Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3807011

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

Binding
Displacement of Fluormone ES2 from human recombinant full length untagged-ERalpha by fluorescence polarization competition binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator.
Shoda T, Kato M, Fujisato T, Misawa T, Demizu Y, Inoue H, Naito M, Kurihara M.
Bioorg Med Chem (2016) 24 : 2914 -2919
PubMed 27185013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.97 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81 RALOXIFENE 4.0 1 9.33
CHEMBL3805385 1 8.74
CHEMBL3805318 1 8.23
CHEMBL3805025 1 7.96
CHEMBL3804907 1 7.55
CHEMBL3806167 1 7.40
CHEMBL3805170 1 7.31
CHEMBL3805921 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81 RALOXIFENE IC50 = 0.47 nM 9.33
CHEMBL3805385 IC50 = 1.8 nM 8.74
CHEMBL3805318 IC50 = 5.9 nM 8.23
CHEMBL3805025 IC50 = 11.0 nM 7.96
CHEMBL3804907 IC50 = 28.0 nM 7.55
CHEMBL3806167 IC50 = 40.0 nM 7.40
CHEMBL3805170 IC50 = 49.0 nM 7.31
CHEMBL3805921 IC50 = 61.0 nM 7.21