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Assay Detail

CHEMBL4401223

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Binding
Inhibition of estrogen receptor-alpha (unknown origin) by ELISA
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 (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based drug design, synthesis, In vitro, and In vivo biological evaluation of indole-based biomimetic analogs targeting estrogen receptor-α inhibition.
Hendy MS, Ali AA, Ahmed L, Hossam R, Mostafa A, Elmazar MM, Naguib BH, Attia YM, Ahmed MS.
Eur J Med Chem (2019) 166 : 281 -290
PubMed 30731397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.00 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83 TAMOXIFEN 4.0 1 8.82
CHEMBL4590512 1 8.75
CHEMBL4435453 1 8.62
CHEMBL4539135 1 8.48
CHEMBL4468912 1 8.33
CHEMBL4444460 1 8.12
CHEMBL4555331 1 8.09
CHEMBL4571261 1 7.64
CHEMBL4553545 1 7.35
CHEMBL4570601 1 7.16
CHEMBL4516755 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83 TAMOXIFEN IC50 = 1.5 nM 8.82
CHEMBL4590512 IC50 = 1.76 nM 8.75
CHEMBL4435453 IC50 = 2.4 nM 8.62
CHEMBL4539135 IC50 = 3.31 nM 8.48
CHEMBL4468912 IC50 = 4.71 nM 8.33
CHEMBL4444460 IC50 = 7.53 nM 8.12
CHEMBL4555331 IC50 = 8.15 nM 8.09
CHEMBL4571261 IC50 = 22.67 nM 7.64
CHEMBL4553545 IC50 = 44.43 nM 7.35
CHEMBL4570601 IC50 = 69.46 nM 7.16
CHEMBL4516755 IC50 = 204.75 nM 6.69