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. Author manuscript; available in PMC: 2020 Jan 31.
Published in final edited form as: J Med Chem. 2017 May 2;60(9):3887–3901. doi: 10.1021/acs.jmedchem.7b00193

Table 2.

Design of BET inhibitors targeting the WPF binding pocket using five-membered aromatic rings

graphic file with name nihms-1065193-t0003.jpg
Compound BRD4 BD1 BRD4 BD2
IC50 (nM) Ki (nM) IC50 (nM) Ki (nM)
9 2060±420 655±269 1882±406 641±200
10 393±127 131±50 199±81 57.0±17.3
11 155±47 44.3±13.9 180±37 56.4±11.7
12 165±50 51.9±18.6 108±37 30.6±9.0
13 1456±441 456±150 1139±198 335±25
14 102±40 41.2±16.9 164±44 68.7±21.4
15 51.7±15.0 19.7±8.2 63.5±16.4 20.2±9.2
16 40.9±14.2 18.5±4.0 89.7±18.5 31.2±11.8
17 24.1±5.5 7.0±3.3 11.7±2.0 2.7±0.5