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Assay Detail

CHEMBL3375484

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

Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
8
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gonadotropin-releasing hormone receptor (CHEMBL1855)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GnRH antagonists: the promise of treating sex-hormone-related diseases.
Abdel-Magid AF.
ACS Med Chem Lett (2014) 5 : 1268 -1269
PubMed 25516782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.54 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3358413 2 8.48
CHEMBL3358416 2 8.26
CHEMBL3358415 2 7.17
CHEMBL3358414 2 6.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3358413 IC50 = 3.3 nM 8.48
CHEMBL3358416 IC50 = 5.5 nM 8.26
CHEMBL3358415 IC50 = 68.0 nM 7.17
CHEMBL3358414 IC50 = 107.0 nM 6.97
CHEMBL3358414 IC50 = 2310.0 nM 5.64
CHEMBL3358413 IC50 = 4080.0 nM 5.39
CHEMBL3358415 IC50 = 4210.0 nM 5.38
CHEMBL3358416 IC50 = 9350.0 nM 5.03