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Assay Detail

CHEMBL4021499

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

Binding
Displacement of [3H]mibolerone from human AR after 3 hrs
20
Total Activities
20
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 III: Discovery of 4-(5-oxopyrrolidine-1-yl)benzonitrile derivative 2f as a clinical candidate.
Aikawa K, Asano M, Ono K, Habuka N, Yano J, Wilson K, Fujita H, Kandori H, Hara T, Morimoto M, Santou T, Yamaoka M, Nakayama M, Hasuoka A.
Bioorg Med Chem (2017) 25 : 3330 -3349
PubMed 28454849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.25 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.17
CHEMBL4090028 1 9.14
CHEMBL4092535 1 9.00
CHEMBL4063939 1 8.96
CHEMBL4074501 1 8.89
CHEMBL4100995 1 8.74
CHEMBL4101232 1 8.49
CHEMBL4067691 1 8.47
CHEMBL4088914 1 8.44
CHEMBL4072533 1 8.41
CHEMBL4093265 1 8.26
CHEMBL4101935 1 8.22
CHEMBL4071751 1 8.11
CHEMBL4087902 1 8.05
CHEMBL4059588 1 8.04
CHEMBL4100278 1 7.96
CHEMBL4077666 1 7.85
CHEMBL4083012 1 7.85
CHEMBL4085514 1 7.82
CHEMBL4082265 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE IC50 = 0.67 nM 9.17
CHEMBL4090028 IC50 = 0.72 nM 9.14
CHEMBL4092535 IC50 = 1.0 nM 9.00
CHEMBL4063939 IC50 = 1.1 nM 8.96
CHEMBL4074501 IC50 = 1.3 nM 8.89
CHEMBL4100995 IC50 = 1.8 nM 8.74
CHEMBL4101232 IC50 = 3.2 nM 8.49
CHEMBL4067691 IC50 = 3.4 nM 8.47
CHEMBL4088914 IC50 = 3.6 nM 8.44
CHEMBL4072533 IC50 = 3.9 nM 8.41
CHEMBL4093265 IC50 = 5.5 nM 8.26
CHEMBL4101935 IC50 = 6.0 nM 8.22
CHEMBL4071751 IC50 = 7.8 nM 8.11
CHEMBL4087902 IC50 = 9.0 nM 8.05
CHEMBL4059588 IC50 = 9.2 nM 8.04
CHEMBL4100278 IC50 = 11.0 nM 7.96
CHEMBL4077666 IC50 = 14.0 nM 7.85
CHEMBL4083012 IC50 = 14.0 nM 7.85
CHEMBL4085514 IC50 = 15.0 nM 7.82
CHEMBL4082265 IC50 = 6600.0 nM 5.18