Proteins > Gonadotropin-releasing hormone receptor
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Gonadotropin-releasing hormone receptor
A gonadotropin-releasing hormone I receptor that is encoded in the genome of rat. [OMA:P30969, PRO:DNx]
Synonyms
GnRH receptor;
GnRH-R
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (11.11) | 18.7374 |
| 1990's | 2 (11.11) | 18.2507 |
| 2000's | 11 (61.11) | 29.6817 |
| 2010's | 3 (16.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (12)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ketoconazole | Rattus norvegicus (Norway rat) | IC50 | 2.0000 | 1 | 1 |
| 2'-deoxyuridylic acid | Rattus norvegicus (Norway rat) | Ki | 6.5000 | 1 | 3 |
| gonadotropin-releasing hormone | Rattus norvegicus (Norway rat) | IC50 | 0.0050 | 3 | 3 |
| gonadotropin-releasing hormone | Rattus norvegicus (Norway rat) | Ki | 794,328,000,000,000.0000 | 1 | 1 |
| leuprolide | Rattus norvegicus (Norway rat) | IC50 | 0.0006 | 3 | 3 |
| leuprolide | Rattus norvegicus (Norway rat) | Ki | 5,370,320,000,000,000.0000 | 1 | 1 |
| tak 013 | Rattus norvegicus (Norway rat) | IC50 | 0.5006 | 2 | 2 |
| t 98475 | Rattus norvegicus (Norway rat) | IC50 | 0.0481 | 5 | 5 |
| t 98475 | Rattus norvegicus (Norway rat) | Ki | 0.0600 | 1 | 1 |
| ag045572 | Rattus norvegicus (Norway rat) | Ki | 0.0038 | 2 | 2 |
| tak 385 | Rattus norvegicus (Norway rat) | IC50 | 0.0003 | 2 | 2 |
| nbi 42902 | Rattus norvegicus (Norway rat) | Ki | 4.0333 | 3 | 3 |
| way 207024 | Rattus norvegicus (Norway rat) | IC50 | 0.2058 | 4 | 4 |
| acyline | Rattus norvegicus (Norway rat) | IC50 | 0.0015 | 1 | 1 |
| deslorelin | Rattus norvegicus (Norway rat) | Ki | 100,000,000,000,000,000.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ketoconazole | Rattus norvegicus (Norway rat) | Kd | 0.2705 | 3 | 3 |
Design and synthesis of potent hexapeptide and heptapeptide gonadotropin-releasing hormone antagonists by truncation of a decapeptide analogue sequence.Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 2000
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
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.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
Discovery of a novel, potent, and orally active nonpeptide antagonist of the human luteinizing hormone-releasing hormone (LHRH) receptor.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists.Journal of medicinal chemistry, , Feb-05, Volume: 36, Issue:3, 1993
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 gonadotJournal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
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.Journal of medicinal chemistry, , Jan-02, Volume: 46, Issue:1, 2003
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
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.Journal of medicinal chemistry, , Jun-29, Volume: 49, Issue:13, 2006
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 inJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
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.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 24, Issue:7, 2014
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
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 gonadotJournal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Non-peptide gonadotropin-releasing hormone receptor antagonists.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
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 Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
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 inJournal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 20, Issue:8, 2010
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).Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009