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Assay Detail

CHEMBL996725

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

Binding
Displacement of [3H[DHT from androgen receptor endogenously expressed in human MDA-MB-453 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-453
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.
Nirschl AA, Zou Y, Krystek SR, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG.
J Med Chem (2009) 52 : 2794 -2798
PubMed 19351168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.75 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484727 1 9.70
CHEMBL520174 1 9.52
CHEMBL484726 1 9.52
CHEMBL484728 1 9.52
CHEMBL483745 1 9.15
CHEMBL484919 1 9.10
CHEMBL229861 1 9.05
CHEMBL229860 1 8.80
CHEMBL519169 1 8.72
CHEMBL521329 1 8.64
CHEMBL229808 1 8.22
CHEMBL483746 1 8.00
CHEMBL229264 1 7.85
CHEMBL482549 1 7.77
CHEMBL483941 1 7.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484727 Ki = 0.2 nM 9.70
CHEMBL520174 Ki = 0.3 nM 9.52
CHEMBL484726 Ki = 0.3 nM 9.52
CHEMBL484728 Ki = 0.3 nM 9.52
CHEMBL483745 Ki = 0.7 nM 9.15
CHEMBL484919 Ki = 0.8 nM 9.10
CHEMBL229861 Ki = 0.9 nM 9.05
CHEMBL229860 Ki = 1.6 nM 8.80
CHEMBL519169 Ki = 1.9 nM 8.72
CHEMBL521329 Ki = 2.3 nM 8.64
CHEMBL229808 Ki = 6.0 nM 8.22
CHEMBL483746 Ki = 10.0 nM 8.00
CHEMBL229264 Ki = 14.0 nM 7.85
CHEMBL482549 Ki = 17.0 nM 7.77
CHEMBL483941 Ki = 19.0 nM 7.72