||
Synonyms |
Protease nexin-II; PreA4; PN-II; Cerebral vascular amyloid peptide; CVAP; Amyloid-beta precursor protein; Amyloid-beta A4 protein; Alzheimer disease amyloid protein; APPI; APP; AD1; ABPP; A4
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Representative Drug(s) | Curcumin | Drug Info | IC50 = 630 nM | [7] | ||
Co-Target Name | Monoamine oxidase type A (MAO-A) | Successful Target | ||||
UniProt ID | AOFA_HUMAN | |||||
Gene Name | MAOA | |||||
Synonyms |
Monoamine oxidase A; Amine oxidase [flavin-containing] A
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Representative Drug(s) | Curcumin | Drug Info | Ki = 710 nM | [8] | ||
Co-Target Name | Transformation-sensitive protein p120 (TRPA1) | Successful Target | ||||
UniProt ID | TRPA1_HUMAN | |||||
Gene Name | TRPA1 | |||||
Synonyms |
TRPA1; Ankyrin-like with transmembrane domains protein 1; ANKTM1
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Representative Drug(s) | Drug Info | IC50 = 750 nM | [10] | |||
Co-Target Name | Estrogen receptor (ESR) | Successful Target | ||||
UniProt ID | ESR1_HUMAN | |||||
Gene Name | ESR1 | |||||
Synonyms |
Nuclear receptor subfamily 3 group A member 1; NR3A1; Estradiol receptor; ESR; ER-alpha; ER
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Representative Drug(s) | Drug Info | Ki = 785 nM | [11] | |||
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 = 830 nM | [12] | |||
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 = 950 nM | [12] | |||
Co-Target Name | Lactoylglutathione lyase (GLO1) | Clinical trial Target | ||||
UniProt ID | LGUL_HUMAN | |||||
Gene Name | GLO1 | |||||
Synonyms |
S-D-lactoylglutathione methylglyoxal lyase; Methylglyoxalase; Ketone-aldehyde mutase; Glyoxalase I; GlxI; Glx I; GLO1; Aldoketomutase
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Representative Drug(s) | Curcumin | Drug Info | Ki = 5 nM | [13] | ||
Co-Target Name | Tissue factor (F3) | Successful Target | ||||
UniProt ID | TF_HUMAN | |||||
Gene Name | F3 | |||||
Synonyms |
Thromboplastin; TF; F3; Coagulation factor III; CD142 antigen
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Representative Drug(s) | Curcumin | Drug Info | IC50 = 13.16 nM | [14] | ||
Co-Target Name | Prostaglandin E synthase (PTGES) | Clinical trial Target | ||||
UniProt ID | PTGES_HUMAN | |||||
Gene Name | PTGES | |||||
Synonyms |
p53-induced gene 12 protein; PIG12; PGES; PGE synthase; P53-induced apoptosis protein 12; Microsomal prostaglandin E synthase 1; Microsomal glutathione S-transferase 1-like 1; MPGES1; MPGES-1; MGST1L1; MGST1-L1
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Representative Drug(s) | Curcumin | Drug Info | IC50 = 200 nM | [15] | ||
Co-Target Name | PI3-kinase beta (PIK3CB) | Clinical trial Target | ||||
UniProt ID | PK3CB_HUMAN | |||||
Gene Name | PIK3CB | |||||
Synonyms |
p110beta; PtdIns3kinase subunit p110beta; PtdIns3kinase subunit beta; PtdIns-3-kinase subunit p110-beta; PtdIns-3-kinase subunit beta; Phosphatidylinositol 4,5bisphosphate 3kinase catalytic subunitbeta isoform; Phosphatidylinositol 4,5bisphosphate 3kinase 110 kDa catalyticsubunit beta; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit beta; PIK3C1; PI3kinase subunit beta; PI3Kbeta; PI3K-beta; PI3-kinase subunit beta
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Representative Drug(s) | Drug Info | IC50 = 500 nM | [6] | |||
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) | Drug Info | Ki = 750 nM | [16] | |||
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 = 810 nM | [12] | |||
Co-Target Name | CDGSH iron-sulfur domain-containing protein 1 (CISD1_HUMAN) | Co-Target | ||||
UniProt ID | CISD1_HUMAN | |||||
Gene Name | CISD1 | |||||
Synonyms |
MitoNEET
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Representative Drug(s) | Curcumin | Drug Info | Ki = 101 nM | [17] | ||
Co-Target Name | Thiosulfate sulfurtransferase (TST) | Co-Target | ||||
UniProt ID | THTR_HUMAN | |||||
