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Assay Detail

CHEMBL828045

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Rat gonadotropin-releasing hormone receptor
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gonadotropin-releasing hormone receptor (CHEMBL3066)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

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.
Tucci FC, Zhu YF, Struthers RS, Guo Z, Gross TD, Rowbottom MW, Acevedo O, Gao Y, Saunders J, Xie Q, Reinhart GJ, Liu XJ, Ling N, Bonneville AK, Chen T, Bozigian H, Chen C.
J Med Chem (2005) 48 : 1169 -1178
PubMed 15715483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120432 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120432 IC50 = 4.0 nM 8.40