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Assay Detail

CHEMBL859226

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

Binding
Inhibitory activity against AR
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Androstenediol analogs 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, Sharma N, Fitzgerald PM, Rohrer SP, Hammond ML.
Bioorg Med Chem Lett (2006) 16 : 834 -838
PubMed 16309907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.62 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386630 TESTOSTERONE 4.0 1 8.57
CHEMBL203748 1 8.10
CHEMBL202007 1 7.96
CHEMBL135 ESTRADIOL 4.0 1 7.72
CHEMBL379441 1 7.70
CHEMBL382097 1 7.48
CHEMBL373019 1 7.48
CHEMBL202400 1 7.07
CHEMBL204317 1 6.92
CHEMBL204642 1 6.77
CHEMBL201569 1 6.76
CHEMBL440283 ANDROSTENEDIOL -1.0 1 6.67
CHEMBL381566 1 6.54
CHEMBL383253 1 6.14
CHEMBL202415 1 6.07
CHEMBL380876 1 5.85
CHEMBL370236 1 5.84
CHEMBL203561 1 5.76
CHEMBL201517 1 5.75
CHEMBL369979 1 5.75
CHEMBL437065 1 5.75
CHEMBL201809 1 5.43
CHEMBL369991 1 5.42
CHEMBL204389 1 5.34
CHEMBL201364 1 -
CHEMBL382632 1 -
CHEMBL380978 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386630 TESTOSTERONE IC50 = 2.7 nM 8.57
CHEMBL203748 IC50 = 7.9 nM 8.10
CHEMBL202007 IC50 = 11.0 nM 7.96
CHEMBL135 ESTRADIOL IC50 = 19.1 nM 7.72
CHEMBL379441 IC50 = 20.0 nM 7.70
CHEMBL382097 IC50 = 33.0 nM 7.48
CHEMBL373019 IC50 = 33.0 nM 7.48
CHEMBL202400 IC50 = 85.0 nM 7.07
CHEMBL204317 IC50 = 120.0 nM 6.92
CHEMBL204642 IC50 = 169.0 nM 6.77
CHEMBL201569 IC50 = 172.0 nM 6.76
CHEMBL440283 ANDROSTENEDIOL IC50 = 212.0 nM 6.67
CHEMBL381566 IC50 = 287.0 nM 6.54
CHEMBL383253 IC50 = 718.0 nM 6.14
CHEMBL202415 IC50 = 843.0 nM 6.07
CHEMBL380876 IC50 = 1402.0 nM 5.85
CHEMBL370236 IC50 = 1436.0 nM 5.84
CHEMBL203561 IC50 = 1717.0 nM 5.76
CHEMBL201517 IC50 = 1769.0 nM 5.75
CHEMBL369979 IC50 = 1768.0 nM 5.75
CHEMBL437065 IC50 = 1761.0 nM 5.75
CHEMBL201809 IC50 = 3733.0 nM 5.43
CHEMBL369991 IC50 = 3767.0 nM 5.42
CHEMBL204389 IC50 = 4617.0 nM 5.34
CHEMBL201364 IC50 > 5000.0 nM -
CHEMBL382632 IC50 > 5000.0 nM -
CHEMBL380978 IC50 > 5000.0 nM -