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92 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
15006412 16 Elimination of antibacterial activities of non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists derived from erythromycin A.EBI Abbott Laboratories
25516782 8 GnRH antagonists: the promise of treating sex-hormone-related diseases.EBI Therachem Research Medilab (India) Pvt. Ltd.
24613701 6 Synthesis and in vitro evaluation of small-molecule [18F] labeled gonadotropin-releasing hormone (GnRH) receptor antagonists as potential PET imaging agents for GnRH receptor expression.EBI Norwegian Medical Cyclotron Centre, PO Box 4950, Nydalen, N-0424 Oslo, Norway.
24018188 4 Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides.EBI University of New Mexico
17517510 24 Synthesis and evaluation of homo-bivalent GnRHR ligands.EBI Leiden University
22967796 8 Enhanced cellular uptake and in vitro antitumor activity of short-chain fatty acid acylated daunorubicin-GnRH-III bioconjugates.EBI TBA
14971889 50 Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.EBI Abbott Laboratories
2552116 37 Active reduced-size hexapeptide analogues of luteinizing hormone-releasing hormone.EBI Abbott Laboratory
23031649 4 The therapeutic journey of benzimidazoles: a review.EBI Punjabi University
18442905 25 5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.EBI Neurocrine Biosciences, Inc.
18282756 35 Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.EBI Leiden University
17920281 16 The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies.EBI Neurocrine Biosciences
16789738 61 Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.EBI Takeda Pharmaceutical Company, Ltd.
16759096 31 Novel analogues of degarelix incorporating hydroxy-, methoxy-, and pegylated-urea moieties at positions 3, 5, 6 and the N-terminus. Part III.EBI Salk Institute
16033265 33 Iterative approach to the discovery of novel degarelix analogues: substitutions at positions 3, 7, and 8. Part II.EBI Salk Institute
14971906 74 Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.EBI Neurocrine Biosciences, Inc.
12502365 41 Discovery of a thieno[2,3-d]pyrimidine-2,4-dione bearing a p-methoxyureidophenyl moiety at the 6-position: a highly potent and orally bioavailable non-peptide antagonist for the human luteinizing hormone-releasing hormone receptor.EBI Takeda Chemical Industries, Ltd.
11462984 64 GnRH antagonists: a new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6.EBI Ferring Research Institute Inc.
9784092 15 Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.EBI Takeda Chemical Industries, Ltd.
21657270 61 Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.EBI Takeda Pharmaceutical Company, Ltd.
21395312 42 Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.EBI Merck Research Laboratories
20236823 41 Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.EBI Wyeth Research
19271735 35 Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R).EBI Wyeth Research
19251413 64 Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.EBI Wyeth Research
19006286 37 Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.EBI Neurocrine Biosciences, Inc.
18667310 49 Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.EBI Neurocrine Biosciences, Inc.
18511284 64 2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.EBI Wyeth Research
18442910 53 Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.EBI Neurocrine Biosciences, Inc.
18419112 63 Non-peptide gonadotropin-releasing hormone receptor antagonists.EBI Neurocrine Biosciences, Inc
17937987 83 Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.EBI Centre de Recherches
17561404 59 Selection, synthesis, and structure-activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists.EBI Neurocrine Biosciences
17521908 66 Identification of 2-(4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-3-yl)-ethylamine derivatives as novel GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
17402723 30 Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.EBI Salk Institute
17034124 140 Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.EBI Neurocrine Biosciences, Inc.
16722655 28 Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.EBI Pfizer Global Research & Development
16420049 355 Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.EBI Neurocrine Biosciences, Inc.
15951171 39 Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.EBI Neurocrine Biosciences, Inc.
15911275 20 Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.EBI Salk Institute
15863308 28 Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers.EBI Neurocrine Biosciences, Inc.
15837306 92 Benzimidazoles as non-peptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 3: Discovery of 1-(1H-benzimidazol-5-yl)-3-tert-butylurea derivatives.EBI Kyoto 619-0216
15715483 88 3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.EBI Neurocrine Biosciences, Inc.
15713397 12 Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.EBI Neurocrine Biosciences, Inc.
15664861 44 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.EBI Kyoto 619-0216
15664860 44 Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 1: Benzimidazole-5-sulfonamides.EBI Kyoto 619-0216
15664839 11 A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.EBI Neurocrine Biosciences, Inc.
