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Assay Detail

CHEMBL4430594

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

Binding
Displacement of [125I]D-Trp6-LHRH from monkey GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gonadotropin-releasing hormone receptor (CHEMBL5647)
Type SINGLE PROTEIN
Organism Macaca mulatta

Publication

Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Kim SM, Lee M, Lee SY, Park E, Lee SM, Kim EJ, Han MY, Yoo T, Ann J, Yoon S, Lee J, Lee J.
J Med Chem (2016) 59 : 9150 -9172
PubMed 27608177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.45 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4593521 1 8.46
CHEMBL4449332 1 8.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4593521 IC50 = 3.5 nM 8.46
CHEMBL4449332 IC50 = 3.7 nM 8.43