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Assay Detail

CHEMBL678663

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

Binding
In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor.
Schmidt JM, Mercure J, Tremblay GB, Pagé M, Kalbakji A, Feher M, Dunn-Dufault R, Peter MG, Redden PR.
J Med Chem (2003) 46 : 1408 -1418
PubMed 12672240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.62 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2137046 1 9.80
CHEMBL411 DIETHYLSTILBESTROL 4.0 1 9.20
CHEMBL1358 FULVESTRANT 4.0 1 8.86
CHEMBL31738 1 6.75
CHEMBL31089 1 6.72
CHEMBL30996 1 6.72
CHEMBL31068 1 6.70
CHEMBL34216 1 6.20
CHEMBL33889 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2137046 Ki = 0.16 nM 9.80
CHEMBL411 DIETHYLSTILBESTROL Ki = 0.63 nM 9.20
CHEMBL1358 FULVESTRANT Ki = 1.39 nM 8.86
CHEMBL31738 Ki = 180.0 nM 6.75
CHEMBL31089 Ki = 190.0 nM 6.72
CHEMBL30996 Ki = 190.0 nM 6.72
CHEMBL31068 Ki = 200.0 nM 6.70
CHEMBL34216 Ki = 630.0 nM 6.20
CHEMBL33889 Ki > 1000.0 nM -