Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T11211 Target Info
Target Name Androgen receptor (AR)
Synonyms
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
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Target Type Successful Target
Gene Name AR
Biochemical Class Nuclear hormone receptor
UniProt ID
ANDR_HUMAN
Co-Targets of This Target  Top
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 [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) TOK-001 Drug Info IC50 = 28.1 nM [2]
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) Testosterone Drug Info IC50 = 34 nM [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 [1]
Co-Target Name Corticosteroid-binding globulin (SERPINA6) Successful Target
UniProt ID CBG_HUMAN
Gene Name SERPINA6
Synonyms
Transcortin; SERPINA6; CBG
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Representative Drug(s) Testosterone Drug Info Ki = 190.55 nM Click to Show More [4]
2 Nandrolone Drug Info Ki = 724.44 nM [4]
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) Dihydrotestosterone Drug Info Ki = 220 nM Click to Show More [5]
2 Testosterone Drug Info Ki = 600 nM [7]
Co-Target Name Mineralocorticoid receptor (MR) Successful Target
UniProt ID MCR_HUMAN
Gene Name NR3C2
Synonyms
Nuclear receptor subfamily 3 group C member 2; Mineralocorticoid receptor; MLR; MCR; Inner ear mineralocorticoid receptor; Delta
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Representative Drug(s) Dihydrotestosterone Drug Info IC50 = 360 nM [6]
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) Dihydrotestosterone Drug Info IC50 = 540 nM [6]
Co-Target Name Progesterone receptor (PGR) Successful Target
UniProt ID PRGR_HUMAN
Gene Name PGR
Synonyms
PR; Nuclear receptor subfamily 3 group C member 3; NR3C3
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Representative Drug(s) RAD-140 Drug Info IC50 = 750 nM [8]
Co-Target Name Sex hormone-binding globulin (SHBG) Co-Target
UniProt ID SHBG_HUMAN
Gene Name SHBG
Synonyms
SHBG; Sex steroid-binding protein; SBP; Testis-specific androgen-binding protein; ABP; Testosterone-estradiol-binding globulin; TeBG; Testosterone-estrogen-binding globulin
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Representative Drug(s) Dihydrotestosterone Drug Info IC50 = 3.8 nM Click to Show More [9]
2 Testosterone Drug Info IC50 = 14 nM [10]
Co-Target Name Cytochrome P450 21 (CYP21A2) Co-Target
UniProt ID CP21A_HUMAN
Gene Name CYP21A2
Synonyms
Steroid 21-hydroxylase; 21-OHase; Cytochrome P-450c21; Cytochrome P450 XXI; Cytochrome P450-C21; Cytochrome P450-C21B
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Representative Drug(s) TOK-001 Drug Info IC50 = 77.2 nM [2]
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 [1]
Co-Target Name Arylacetamide deacetylase (AADAC) Co-Target
UniProt ID AAAD_HUMAN
Gene Name AADAC
Representative Drug(s) Flutamide Drug Info Ki = 600 nM [11]
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 [12]
References  Top
REF 1 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 2 Structure-Based Design of Inhibitors with Improved Selectivity for Steroidogenic Cytochrome P450 17A1 over Cytochrome P450 21A2. J Med Chem. 2018 Jun 14;61(11):4946-60.
REF 3 Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. J Appl Toxicol. 2012 Oct;32(10):858-66.
REF 4 Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR. J Med Chem. 2004 May 20;47(11):2732-42.
REF 5 Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione. J Med Chem. 1989 Mar;32(3):651-8.
REF 6 Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs) Part III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate. Bioorg Med Chem. 2017 Jul 1;25(13):3330-49.
REF 7 Analogues of aminoglutethimide: selective inhibition of cholesterol side-chain cleavage. J Med Chem. 1983 Jan;26(1):50-4.
REF 8 Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-9.
REF 9 A novel, nonsteroidal inhibitor of androgen binding to the rat androgen binding protein: diethyl [[[3-(2,6-dimethyl-4-pyridinyl)-4-fluorophenyl]amino]methylene] propanedioate. J Med Chem. 1990 Jan;33(1):129-32.
REF 10 Progressive docking: a hybrid QSAR/docking approach for accelerating in silico high throughput screening. J Med Chem. 2006 Dec 14;49(25):7466-78.
REF 11 Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse. Drug Metab Dispos. 2012 Apr;40(4):671-9.
REF 12 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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