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Assay Detail

CHEMBL4356686

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

Binding
Antagonist activity at ERalpha in human MCF7:WS8 cells incubated for 18 hrs by dual luciferase reporter gene assay relative to control
15
Total Activities
15
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

Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ.
J Med Chem (2019) 62 : 11301 -11323
PubMed 31746603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.29 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4586663 1 9.30
CHEMBL4532671 1 8.82
CHEMBL4527655 1 8.72
CHEMBL4448178 1 8.68
CHEMBL4578883 1 8.57
CHEMBL4533964 1 8.51
CHEMBL4543096 1 8.46
CHEMBL4515212 1 8.37
CHEMBL4538085 1 8.28
CHEMBL4483006 1 8.13
CHEMBL4436415 1 7.96
CHEMBL4440649 1 7.92
CHEMBL4564385 1 7.85
CHEMBL4524872 1 7.55
CHEMBL4464171 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4586663 IC50 = 0.5 nM 9.30
CHEMBL4532671 IC50 = 1.5 nM 8.82
CHEMBL4527655 IC50 = 1.9 nM 8.72
CHEMBL4448178 IC50 = 2.1 nM 8.68
CHEMBL4578883 IC50 = 2.7 nM 8.57
CHEMBL4533964 IC50 = 3.1 nM 8.51
CHEMBL4543096 IC50 = 3.5 nM 8.46
CHEMBL4515212 IC50 = 4.3 nM 8.37
CHEMBL4538085 IC50 = 5.2 nM 8.28
CHEMBL4483006 IC50 = 7.4 nM 8.13
CHEMBL4436415 IC50 = 11.0 nM 7.96
CHEMBL4440649 IC50 = 12.0 nM 7.92
CHEMBL4564385 IC50 = 14.0 nM 7.85
CHEMBL4524872 IC50 = 28.0 nM 7.55
CHEMBL4464171 IC50 = 64.0 nM 7.19