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. 2015 Aug 3;6(9):961–965. doi: 10.1021/ml500526p

Table 1. Key Amide Transformationsa.

graphic file with name ml-2014-00526p_0004.jpg

Cpd R1 B-RAFV600Eb pERK SKMEL-28c SKMEL-28d
2 –CONHMe 0.045 (1) 0.28 (3) 0.90 (3)
3 –NHCOMe 0.003 (1) 0.044 (7) 0.18 (8)
4 2-imidazolyl 0.090 (1) 0.39 (1)  
a

IC50 in μM. Numbers in parentheses represent number of determinations.

b

B-RAFV600E enzymatic assay.6,7 Assay variability within 2-fold of the mean value of the control.

c

pERK SKMEL target modulation.5,9 Assay variability within 3-fold of mean value for applicable entries.

d

SKMEL-28 cell proliferation assay.5,9 Assay variability within 3-fold of mean value.