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Assay Detail

CHEMBL682162

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

Binding
Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Toward selective ERbeta agonists for central nervous system disorders: synthesis and characterization of aryl benzthiophenes.
Schopfer U, Schoeffter P, Bischoff SF, Nozulak J, Feuerbach D, Floersheim P.
J Med Chem (2002) 45 : 1399 -1401
PubMed 11906280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.33 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411 DIETHYLSTILBESTROL 4.0 1 8.05
CHEMBL135 ESTRADIOL 4.0 1 7.62
CHEMBL31684 1 6.94
CHEMBL431698 RALOXIFENE CORE 1 6.94
CHEMBL31721 1 6.89
CHEMBL44 GENISTEIN 2.0 1 6.70
CHEMBL32459 1 6.60
CHEMBL81 RALOXIFENE 4.0 1 6.58
CHEMBL284054 1 6.13
CHEMBL1405 ESTRONE 4.0 1 5.95
CHEMBL286452 ALFATRADIOL 2.0 1 5.91
CHEMBL31333 1 5.74
CHEMBL32072 1 5.41
CHEMBL32511 1 5.37
CHEMBL31236 1 5.33
CHEMBL280645 1 5.13
CHEMBL418212 1 -
CHEMBL284949 1 -
CHEMBL31685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411 DIETHYLSTILBESTROL EC50 = 9.0 nM 8.05
CHEMBL135 ESTRADIOL EC50 = 24.0 nM 7.62
CHEMBL31684 EC50 = 115.0 nM 6.94
CHEMBL431698 RALOXIFENE CORE EC50 = 114.0 nM 6.94
CHEMBL31721 EC50 = 129.0 nM 6.89
CHEMBL44 GENISTEIN EC50 = 200.0 nM 6.70
CHEMBL32459 EC50 = 249.0 nM 6.60
CHEMBL81 RALOXIFENE EC50 = 260.0 nM 6.58
CHEMBL284054 EC50 = 740.0 nM 6.13
CHEMBL1405 ESTRONE EC50 = 1135.0 nM 5.95
CHEMBL286452 ALFATRADIOL EC50 = 1230.0 nM 5.91
CHEMBL31333 EC50 = 1830.0 nM 5.74
CHEMBL32072 EC50 = 3940.0 nM 5.41
CHEMBL32511 EC50 = 4310.0 nM 5.37
CHEMBL31236 EC50 = 4710.0 nM 5.33
CHEMBL280645 EC50 = 7470.0 nM 5.13
CHEMBL418212 EC50 > 10000.0 nM -
CHEMBL284949 EC50 > 10000.0 nM -
CHEMBL31685 EC50 > 10000.0 nM -