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Assay Detail

CHEMBL835873

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

Functional
Antagonist activity as inhibition of 1 nM 17-beta-estradiol stimulated alkaline phosphatase induction in Ishikawa endometrial cells
13
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Ishikawa
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Estrogen receptor (CHEMBL2093866)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Benzothiophene and naphthalene derived constrained SERMs.
Wallace OB, Bryant HU, Shetler PK, Adrian MD, Geiser AG.
Bioorg Med Chem Lett (2004) 14 : 5103 -5106
PubMed 15380208 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.75 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360872 3 7.55
CHEMBL184958 1 7.35
CHEMBL184976 1 7.30
CHEMBL185412 1 7.28
CHEMBL184423 1 6.89
CHEMBL2137046 1 6.29
CHEMBL360005 1 6.24
CHEMBL185284 1 6.17
CHEMBL182342 1 6.16
CHEMBL185064 1 6.15
CHEMBL183685 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360872 IC50 = 28.0 nM 7.55
CHEMBL360872 IC50 = 31.0 nM 7.51
CHEMBL184958 IC50 = 45.0 nM 7.35
CHEMBL184976 IC50 = 50.0 nM 7.30
CHEMBL185412 IC50 = 53.0 nM 7.28
CHEMBL184423 IC50 = 130.0 nM 6.89
CHEMBL360872 IC50 = 160.0 nM 6.80
CHEMBL2137046 IC50 = 510.0 nM 6.29
CHEMBL360005 IC50 = 580.0 nM 6.24
CHEMBL185284 IC50 = 680.0 nM 6.17
CHEMBL182342 IC50 = 690.0 nM 6.16
CHEMBL185064 IC50 = 710.0 nM 6.15
CHEMBL183685 IC50 = 820.0 nM 6.09