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Assay Detail

CHEMBL652259

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Functional
In vitro antagonist activity against rat prostatic androgen receptor (AR)
132
Total Activities
130
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL3072)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Azasteroids: structure-activity relationships for inhibition of 5 alpha-reductase and of androgen receptor binding.
Rasmusson GH, Reynolds GF, Steinberg NG, Walton E, Patel GF, Liang T, Cascieri MA, Cheung AH, Brooks JR, Berman C.
J Med Chem (1986) 29 : 2298 -2315
PubMed 3783591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 132 6.13 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3349077 1 8.82
CHEMBL27769 STANOLONE 2.0 1 8.66
CHEMBL559246 1 8.62
CHEMBL386630 TESTOSTERONE 4.0 1 8.49
CHEMBL3349086 1 8.13
CHEMBL3349122 1 7.92
CHEMBL3349134 1 7.89
CHEMBL3349148 1 7.82
CHEMBL2311174 1 7.72
CHEMBL1230438 1 7.70
CHEMBL3349210 1 7.64
CHEMBL3349120 1 7.52
CHEMBL3349150 1 7.19
CHEMBL274826 ANDROSTENEDIONE -1.0 1 7.19
CHEMBL2298410 1 7.18
CHEMBL1790280 1 7.13
CHEMBL584295 1 7.08
CHEMBL3349146 1 7.05
CHEMBL3349100 1 7.05
CHEMBL3349114 1 7.05
CHEMBL3349095 1 7.00
CHEMBL3349087 1 6.96
CHEMBL3349116 1 6.92
CHEMBL3349105 1 6.89
CHEMBL3349293 1 6.85
CHEMBL3349078 1 6.85
CHEMBL3349165 1 6.82
CHEMBL3349180 2 6.82
CHEMBL3349160 1 6.82
CHEMBL583743 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3349077 IC50 = 1.5 nM 8.82
CHEMBL27769 STANOLONE IC50 = 2.2 nM 8.66
CHEMBL559246 IC50 = 2.4 nM 8.62
CHEMBL386630 TESTOSTERONE IC50 = 3.2 nM 8.49
CHEMBL3349086 IC50 = 7.4 nM 8.13
CHEMBL3349122 IC50 = 12.0 nM 7.92
CHEMBL3349134 IC50 = 13.0 nM 7.89
CHEMBL3349148 IC50 = 15.0 nM 7.82
CHEMBL2311174 IC50 = 19.0 nM 7.72
CHEMBL1230438 IC50 = 20.0 nM 7.70
CHEMBL3349210 IC50 = 23.0 nM 7.64
CHEMBL3349120 IC50 = 30.0 nM 7.52
CHEMBL3349150 IC50 = 64.0 nM 7.19
CHEMBL274826 ANDROSTENEDIONE IC50 = 64.0 nM 7.19
CHEMBL2298410 IC50 = 66.0 nM 7.18
CHEMBL1790280 IC50 = 74.0 nM 7.13
CHEMBL584295 IC50 = 83.0 nM 7.08
CHEMBL3349100 IC50 = 89.0 nM 7.05
CHEMBL3349146 IC50 = 89.0 nM 7.05
CHEMBL3349114 IC50 = 89.0 nM 7.05
CHEMBL3349095 IC50 = 100.0 nM 7.00
CHEMBL3349087 IC50 = 110.0 nM 6.96
CHEMBL3349116 IC50 = 120.0 nM 6.92
CHEMBL3349105 IC50 = 130.0 nM 6.89
CHEMBL3349293 IC50 = 140.0 nM 6.85
CHEMBL3349078 IC50 = 140.0 nM 6.85
CHEMBL3349160 IC50 = 150.0 nM 6.82
CHEMBL3349180 IC50 = 150.0 nM 6.82
CHEMBL3349165 IC50 = 150.0 nM 6.82
CHEMBL3349113 IC50 = 170.0 nM 6.77
CHEMBL583743 IC50 = 170.0 nM 6.77
CHEMBL3349512 IC50 = 190.0 nM 6.72
CHEMBL3349130 IC50 = 210.0 nM 6.68
CHEMBL3349180 IC50 = 240.0 nM 6.62
CHEMBL3349119 IC50 = 250.0 nM 6.60
CHEMBL3349094 IC50 = 270.0 nM 6.57
CHEMBL3349082 IC50 = 290.0 nM 6.54
CHEMBL3349141 IC50 = 290.0 nM 6.54
CHEMBL1563246 IC50 = 330.0 nM 6.48
CHEMBL3349129 IC50 = 340.0 nM 6.47
CHEMBL3349126 IC50 = 340.0 nM 6.47
CHEMBL575767 IC50 = 400.0 nM 6.40
CHEMBL3349144 IC50 = 420.0 nM 6.38
CHEMBL1790287 IC50 = 430.0 nM 6.37
CHEMBL3349104 IC50 = 440.0 nM 6.36
CHEMBL572724 IC50 = 450.0 nM 6.35
CHEMBL3349147 IC50 = 500.0 nM 6.30
CHEMBL3349098 IC50 = 540.0 nM 6.27
CHEMBL3085570 IC50 = 560.0 nM 6.25
CHEMBL3349084 IC50 = 580.0 nM 6.24