| Assay Method Information | |
| | Androgen Receptor (AR) Radioligand Binding Assay |
| Description: | Human androgen receptors obtained from human LNCaP cells are used in modified HEPES buffer pH 7.4. A 70 μg (adjusted if necessary) aliquot is incubated with 0.5 nM [3H]Methyltrienolone for 20 hours at 4 C. Non-specific binding is estimated in the presence of 1 μM testosterone. Receptors are filtered and washed, the filters are then counted to determine [3H]methyltrienolone specifically bound (Historic values: Kd=0.71 nM: Specific binding=75%; Bmax=0.25 pmole/mg protein). (See, e.g., Traish, A. M et al., Binding of 7α, 17α-dimethyl-19-nortestosterone (Mibolerone) to androgen and progesterone receptors in human and animal tissues. Endocrinology. 118(4): 1327-1333, 1986).Compounds are screened at 10 μM.Where presented, IC50 values were determined by a non-linear, least squares regression analysis using MathIQ (ID Business Solutions Ltd., UK). |
| Affinity data for this assay | |
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