Assay Report Card

Basic Information

ID: ALA3888926

Type: Binding

Description: Functional Assay: Chinese Hamster Ovary recombinant cells expressing the human NK-3 receptor and a construct that encodes the photoprotein apoaequorin were used for this assay. The antagonist activity of compounds of the invention is measured following pre-incubation (3 minutes) of the compound (at various concentrations) with the cells, followed by addition of the reference agonist (NKA) at a final concentration equivalent to the EC80 (3 nM) and recording of emitted light (FDSS 6000 Hamamatsu) over the subsequent 90-second period. The intensity of the emitted light is integrated using the reader software. Compound antagonist activity is measured based on the concentration-dependent inhibition of the luminescence response to the addition of Neurokinin A.

Organism: Homo sapiens

Activity Charts

Bioactivity

Activity Types for Assay ALA3888926

IC50

Total(47)

Compound Summary

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