15482932 32 Identification of neutral 4-O-alkyl quinolone nonpeptide GnRH receptor antagonists.EBI Merck Research Laboratories
15341961 31 Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.EBI Neurocrine Biosciences Inc.
15214774 28 3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.EBI Neurocrine Biosciences Inc.
15081023 26 Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc
15026074 16 Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.EBI Merck
14505682 29 Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12954050 2 Receptor-mediated targeting of a photosensitizer by its conjugation to gonadotropin-releasing hormone analogues.EBI Institute of Science
12951117 31 Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.EBI Neurocrine Biosciences, Inc.
12951116 30 Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12747774 17 Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.EBI Neurocrine Biosciences, Inc.
12699396 28 Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12443792 51 Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.EBI Pfizer Global Research and Development-La Jolla/Agouron Pharmaceuticals
12419391 8 A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12419385 48 The discovery of novel small molecule non-peptide gonadotropin releasing hormone (GnRH) receptor antagonists.EBI Pfizer Global Research and Development-La Jolla/Agouron Pharmaceuticals
12392744 36 Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.EBI Merck Research Laboratories
12127533 23 Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12127532 22 Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
12127507 11 A new class of potent nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists: design and synthesis of 2-phenylimidazo[1,2-a]pyrimidin-5-ones.EBI Takeda Chemical Industries, Ltd.
11859012 86 2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.EBI Merck Research Laboratories
11814807 30 A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
11814806 39 Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.EBI Neurocrine Biosciences, Inc.
11606129 4 Design, synthesis, and evaluation of a long-acting, potent analogue of gonadotropin-releasing hormone.EBI Institute of Science
11551758 58 Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.EBI Merck Research Laboratories
11425547 137 Potent nonpeptide GnRH receptor antagonists derived from substituted indole-5-carboxamides and -acetamides bearing a pyridine side-chain terminus.EBI Merck Research Laboratories
11425546 89 Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.EBI Merck Research Laboratories
11327594 26 Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.EBI Merck Research Laboratories
11327593 16 2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.EBI Merck Research Laboratories
11300873 8 A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.EBI Merck Research Laboratories
11229760 20 SAR studies of novel 5-substituted 2-arylindoles as nonpeptidyl GnRH receptor antagonists.EBI Merck Research Laboratories
11229759 40 Initial structure-activity relationship of a novel class of nonpeptidyl GnRH receptor antagonists: 2-arylindoles.EBI Merck Research Laboratories
10956191 31 Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.EBI Institute of Science
10956190 11 Structure-activity studies of reduced-size gonadotropin-releasing hormone agonists derived from the sequence of an endothelin antagonist.EBI Institute of Science
10937733 70 Quinolones as gonadotropin releasing hormone (GnRH) antagonists: simultaneous optimization of the C(3)-aryl and C(6)-substituents.EBI Merck Research Laboratories
10743944 68 Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides.EBI Merck Research Laboratories
10715150 5 Consensus bioactive conformation of cyclic GnRH antagonists defined by NMR and molecular modeling.EBI Salk Institute
10715149 46 Design of potent dicyclic (1-5/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI Salk Institute
10715148 27 Design of monocyclic (1-3) and dicyclic (1-3/4-10) gonadotropin releasing hormone (GnRH) antagonists.EBI Salk Institute
10715147 41 Design of potent dicyclic (4-10/5-8) gonadotropin releasing hormone (GnRH) antagonists.EBI Salk Institute
10498221 11 Investigation of the 4-O-alkylamine substituent of non-peptide quinolone GnRH receptor antagonists.EBI Merck Research Laboratories
10498220 22 Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.EBI Merck Research Laboratories
9371239 43 Betidamino acid scan of the GnRH antagonist acyline.EBI Salk Institute
3279211 16 Design of potent cyclic gonadotropin releasing hormone antagonists.EBI Salk Institute
2549244 13 LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.EBI Abbott Laboratories
1714956 17 Novel gonadotropin-releasing hormone antagonists: peptides incorporating modified N omega-cyanoguanidino moieties.EBI Salk Institute
1280300 7 Gonadotropin-releasing hormone antagonists with N omega-triazolylornithine, -lysine, or -p-aminophenylalanine residues at positions 5 and 6.EBI Salk Institute