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Assay Detail

CHEMBL871112

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

Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and structure-activity relationships of thieno[2,3-b]pyridin-4-one derivatives as a novel class of potent, orally active, non-peptide luteinizing hormone-releasing hormone receptor antagonists.
Imada T, Cho N, Imaeda T, Hayase Y, Sasaki S, Kasai S, Harada M, Matsumoto H, Endo S, Suzuki N, Furuya S.
J Med Chem (2006) 49 : 3809 -3825
PubMed 16789738 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.57 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1201199 LEUPROLIDE 4.0 1 9.10
CHEMBL71917 1 8.40
CHEMBL438652 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1201199 LEUPROLIDE IC50 = 0.8 nM 9.10
CHEMBL71917 IC50 = 4.0 nM 8.40
CHEMBL438652 IC50 = 6.0 nM 8.22