Co-Target(s) Information

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Target General Information
Co-Targets of This Target
References
Target General Information  Top
Target ID T46521 Target Info
Target Name Androgen receptor messenger RNA (AR mRNA)
Synonyms
Testosterone receptor (mRNA); Nuclear receptor subfamily 3 group C member 4 (mRNA); NR3C4 (mRNA); Dihydrotestosterone receptor (mRNA); DHTR (mRNA); Androgen receptor (mRNA)
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Target Type Clinical trial Target
Gene Name AR
Biochemical Class mRNA target
UniProt ID
ANDR_HUMAN
Co-Targets of This Target  Top
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) BAY 86-5044 Drug Info IC50 = 0.0025 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) Dihydrotestosterone Drug Info Ki = 220 nM [2]
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 [3]
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 [3]
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 [4]
References  Top
REF 1 Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
REF 2 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 3 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 4 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.

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