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

CHEMBL677099

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

Binding
Displacement of [3H]17-beta-estradiol from Estrogen receptor of rabbit uterine tissue
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
Christiansen LB, Wenckens M, Bury PS, Gissel B, Hansen BS, Thorpe SM, Jacobsen P, Kanstrup A, Jørgensen AS, Naerum L, Wassermann K.
Bioorg Med Chem Lett (2002) 12 : 17 -19
PubMed 11738564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.14 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.30
CHEMBL299942 1 8.51
CHEMBL554789 1 8.19
CHEMBL6318 IDOXIFENE 2.0 1 8.12
CHEMBL81 RALOXIFENE 4.0 1 8.11
CHEMBL52598 1 8.01
CHEMBL417596 1 7.72
CHEMBL301327 LEVORMELOXIFENE 2.0 1 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.5 nM 9.30
CHEMBL299942 IC50 = 3.1 nM 8.51
CHEMBL554789 IC50 = 6.5 nM 8.19
CHEMBL6318 IDOXIFENE IC50 = 7.5 nM 8.12
CHEMBL81 RALOXIFENE IC50 = 7.7 nM 8.11
CHEMBL52598 IC50 = 9.7 nM 8.01
CHEMBL417596 IC50 = 19.0 nM 7.72
CHEMBL301327 LEVORMELOXIFENE IC50 = 73.0 nM 7.14