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Assay Detail

CHEMBL679891

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

Binding
In vitro concentration required to inhibit [3H]estradiol binding to human estrogen receptor alpha expressed in 293T cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type 293T
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.
Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, DaSilva-Jardine P.
Bioorg Med Chem Lett (2004) 14 : 2729 -2733
PubMed 15125923 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.51 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92748 1 9.30
CHEMBL94280 1 8.33
CHEMBL420244 1 8.28
CHEMBL93230 1 8.25
CHEMBL93586 1 8.23
CHEMBL315866 1 8.17
CHEMBL93391 1 8.10
CHEMBL92900 1 8.04
CHEMBL316080 1 7.94
CHEMBL93826 1 7.70
CHEMBL330307 1 7.61
CHEMBL93792 1 7.55
CHEMBL89994 1 7.54
CHEMBL412907 1 7.53
CHEMBL91740 1 7.53
CHEMBL91052 1 7.51
CHEMBL90008 1 7.37
CHEMBL94080 1 7.35
CHEMBL328675 1 7.30
CHEMBL89995 1 7.28
CHEMBL93326 1 7.27
CHEMBL328475 1 6.95
CHEMBL421368 1 6.92
CHEMBL93266 1 6.91
CHEMBL93207 1 6.80
CHEMBL313849 1 6.78
CHEMBL329630 1 6.63
CHEMBL91452 1 6.42
CHEMBL316292 1 6.25
CHEMBL330029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92748 IC50 = 0.5 nM 9.30
CHEMBL94280 IC50 = 4.7 nM 8.33
CHEMBL420244 IC50 = 5.2 nM 8.28
CHEMBL93230 IC50 = 5.6 nM 8.25
CHEMBL93586 IC50 = 5.9 nM 8.23
CHEMBL315866 IC50 = 6.7 nM 8.17
CHEMBL93391 IC50 = 8.0 nM 8.10
CHEMBL92900 IC50 = 9.2 nM 8.04
CHEMBL316080 IC50 = 11.5 nM 7.94
CHEMBL93826 IC50 = 20.1 nM 7.70
CHEMBL330307 IC50 = 24.8 nM 7.61
CHEMBL93792 IC50 = 28.0 nM 7.55
CHEMBL89994 IC50 = 28.7 nM 7.54
CHEMBL412907 IC50 = 29.8 nM 7.53
CHEMBL91740 IC50 = 29.4 nM 7.53
CHEMBL91052 IC50 = 30.7 nM 7.51
CHEMBL90008 IC50 = 42.7 nM 7.37
CHEMBL94080 IC50 = 44.3 nM 7.35
CHEMBL328675 IC50 = 50.0 nM 7.30
CHEMBL89995 IC50 = 53.1 nM 7.28
CHEMBL93326 IC50 = 53.6 nM 7.27
CHEMBL328475 IC50 = 112.0 nM 6.95
CHEMBL421368 IC50 = 120.0 nM 6.92
CHEMBL93266 IC50 = 122.7 nM 6.91
CHEMBL93207 IC50 = 160.0 nM 6.80
CHEMBL313849 IC50 = 165.0 nM 6.78
CHEMBL329630 IC50 = 235.0 nM 6.63
CHEMBL91452 IC50 = 385.0 nM 6.42
CHEMBL316292 IC50 = 562.0 nM 6.25
CHEMBL330029 IC50 > 3200.0 nM -