Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T56923 Target Info
Target Name C-X-C chemokine receptor type 2 (CXCR2)
Synonyms
Interleukin-8 receptor B; IL8RB; IL-8R B; IL-8 receptor type 2; High affinity interleukin-8 receptor B; GRO/MGSA receptor; CXCR-2; CXC-R2; CDw128b; CD182
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Target Type Successful Target
Gene Name CXCR2
Biochemical Class GPCR rhodopsin
UniProt ID
CXCR2_HUMAN
Co-Targets of This Target  Top
Co-Target Name C-X-C chemokine receptor type 1 (CXCR1) Successful Target
UniProt ID CXCR1_HUMAN
Gene Name CXCR1
Synonyms
Interleukin-8 receptor A; IL8RA; IL-8R A; IL-8 receptor type 1; High affinity interleukin-8 receptor A; CXCR-1; CXC-R1; CMKAR1; CDw128a; CD181
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Representative Drug(s) Reparixin Drug Info IC50 = 1 nM Click to Show More [1]
2 SCH-527123 Drug Info IC50 = 3.9 nM [1]
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) Clotrimazole Drug Info IC50 = 1.8 nM [2]
Co-Target Name Orphan nuclear receptor NR1I3 (NR1I3) Successful Target
UniProt ID NR1I3_HUMAN
Gene Name NR1I3
Synonyms
Orphan nuclear receptor MB67; Orphan nuclear receptor CAR; Nuclear receptor subfamily 1 group I member 3; Nuclear receptor CAR; Constitutive androstane receptor; Constitutive active response; Constitutive activator of retinoid response; CAR
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Representative Drug(s) Clotrimazole Drug Info IC50 = 80 nM [3]
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) Clotrimazole Drug Info Ki = 81.5 nM [4]
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) Ibuprofen Drug Info IC50 = 100 nM [5]
Co-Target Name S-mephenytoin 4-hydroxylase (CYP2C9) Successful Target
UniProt ID CP2C9_HUMAN
Gene Name CYP2C9
Synonyms
Cytochrome P450 PB-1; Cytochrome P450 MP-8; Cytochrome P450 MP-4; Cytochrome P450 2C9; Cytochrome P-450MP; Cholesterol 25-hydroxylase; CYPIIC9; CYP2C10; (S)-limonene 7-monooxygenase; (S)-limonene 6-monooxygenase; (R)-limonene 6-monooxygenase
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Representative Drug(s) Clotrimazole Drug Info IC50 = 136 nM [6]
Co-Target Name Prostaglandin G/H synthase 1 (COX-1) Successful Target
UniProt ID PGH1_HUMAN
Gene Name PTGS1
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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Representative Drug(s) Ibuprofen Drug Info IC50 = 290 nM [7]
Co-Target Name Voltage-gated calcium channel alpha Cav1.2 (CACNA1C) Successful Target
UniProt ID CAC1C_HUMAN
Gene Name CACNA1C
Synonyms
Voltage-gated calcium channel subunit alpha Cav1.2; Voltage-dependent L-type calcium channel subunit alpha-1C; Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle; CCHL1A1; CACNL1A1; CACN2; CACH2
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Representative Drug(s) Clotrimazole Drug Info IC50 = 590 nM [8]
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) Clotrimazole Drug Info IC50 = 883 nM [6]
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) Clotrimazole Drug Info IC50 = 20 nM [9]
Co-Target Name Calcium-activated potassium channel KCa3.1 (KCNN4) Clinical trial Target
UniProt ID KCNN4_HUMAN
Gene Name KCNN4
Synonyms
SKCa4; SKCa 4; SK4; Putative Gardos channel; KCa4; KCa3.1; Intermediate conductance calcium-activated potassium channel protein 4; IKCa1; IK1
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Representative Drug(s) Clotrimazole Drug Info IC50 = 70 nM [10]
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) Clotrimazole Drug Info IC50 = 130 nM [11]
Co-Target Name Cytochrome P450 2C8 (CYP2C8) Co-Target
UniProt ID CP2C8_HUMAN
Gene Name CYP2C8
Synonyms
CYPIIC8; Cytochrome P450 IIC2; Cytochrome P450 MP-12; Cytochrome P450 MP-20; Cytochrome P450 form 1; S-mephenytoin 4-hydroxylase
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Representative Drug(s) Clotrimazole Drug Info IC50 = 803 nM [6]
References  Top
REF 1 Chemokine receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9363-92.
REF 2 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 3 Development of CINPA1 analogs as novel and potent inverse agonists of constitutive androstane receptor. Eur J Med Chem. 2016 Jan 27;108:505-528.
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 Nonsteroidal anti-inflammatory drugs as scaffolds for the design of 5-lipoxygenase inhibitors. J Med Chem. 1997 Feb 28;40(5):819-24.
REF 6 Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.
REF 7 Synthesis, pharmacological characterization, and docking analysis of a novel family of diarylisoxazoles as highly selective cyclooxygenase-1 (COX-1) inhibitors. J Med Chem. 2013 Jun 13;56(11):4277-99.
REF 8 Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. J Appl Toxicol. 2012 Oct;32(10):858-66.
REF 9 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 10 Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304.
REF 11 Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors. Drug Metab Dispos. 2007 Mar;35(3):493-500.

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