Target Information
Target General Infomation | |||||
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Target ID |
T22939
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Former ID |
TTDS00245
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Target Name |
Progesterone receptor
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Gene Name |
PGR
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Synonyms |
PR; PGR
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Target Type |
Successful
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Disease | Advanced breast carcinoma; Advanced endometrium carcinoma [ICD9: 174, 175, 182.0; ICD10: C50, C54.1] | ||||
Contraception [ICD10: Z30] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Dysmenorrhea [ICD9: 625.3; ICD10: N94.4-N94.6] | |||||
Estrogen deficiency [ICD10: E28.39] | |||||
Endometrial cancer [ICD9: 182; ICD10: C54.1] | |||||
Endometriosis [ICD9: 617; ICD10: N80] | |||||
Female contraception [ICD10: Z30] | |||||
Gynecological disorder [ICD10: N70-N98] | |||||
Hormonal contraceptives [ICD10: Z30] | |||||
Menstrual disorders [ICD9: 626; ICD10: N91-N95] | |||||
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890] | |||||
Premature labour [ICD9: 644, 765; ICD10: O60.1, P07.3] | |||||
Uterine fibroids [ICD10: D25] | |||||
Uterine leiomyoma [ICD9: 218.9; ICD10: D25] | |||||
Unspecified [ICD code not available] | |||||
Function |
Isoform 4: Increases mitochondrial membrane potential and cellular respiration upon stimulation by progesterone.
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BioChemical Class |
Zinc-finger
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Target Validation |
T22939
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UniProt ID | |||||
Sequence |
MTELKAKGPRAPHVAGGPPSPEVGSPLLCRPAAGPFPGSQTSDTLPEVSAIPISLDGLLF
PRPCQGQDPSDEKTQDQQSLSDVEGAYSRAEATRGAGGSSSSPPEKDSGLLDSVLDTLLA PSGPGQSQPSPPACEVTSSWCLFGPELPEDPPAAPATQRVLSPLMSRSGCKVGDSSGTAA AHKVLPRGLSPARQLLLPASESPHWSGAPVKPSPQAAAVEVEEEDGSESEESAGPLLKGK PRALGGAAAGGGAAAVPPGAAAGGVALVPKEDSRFSAPRVALVEQDAPMAPGRSPLATTV MDFIHVPILPLNHALLAARTRQLLEDESYDGGAGAASAFAPPRSSPCASSTPVAVGDFPD CAYPPDAEPKDDAYPLYSDFQPPALKIKEEEEGAEASARSPRSYLVAGANPAAFPDFPLG PPPPLPPRATPSRPGEAAVTAAPASASVSSASSSGSTLECILYKAEGAPPQQGPFAPPPC KAPGASGCLLPRDGLPSTSASAAAAGAAPALYPALGLNGLPQLGYQAAVLKEGLPQVYPP YLNYLRPDSEASQSPQYSFESLPQKICLICGDEASGCHYGVLTCGSCKVFFKRAMEGQHN YLCAGRNDCIVDKIRRKNCPACRLRKCCQAGMVLGGRKFKKFNKVRVVRALDAVALPQPV GVPNESQALSQRFTFSPGQDIQLIPPLINLLMSIEPDVIYAGHDNTKPDTSSSLLTSLNQ LGERQLLSVVKWSKSLPGFRNLHIDDQITLIQYSWMSLMVFGLGWRSYKHVSGQMLYFAP DLILNEQRMKESSFYSLCLTMWQIPQEFVKLQVSQEEFLCMKVLLLLNTIPLEGLRSQTQ FEEMRSSYIRELIKAIGLRQKGVVSSSQRFYQLTKLLDNLHDLVKQLHLYCLNTFIQSRA LSVEFPEMMSEVIAAQLPKILAGMVKPLLFHKK |
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Drugs and Mode of Action | |||||
Drug(s) | Desogestrel | Drug Info | Approved | Hormonal contraceptives | [536361], [542071] |
Dydrogesterone | Drug Info | Approved | Menstrual disorders | [539904], [550691] | |
Estradiol valerate/dienogest | Drug Info | Approved | Unspecified | [551871] | |
Ethynodiol Diacetate | Drug Info | Approved | Hormonal contraceptives | [538500], [542078] | |
Etonogestrel | Drug Info | Approved | Female contraception | [536361], [542580] | |
Levonorgestrel | Drug Info | Approved | Hormonal contraceptives | [536361], [539908] | |
Medroxyprogesterone | Drug Info | Approved | Cancer | [551871] | |
Megestrol | Drug Info | Approved | Advanced breast carcinoma; Advanced endometrium carcinoma | [536165] | |
Norethindrone | Drug Info | Approved | Cancer | [551871] | |
Norgestimate | Drug Info | Approved | Hormonal contraceptives | [536361], [542097] | |
Norgestrel | Drug Info | Approved | Contraception | [538483], [551871] | |
Progesterone | Drug Info | Approved | Premature labour | [539513], [549497] | |
Ulipristal | Drug Info | Approved | Contraception | [531351] | |
Nestorone transdermal spray | Drug Info | Phase 3 | Endometriosis | [522001] | |
NPC-01 | Drug Info | Phase 3 | Dysmenorrhea | [523263] | |
