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Assay Detail

CHEMBL4136958

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

ADMET
Displacement of Fluor.ES2 Green from human ERalpha by TR-FRET competitive binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Disconnecting the Estrogen Receptor Binding Properties and Antimicrobial Properties of Parabens through 3,5-Substitution.
Bergquist BL, Jefferson KG, Kintz HN, Barber AE, Yeagley AA.
ACS Med Chem Lett (2018) 9 : 51 -55
PubMed 29348811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.11 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 9.35
CHEMBL459008 BUTYLPARABEN -1.0 1 5.85
CHEMBL4166909 1 5.10
CHEMBL4170305 1 5.09
CHEMBL277346 OCTYL_GALLATE 1 5.06
CHEMBL494005 BUTYL GALLATE 1 5.05
CHEMBL4169994 1 4.88
CHEMBL4165518 1 4.79
CHEMBL4163053 1 4.53
CHEMBL4171348 1 4.49
CHEMBL4174801 1 4.46
CHEMBL4159672 1 4.41
CHEMBL4173755 1 4.26
CHEMBL4168938 1 4.22
CHEMBL4163451 1 -
CHEMBL4160086 1 -
CHEMBL4162076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 0.452 nM 9.35
CHEMBL459008 BUTYLPARABEN IC50 = 1420.0 nM 5.85
CHEMBL4166909 IC50 = 7980.0 nM 5.10
CHEMBL4170305 IC50 = 8210.0 nM 5.09
CHEMBL277346 OCTYL_GALLATE IC50 = 8740.0 nM 5.06
CHEMBL494005 BUTYL GALLATE IC50 = 8970.0 nM 5.05
CHEMBL4169994 IC50 = 13200.0 nM 4.88
CHEMBL4165518 IC50 = 16200.0 nM 4.79
CHEMBL4163053 IC50 = 29400.0 nM 4.53
CHEMBL4171348 IC50 = 32500.0 nM 4.49
CHEMBL4174801 IC50 = 34600.0 nM 4.46
CHEMBL4159672 IC50 = 39400.0 nM 4.41
CHEMBL4173755 IC50 = 55300.0 nM 4.26
CHEMBL4168938 IC50 = 60400.0 nM 4.22
CHEMBL4163451 IC50 > 200000.0 nM -
CHEMBL4160086 IC50 > 200000.0 nM -
CHEMBL4162076 IC50 > 200000.0 nM -