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Assay Detail

CHEMBL3404787

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

Binding
Displacement of [3H]mibolerone from androgen receptor (unknown origin) after 3 hrs
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part I.
Aikawa K, Miyawaki T, Hitaka T, Imai YN, Hara T, Miyazaki J, Yamaoka M, Kusaka M, Kanzaki N, Tasaka A, Shiraishi M, Yamamoto S.
Bioorg Med Chem (2015) 23 : 2568 -2578
PubMed 25862209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.43 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3402221 1 9.08
CHEMBL3402227 1 9.00
CHEMBL3402224 1 8.96
CHEMBL3402225 1 8.85
CHEMBL3402232 1 8.85
CHEMBL3402228 1 8.66
CHEMBL3402229 1 8.62
CHEMBL570897 1 8.60
CHEMBL570898 1 8.60
CHEMBL3402231 1 8.39
CHEMBL3402223 1 8.15
CHEMBL3402233 1 8.12
CHEMBL3402222 1 7.70
CHEMBL3402226 1 7.47
CHEMBL3402230 1 7.43
CHEMBL3402220 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3402221 IC50 = 0.84 nM 9.08
CHEMBL3402227 IC50 = 1.0 nM 9.00
CHEMBL3402224 IC50 = 1.1 nM 8.96
CHEMBL3402225 IC50 = 1.4 nM 8.85
CHEMBL3402232 IC50 = 1.4 nM 8.85
CHEMBL3402228 IC50 = 2.2 nM 8.66
CHEMBL3402229 IC50 = 2.4 nM 8.62
CHEMBL570897 IC50 = 2.5 nM 8.60
CHEMBL570898 IC50 = 2.5 nM 8.60
CHEMBL3402231 IC50 = 4.1 nM 8.39
CHEMBL3402223 IC50 = 7.0 nM 8.15
CHEMBL3402233 IC50 = 7.5 nM 8.12
CHEMBL3402222 IC50 = 20.0 nM 7.70
CHEMBL3402226 IC50 = 34.0 nM 7.47
CHEMBL3402230 IC50 = 37.0 nM 7.43
CHEMBL3402220 IC50 > 10000.0 nM -