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Assay Detail

CHEMBL987689

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

Binding
Displacement of [3H]DHT from human cloned androgen receptor expressed in insect Sf9 cell system
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diphenyl ethers as androgen receptor antagonists for the topical suppression of sebum production.
Mitchell LH, Hu LY, Nguyen M, Fakhoury S, Smith Y, Iula D, Kostlan C, Carroll M, Dettling D, Du D, Pocalyko D, Wade K, Lefker B.
Bioorg Med Chem Lett (2009) 19 : 2176 -2178
PubMed 19286380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.77 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471644 1 8.00
CHEMBL9337 RU-58841 1 7.80
CHEMBL513195 1 7.70
CHEMBL470204 1 7.52
CHEMBL471645 1 7.47
CHEMBL490955 1 7.19
CHEMBL469334 1 7.16
CHEMBL504179 1 7.13
CHEMBL469380 1 7.08
CHEMBL499137 1 7.04
CHEMBL512837 1 6.99
CHEMBL449804 1 6.92
CHEMBL470629 1 6.91
CHEMBL469982 1 6.90
CHEMBL469983 1 6.80
CHEMBL469333 1 6.80
CHEMBL513768 1 6.70
CHEMBL469602 1 6.70
CHEMBL451153 1 6.67
CHEMBL470395 1 6.64
CHEMBL510289 1 6.59
CHEMBL511145 1 6.45
CHEMBL471876 1 6.37
CHEMBL464764 1 6.11
CHEMBL507267 1 5.64
CHEMBL470841 1 5.57
CHEMBL465539 1 5.40
CHEMBL470842 1 5.18
CHEMBL469600 1 -
CHEMBL469601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471644 IC50 = 10.0 nM 8.00
CHEMBL9337 RU-58841 IC50 = 16.0 nM 7.80
CHEMBL513195 IC50 = 20.0 nM 7.70
CHEMBL470204 IC50 = 30.0 nM 7.52
CHEMBL471645 IC50 = 34.0 nM 7.47
CHEMBL490955 IC50 = 64.0 nM 7.19
CHEMBL469334 IC50 = 69.0 nM 7.16
CHEMBL504179 IC50 = 74.0 nM 7.13
CHEMBL469380 IC50 = 83.0 nM 7.08
CHEMBL499137 IC50 = 92.0 nM 7.04
CHEMBL512837 IC50 = 103.0 nM 6.99
CHEMBL449804 IC50 = 120.0 nM 6.92
CHEMBL470629 IC50 = 123.0 nM 6.91
CHEMBL469982 IC50 = 127.0 nM 6.90
CHEMBL469983 IC50 = 158.0 nM 6.80
CHEMBL469333 IC50 = 157.0 nM 6.80
CHEMBL513768 IC50 = 198.0 nM 6.70
CHEMBL469602 IC50 = 202.0 nM 6.70
CHEMBL451153 IC50 = 216.0 nM 6.67
CHEMBL470395 IC50 = 229.0 nM 6.64
CHEMBL510289 IC50 = 257.0 nM 6.59
CHEMBL511145 IC50 = 354.0 nM 6.45
CHEMBL471876 IC50 = 430.0 nM 6.37
CHEMBL464764 IC50 = 770.0 nM 6.11
CHEMBL507267 IC50 = 2280.0 nM 5.64
CHEMBL470841 IC50 = 2720.0 nM 5.57
CHEMBL465539 IC50 = 4000.0 nM 5.40
CHEMBL470842 IC50 = 6650.0 nM 5.18
CHEMBL469600 IC50 > 10000.0 nM -
CHEMBL469601 IC50 > 10000.0 nM -