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Assay Detail

CHEMBL4151747

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

Binding
Binding affinity to ERalpha (unknown origin)
3
Total Activities
3
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

Identification of an Orally Bioavailable Chromene-Based Selective Estrogen Receptor Degrader (SERD) That Demonstrates Robust Activity in a Model of Tamoxifen-Resistant Breast Cancer.
Nagasawa J, Govek S, Kahraman M, Lai A, Bonnefous C, Douglas K, Sensintaffar J, Lu N, Lee K, Aparicio A, Kaufman J, Qian J, Shao G, Prudente R, Joseph JD, Darimont B, Brigham D, Maheu K, Heyman R, Rix PJ, Hager JH, Smith ND.
J Med Chem (2018) 61 : 7917 -7928
PubMed 30086626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.90 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4164133 1 8.55
CHEMBL4175085 1 8.29
CHEMBL4159656 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4164133 IC50 = 2.8 nM 8.55
CHEMBL4175085 IC50 = 5.1 nM 8.29
CHEMBL4159656 IC50 = 136.0 nM 6.87