Androgen restored contraceptive | Drug Info | Phase 2 | Contraception | [527054] | |
MK-8342 | Drug Info | Phase 2 | Contraception | [550004] | |
S-PRAnt | Drug Info | Phase 2 | Uterine leiomyoma | [549157] | |
Telapristone | Drug Info | Phase 2 | Endometriosis | [547243] | |
Tosagestin | Drug Info | Phase 2 | Contraception | [525775] | |
Vilaprisan | Drug Info | Phase 2 | Endometriosis | [525223] | |
Virexxa | Drug Info | Phase 2 | Endometrial cancer | [524647] | |
ONAPRISTONE | Drug Info | Phase 1/2 | Contraception | [524622], [539909] | |
PF-2413873 | Drug Info | Phase 1 | Endometriosis | [522505] | |
Asoprisnil | Drug Info | Discontinued in Phase 3 | Endometriosis | [536772], [539910] | |
Org-31710 | Drug Info | Discontinued in Phase 1 | Contraception | [545237] | |
BAY-39-9624 | Drug Info | Terminated | Osteoporosis | [547256] | |
RU-46556 | Drug Info | Terminated | Endometrial cancer | [545435] | |
Inhibitor | 1-Benzyl-3-phenylquinazoline-2,4(1H,3H)-dione | Drug Info | [529568] | ||
2,2,4-Trimethyl-6-phenyl-1,2-dihydro-quinoline | Drug Info | [534695] | |||
2-(4-Amino-3'-chloro-biphenyl-3-yl)-propan-2-ol | Drug Info | [526276] | |||
3,3-dimethyl-5-m-tolyl-2,3-dihydro-1H-inden-1-one | Drug Info | [530484] | |||
3-(3,3-dimethyl-2-oxoindolin-5-yl)benzonitrile | Drug Info | [529352] | |||
3-Phenyl-1-propylquinazoline-2,4(1H,3H)-dione | Drug Info | [529568] | |||
4-(2,4-diethyl-1H-pyrrol-3-yloxy)benzonitrile | Drug Info | [530880] | |||
5,N-Dihydroxythalidomide | Drug Info | [529568] | |||
5-(2-oxoindolin-5-yl)-1H-pyrrole-2-carbonitrile | Drug Info | [529352] | |||
6-(3-Nitro-phenyl)-3H-benzothiazol-2-one | Drug Info | [527672] | |||
AL-43 | Drug Info | [526567] | |||
GSK-1564023A | Drug Info | [530767] | |||
GSK-325971A | Drug Info | [530767] | |||
Lecanindole D | Drug Info | [530483] | |||
LGD-5552 | Drug Info | [529166] | |||
Methyltrienolone | Drug Info | [551393] | |||
PF-02367982 | Drug Info | [530880] | |||
Tanaproget | Drug Info | [551374] | |||
WAY-255348 | Drug Info | [529352] | |||
ZK-230211 | Drug Info | [525950] | |||
Agonist | Androgen restored contraceptive | Drug Info | [551483] | ||
BAY-39-9624 | Drug Info | [551732] | |||
Dydrogesterone | Drug Info | [536560] | |||
GSK-008A | Drug Info | [543903] | |||
Medroxyprogesterone | Drug Info | [536560] | |||
MK-8342 | Drug Info | [543903] | |||
Nestorone transdermal spray | Drug Info | [532946] | |||
Norethindrone | Drug Info | [535980] | |||
Norgestimate | Drug Info | [536305], [537309] | |||
Norgestrel | Drug Info | [536668] | |||
NPC-01 | Drug Info | [523263] | |||
ORG2058 | Drug Info | [543903] | |||
Progesterone | Drug Info | [551103] | |||
Tosagestin | Drug Info | [527744] | |||
[3H]ORG2058 | Drug Info | [543903] | |||
Antagonist | APR19 | Drug Info | [532304] | ||
PF-2413873 | Drug Info | [550034] | |||
S-PRAnt | Drug Info | [532387] | |||
Telapristone | Drug Info | [527064] | |||
Vilaprisan | Drug Info | [549227], [551871] | |||
Modulator | Asoprisnil | Drug Info | [536772] | ||
Desogestrel | Drug Info | [535085] | |||
Estradiol valerate/dienogest | Drug Info | [531351] | |||
ONAPRISTONE | Drug Info | ||||
Org-31710 | Drug Info | [526214] | |||
RU-46556 | Drug Info | [533113] | |||
SPRMs, oral, uterine fibroids, Tokai Pharmaceuticals | Drug Info | [543903] | |||
Ulipristal | Drug Info | [531351] | |||
ZK-112993 | Drug Info | ||||
ZK-114043 | Drug Info | ||||
ZK-136798 | Drug Info | ||||
Binder | Ethynodiol Diacetate | Drug Info | [537774], [537954] | ||
Etonogestrel | Drug Info | [535188], [537309] | |||
Levonorgestrel | Drug Info | [537153] | |||
Megestrol | Drug Info | [535883] | |||
Inducer | Virexxa | Drug Info | [543903] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Oocyte meiosis | ||||
Progesterone-mediated oocyte maturation | |||||
Pathway Interaction Database | Cellular roles of Anthrax toxin | ||||
Reactome | Nuclear signaling by ERBB4 | ||||
Nuclear Receptor transcription pathway | |||||
WikiPathways | Ovarian Infertility Genes | ||||
Signaling by ERBB4 | |||||
Nuclear Receptors | |||||
