Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T12475 | Target Info | |||
| Target Name | Gonadotropin-releasing hormone receptor (GNRHR) | ||||
| Synonyms |
Hypothalamic gonadotropin-releasing hormone receptor; Gonadotrophin releasing hormone receptor; GnRH-R; GnRH receptor; GRHR
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| Target Type | Successful Target | ||||
| Gene Name | GNRHR | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
1-(2,4-Difluorobenzyl)-4-oxo-6-(methylphenethylaminomethyl)-7-(4-isobutoxyphenyl)-8-cyano-1,4-dihydropyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL337891; BDBM50109225
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(2,4-Difluorobenzyl)-4-oxo-6-[methyl[2-(4-pyridinyl)ethyl]aminomethyl]-7-(4-isobutoxyphenyl)-8-cyano-1,4-dihydropyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL129010; BDBM50109202
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
1-(Cyclopropylmethyl)-4-oxo-6-[methyl[2-(2-pyridinyl)ethyl]aminomethyl]-7-(4-methoxyphenyl)-8-cyano-1,4-dihydropyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL334816; BDBM50109206
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
1-Benzyl-4-oxo-6-(dimethylaminomethyl)-7-(4-methoxyphenyl)-8-cyano-1,4-dihydropyrrolo[1,2-a]pyrimidine-3-carboxylic acid ethyl ester
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL340524; BDBM50109215
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| Activity |
Ki ~ 50000 nM
|
[1] | |||
| Compound Name |
3-((R)-2-Amino-2-phenyl-ethyl)-5-(2-fluoro-phenyl)-6-methyl-[1,3]oxazine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL369749; SCHEMBL13996064; BDBM50162002
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| Activity |
Ki ~ 100000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):399-402. | ||||
| REF 2 | 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. J Med Chem. 2005 Feb 24;48(4):1169-78. | ||||
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