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Assay Detail

CHEMBL4323804

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

Binding
Inhibition of human ERG expressed in HEK293 cells at holding potential -80 mV by whole-cell voltage-clamp method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo.
Wortmann L, Lindenthal B, Muhn P, Walter A, Nubbemeyer R, Heldmann D, Sobek L, Morandi F, Schrey AK, Moosmayer D, Günther J, Kuhnke J, Koppitz M, Lücking U, Röhn U, Schäfer M, Nowak-Reppel K, Kühne R, Weinmann H, Langer G.
J Med Chem (2019) 62 : 10321 -10341
PubMed 31670515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.25 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4537998 1 5.52
CHEMBL4458424 BAY-899 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4537998 IC50 = 3000.0 nM 5.52
CHEMBL4458424 BAY-899 IC50 = 10600.0 nM 4.97