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Assay Detail

CHEMBL886322

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

Binding
Binding affinity to human recombinant ERbeta by scintillation proximity assay
17
Total Activities
17
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 beta (CHEMBL242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bridged androstenediol analogs as ER-beta selective SERMs.
Blizzard TA, Gude C, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Holmes MA, Rohrer SP, Hammond ML.
Bioorg Med Chem Lett (2007) 17 : 2944 -2948
PubMed 17448656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.96 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135 ESTRADIOL 4.0 1 8.92
CHEMBL246138 1 7.96
CHEMBL391795 1 7.80
CHEMBL246139 1 7.80
CHEMBL245378 1 7.30
CHEMBL246341 1 6.80
CHEMBL393278 1 6.49
CHEMBL246140 1 6.11
CHEMBL245575 1 6.07
CHEMBL397344 1 5.84
CHEMBL392000 1 5.52
CHEMBL397343 1 -
CHEMBL386630 TESTOSTERONE 4.0 1 -
CHEMBL245771 1 -
CHEMBL438863 1 -
CHEMBL245577 1 -
CHEMBL245576 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135 ESTRADIOL IC50 = 1.2 nM 8.92
CHEMBL246138 IC50 = 11.0 nM 7.96
CHEMBL391795 IC50 = 16.0 nM 7.80
CHEMBL246139 IC50 = 16.0 nM 7.80
CHEMBL245378 IC50 = 50.0 nM 7.30
CHEMBL246341 IC50 = 157.0 nM 6.80
CHEMBL393278 IC50 = 322.0 nM 6.49
CHEMBL246140 IC50 = 782.0 nM 6.11
CHEMBL245575 IC50 = 854.0 nM 6.07
CHEMBL397344 IC50 = 1460.0 nM 5.84
CHEMBL392000 IC50 = 3020.0 nM 5.52
CHEMBL397343 IC50 > 10000.0 nM -
CHEMBL386630 TESTOSTERONE IC50 > 10000.0 nM -
CHEMBL245771 IC50 > 10000.0 nM -
CHEMBL438863 IC50 > 10000.0 nM -
CHEMBL245577 IC50 > 10000.0 nM -
CHEMBL245576 IC50 > 10000.0 nM -