Assay Report Card

Basic Information

ID: ALA3706377

Type: Binding

Description: In Vitro Assay: The in vitro affinity of the compounds of the present invention for the CXCR1 and CXCR2 receptors was determined on a functional test of the .beta.-arrestin recruitment type after receptor activation.It was demonstrated that the activation by CXCL8 of the CXCR2 receptor in cells of the PathHunter HEK293-CXCR2 line or of the CXCR1 receptor in cells of the U2OS h CXCR1 .beta.-arrestin line results in the recruitment of .beta.-arrestin (Richardson et al. 2003 Role of the cytoplasmic tails of CXCR1 and CXCR2 in mediating leukocyte migration, activation, and regulation. J. Immunol. 170: 2904-2911.)In order to evaluate the direct interaction of the CXCR2 or CXCR1 receptor with .beta.-arrestin 2, a .beta.-arrestin 2 recruitment test for CXCR2 or CXCR1 based on of .beta.-galactosidase enzyme complementation (Olson K R, Eglen R M. Beta galactosidase complementation: a cell-based luminescent assay platform for drug discovery. Assay Drug Dev Technol. 2007 February; 5(1); 137-44).

Activity Charts

Bioactivity

Activity Types for Assay ALA3706377

IC50

Total(37)

Compound Summary

Parent Molecular Weight	ALogP	Polar Surface Area
457.46	2.47	2.47
453.50	2.91	2.91
481.51	2.03	2.03
481.51	2.03	2.03
565.62	3.77	3.77
523.54	2.60	2.60
523.54	2.60	2.60
412.44	2.88	2.88
438.48	3.66	3.66
465.51	3.06	3.06
481.51	2.30	2.30
383.40	1.82	1.82
369.38	2.22	2.22
475.52	2.07	2.07
509.97	2.73	2.73
445.50	2.59	2.59
453.50	2.83	2.83
465.51	2.63	2.63
465.51	2.63	2.63
479.49	2.35	2.35
465.51	2.32	2.32
523.54	2.60	2.60
441.51	2.68	2.68
455.54	2.99	2.99
425.44	2.22	2.22
439.47	2.52	2.52
467.52	3.34	3.34
399.40	2.23	2.23
403.82	2.87	2.87
393.40	2.69	2.69
507.47	3.46	3.46
439.47	2.52	2.52
453.50	2.91	2.91
473.91	3.18	3.18
565.05	2.41	2.41
439.47	2.52	2.52