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
Bioactivity
Activity Types for Assay ALA3888927
Ki
Parent Molecular Weight | ALogP | Polar Surface Area |
---|---|---|
358.40 | 2.46 | 2.46 |
342.33 | 1.99 | 1.99 |
374.86 | 2.98 | 2.98 |
412.37 | 3.17 | 3.17 |
340.41 | 2.32 | 2.32 |
388.43 | 1.82 | 1.82 |
412.37 | 2.88 | 2.88 |
372.43 | 2.85 | 2.85 |
374.86 | 2.98 | 2.98 |
388.43 | 1.82 | 1.82 |
374.35 | 2.71 | 2.71 |
392.85 | 3.11 | 3.11 |
394.38 | 2.74 | 2.74 |
392.85 | 3.11 | 3.11 |
409.30 | 3.63 | 3.63 |
356.36 | 2.25 | 2.25 |
372.43 | 2.72 | 2.72 |
358.40 | 2.46 | 2.46 |
394.38 | 2.74 | 2.74 |
376.39 | 2.60 | 2.60 |
392.85 | 3.11 | 3.11 |
365.42 | 2.19 | 2.19 |
374.35 | 2.71 | 2.71 |
409.30 | 3.63 | 3.63 |
420.50 | 3.84 | 3.84 |
408.41 | 3.34 | 3.34 |
376.39 | 2.60 | 2.60 |
386.46 | 3.24 | 3.24 |
356.36 | 2.25 | 2.25 |
374.86 | 2.98 | 2.98 |
358.40 | 2.46 | 2.46 |
354.44 | 2.63 | 2.63 |
376.39 | 2.60 | 2.60 |
376.39 | 2.60 | 2.60 |
372.43 | 2.85 | 2.85 |
394.38 | 3.09 | 3.09 |
392.34 | 2.80 | 2.80 |
412.37 | 2.88 | 2.88 |
410.33 | 2.79 | 2.79 |
372.43 | 2.72 | 2.72 |
354.44 | 2.63 | 2.63 |
370.44 | 2.33 | 2.33 |
392.85 | 3.11 | 3.11 |
388.43 | 2.47 | 2.47 |
394.38 | 2.74 | 2.74 |
394.38 | 2.74 | 2.74 |