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Assay Detail

CHEMBL655408

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Functional
In vitro inhibitory concentration against GnRH-stimulated phosphatidyl inositol hydrolysis by cloned chinese hamster ovary cells stably expressing human GnRH receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Cell Type CHO
Confidence 1 — Organism
Curated By Intermediate

Target

CHO (CHEMBL613853)
Type CELL-LINE
Organism Cricetulus griseus

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 6 8.12 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48192 1 8.66
CHEMBL52278 1 8.30
CHEMBL295948 1 8.06
CHEMBL48879 1 8.01
CHEMBL300295 1 7.94
CHEMBL298937 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48192 IC50 = 2.2 nM 8.66
CHEMBL52278 IC50 = 5.0 nM 8.30
CHEMBL295948 IC50 = 8.7 nM 8.06
CHEMBL48879 IC50 = 9.8 nM 8.01
CHEMBL300295 IC50 = 11.5 nM 7.94
CHEMBL298937 IC50 = 18.0 nM 7.75