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Assay Detail

CHEMBL1120815

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

Binding
Transactivation of human ERbeta expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
9
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Estrogen receptor beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 17alpha-arylestradiols as ligands for estrogen receptor alpha and beta.
Sedlák D, Novák P, Kotora M, Bartůnek P.
J Med Chem (2010) 53 : 4290 -4294
PubMed 20408532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.48 10.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 10.21
CHEMBL1098710 2 7.64
CHEMBL1097377 1 7.57
CHEMBL1098709 1 7.46
CHEMBL1096975 2 6.76
CHEMBL1094732 1 6.66
CHEMBL1097284 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL EC50 = 0.06166 nM 10.21
CHEMBL1098710 EC50 = 22.7 nM 7.64
CHEMBL1098710 EC50 = 22.65 nM 7.64
CHEMBL1097377 EC50 = 26.67 nM 7.57
CHEMBL1098709 EC50 = 34.59 nM 7.46
CHEMBL1096975 EC50 = 175.39 nM 6.76
CHEMBL1096975 EC50 = 174.0 nM 6.76
CHEMBL1094732 EC50 = 221.31 nM 6.66
CHEMBL1097284 EC50 = 242.1 nM 6.62