Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL984569

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

Binding
Inhibition of estradiol-induced coactivator peptide SRC1 binding to estrogen receptor alpha expressed in human HEC1 cells after 24 hrs by luciferase based mammalian two-hybrid assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEC-1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Envelope glycoprotein gp70 (CHEMBL5825)
Type SINGLE PROTEIN
Organism Mouse mammary tumor virus (strain GR) (MMTV)

Publication

Synthesis and biological evaluation of guanylhydrazone coactivator binding inhibitors for the estrogen receptor.
LaFrate AL, Gunther JR, Carlson KE, Katzenellenbogen JA.
Bioorg Med Chem (2008) 16 : 10075 -10084
PubMed 18976929 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.31 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL456106 1 5.68
CHEMBL456392 1 5.60
CHEMBL460174 1 5.58
CHEMBL448651 1 5.44
CHEMBL456179 1 5.42
CHEMBL456594 1 5.40
CHEMBL458496 1 5.34
CHEMBL456599 1 5.31
CHEMBL512206 1 5.23
CHEMBL456598 1 5.17
CHEMBL456393 1 5.03
CHEMBL285853 1 4.95
CHEMBL33663 1 4.94
CHEMBL456600 1 -
CHEMBL458495 1 -
CHEMBL459968 1 -
CHEMBL508968 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL456106 IC50 = 2100.0 nM 5.68
CHEMBL456392 IC50 = 2500.0 nM 5.60
CHEMBL460174 IC50 = 2600.0 nM 5.58
CHEMBL448651 IC50 = 3600.0 nM 5.44
CHEMBL456179 IC50 = 3800.0 nM 5.42
CHEMBL456594 IC50 = 4000.0 nM 5.40
CHEMBL458496 IC50 = 4600.0 nM 5.34
CHEMBL456599 IC50 = 4900.0 nM 5.31
CHEMBL512206 IC50 = 5900.0 nM 5.23
CHEMBL456598 IC50 = 6800.0 nM 5.17
CHEMBL456393 IC50 = 9400.0 nM 5.03
CHEMBL285853 IC50 = 11300.0 nM 4.95
CHEMBL33663 IC50 = 11500.0 nM 4.94
CHEMBL456600 IC50 >= 50000.0 nM -
CHEMBL458495 IC50 - -
CHEMBL459968 IC50 >= 50000.0 nM -
CHEMBL508968 IC50 - -