References | |||||
Ref 522001 | ClinicalTrials.gov (NCT00455156) Study of the Safety, Efficacy and Cycle Control of a Contraceptive Vaginal Ring. U.S. National Institutes of Health. | ||||
Ref 522505 | ClinicalTrials.gov (NCT00800618) A Study To Investigate How The Body Handles Multiple Doses Of PF-0243873 And To Investigate The Effect Of PF-02413873 On Sex Hormone Levels In Healthy Young Women. U.S. National Institutes of Health. | ||||
Ref 523263 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | ||||
Ref 524622 | ClinicalTrials.gov (NCT02049190) Phase 1-2 Study of Onapristone in Patients With Advanced Castration-resistant Prostate Cancer. U.S. National Institutes of Health. | ||||
Ref 524647 | ClinicalTrials.gov (NCT02064725) Virexxa (Sodium Cridanimod) w/Progestin Therapy in Pts w/Progesterone Receptor Neg Recurrent/Persistent Endometrial CA. U.S. National Institutes of Health. | ||||
Ref 525223 | ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids. | ||||
Ref 525775 | Excretion balance and metabolism of the progestagen Org 30659 in healthy postmenopausal women. J Steroid Biochem Mol Biol. 2000 May;73(1-2):39-48. | ||||
Ref 527054 | Treatment outcome in endodontics-the Toronto Study. Phase II: initial treatment. J Endod. 2004 May;30(5):302-9. | ||||
Ref 536165 | Hormonal therapy in epithelial ovarian cancer. Expert Rev Anticancer Ther. 2006 Jan;6(1):43-7. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536772 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | ||||
Ref 538483 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017031. | ||||
Ref 538500 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018168. | ||||
Ref 539513 | (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. (Ligand id: 2377). | ||||
Ref 539904 | (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. (Ligand id: 2878). | ||||
Ref 539908 | (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. (Ligand id: 2881). | ||||
Ref 539909 | (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. (Ligand id: 2882). | ||||
Ref 539910 | (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. (Ligand id: 2883). | ||||
Ref 542071 | (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. (Ligand id: 7065). | ||||
Ref 542078 | (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. (Ligand id: 7072). | ||||
Ref 542097 | (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. (Ligand id: 7091). | ||||
Ref 542580 | (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. (Ligand id: 7590). | ||||
Ref 545237 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002550) | ||||
Ref 545435 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003252) | ||||
Ref 547243 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014404) | ||||
Ref 547256 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014491) | ||||
Ref 549157 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033040) | ||||
Ref 523263 | ClinicalTrials.gov (NCT01246791) Pharmacokinetics of NPC-01 After Single Oral Administration in Healthy Female Volunteers. U.S. National Institutes of Health. | ||||
Ref 525950 | J Med Chem. 2000 Dec 28;43(26):5010-6.Synthesis and biological activity of a novel, highly potent progesterone receptor antagonist. | ||||
Ref 526214 | Progesterone receptor antagonists Org 31710 and RU 486 increase apoptosis in human periovulatory granulosa cells. Fertil Steril. 2001 Dec;76(6):1225-31. | ||||
Ref 526276 | Bioorg Med Chem Lett. 2002 Mar 11;12(5):787-90.Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines. | ||||
Ref 526567 | J Med Chem. 2003 Mar 13;46(6):1016-30.Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines. | ||||
Ref 527064 | In vitro antiprogestational/antiglucocorticoid activity and progestin and glucocorticoid receptor binding of the putative metabolites and synthetic derivatives of CDB-2914, CDB-4124, and mifepristone. J Steroid Biochem Mol Biol. 2004 Mar;88(3):277-88. | ||||
Ref 527672 | J Med Chem. 2005 Aug 11;48(16):5092-5.Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potentand selective nonsteroidal progesterone receptor agonist tanaproget. | ||||
