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Assay Detail

CHEMBL954344

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

Functional
Reduction in leutinizing hormone release in (D-Trp6)-GnRH-stimulated rat primary pituitary cells by RIA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Pituitary gland cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Small molecule antagonists of the gonadotropin-releasing hormone (GnRH) receptor: structure-activity relationships of small heterocyclic groups appended to the 2-phenyl-4-piperazinyl-benzimidazole template.
Hauze DB, Chengalvala MV, Cottom JE, Feingold IB, Garrick L, Green DM, Huselton C, Kao W, Kees K, Lundquist JT, Mann CW, Mehlmann JF, Rogers JF, Shanno L, Wrobel J, Pelletier JC.
Bioorg Med Chem Lett (2009) 19 : 1986 -1990
PubMed 19251413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.63 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL460480 1 7.23
CHEMBL521674 1 6.70
CHEMBL493344 1 6.62
CHEMBL494400 1 6.60
CHEMBL493731 1 6.53
CHEMBL492327 1 6.52
CHEMBL493565 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL460480 IC50 = 59.0 nM 7.23
CHEMBL521674 IC50 = 200.0 nM 6.70
CHEMBL493344 IC50 = 240.0 nM 6.62
CHEMBL494400 IC50 = 250.0 nM 6.60
CHEMBL493731 IC50 = 296.0 nM 6.53
CHEMBL492327 IC50 = 300.0 nM 6.52
CHEMBL493565 IC50 = 570.0 nM 6.24