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Assay Detail

CHEMBL4263474

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Binding
Agonist activity at full length ERbeta (unknown origin) after 24 hrs by cell based ERE-driven luciferase reporter gene assay
11
Total Activities
11
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

Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).
Sampathi Perera KLI, Hanson AM, Lindeman S, Imhoff A, Lu X, Sem DS, Donaldson WA.
Eur J Med Chem (2018) 157 : 791 -804
PubMed 30144697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.53 10.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.66
CHEMBL4293810 1 7.48
CHEMBL4278672 1 7.32
CHEMBL4283229 1 7.30
CHEMBL4290786 1 7.29
CHEMBL3099433 1 6.92
CHEMBL4290019 1 6.86
CHEMBL4279577 1 6.44
CHEMBL4293632 1 -
CHEMBL4283040 1 -
CHEMBL4290239 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.022 nM 10.66
CHEMBL4293810 EC50 = 33.0 nM 7.48
CHEMBL4278672 EC50 = 48.0 nM 7.32
CHEMBL4283229 EC50 = 50.0 nM 7.30
CHEMBL4290786 EC50 = 51.0 nM 7.29
CHEMBL3099433 EC50 = 121.0 nM 6.92
CHEMBL4290019 EC50 = 139.0 nM 6.86
CHEMBL4279577 EC50 = 362.0 nM 6.44
CHEMBL4293632 EC50 - -
CHEMBL4283040 EC50 - -
CHEMBL4290239 EC50 > 800.0 nM -