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Assay Detail

CHEMBL684407

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

Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Syntheses and structure-activity relationship studies of piperidine-substituted quinolones as nonpeptide gonadotropin releasing hormone antagonists.
Jiang J, DeVita RJ, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Cui J, Yang YT, Cheng K, Rohrer SP.
Bioorg Med Chem Lett (2004) 14 : 1795 -1798
PubMed 15026074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 9.05 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48192 1 9.52
CHEMBL295948 1 9.30
CHEMBL300295 1 9.30
CHEMBL48879 1 9.22
CHEMBL52278 1 9.05
CHEMBL298937 1 8.70
CHEMBL51841 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48192 IC50 = 0.3 nM 9.52
CHEMBL295948 IC50 = 0.5 nM 9.30
CHEMBL300295 IC50 = 0.5 nM 9.30
CHEMBL48879 IC50 = 0.6 nM 9.22
CHEMBL52278 IC50 = 0.9 nM 9.05
CHEMBL298937 IC50 = 2.0 nM 8.70
CHEMBL51841 IC50 = 5.7 nM 8.24