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Assay Detail

CHEMBL837410

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

Functional
Agonist activity as alkaline phosphatase induction in Ishikawa endometrial cells compared to E2
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
EC50 13 8.73 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184958 1 9.40
CHEMBL360872 3 9.30
CHEMBL184976 1 9.15
CHEMBL2137046 1 9.10
CHEMBL185412 1 9.05
CHEMBL182342 1 8.80
CHEMBL184423 1 8.59
CHEMBL185284 1 8.51
CHEMBL185064 1 8.46
CHEMBL183685 1 8.00
CHEMBL360005 1 7.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184958 EC50 = 0.4 nM 9.40
CHEMBL360872 EC50 = 0.5 nM 9.30
CHEMBL184976 EC50 = 0.7 nM 9.15
CHEMBL360872 EC50 = 0.8 nM 9.10
CHEMBL2137046 EC50 = 0.8 nM 9.10
CHEMBL185412 EC50 = 0.9 nM 9.05
CHEMBL182342 EC50 = 1.6 nM 8.80
CHEMBL184423 EC50 = 2.6 nM 8.59
CHEMBL360872 EC50 = 3.1 nM 8.51
CHEMBL185284 EC50 = 3.1 nM 8.51
CHEMBL185064 EC50 = 3.5 nM 8.46
CHEMBL183685 EC50 = 10.0 nM 8.00
CHEMBL360005 EC50 = 28.0 nM 7.55