Assay Report Card

Basic Information

ID: ALA3705176

Type: Binding

Description: Binding Assay: Methods for performing in vitro dopamine receptor binding studies are described in Huang et al. J. Med. Chem. 44:1815-1826 (2001) and Luedtke et al. Synapse 38:438-439 (2000). These papers describe radioactively labeled dopamine receptor selective ligands binding with picomolar affinity and nonselectivity to D2 and D3 dopamine receptors expressed in Sf9 and HEK 293 cells. 125I-IABN binds with 7- to 10-fold lower affinity to human D4.4 dopamine receptors expressed in HEK 293 cells. Dissociation constants (Kd) calculated from kinetic experiments were found to be in agreement with equilibrium Kd values obtained from saturation binding studies. Saturation plots of the binding of 125I-IABN with rat caudate membrane preparations were monophasic and exhibited low nonspecific binding.

Organism: Homo sapiens

Cell type: Sf9

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
497.434.464.46
495.455.475.47
495.455.475.47
497.434.404.40
497.435.185.18
442.563.873.87
453.594.374.37
499.444.364.36
510.474.874.87
460.583.063.06
471.603.573.57
541.484.934.93
499.444.364.36
510.474.874.87
471.603.573.57
461.393.783.78
422.532.482.48
450.583.263.26
462.384.044.04
423.512.742.74
588.274.654.65
549.413.353.35
439.583.213.21
461.393.783.78
422.532.482.48
480.374.184.18
441.502.882.88
492.404.054.05
453.542.752.75