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Assay Detail

CHEMBL3136539

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

Binding
Agonist activity at ER-beta (unknown origin) transfected in HEK293T cells after 24 hrs by Steady-Glo luciferase reporter gene assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The A-CD analogue of 16,17-estriol is a potent and highly selective estrogen receptor agonist
Sauvee C, Schafer A, Sunden H, Ma J, Gustavsson A, Burstein ES, Olsson R
Medchemcomm (2013) 4 : 1439 -1442
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.48 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.40
CHEMBL193482 ESTRIOL 4.0 1 9.90
CHEMBL3134122 1 9.40
CHEMBL3134124 1 7.70
CHEMBL3134123 1 6.90
CHEMBL1651148 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.03981 nM 10.40
CHEMBL193482 ESTRIOL EC50 = 0.1259 nM 9.90
CHEMBL3134122 EC50 = 0.3981 nM 9.40
CHEMBL3134124 EC50 = 19.95 nM 7.70
CHEMBL3134123 EC50 = 125.89 nM 6.90
CHEMBL1651148 EC50 = 251.19 nM 6.60