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. Author manuscript; available in PMC: 2014 Oct 17.
Published in final edited form as: ACS Chem Biol. 2013 Apr 16;8(6):1344–1351. doi: 10.1021/cb300674x

Table 2. Comparison of the inhibition of NaV1.3 by μ-BuIIIB and N-terminal analogsa.

Peptide kon
(μM•min)-1
koff
(min1)
Kd
(μM)
μ-BuIIIB 0.085 ± 0.01 0.017 ± 0.007 0.2 ± 0.086
[Ala1]BuIIIB 0.014 ± 0.004 0.01 ± 0.003 0.71 ± 0.3
[d-Ala2]BuIIIB 0.83 ± 0.05 0.004 ± 0.0017 0.0048 ± 0.002
[Ala2]BuIIIB 0.25 ± 0.03 0.009 ± 0.002 0.036 ± 0.009
[Ala3]BuIIIB 0.46 ± 0.03 0.007 ± 0.0013 0.015 ± 0.003
[Ala4]BuIIIB 0.056 ± 0.008 0.01 ± 0.002 0.18 ± 0.044
[des1-4]BuIIIB 0.47 ± 0.06 0.025 ± 0.005 0.053 ± 0.013
a

Rate constants were determined as described in Methods. Kd was determined from koff/kon. Data for μ-BuIIIB are from Wilson et al.(20)