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. Author manuscript; available in PMC: 2020 Oct 23.
Published in final edited form as: J Med Chem. 2018 Jul 9;61(14):6350–6363. doi: 10.1021/acs.jmedchem.8b00810

Table 4.

Relative binding affinities and selectivity for XIAP BIR3 targeting covalent agents.

N-Me-Ala-P2-P3/P4
XIAP cIAP1 cIAP2
Compd Structure IC50 (nM) IC50 (nM) Selectivity cIAP1/XIAP IC50 (nM) Selectivity cIAP2/XIAP
32 graphic file with name nihms-1636520-t0013.jpg 11.3 ± 0.8 181.0 ± 20.1 16.0 304.0 ± 60.2 27.0
33 graphic file with name nihms-1636520-t0014.jpg 47.3 ± 3.3 264.1 ± 35.5 5.6 212.1 ± 8.9 4.5
34 graphic file with name nihms-1636520-t0015.jpg 16.6 ± 2.1 >200 >12.0 353.3 ± 118.2 17.6
34* graphic file with name nihms-1636520-t0016.jpg 189.4 ± 1.3 >1000 >5.3 >1000 >5.3

IC50 values with respective standard errors for the ability of test agents to displace a reference AVPI peptide from the BIR3 domains of XIAP, cIAP1, and cIAP2, were obtained with a DELFIA assay. Selectivity was calculated as the ratio of cIAP1 or cIAP2 IC50 values versus IC50 values for XIAP.