Assay Report Card

Basic Information

ID: ALA3705382

Type: Binding

Description: Binding Assay: Cells expressing recombinant human CL receptor/RAMP1 were washed with PBS and harvested in harvest buffer containing 50 mM HEPES, 1 mM EDTA and Complete protease inhibitors (Roche). The cell suspension was disrupted with a laboratory homogenizer and centrifuged at 48,000 g to isolate membranes. The pellets were resuspended in harvest buffer plus 250 mM sucrose and stored at −70C. For binding assays, 20 μg of membranes were incubated in 1 ml binding buffer (10 mM HEPES, pH 7.4, 5 mM MgCl2, and 0.2% BSA) for 3 hours at room temperature containing 10 pM 125I-hCGRP (GE Healthcare) and antagonist. The assay was terminated by filtration through 96-well GFB glass fiber filter plates (PerkinElmer) that had been blocked with 0.05% polyethyleneimine. The filters were washed 3 times with ice-cold assay buffer (10 mM HEPES, pH 7.4 and 5 mM MgCl2). Scintillation fluid was added and the plates were counted on a Topeount (Packard).

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
517.633.943.94
479.563.903.90
434.504.024.02
543.674.474.47
461.573.773.77
557.704.864.86
565.684.904.90
543.674.474.47
385.472.022.02
529.644.604.60
561.695.415.41
425.542.612.61
455.522.992.99
454.573.713.71
516.604.624.62
488.594.644.64
453.594.074.07
420.562.382.38
443.552.722.72
471.564.664.66