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Assay Detail

CHEMBL3767969

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

Binding
Agonist activity at human androgen receptor expressed in mouse C2C12 cells cotransfected with GRE/ARE reporter plasmid assessed as receptor transactivation after 48 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C2C12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.
Saeed A, Vaught GM, Gavardinas K, Matthews D, Green JE, Losada PG, Bullock HA, Calvert NA, Patel NJ, Sweetana SA, Krishnan V, Henck JW, Luz JG, Wang Y, Jadhav P.
J Med Chem (2016) 59 : 750 -755
PubMed 26683992 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 9.21 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166444 METRIBOLONE 2.0 1 10.89
CHEMBL3765171 1 10.40
CHEMBL3764185 1 9.30
CHEMBL3765823 1 8.31
CHEMBL3764446 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166444 METRIBOLONE EC50 = 0.013 nM 10.89
CHEMBL3765171 EC50 = 0.0398 nM 10.40
CHEMBL3764185 EC50 = 0.499 nM 9.30
CHEMBL3765823 EC50 = 4.88 nM 8.31
CHEMBL3764446 EC50 = 73.7 nM 7.13