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Assay Detail

CHEMBL4627506

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

Binding
Displacement of [3H]17-beta estradiol from GST-fused human recombinant ERbeta ligand binding domain expressed in Escherichia coli BL21alpha cells incubated for 1 hr by liquid scintillation counting method
7
Total Activities
7
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

Bisphenol AF: Halogen bonding effect is a major driving force for the dual ERα-agonist and ERβ-antagonist activities.
Liu X, Suyama K, Shiki J, Torikai K, Nose T, Shimohigashi M, Shimohigashi Y.
Bioorg Med Chem (2020) 28 : 115274 -115274
PubMed 31879182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.38 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.17
CHEMBL4642117 1 8.13
CHEMBL1900054 1 7.83
CHEMBL196585 1 7.81
CHEMBL4646249 1 7.01
CHEMBL418971 BISPHENOL A 1 6.06
CHEMBL2392656 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.67 nM 9.17
CHEMBL4642117 IC50 = 7.39 nM 8.13
CHEMBL1900054 IC50 = 14.7 nM 7.83
CHEMBL196585 IC50 = 15.4 nM 7.81
CHEMBL4646249 IC50 = 96.8 nM 7.01
CHEMBL418971 BISPHENOL A IC50 = 870.0 nM 6.06
CHEMBL2392656 IC50 = 2400.0 nM 5.62