| Assay ID | Title | Year | Journal | Article |
|---|
| AID257963 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257994 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID237001 | Time taken for plasma concentration reached maximum value in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID257984 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257992 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347125 | Dissociation rate assessed as half life | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257954 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257993 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID332097 | Binding affinity to human GnRHR | 2008 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 18, Issue:11
| 5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers. |
| AID347168 | Suppression of circulating plasma LH levels in cynomolgus monkey at 30 mg/kg, po after 4 to 8 hrs | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257970 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257934 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257950 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347130 | Ratio of permeability from apical to basolateral side over basolateral to apical side in human Caco-2 cells | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID347129 | Apparent permeability across human Caco-2 cell membrane | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257933 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID1352078 | Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists. |
| AID257961 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257959 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257955 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID242210 | Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID257999 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347137 | AUC in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257951 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257942 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257953 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257948 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257939 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347134 | Volume of distribution in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257989 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID236205 | Plasma clearance in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID258007 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258006 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257956 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347127 | Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from monkey GnRH receptor expressed in CHO cells by liquid scintillation counting | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257976 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258001 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257980 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257974 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257978 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID238751 | Binding affinity for Human gonadotropin-releasing hormone receptor | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID347132 | Half life in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257971 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID407922 | Tmax in postmenopausal women at 5 to 200 mg, po | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID258005 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID238765 | Binding affinity for Monkey gonadotropin-releasing hormone receptor | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID347133 | Plasma clearance in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257945 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID239190 | Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand | 2005 | Bioorganic & medicinal chemistry letters, May-16, Volume: 15, Issue:10
| Uracils as potent antagonists of the human gonadotropin-releasing hormone receptor without atropisomers. |
| AID257944 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257941 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N102D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258004 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257962 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257958 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257975 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257981 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID236308 | Volume distribution in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID257968 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347122 | Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID258002 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257979 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257973 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257965 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID236133 | Oral bioavailability value determined in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID347136 | Tmax in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID347138 | Oral bioavailability in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID1630533 | Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. |
| AID257938 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257966 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257996 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257949 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257969 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257940 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257983 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347126 | Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID347135 | Cmax in rat at 10 mg/kg, iv and 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID237285 | Terminal half-life in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID257990 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257982 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257991 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID407893 | Binding affinity at human GnRH receptor | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID407923 | Half life in postmenopausal women at 5 to 200 mg, po | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID258009 | Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257937 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257957 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347123 | Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257964 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID1630534 | Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
| Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. |
| AID257935 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257977 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257986 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347124 | Inhibition of CYP3A4 | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257947 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID238725 | Binding affinity for rat gonadotropin-releasing hormone receptor | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID407915 | Suppression of circulating luteinizing hormone in monkey | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID236478 | Plasma level area under the curve value in monkey after treatment with 10 mg/kg (po. and iv.) | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID257972 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258003 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID407895 | Binding affinity at rat GnRH receptor | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID257987 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257988 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257985 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258008 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID347131 | Lipophilicity, log D of the compound | 2008 | Journal of medicinal chemistry, Dec-11, Volume: 51, Issue:23
| 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 |
| AID257998 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257952 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118D | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257946 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID258000 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257967 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID236747 | Plasma concentration reached maximum value at a dose of 10 mg/kg (po. and iv.) administered into monkey | 2005 | Journal of medicinal chemistry, Feb-24, Volume: 48, Issue:4
| 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 |
| AID407894 | Binding affinity at monkey GnRH receptor | 2008 | Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
| Non-peptide gonadotropin-releasing hormone receptor antagonists. |
| AID257943 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257995 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257960 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257936 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID257997 | Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q | 2006 | Journal of medicinal chemistry, Jan-26, Volume: 49, Issue:2
| Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor. |
| AID1346002 | Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 2007 | Endocrinology, Feb, Volume: 148, Issue:2
| Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. |
| AID1346002 | Human GnRH1 receptor (Gonadotrophin-releasing hormone receptors) | 2006 | Biochemical pharmacology, Sep-28, Volume: 72, Issue:7
| Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |