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. Author manuscript; available in PMC: 2014 Jul 15.
Published in final edited form as: Bioorg Med Chem Lett. 2013 May 14;23(14):4253–4257. doi: 10.1016/j.bmcl.2013.04.096

Table 3.

Binding affinities to BIR2 or BIR3 domains of XIAP for tripeptide analogues 2b and 8q–8y.

graphic file with name nihms482181t3.jpg
Cmpds. R R1 P3 R4 BIR2 Ki, μMa BIR3 Ki, μMa BIR2 vs BIR3 Selectivity
2b CH3 CH3 Pro 1-naphthyl 0.44 (± 0.02) 1.51 (± 0.13) 3.4 : 1
8q CH3 CH3 Ala 1-naphthyl 1.74 (± 0.30) > 39 > 22.4 : 1
8r CH3 CH3 Val 1-naphthyl 4.54 (± 0.23) > 39 > 8.6 : 1
8s CH3 CH3 OrnCBZ 1-naphthyl 1.94 (± 0.11) > 39 > 20.1 : 1
8t H CH3 Ala 1-naphthyl 0.64 (± 0.01) 40.15 (± 2.69) 62.7 : 1
8u H CH2OH Ala 1-naphthyl 2.43 (± 0.25) > 39 > 16 : 1
8v H CH2CH3 Ala 1-naphthyl 3.78 (± 0.37) > 39 > 10.3 : 1
8w CH3 CH3 Ala CH2-1-naphthyl 3.00 (± 0.40) 34.18 (± 2.15) 11.4 : 1
8x H CH3 Ala NHPh 1.83 (± 0.19) 41.32 (± 0.86) 22.6 : 1
8y CH3 CH3 Val NH-3-FPh 2.38 (± 0.28) > 39 > 16.4 : 1
a

Values are determined in duplicate and reported ± standard deviation which is given in parentheses.