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Assay Detail

CHEMBL679886

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

Functional
Potency in cellular transactivation assay utilizing HEK293 cells stably co-transfected with human estrogen receptor alpha and the alkaline phosphatase reporter gene.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen receptor ligands. Part 4: The SAR of the syn-dihydrobenzoxathiin SERAMs.
Kim S, Wu J, Chen HY, Birzin ET, Chan W, Yang YT, Colwell L, Li S, Dahllund J, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML.
Bioorg Med Chem Lett (2004) 14 : 2741 -2745
PubMed 15125925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 8.02 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92660 1 9.00
CHEMBL327320 1 8.77
CHEMBL329902 1 8.64
CHEMBL328716 1 8.60
CHEMBL94116 1 8.47
CHEMBL94225 1 8.46
CHEMBL91807 1 8.44
CHEMBL92635 1 8.40
CHEMBL92027 1 8.33
CHEMBL71584 1 8.30
CHEMBL93705 1 8.27
CHEMBL93793 1 8.26
CHEMBL94030 1 8.21
CHEMBL329849 1 8.03
CHEMBL539927 1 8.02
CHEMBL90072 1 7.83
CHEMBL327471 1 7.65
CHEMBL441457 1 7.59
CHEMBL420623 1 7.21
CHEMBL93546 1 7.03
CHEMBL92720 1 6.56
CHEMBL94170 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92660 IC50 = 1.0 nM 9.00
CHEMBL327320 IC50 = 1.7 nM 8.77
CHEMBL329902 IC50 = 2.3 nM 8.64
CHEMBL328716 IC50 = 2.5 nM 8.60
CHEMBL94116 IC50 = 3.4 nM 8.47
CHEMBL94225 IC50 = 3.5 nM 8.46
CHEMBL91807 IC50 = 3.6 nM 8.44
CHEMBL92635 IC50 = 4.0 nM 8.40
CHEMBL92027 IC50 = 4.7 nM 8.33
CHEMBL71584 IC50 = 5.0 nM 8.30
CHEMBL93705 IC50 = 5.4 nM 8.27
CHEMBL93793 IC50 = 5.5 nM 8.26
CHEMBL94030 IC50 = 6.1 nM 8.21
CHEMBL329849 IC50 = 9.3 nM 8.03
CHEMBL539927 IC50 = 9.6 nM 8.02
CHEMBL90072 IC50 = 14.8 nM 7.83
CHEMBL327471 IC50 = 22.6 nM 7.65
CHEMBL441457 IC50 = 25.4 nM 7.59
CHEMBL420623 IC50 = 61.0 nM 7.21
CHEMBL93546 IC50 = 94.0 nM 7.03
CHEMBL92720 IC50 = 274.0 nM 6.56
CHEMBL94170 IC50 = 341.9 nM 6.47