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Assay Detail

CHEMBL1008660

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

Binding
Displacement of [3H]tamoxifen from antiestrogen binding site in Sprague-Dawley rat liver by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Anti-estrogen binding site (AEBS) (CHEMBL612409)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Activity-guided isolation of steroidal alkaloid antiestrogen-binding site inhibitors from Pachysandra procumbens.
Chang LC, Bhat KP, Pisha E, Kennelly EJ, Fong HH, Pezzuto JM, Kinghorn AD.
J Nat Prod (1998) 61 : 1257 -1262
PubMed 9784163 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.66 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL342394 1 6.40
CHEMBL464782 (+)-PACHYSAMINE B 1 6.22
CHEMBL455316 1 6.22
CHEMBL457817 1 5.55
CHEMBL458033 1 5.46
CHEMBL505436 1 5.17
CHEMBL456512 1 5.13
CHEMBL335133 1 5.10
CHEMBL136933 EPIPACHYSAMINE D 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL342394 IC50 = 400.0 nM 6.40
CHEMBL464782 (+)-PACHYSAMINE B IC50 = 600.0 nM 6.22
CHEMBL455316 IC50 = 600.0 nM 6.22
CHEMBL457817 IC50 = 2800.0 nM 5.55
CHEMBL458033 IC50 = 3500.0 nM 5.46
CHEMBL505436 IC50 = 6800.0 nM 5.17
CHEMBL456512 IC50 = 7400.0 nM 5.13
CHEMBL335133 IC50 = 8000.0 nM 5.10
CHEMBL136933 EPIPACHYSAMINE D IC50 > 20000.0 nM -