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Assay Detail

CHEMBL3767968

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

Binding
Displacement of [3H]-methyltrienolone from progesterone receptor (unknown origin) expressed in HEK293 cell lysate incubated overnight by microbeta scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Progesterone receptor (CHEMBL208)
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
Ki 5 6.78 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166444 METRIBOLONE 2.0 1 9.31
CHEMBL3765171 1 6.35
CHEMBL3765823 1 6.28
CHEMBL3764185 1 6.06
CHEMBL3764446 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166444 METRIBOLONE Ki = 0.49 nM 9.31
CHEMBL3765171 Ki = 448.0 nM 6.35
CHEMBL3765823 Ki = 520.0 nM 6.28
CHEMBL3764185 Ki = 872.0 nM 6.06
CHEMBL3764446 Ki = 1220.0 nM 5.91