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Assay Detail

CHEMBL1115144

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

Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gonadotropin-releasing hormone receptor (CHEMBL3066)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor.
Vera MD, Lundquist JT, Chengalvala MV, Cottom JE, Feingold IB, Garrick LM, Green DM, Hauze DB, Mann CW, Mehlmann JF, Rogers JF, Shanno L, Wrobel JE, Pelletier JC.
Bioorg Med Chem Lett (2010) 20 : 2512 -2515
PubMed 20236823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.40 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1091579 1 8.24
CHEMBL1088866 1 7.92
CHEMBL521674 1 7.62
CHEMBL1091580 1 7.54
CHEMBL468565 1 7.47
CHEMBL1092638 1 7.43
CHEMBL474991 1 7.14
CHEMBL1092245 1 7.09
CHEMBL1091209 1 7.02
CHEMBL1092626 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1091579 IC50 = 5.7 nM 8.24
CHEMBL1088866 IC50 = 12.0 nM 7.92
CHEMBL521674 IC50 = 24.0 nM 7.62
CHEMBL1091580 IC50 = 29.0 nM 7.54
CHEMBL468565 IC50 = 34.0 nM 7.47
CHEMBL1092638 IC50 = 37.0 nM 7.43
CHEMBL474991 IC50 = 72.0 nM 7.14
CHEMBL1092245 IC50 = 81.0 nM 7.09
CHEMBL1091209 IC50 = 95.0 nM 7.02
CHEMBL1092626 IC50 = 290.0 nM 6.54