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Assay Detail

CHEMBL689135

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Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
2
Total Activities
2
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 (CHEMBL3066)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
IC50 2 8.81 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71917 1 9.22
CHEMBL71561 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71917 IC50 = 0.6 nM 9.22
CHEMBL71561 IC50 = 4.0 nM 8.40