Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T40016 | Target Info | |||
| Target Name | Glucocorticoid receptor (NR3C1) | ||||
| Synonyms |
Nuclear receptor subfamily 3 group C member 1; GRL; GR
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| Target Type | Successful Target | ||||
| Gene Name | NR3C1 | ||||
| Biochemical Class | Nuclear hormone receptor | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| 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) | Prednisolone | Drug Info | EC50 = 0.002 nM | Click to Show More | [1] | |
| 2 | Dexamethasone | Drug Info | Ki = 0.36 nM | [4] | ||
| 3 | Budesonide | Drug Info | EC50 = 4.8 nM | [7] | ||
| 4 | GW685698X | Drug Info | IC50 = 166 nM | [9] | ||
| 5 | Mifepristone | Drug Info | IC50 = 590 nM | [11] | ||
| 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 | Click to Show More | [2] | |
| 2 | Mifepristone | Drug Info | IC50 = 0.021 nM | [3] | ||
| 3 | GW685698X | Drug Info | IC50 = 21 nM | [9] | ||
| 4 | Budesonide | Drug Info | IC50 = 28 nM | [9] | ||
| 5 | Dexamethasone | Drug Info | IC50 = 440 nM | [10] | ||
| 6 | Prednisolone | Drug Info | IC50 ~ 1000 nM | [14] | ||
| Co-Target Name | Androgen receptor (AR) | Successful Target | ||||
| UniProt ID | ANDR_HUMAN | |||||
| Gene Name | AR | |||||
| Synonyms |
Testosterone receptor; Nuclear receptor subfamily 3 group C member 4; NR3C4; Dihydrotestosterone receptor; DHTR
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| Representative Drug(s) | Mifepristone | Drug Info | Ki = 0.65 nM | Click to Show More | [5] | |
| 2 | BAY 86-5044 | Drug Info | IC50 = 54 nM | [2] | ||
| 3 | Dexamethasone | Drug Info | IC50 ~ 1000 nM | [13] | ||
| Co-Target Name | Interleukin-6 (IL6) | Successful Target | ||||
| UniProt ID | IL6_HUMAN | |||||
| Gene Name | IL6 | |||||
| Synonyms |
Interferon beta-2; IL-6; IFNB2; IFN-beta-2; Hybridoma growth factor; CTL differentiation factor; CDF; BSF-2; B-cell stimulatory factor 2
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| Representative Drug(s) | Prednisolone | Drug Info | IC50 = 4.2 nM | [6] | ||
| 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) | Hydrocortisone | Drug Info | Ki = 13.18 nM | Click to Show More | [8] | |
| 2 | Prednisolone | Drug Info | Ki = 30.9 nM | [8] | ||
| 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) | Mifepristone | Drug Info | Ki ~ 200 nM | [5] | ||
| Co-Target Name | Estrogen receptor beta (ESR2) | Successful Target | ||||
| UniProt ID | ESR2_HUMAN | |||||
| Gene Name | ESR2 | |||||
| Synonyms |
Oestrogen receptor beta; Nuclear receptor subfamily 3 group A member 2; NR3A2; Erbeta; ESTRB; ER-beta; Beta-1
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| Representative Drug(s) | Mifepristone | Drug Info | Ki ~ 750 nM | [5] | ||
| Co-Target Name | Opioid receptor mu (MOP) | Successful Target | ||||
| UniProt ID | OPRM_HUMAN | |||||
| Gene Name | OPRM1 | |||||
| Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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| Representative Drug(s) | Mifepristone | Drug Info | Ki = 997 nM | [12] | ||
| Co-Target Name | TNF alpha converting enzyme (ADAM17) | Clinical trial Target | ||||
| UniProt ID | ADA17_HUMAN | |||||
| Gene Name | ADAM17 | |||||
| Synonyms |
TNFalpha converting enzyme; TNF-alpha-converting enzyme; TNF-alpha converting enzyme; TNF-alpha convertase; TACE; Snake venom-like protease; Disintegrin and metalloproteinase domain-containing protein 17; CSVP; CD156b antigen; CD156b; ADAM 17; A disintegrin and metalloproteinase domain 17
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| Representative Drug(s) | Prednisolone | Drug Info | IC50 = 14.9 nM | [6] | ||
| Co-Target Name | G-protein coupled bile acid receptor 1 (GPBAR1) | Clinical trial Target | ||||
| UniProt ID | GPBAR_HUMAN | |||||
| Gene Name | GPBAR1 | |||||
| Synonyms |
hGPCR19; hBG37; TGR5; Membrane-type receptor for bile acids; M-BAR; G-protein coupled receptor GPCR19; BG37
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| Representative Drug(s) | Prednisolone | Drug Info | IC50 = 251 nM | [15] | ||
| Co-Target Name | Glutamate decarboxylase (GLUL) | Discontinued Target | ||||
| UniProt ID | GLNA_HUMAN | |||||
| Gene Name | GLUL | |||||
| Synonyms |
Glutamateammonia ligase
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| Representative Drug(s) | Prednisolone | Drug Info | EC50 = 32 nM | [16] | ||
| 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) | CORT-125134 | Drug Info | IC50 = 210 nM | [17] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791826). J Med Chem. 2011 Oct 27;54(20):7318-33. | ||||
| REF 2 | Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6. | ||||
| REF 3 | Syntheses and antigestagenic activity of mifepristone derivatives. J Med Chem. 2009 Mar 12;52(5):1268-74. | ||||
| REF 4 | Glucocorticoid receptor modulators informed by crystallography lead to a new rationale for receptor selectivity, function, and implications for structure-based design. J Med Chem. 2014 Feb 13;57(3):849-60. | ||||
| REF 5 | Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes. J Med Chem. 2004 Aug 12;47(17):4213-30. | ||||
| REF 6 | US patent application no. 8901310B2, Tricyclic compounds, compositions, and methods | ||||
| REF 7 | Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases. J Med Chem. 2018 Jun 14;61(11):4757-73. | ||||
| REF 8 | 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 9 | Selective Nonsteroidal Glucocorticoid Receptor Modulators for the Inhaled Treatment of Pulmonary Diseases. J Med Chem. 2017 Oct 26;60(20):8591-605. | ||||
| REF 10 | Discovery of indazole ethers as novel, potent, non-steroidal glucocorticoid receptor modulators. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5741-8. | ||||
| REF 11 | 1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5015-7. | ||||
| REF 12 | DrugMatrix in vitro pharmacology data. National Toxicology Program | ||||
| REF 13 | Discovery of new selective glucocorticoid receptor agonist leads. Bioorg Med Chem Lett. 2017 Feb 1;27(3):437-42. | ||||
| REF 14 | Discovery of a subnanomolar and selective spirocyclic agonist of the glucocorticoid receptor. Eur J Med Chem. 2019 Jan 1;161:354-363. | ||||
| REF 15 | Discovery of a Potent and Orally Efficacious TGR5 Receptor Agonist. ACS Med Chem Lett. 2015 Nov 20;7(1):51-5. | ||||
| REF 16 | Novel N-arylpyrazolo[3,2-c]-based ligands for the glucocorticoid receptor: receptor binding and in vivo activity. J Med Chem. 2004 May 6;47(10):2441-52. | ||||
| REF 17 | Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist. J Med Chem. 2017 Apr 27;60(8):3405-3421. | ||||
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