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Assay Detail

CHEMBL964137

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

Functional
Antagonist activity at human androgen receptor expressed in human MDA-MB453 cells by luciferase reporter gene assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB453
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production.
Mitchell L, Wang Z, Hu LY, Kostlan C, Carroll M, Dettling D, Du D, Pocalyko D, Wade K.
Bioorg Med Chem Lett (2009) 19 : 1310 -1313
PubMed 19201190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.11 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445429 1 8.00
CHEMBL462664 1 7.96
CHEMBL448454 1 7.52
CHEMBL510145 1 7.46
CHEMBL462026 1 7.43
CHEMBL490955 1 7.34
CHEMBL449867 1 7.32
CHEMBL507671 1 7.27
CHEMBL504110 1 7.26
CHEMBL455566 1 7.18
CHEMBL462022 1 7.16
CHEMBL490956 1 7.11
CHEMBL491493 1 7.09
CHEMBL453740 1 7.05
CHEMBL462025 1 6.91
CHEMBL453623 1 6.88
CHEMBL449371 1 6.78
CHEMBL490957 1 6.71
CHEMBL501649 1 6.68
CHEMBL453624 1 6.15
CHEMBL462665 1 6.08
CHEMBL491492 1 -
CHEMBL447604 1 -
CHEMBL464929 1 -
CHEMBL499137 1 -
CHEMBL464764 1 -
CHEMBL465539 1 -
CHEMBL462027 1 -
CHEMBL462234 1 -
CHEMBL453244 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445429 IC50 = 10.0 nM 8.00
CHEMBL462664 IC50 = 11.0 nM 7.96
CHEMBL448454 IC50 = 30.0 nM 7.52
CHEMBL510145 IC50 = 35.0 nM 7.46
CHEMBL462026 IC50 = 37.0 nM 7.43
CHEMBL490955 IC50 = 46.0 nM 7.34
CHEMBL449867 IC50 = 48.0 nM 7.32
CHEMBL507671 IC50 = 54.0 nM 7.27
CHEMBL504110 IC50 = 55.0 nM 7.26
CHEMBL455566 IC50 = 66.0 nM 7.18
CHEMBL462022 IC50 = 69.0 nM 7.16
CHEMBL490956 IC50 = 78.0 nM 7.11
CHEMBL491493 IC50 = 81.0 nM 7.09
CHEMBL453740 IC50 = 89.0 nM 7.05
CHEMBL462025 IC50 = 123.0 nM 6.91
CHEMBL453623 IC50 = 133.0 nM 6.88
CHEMBL449371 IC50 = 167.0 nM 6.78
CHEMBL490957 IC50 = 197.0 nM 6.71
CHEMBL501649 IC50 = 209.0 nM 6.68
CHEMBL453624 IC50 = 702.0 nM 6.15
CHEMBL462665 IC50 = 838.0 nM 6.08
CHEMBL491492 IC50 - -
CHEMBL447604 IC50 - -
CHEMBL464929 IC50 - -
CHEMBL499137 IC50 - -
CHEMBL464764 IC50 - -
CHEMBL465539 IC50 - -
CHEMBL462027 IC50 - -
CHEMBL462234 IC50 - -
CHEMBL453244 IC50 - -
CHEMBL462663 IC50 - -
CHEMBL503687 IC50 - -
CHEMBL448978 IC50 - -
CHEMBL443970 IC50 > 1000.0 nM -