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. Author manuscript; available in PMC: 2019 Jul 26.
Published in final edited form as: J Med Chem. 2018 Jul 17;61(14):6110–6120. doi: 10.1021/acs.jmedchem.8b00483

Table 2:

Optimization of 9 with N-pyrazole type substitutions

graphic file with name nihms-1020002-t0010.jpg
ID BRD4 BD1
IC50 (nM)a Ki (nM)
24 9.4±0.6 0.8±0.2
25 15.8±0.4 3.1±0.1
26 6.1±0.1 <1
27 10.5±1.2 1.2±0.4
28 (CF53) 2.0±0.3 <1
29 12.8±2.1 2.0±0.7
30 13.8±0.6 2.4±0.2
31 16.8±2.5 3.4±0.8
32 6.1±0.2 0.5±0.1
33 4.4±0.4 <1
34 14.3±2.5 2.6±0.9
35 4.0±0.2 <1
36 24.9±1.8 6.3±0.6
37 51.7±7.9 15.8±2.8
38 5.5±1.0 <1
39 4.9±0.5 <1
40 5.0±0.3 <1
a

Mean of three experiments