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. Author manuscript; available in PMC: 2015 Mar 4.
Published in final edited form as: Bioorg Med Chem. 2013 Nov 14;22(1):478–487. doi: 10.1016/j.bmc.2013.11.003

Table 1.

Binding Affinities of Analogs to Recombinant Ezrin: Heterocyclic-diones

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ID NSC668394 18a 19a 20a 22a
R graphic file with name nihms541385t1.jpg graphic file with name nihms541385t2.jpg graphic file with name nihms541385t3.jpg graphic file with name nihms541385t4.jpg graphic file with name nihms541385t5.jpg
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a KD (μ M) 10.6 ±2.9 Agg 40.1 ±16.3 Agg NBb
Kon (M−1s−1) 289.24±92.08 - 84.9 ±1.4 - -
Koff (s−1) 0.00293 ± 0.0005 - 0.00328 ± 0.00133 - -
cLogP 3.96 5.01 3.96 3.05 3.40
a

Binding affinities determined by surface plasmon resonance spectrometry (BIACORE). Kinetics experiments were run in triplicate unless noted. In each kinetics experiment, compound was injected in triplicate at 7 different concentrations, ranging from 0 to 50 μ M. Mean KD values and standard deviations were calculated from three independent experiments for each compound.

b

NB= no binding.

c

Agg= aggregate formed during binding study.