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. Author manuscript; available in PMC: 2016 Jun 1.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Apr 23;25(11):2280–2284. doi: 10.1016/j.bmcl.2015.04.041

Table 2.

Comparison of compounds 5 and 6.

compound RBL cell line IC50 (nM) a CXCR2 PathHunter
cell line (nM) b 		Microsome stability
(% remaining @ 60 min)		 Rat PK AUC
(μmol-hr/L)
CXCR1 c CXCR2 c IC50 β-arrestin c rat monkey IV Oral
5 903 ± 361 356 ± 219 730 ± 72 37 25 0.39 <LLOQ
6 31 ± 4 21 ± 6 130 ± 6 92 95 5.40 <LLOQ
a

Experiments performed in triplicate, reported as mean ± SE;

b

Experiments performed in quadruplicate, reported as mean ± SE;

c

IL8 used as agonist.