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. Author manuscript; available in PMC: 2018 Feb 15.
Published in final edited form as: Eur J Med Chem. 2016 Oct 27;127:793–809. doi: 10.1016/j.ejmech.2016.10.059

Table 1.

Inhibition constants for SAP inhibitors.

Compound Construct Inhibition constant
Ki(nM)a
2 PDpDIApGpPD 3.3 ± 0.2
3 GpDIApGpPD 10.5 ± 0.9
4 GpDIApGpA 6.1 ± 0.3
23 DIApGpPD 10,700 ± 800
25 PDpGpDIApGpPD 7.4 ± 0.4
30 DIApG 21,300 ± 800
32 GpDIApG 33.0 ± 1.7
33 PDpDIApG 19.3 ± 1.7
39 PDpGpDIApPD 188 ± 12
41 GpGpDIApPD 212 ± 17
45 PDpDEIApGpPD 12.4 ± 0.9
52 PDpHomoSerpGpPD 26.8 ± 0.3
PDpSerpGpPD 43.2 ± 1.1b
PDpApGpPD (substrate analogue) 16,000 ± 1500
a

Ki is the dissociation constant Kd for the inhibitor interactions with SAP following slow–onset inhibition.

b

Values taken from Schramm et al. [19].