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Assay Detail

CHEMBL682161

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Functional
Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct 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 8 7.89 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.00
CHEMBL44 GENISTEIN 2.0 1 8.77
CHEMBL431698 RALOXIFENE CORE 1 8.00
CHEMBL31684 1 7.89
CHEMBL31721 1 7.80
CHEMBL32511 1 7.16
CHEMBL31685 1 6.92
CHEMBL32072 1 6.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.1 nM 10.00
CHEMBL44 GENISTEIN EC50 = 1.7 nM 8.77
CHEMBL431698 RALOXIFENE CORE EC50 = 10.0 nM 8.00
CHEMBL31684 EC50 = 13.0 nM 7.89
CHEMBL31721 EC50 = 16.0 nM 7.80
CHEMBL32511 EC50 = 69.0 nM 7.16
CHEMBL31685 EC50 = 120.0 nM 6.92
CHEMBL32072 EC50 = 257.0 nM 6.59