Assay Report Card

Basic Information

ID: ALA3888927

Type: Binding

Description: Competitive Binding Assay: The affinity of compounds of the invention for the human NK-3 receptor was determined by measuring the ability of compounds of the invention to competitively and reversibly displace a well-characterized NK-3 radioligand in a concentration-dependent manner.3H-SB222200 Binding Competition Assay with Human NK-3 ReceptorThe ability of compounds of the invention to inhibit the binding of the NK-3 receptor selective antagonist 3H-SB222200 was assessed by an in vitro radioligand binding assay. Membranes were prepared from Chinese hamster ovary recombinant cells stably expressing the human NK-3 receptor. The membranes were incubated with 5 nM 3H-SB222200 (ARC) in a HEPES 25 mM/NaCl 0.1M/CaCl2 1 mM/MgCl2 5 mM/BSA 0.5%/Saponin 10 μg/ml buffer at pH 7.4 and various concentrations of compounds of the invention. The amount of 3H-SB222200 bound to the receptor was determined after filtration by the quantification of membrane associated radioactivity using the TopCount-NXT reader (Packard).

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
358.402.462.46
342.331.991.99
374.862.982.98
412.373.173.17
340.412.322.32
388.431.821.82
412.372.882.88
372.432.852.85
374.862.982.98
388.431.821.82
374.352.712.71
392.853.113.11
394.382.742.74
392.853.113.11
409.303.633.63
356.362.252.25
372.432.722.72
358.402.462.46
394.382.742.74
376.392.602.60
392.853.113.11
365.422.192.19
374.352.712.71
409.303.633.63
420.503.843.84
408.413.343.34
376.392.602.60
386.463.243.24
356.362.252.25
374.862.982.98
358.402.462.46
354.442.632.63
376.392.602.60
376.392.602.60
372.432.852.85
394.383.093.09
392.342.802.80
412.372.882.88
410.332.792.79
372.432.722.72
354.442.632.63
370.442.332.33
392.853.113.11
388.432.472.47
394.382.742.74
394.382.742.74