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Figure 2.
(a) Experimental strategy for the discovery of dual
inhibitors, and IC[50] values (  M)
for 8 molecules tested against 14 tyrosine kinases and PI(3)Ks
(10 M
ATP). IC[50] values less than 0.1 M
are shaded red. Pyrazolopyrimidine N4 and N5, which make
hydrogen bonds to the kinase, are labeled. (b) Percentage
inhibition of 84 tyrosine kinases (right) and 135
serine-threonine kinases (left) by 7 inhibitors from this study
(right columns) and 5 reference compounds (left columns). PP
inhibitors were tested at 1 M
drug and, typically, 10 M
ATP. Data from the Invitrogen SelectScreen assay. (c) Principal
component analysis of the target selectivity of 172
pyrazolopyrimidine inhibitors and 8 reference compounds. Key
compounds are labeled.
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