Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T73726 | Target Info | |||
Target Name | Candida Cytochrome P450 51 (Candi ERG11) | ||||
Synonyms |
Sterol 14alpha-demethylase; Sterol 14-alpha demethylase; P450LI; P450L1; P450-14DM; Lanosterol 14 alpha-demethylase; LDM; Erg11p; ERG11; Cytochrome P450-dependent lanosterol 14-demethylase; Cytochrome P-450 lanosterol 14-alpha-demethylase; Cyt P450 14DM; CYPLI; CYPL1
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Target Type | Successful Target | ||||
Gene Name | Candi ERG11 | ||||
Biochemical Class | Paired donor oxygen oxidoreductase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Debrisoquine 4-hydroxylase (CYP2D6) | Successful Target | ||||
UniProt ID | CP2D6_HUMAN | |||||
Gene Name | CYP2D6 | |||||
Synonyms |
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) | Ketoconazole | Drug Info | IC50 = 10 nM | [1] | ||
Co-Target Name | Steroid 17-alpha-monooxygenase (S17AH) | Successful Target | ||||
UniProt ID | CP17A_HUMAN | |||||
Gene Name | CYP17A1 | |||||
Synonyms |
Steroid 17-alpha-hydroxylase/17,20 lyase; P450c17; P450-C17; P450 17; CYPXVII; CYP17A1; CYP 17; 17 alpha-Hydroxylase/C17-20-lyase
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Representative Drug(s) | Posaconazole | Drug Info | IC50 = 42 nM | Click to Show More | [2] | |
2 | Ketoconazole | Drug Info | IC50 = 48 nM | [3] | ||
3 | Bifonazole | Drug Info | Ki = 56.5 nM | [4] | ||
4 | Miconazole | Drug Info | Ki = 243 nM | [4] | ||
5 | Econazole | Drug Info | Ki = 325 nM | [4] | ||
6 | Tioconazole | Drug Info | Ki = 505 nM | [4] | ||
Co-Target Name | Steroid 11-beta-hydroxylase (CYP11B1) | Successful Target | ||||
UniProt ID | C11B1_HUMAN | |||||
Gene Name | CYP11B1 | |||||
Synonyms |
S11BH; P450C11; P-450c11; CYPXIB1; CYP11B1
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Representative Drug(s) | Posaconazole | Drug Info | IC50 = 310 nM | [2] | ||
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) | Miconazole | Drug Info | IC50 = 600 nM | Click to Show More | [5] | |
2 | Ketoconazole | Drug Info | IC50 = 951.48 nM | [7] | ||
Co-Target Name | Collagen (CO) | Successful Target | ||||
UniProt ID | CP3A4_HUMAN; CP3A5_HUMAN; CP3A7_HUMAN; CP343_HUMAN | |||||
Gene Name | NO-GeName | |||||
Representative Drug(s) | Voriconazole | Drug Info | Ki = 660 nM | [6] | ||
Co-Target Name | Lanosterol 14-alpha demethylase (CYP51A1) | Clinical trial Target | ||||
UniProt ID | CP51A_HUMAN | |||||
Gene Name | CYP51A1 | |||||
Synonyms |
Cytochrome P450LI; Cytochrome P45014DM; Cytochrome P450-14DM; Cytochrome P450 51A1
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Representative Drug(s) | Fluconazole | Drug Info | IC50 = 0.039 ug.mL-1 | Click to Show More | [8] | |
2 | Econazole | Drug Info | IC50 = 50 nM | [11] | ||
3 | Miconazole | Drug Info | IC50 = 200 nM | [11] | ||
4 | Bifonazole | Drug Info | IC50 = 342 nM | [11] | ||
Co-Target Name | Albendazole monooxygenase (CYP3A4) | Clinical trial Target | ||||
UniProt ID | CP3A4_HUMAN | |||||
Gene Name | CYP3A4 | |||||
Synonyms |
Taurochenodeoxycholate 6-alpha-hydroxylase; Quinine 3-monooxygenase; P450-PCN1; Nifedipine oxidase; NF-25; HLp; Cytochrome P450-PCN1; Cytochrome P450 NF-25; Cytochrome P450 HLp; Cytochrome P450 3A4; Cytochrome P450 3A3; CYPIIIA4; CYPIIIA3; CYP3A3; Albendazole sulfoxidase; Albendazole monooxygenase (sulfoxide-forming); 1,8-cineole 2-exo-monooxygenase
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Representative Drug(s) | Ketoconazole | Drug Info | IC50 = 17 nM | Click to Show More | [9] | |
2 | Posaconazole | Drug Info | IC50 = 50 nM | [10] | ||
3 | Miconazole | Drug Info | IC50 = 180 nM | [12] | ||
4 | Econazole | Drug Info | IC50 = 430 nM | [13] | ||
