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Assay Detail

CHEMBL689134

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

Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Wilcoxen KM, Zhu YF, Connors PJ, Saunders J, Gross TD, Gao Y, Reinhart GJ, Struthers RS, Chen C.
Bioorg Med Chem Lett (2002) 12 : 2179 -2183
PubMed 12127532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303274 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303274 Ki = 1.995 nM 8.70