Ref 527744 | Effects of progestins on the proliferation of estrogen-dependent human breast cancer cells under growth factor-defined conditions. J Steroid Biochem Mol Biol. 1992 Jun;42(5):457-65. | ||||
Ref 529166 | Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19244-9. Epub 2007 Nov 21.Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile. | ||||
Ref 529352 | J Med Chem. 2008 Mar 27;51(6):1861-73. Epub 2008 Mar 5.Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348). | ||||
Ref 529568 | Bioorg Med Chem. 2008 Jul 15;16(14):7046-54. Epub 2008 May 10.Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton. | ||||
Ref 530483 | J Nat Prod. 2009 Nov;72(11):1944-8.The lecanindoles, nonsteroidal progestins from the terrestrial fungus Verticillium lecanii 6144. | ||||
Ref 530484 | Bioorg Med Chem Lett. 2009 Dec 1;19(23):6666-9. Epub 2009 Oct 7.5-Aryl indanones and derivatives as non-steroidal progesterone receptor modulators. | ||||
Ref 530767 | Bioorg Med Chem Lett. 2010 Apr 1;20(7):2340-3. Epub 2010 Feb 4.The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist. | ||||
Ref 530880 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3384-6. Epub 2010 Apr 13.Optimisation of a pyrazole series of progesterone antagonists; Part 1. | ||||
Ref 532304 | A new strategy for selective targeting of progesterone receptor with passive antagonists. Mol Endocrinol. 2013 Jun;27(6):909-24. | ||||
Ref 532387 | BAY 1002670: a novel, highly potent and selective progesterone receptor modulator for gynaecological therapies. Hum Reprod. 2013 Aug;28(8):2253-64. | ||||
Ref 532946 | Efficacy of the selective progesterone receptor agonist Nestorone for chronic experimental autoimmune encephalomyelitis. J Neuroimmunol. 2014 Nov 15;276(1-2):89-97. | ||||
Ref 533113 | New analogues of mifepristone with more dissociated antiprogesterone activities. J Steroid Biochem. 1989;34(1-6):413-7. | ||||
Ref 534695 | J Med Chem. 1998 Aug 27;41(18):3461-6.Discovery and preliminary SAR studies of a novel, nonsteroidal progesterone receptor antagonist pharmacophore. | ||||
Ref 535085 | Preclinical experience with two selective progesterone receptor modulators on breast and endometrium. Steroids. 2000 Oct-Nov;65(10-11):733-40. | ||||
Ref 535188 | Endometrial effects of etonogestrel (Implanon) contraceptive implant. Curr Opin Obstet Gynecol. 2001 Jun;13(3):335-41. | ||||
Ref 535980 | Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes. J Med Chem. 2004 Jun 17;47(13):3381-7. | ||||
Ref 536305 | A review of transdermal hormonal contraception : focus on the ethinylestradiol/norelgestromin contraceptive patch. Treat Endocrinol. 2006;5(6):359-65. | ||||
Ref 536560 | Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008 Feb;73(2):222-31.Epub 2007 Oct 22. | ||||
Ref 536668 | Toll-like receptor-4-mediated macrophage activation is differentially regulated by progesterone via the glucocorticoid and progesterone receptors. Immunology. 2008 Sep;125(1):59-69. Epub 2008 Mar 28. | ||||
Ref 536772 | New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202. | ||||
Ref 537153 | Met909 plays a key role in the activation of the progesterone receptor and also in the high potency of 13-ethyl progestins. Mol Pharmacol. 2009 Jun;75(6):1317-24. Epub 2009 Mar 16. | ||||
Ref 537774 | The place of progestational hormones in gynecological therapy. Ginekol Pol. 1970 May;41(5):497-502. | ||||
Ref 537954 | 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. | ||||
Ref 543903 | (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: 627). | ||||
Ref 549227 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033939) | ||||
Ref 550034 | Unusual base-catalyzed exchange in the synthesis of deuterated PF-2413873. Journal of Labelled Compounds. 08/2009; 52(10):435 - 442. | ||||
Ref 551732 | Bayer is seeking an exclusive licensee for its end-of-Phase I progestinagonist Bay 39-9624. Thepharmaletter. 29-04-2002. |
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