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Assay Detail

CHEMBL925473

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

Binding
Binding affinity at AR
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Androstene-3,5-dienes as ER-beta selective SERMs.
Blizzard TA, Gude C, Morgan JD, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Rohrer SP, Hammond ML.
Bioorg Med Chem Lett (2007) 17 : 6295 -6298
PubMed 17890084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.65 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386630 TESTOSTERONE 4.0 1 8.57
CHEMBL246140 1 8.10
CHEMBL135 ESTRADIOL 4.0 1 7.58
CHEMBL246138 1 7.48
CHEMBL249700 1 7.40
CHEMBL250109 1 6.77
CHEMBL440283 ANDROSTENEDIOL -1.0 1 6.64
CHEMBL398841 1 6.54
CHEMBL400480 1 6.48
CHEMBL249903 1 6.30
CHEMBL398634 1 6.28
CHEMBL398456 1 6.25
CHEMBL398455 1 6.08
CHEMBL249904 1 5.79
CHEMBL250110 1 5.65
CHEMBL251515 1 5.58
CHEMBL398840 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386630 TESTOSTERONE IC50 = 2.7 nM 8.57
CHEMBL246140 IC50 = 7.9 nM 8.10
CHEMBL135 ESTRADIOL IC50 = 26.0 nM 7.58
CHEMBL246138 IC50 = 33.0 nM 7.48
CHEMBL249700 IC50 = 40.0 nM 7.40
CHEMBL250109 IC50 = 170.0 nM 6.77
CHEMBL440283 ANDROSTENEDIOL IC50 = 230.0 nM 6.64
CHEMBL398841 IC50 = 290.0 nM 6.54
CHEMBL400480 IC50 = 330.0 nM 6.48
CHEMBL249903 IC50 = 500.0 nM 6.30
CHEMBL398634 IC50 = 520.0 nM 6.28
CHEMBL398456 IC50 = 560.0 nM 6.25
CHEMBL398455 IC50 = 842.0 nM 6.08
CHEMBL249904 IC50 = 1615.0 nM 5.79
CHEMBL250110 IC50 = 2250.0 nM 5.65
CHEMBL251515 IC50 = 2610.0 nM 5.58
CHEMBL398840 IC50 = 3160.0 nM 5.50