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. 2021 Apr 8;12(5):836–845. doi: 10.1021/acsmedchemlett.1c00113

Table 2. CXCR1/2 Antagonistic Activity for Compounds B1B10.

graphic file with name ml1c00113_0009.jpg

  R1 CXCR1 IC50 (μM)a CXCR2 IC50 (μM)a ratiob
2 Ph 4.7 0.006 778
B1 H >100 29.7 3
B2 4-Cl-Ph 38.1 0.915 42
B3 3-Cl-Ph 47.8 0.305 157
B4 2-Cl-Ph 21.7 0.054 402
B5 4-F-Ph ∼100 2.19 ∼46
B6 methyl >100 0.269 >372
B7 ethyl ∼100 0.140 ∼714
B8 propyl 14.7 0.068 216
B9 n-butyl 54.6 0.043 1270
B10 isobutyl 41.8 0.305 137
SCH527123   0.16 0.01 16
a

The IC50 values are an average of triplicate determinations.

b

Ratio = CXCR1 IC50/CXCR2 IC50.