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Assay Detail

CHEMBL4371261

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Binding
Agonist activity at estrogen receptor beta (unknown origin) after 22 hrs by cell-based luciferase reporter gene assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.
Hanson AM, Perera KLIS, Kim J, Pandey RK, Sweeney N, Lu X, Imhoff A, Mackinnon AC, Wargolet AJ, Van Hart RM, Frick KM, Donaldson WA, Sem DS.
J Med Chem (2018) 61 : 4720 -4738
PubMed 29741891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 7.99 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.66
CHEMBL334773 DIARYLPROPIONITRILE 1 8.96
CHEMBL4526434 1 7.57
CHEMBL4453541 1 7.40
CHEMBL4593988 1 7.19
CHEMBL4442761 1 7.12
CHEMBL4561540 1 7.00
CHEMBL4588840 1 -
CHEMBL4581589 1 -
CHEMBL4472153 1 -
CHEMBL4528491 1 -
CHEMBL4458536 1 -
CHEMBL4592747 1 -
CHEMBL4459147 1 -
CHEMBL4554635 1 -
CHEMBL4444171 1 -
CHEMBL4552891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.022 nM 10.66
CHEMBL334773 DIARYLPROPIONITRILE EC50 = 1.1 nM 8.96
CHEMBL4526434 EC50 = 27.0 nM 7.57
CHEMBL4453541 EC50 = 40.0 nM 7.40
CHEMBL4593988 EC50 = 65.0 nM 7.19
CHEMBL4442761 EC50 = 75.0 nM 7.12
CHEMBL4561540 EC50 = 101.0 nM 7.00
CHEMBL4588840 EC50 - -
CHEMBL4581589 EC50 - -
CHEMBL4472153 EC50 - -
CHEMBL4528491 EC50 - -
CHEMBL4458536 EC50 - -
CHEMBL4592747 EC50 - -
CHEMBL4459147 EC50 - -
CHEMBL4554635 EC50 - -
CHEMBL4444171 EC50 - -
CHEMBL4552891 EC50 - -