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. Author manuscript; available in PMC: 2016 Feb 1.
Published in final edited form as: Medchemcomm. 2014 Aug 11;5(10):1507–1514. doi: 10.1039/C4MD00251B

Table 2.

TrkA activity for compounds 36–38 generated from Scheme 2

graphic file with name nihms739090u2.jpg
Compound R1 (A-region) R2 (B-region) %TrkA inhibition,a 20 μM TrkA IC50b (μM)
38 –Cl 5-(tert-Butyl)isoxazol-3-amine 41.4 ± 3.3 —
39 4-1-Methyl-1H-pyrazole 5-(tert-Butyl)isoxazol-3-amine 96.1 ± 2.3 0.005 ± 0.012
40 4-1-Methyl-1H-pyrazole 3-(tert-Butyl)-1-methyl-1H-pyrazol-5-amine 99.7 ± 0.8 0.012 ± 0.005
a

The amount of activity at a 20 μM concentration of inhibitor: 100 is complete inhibition, 0 is complete activity. Completed in quadruplicate.

b

IC50 is the concentration of the inhibitor to block the enzyme activity by half. Completed in duplicate, reported value represents the average. Error is reported as the standard deviation of the average. [ATP] 190 μM.