General Information of Drug (ID: DMXLZAT)

Drug Name
4-Ethynyl-2-(4-hydroxy-phenyl)-quinolin-6-ol Drug Info
Synonyms 4-ethynyl-2-(4-hydroxyphenyl)quinolin-6-ol
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
135524856
TTD Drug ID
DMXLZAT

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Rimexolone DMTAREC Arthritis FA20 Approved [3]
Pregnenolone DM6VFO1 Schizophrenia 6A20 Phase 4 [4]
D-5519 DM9FAJM Asthma CA23 Phase 3 [5]
Dexamethasone palmitate DMCMT4V Choroidal neovascularization 9B76 Phase 1/2 [6]
RPR-106541 DMRGC5B Asthma CA23 Discontinued in Phase 2 [7]
Rofleponide DM6OSPQ Allergic rhinitis CA08.0 Discontinued in Phase 2 [8]
AD-121 DMB8XJM Rheumatoid arthritis FA20 Discontinued in Phase 1/2 [3]
GW-250495 DMWJZAP Asthma CA23 Discontinued in Phase 1 [3]
PLD-177 DMPHUBO Allergic rhinitis CA08.0 Terminated [3]
Steroid hormone conjugates DMOJM08 Cachexia MG20 Terminated [9]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Conjugated Estrogens DMLT0E1 Dyspareunia GA12 Approved [10]
Trilostane DMQZ9GF Cushing disease 5A70 Approved [11]
ARZOXIFENE DMOKCVI Breast cancer 2C60-2C65 Approved [12]
Estrogen DMGY0UT Menopause symptom GA30.0 Approved [13]
MF-101 DM8Z0I3 Hepatitis virus infection 1E50-1E51 Phase 3 [14]
Genistein DM0JETC Menopause symptom GA30.0 Phase 2/3 [15]
AUS-131 DMUXO3Z Hot flushes GA30 Phase 2 [16]
ERB-041 DMCEPUA Inflammatory bowel disease DD72 Phase 2 [17]
Erteberel DMU1XZD Prostate hyperplasia GA90 Phase 2 [18]
VG-101 DMAN21O Menopause symptom GA30.0 Phase 1/2 [19]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Estrogen receptor (ESR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [20]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [21]
Estrone DM5T6US Acne vulgaris ED80 Approved [21]
Estradiol Valerate DM8MC6O Hormone replacement therapy 8E01 Approved [11]
Estradiol Acetate DM07U2A Hormone replacement therapy 8E01 Approved [11]
Estradiol Cypionate DM27Z5T Hormone replacement therapy 8E01 Approved [11]
Ethinyl Estradiol DMODJ40 Acne vulgaris ED80 Approved [22]
Raloxifene DMDKF3M Osteoporosis FB83.0 Approved [23]
Ospemifene DMC4GEI Dyspareunia GA12 Approved [24]
Toremifene DMQYUWG Breast cancer 2C60-2C65 Approved [25]
⏷ 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
Estrogen receptor (ESR) TTZAYWL ESR1_HUMAN Inhibitor [1]
Estrogen receptor beta (ESR2) TTOM3J0 ESR2_HUMAN Inhibitor [1]
Estrogen-related receptor-alpha (ESRRA) TTPNQAC ERR1_HUMAN Inhibitor [2]

References

1 ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4520-5.
2 ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4053-6.
3 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: 622).
4 Suppression of adrenal function by low-dose prednisone: assessment with 24-hour urinary steroid hormone profiles--a review of five cases. Altern Med Rev. 2006 Mar;11(1):40-6.
5 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007199)
6 Dexamethasone treatment in childhood bacterial meningitis in Malawi: a randomised controlled trial. Lancet. 2002 Jul 20;360(9328):211-8.
7 Use of the steroid derivative RPR 106541 in combination with site-directed mutagenesis for enhanced cytochrome P-450 3A4 structure/function analysis. J Pharmacol Exp Ther. 1999 Aug;290(2):594-602.
8 Direct activation of GABAA receptors by loreclezole, an anticonvulsant drug with selectivity for the beta-subunit. Neuropharmacology. 1996;35(12):1753-60.
9 The effect of six months treatment with a 100 mg daily dose of dehydroepiandrosterone (DHEA) on circulating sex steroids, body composition and muscle strength in age-advanced men and women. Clin Endocrinol (Oxf). 1998 Oct;49(4):421-32.
10 Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
11 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
12 Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007 May 31;50(11):2682-92.
13 Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6.
14 MF101, a selective estrogen receptor beta modulator for the treatment of menopausal hot flushes: a phase II clinical trial. Menopause. 2009 May-Jun;16(3):458-65.
15 Company report (Axcentua)
16 S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
17 Erb-041, an estrogen receptor-beta agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
18 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
19 Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.
20 Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause. Recent Pat Cardiovasc Drug Discov. 2008 Nov;3(3):165-86.
21 Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
22 17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
23 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: 620).
24 Clinical pipeline report, company report or official report of Shionogi (2011).
25 Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithe... Prostate Cancer Prostatic Dis. 2009;12(4):375-81.