General Information of Drug (ID: DMLEDHR)

Drug Name
AL-43 Drug Info
Synonyms
AL-438; CHEMBL266282; A-240610.0; SCHEMBL4172433; BDBM50107347; A-224817.0; 5-Allyl-2,2,4-trimethyl-10-methoxy-2,5-dihydro-1H-1-aza-6-oxachrysene; 5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene; 5-allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno[3,4-f]quinoline; (+/-)5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene; (+)5-Allyl-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-6-oxa-1-aza-chrysene
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
9906282
TTD Drug ID
DMLEDHR

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Investigative Drug(s)
Patented Agent(s)
Discontinued Drug(s)
Drug(s) Targeting Progesterone receptor (PGR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [3]
Desogestrel DM27U4Y Contraception QA21 Approved [4]
Ulipristal DMBNI20 Contraception QA21 Approved [5]
Etonogestrel DMKA8J4 Contraception QA21 Approved [6]
Megestrol DMDH9KX Breast cancer 2C60-2C65 Approved [7]
Segesterone acetate; ethinyl estradiol DMFEGB0 Contraception QA21 Approved [8]
Norgestimate DMYP4XC Acne vulgaris ED80 Approved [6]
Dydrogesterone DMAKIDV Menstrual disorder GA20.3 Approved [9]
Medroxyprogesterone DMBGWPH Solid tumour/cancer 2A00-2F9Z Approved [9]
Ethynodiol Diacetate DMZM84R Contraception QA21 Approved [10]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Vamorolone DM047HI Duchenne muscular dystrophy 8C70.1 Approved [11]
CORT125281 DMHBOUX Prostate cancer 2C82.0 Phase 2 [12]
ISIS-GCCR DMICMNU Diabetic complication 5A2Y Phase 2 [13]
ORIC-101 DMR12S0 Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
AZD9567 DMAXHC0 Rheumatoid arthritis FA20 Phase 1 [11]
A-348441 DM25CBW Type-2 diabetes 5A11 Phase 1 [14]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one DMM9X0G Discovery agent N.A. Investigative [15]
(11-BETA)-11,21-DIHYDROXY-PREGN-4-ENE-3,20-DIONE DMTPQ84 Discovery agent N.A. Investigative [16]
deoxycorticosterone DMW6YLS Discovery agent N.A. Investigative [16]
LGD-5552 DM67KWM Discovery agent N.A. Investigative [17]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dihydrotestosterone DM3S8XC Prostate hyperplasia GA90 Phase 4 [18]
BAY 86-5044 DMRZLU4 Breast cancer 2C60-2C65 Phase 2 [19]
TRC-253 DMXI8CD Prostate cancer 2C82.0 Phase 1/2 [12]
IONIS-AR-2.5Rx DMF2DMS Prostate cancer 2C82.0 Phase 1/2 [20]
ISIS-AR DM8P3N5 Prostate cancer 2C82.0 Phase 1 [21]
EZN-4176 DMNPS59 Prostate cancer 2C82.0 Phase 1 [22]
EUGENOL DM7US1H Discovery agent N.A. Patented [23]
RU-58841 DMMEAZ2 Acne vulgaris ED80 Discontinued in Phase 1 [24]
flavone DMEQH6J Discovery agent N.A. Investigative [25]
APIGENIN DMI3491 Discovery agent N.A. Investigative [25]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Aldosterone DM9S2JW Hypertension BA00-BA04 Approved [26]
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [27]
Fludrocortisone DMUDIR8 Addison disease 5A74.0 Approved [28]
Desoxycorticosterone Acetate DMS0AFE Discovery agent N.A. Approved [27]
Desoxycorticosterone Pivalate DMSA4B3 Addison disease 5A74.0 Approved [29]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [30]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [27]
Finerenone DMM4FJ3 Chronic kidney disease GB61 Approved [31]
ZK-91587 DMJ94L0 Cardiovascular disease BA00-BE2Z Phase 2 [32]
Nerenone DMBJ3GL Diabetic nephropathy GB61.Z Phase 2 [33]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Androgen receptor messenger RNA (AR mRNA) TTKPW01 ANDR_HUMAN Inhibitor [1]
Glucocorticoid receptor messenger RNA (GCR mRNA) TTOZRK6 GCR_HUMAN Inhibitor [2]
Mineralocorticoid receptor (MR) TT26PHO MCR_HUMAN Inhibitor [1]
Progesterone receptor (PGR) TTUV8G9 PRGR_HUMAN Inhibitor [1]

References

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2 Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.
3 Clinical pipeline report, company report or official report of lipocine.
4 Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40.
5 Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
6 Pharmacological profile of progestins. Maturitas. 2008 Sep-Oct;61(1-2):151-7.
7 Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8.
8 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
9 Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharm... Steroids. 2008 Feb;73(2):222-31.
10 Contribution of functional groups of 19-nor-progestogens to binding to progesterone and estradiol-17beta receptors in rabbit uterus. Endocrinology. 1977 Jun;100(6):1579-84.
11 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals (2011).
14 Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90.
15 Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
16 Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding. J Biol Chem. 2000Jun 23;275(25):19041-9.
17 Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9.
18 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 628).
19 Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. J Med Chem. 2000 Dec 28;43(26):5010-6.
20 Perspectives on the current and emerging chemical androgen receptor antagonists for the treatment of prostate cancer. Expert Opin Pharmacother. 2019 Feb;20(2):163-172.
21 Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.
22 2011 Pipeline of Santaris Pharma.
23 Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2111-4.
24 Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen recepto... J Med Chem. 2008 Nov 13;51(21):7010-4.
25 Effect of flavonoids on androgen and glucocorticoid receptors based on in vitro reporter gene assay. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4706-10.
26 Stimulation of testosterone production in rat Leydig cells by aldosterone is mineralocorticoid receptor mediated. Mol Cell Endocrinol. 2005 Nov 24;243(1-2):35-42.
27 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
28 Mineralocorticoid receptor-mediated inhibition of the hypothalamic-pituitary-adrenal axis in aged humans. J Gerontol A Biol Sci Med Sci. 2003 Oct;58(10):B900-5.
29 Characterization of rat brain aldosterone receptors reveals high affinity for corticosterone. Endocrinology. 1983 Dec;113(6):2043-51.
30 Biochemical mechanisms of New Molecular Entities (NMEs) approved by United States FDA during 2001-2004: mechanisms leading to optimal efficacy and ... Curr Top Med Chem. 2006;6(5):461-78.
31 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
32 ZK91587: a novel synthetic antimineralocorticoid displays high affinity for corticosterone (type I) receptors in the rat hippocampus. Life Sci. 1988;43(19):1537-43.
33 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 626).