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Assay Detail

CHEMBL1045063

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

Binding
Activity at human recombinant ERalpha by fluorescence polarization assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Estrogen receptor (CHEMBL206)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors based on a thieno[2,3-d]pyrimidin-4(3H)-one core.
Lilienkampf A, Karkola S, Alho-Richmond S, Koskimies P, Johansson N, Huhtinen K, Vihko K, Wähälä K.
J Med Chem (2009) 52 : 6660 -6671
PubMed 19824648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1405 ESTRONE 4.0 1 8.15
CHEMBL569630 1 -
CHEMBL570584 1 -
CHEMBL570358 1 -
CHEMBL583044 1 -
CHEMBL572155 1 -
CHEMBL566312 1 -
CHEMBL572148 1 -
CHEMBL584092 1 -
CHEMBL578830 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1405 ESTRONE EC50 = 7.0 nM 8.15
CHEMBL569630 EC50 > 1000.0 nM -
CHEMBL570584 EC50 > 10000.0 nM -
CHEMBL570358 EC50 > 10000.0 nM -
CHEMBL583044 EC50 > 10000.0 nM -
CHEMBL572155 EC50 > 10000.0 nM -
CHEMBL566312 EC50 > 1000.0 nM -
CHEMBL572148 EC50 > 1000.0 nM -
CHEMBL584092 EC50 > 1000.0 nM -
CHEMBL578830 EC50 > 10000.0 nM -