Co-Target Name | Aldosterone synthase (CYP11B2) | Clinical trial Target | ||||
UniProt ID | C11B2_HUMAN | |||||
Gene Name | CYP11B2 | |||||
Synonyms |
Steroid 18hydroxylase; Cytochrome P450C18; Cytochrome P450Aldo; Cytochrome P450 11B2, mitochondrial; CYPXIB2; CYP11B2; Aldosteronesynthesizing enzyme; ALDOS
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Representative Drug(s) | Posaconazole | Drug Info | IC50 = 21 nM | [2] | ||
Co-Target Name | Cytochrome P450 2B6 (CYP2B6) | Literature-reported Target | ||||
UniProt ID | CP2B6_HUMAN | |||||
Gene Name | CYP2B6 | |||||
Synonyms |
Cytochrome P450 IIB1; CYPIIB6; 1,4-cineole 2-exo-monooxygenase
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Representative Drug(s) | Voriconazole | Drug Info | Ki = 340 nM | [6] | ||
Co-Target Name | Cytochrome P450 3A5 (CYP3A5) | Co-Target | ||||
UniProt ID | CP3A5_HUMAN | |||||
Gene Name | CYP3A5 | |||||
Synonyms |
Cytochrome P450-PCN3; CYPIIIA5
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Representative Drug(s) | Ketoconazole | Drug Info | IC50 = 141 nM | [14] | ||
Co-Target Name | Cytochrome P450 2J2 (CYP2J2) | Co-Target | ||||
UniProt ID | CP2J2_HUMAN | |||||
Gene Name | CYP2J2 | |||||
Synonyms |
Albendazole monooxygenase (hydroxylating); Albendazole monooxygenase (sulfoxide-forming); Arachidonic acid epoxygenase; Hydroperoxy icosatetraenoate isomerase; CYPIIJ2
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Representative Drug(s) | Miconazole | Drug Info | IC50 = 580 nM | [15] |
References | Top | ||||
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REF 1 | Novel non-sulfonamide 5-HT6 receptor partial inverse agonist in a group of imidazo[4,5-b]pyridines with cognition enhancing properties. Eur J Med Chem. 2018 Jan 20;144:716-29. | ||||
REF 2 | Design and optimization of highly-selective, broad spectrum fungal CYP51 inhibitors. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3243-3248. | ||||
REF 3 | Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17alpha-hydroxylase-C17,20-lyase (Cyp17). Bioorg Med Chem Lett. 2018 Jul 15;28(13):2270-4. | ||||
REF 4 | Three dimensional pharmacophore modeling of human CYP17 inhibitors. Potential agents for prostate cancer therapy. J Med Chem. 2003 Jun 5;46(12):2345-51. | ||||
REF 5 | Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. | ||||
REF 6 | Comprehensive in vitro analysis of voriconazole inhibition of eight cytochrome P450 (CYP) enzymes: major effect on CYPs 2B6, 2C9, 2C19, and 3A. Antimicrob Agents Chemother. 2009 Feb;53(2):541-51. | ||||
REF 7 | Studies on non-steroidal inhibitors of aromatase enzyme; 4-(aryl/heteroaryl)-2-(pyrimidin-2-yl)thiazole derivatives. Bioorg Med Chem. 2018 May 1;26(8):1986-1995. | ||||
REF 8 | Modeling, synthesis and biological activity of novel antifungal agents (1). Bioorg Med Chem Lett. 1998 Jul 21;8(14):1819-24. | ||||
REF 9 | Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate. J Med Chem. 2019 Dec 12;62(23):10563-10582. | ||||
REF 10 | Design and optimization of highly-selective fungal CYP51 inhibitors. Bioorg Med Chem Lett. 2014 Aug 1;24(15):3455-8. | ||||
REF 11 | Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. Drug Metab Dispos. 2007 Mar;35(3):493-500. | ||||
REF 12 | Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. | ||||
REF 13 | Strategies for the development of highly selective cytochrome P450 inhibitors: Several CYP targets in current research. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2016-2024. | ||||
REF 14 | Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. J Med Chem. 2020 Feb 13;63(3):1415-1433. | ||||
REF 15 | Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51. |
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