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. 2018 Sep 17;175(20):3891–3910. doi: 10.1111/bph.14458

Table 1.

SPA binding to bead‐associated α4β1 integrin and inhibition of Jurkat E6.1 cell adhesion of the reference compound BIO1211 and hybrid α/β‐peptidesa to VCAM‐1 (2 μg·mL−1) or FN (10 μg·mL−1).

Compound SPA IC50 (nM)b Cell adhesion Jurkat/VCAM‐1 IC50 (nM) Cell adhesion Jurkat/FN IC50 (nM)
BIO1211 8.80 ± 3.4 (0.08–46.7) c 4.60 ± 3.0 (0.05–25.1) 5.50 ± 4.0 (0.09–37.6)
DS‐70 8.3 ± 3.2 (0.1–37.2) 5.04 ± 0.51 (0.05–37.3) 4.3 ± 1.7 (0.04–23.4)
DS‐23 47.7 ± 4.1 (4.6–161.4) 40.3 ± 7.1 (3.4–127.6) 51 ± 5.0 (4.8–192.4)
a

Results were generated by measuring, in a cell‐free SPA, the inhibition of [125I]‐FN binding by the assayed compounds on Jurkat E6.1 cell lysates in the presence of 10 increasing concentrations of each compound (10−12–10−3 M) and a fixed amount of radioligand (100 000 counts per minute).

b

Six independent experiments were run in quadruplicate.

Data are expressed as means ± SD (with c95% confidence limits).