Integrin selectivity data for BIO5192
The selectivity of BIO5192 toward the five integrins indicated were tested in adhesion formats for α2β1 and α9β1 by direct binding for α4β1 and α4β7, and by platelet aggregation for αIIBβ3, as described under Materials and Methods. For all assay formats, serial dilutions of each compound (from 1 nM to 100 μM) were evaluated and IC50 values were calculated from the concentration dependence of the inhibition curves.
Integrin | IC50 (n) |
|---|---|
| nM | |
| α4β1a | 1.8 ± 0.7 (10) |
| α4β7 | >500 (1) |
| α9β1 | 138 (2) |
| α2β1 | 1,053 ± 143 (3) |
| αIIbβ3 | >10,000 (1) |
↵ a Due to the high affinity of BIO5192 for α4β1, its binding constants were also calculated from kinetic measurements (KD = <10 pM)