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. Author manuscript; available in PMC: 2021 Oct 22.
Published in final edited form as: J Med Chem. 2020 Oct 15;63(20):11522–11547. doi: 10.1021/acs.jmedchem.0c00531

Table 6.

Quantitative Determination of Protein:ligand Binding of Compound 2 Analogs to FGF14 and Nav1.6 by SPR.

Compound FGF14 Nav1.6 C-terminal tail
KD*
(μM)
kon
(M−1 s−1)
koff
(s−1)
KD*
(μM)
kon
(M−1 s−1)
koff
(s−1)
19k ND ND ND > 200 2.57 × 105 4.49 × 10−3
19e 188.9 ± 3.7 4.61 × 102 9.91 × 10−4 ND ND ND
21a 4.05 ± 0.17 4.66 × 103 9.33 × 10−3 16.43 ± 2.05 6.23 × 104 3.57 × 10−3
23a 1.31 ± 0.37 1.79 × 104 9.32 × 10−3 > 200 6.16 × 106 2.73 × 10−3
23b 14.72 ± 1.40 2.58 × 104 2.69 × 10−7 > 200 1.26 × 105 1.45 × 10−3
23d 6.94 ± 1.08 1.62 × 103 5.80 × 10−3 > 200 8.29 × 105 7.94 × 10−3
23e 7.02 ± 1.20 7.35 × 103 1.39 × 10−2 > 200 7.16 × 105 1.70 × 10−4
23f 9.47 ± 1.22 2.17 × 102 2.05 × 10−2 67.34 ± 7.3 2.64 × 103 1.22 × 10−2
23g 11.39 ± 2.15 2.89 × 102 2.04 × 10−2 90.14 ± 10.1 3.40 × 102 4.92 × 10−2
*

The equilibrium dissociation constants (KD) were calculated using data represented in Figure 6. The KD shown for each protein:ligand interaction is an average of the values calculated using the simplest Langmuir 1:1 interaction model (KD = koff/kon) and the steady-state saturation model. ND, non-determinable.