Gene Name | TST | |||||
Synonyms |
Rhodanese
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Representative Drug(s) | Mesalazine | Drug Info | IC50 = 280 nM | [18] | ||
Co-Target Name | Aldo-keto reductase family 1 member C2 (AKR1C2) | Co-Target | ||||
UniProt ID | AK1C2_HUMAN | |||||
Gene Name | AKR1C2 | |||||
Synonyms |
Dihydrodiol dehydrogenase 2; DD-2; DD2; 3-alpha-HSD3; Chlordecone reductase homolog HAKRD; Dihydrodiol dehydrogenase/bile acid-binding protein; DD/BABP; Type III 3-alpha-hydroxysteroid dehydrogenase
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Representative Drug(s) | Flufenamic Acid | Drug Info | IC50 = 370 nM | [2] | ||
Co-Target Name | Aldo-keto reductase family 1 member B10 (AKR1B10) | Co-Target | ||||
UniProt ID | AK1BA_HUMAN | |||||
Gene Name | AKR1B10 | |||||
Synonyms |
ARL-1; Aldose reductase-like; Aldose reductase-related protein; ARP; hARP; Small intestine reductase; SI reductase
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Representative Drug(s) | Flufenamic Acid | Drug Info | IC50 = 760 nM | [19] |
References | Top | ||||
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REF 1 | 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 2 | Development of potent and selective inhibitors of aldo-keto reductase 1C3 (type 5 17-hydroxysteroid dehydrogenase) based on N-phenyl-aminobenzoates and their structure-activity relationships. J Med Chem. 2012 Mar 8;55(5):2311-23. | ||||
REF 3 | Aromatase inhibitors from Broussonetia papyrifera. J Nat Prod. 2001 Oct;64(10):1286-93. | ||||
REF 4 | Design, synthesis, biological and structural evaluation of functionalized resveratrol analogues as inhibitors of quinone reductase 2. Bioorg Med Chem. 2013 Oct 1;21(19):6022-37. | ||||
REF 5 | Discovery of (R)-2-(6-Methoxynaphthalen-2-yl)butanoic Acid as a Potent and Selective Aldo-keto Reductase 1C3 Inhibitor. J Med Chem. 2016 Aug 25;59(16):7431-44. | ||||
REF 6 | Small molecules targeting phosphoinositide 3-kinases. Medchemcomm. 2012;3:1337-55. | ||||
REF 7 | Neuritogenic activity of bi-functional bis-tryptoline triazole. Bioorg Med Chem. 2017 Feb 1;25(3):1195-1201. | ||||
REF 8 | Monoamine Oxidase Inhibitory Activity of Novel Pyrazoline Analogues: Curcumin Based Design and Synthesis. ACS Med Chem Lett. 2015 Dec 1;7(1):56-61. | ||||
REF 9 | Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites. J Med Chem. 2010 Jul 8;53(13):5033-43. | ||||
REF 10 | Synthesis of resveratrol derivatives as new analgesic drugs through desensitization of the TRPA1 receptor. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3167-72. | ||||
REF 11 | Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem. 2005 Jan 13;48(1):287-91. | ||||
REF 12 | Carbonic anhydrase inhibitors. Antioxidant polyphenols effectively inhibit mammalian isoforms I-XV. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5050-3. | ||||
REF 13 | Recent advances in the discovery and development of glyoxalase I inhibitors. Bioorg Med Chem. 2020 Feb 15;28(4):115243. | ||||
REF 14 | Microbial hydroxylation and glycosylation of pentacyclic triterpenes as inhibitors on tissue factor procoagulant activity. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1026-30. | ||||
REF 15 | Targeting microsomal prostaglandin E2 synthase-1 (mPGES-1): the development of inhibitors as an alternative to non-steroidal anti-inflammatory drugs (NSAIDs). Medchemcomm. 2015;6:2081-123. | ||||
REF 16 | Phytoestrogens and their synthetic analogues as substrate mimic inhibitors of CYP1B1. Eur J Med Chem. 2019 Feb 1;163:28-36. | ||||
REF 17 | Identification of small molecules that bind to the mitochondrial protein mitoNEET. Bioorg Med Chem Lett. 2016 Nov 1;26(21):5350-5353. | ||||
REF 18 | 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. | ||||
REF 19 | Flavones Inhibit the Activity of AKR1B10, a Promising Therapeutic Target for Cancer Treatment. J Nat Prod. 2015 Nov 25;78(11):2666-74. |
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