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. Author manuscript; available in PMC: 2019 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2017 Nov 4;26(1):25–36. doi: 10.1016/j.bmc.2017.10.042

Table 2.

TR-FRET competitive binding data for exemplar BETi and THQ analogs 9–14.

graphic file with name nihms922571u1.jpg
Comp. R TR-FRET, IC50 [μM]*
BRD2-BD1 BRD2-BD2 Selectivity [BD1/BD2]
1 -- 0.37 (0.26 – 0.52) 0.17 (0.11 – 0.28) 2.1
4 -- 0.72 (0.39 – 1.33) 0.03 (0.01 – 0.08) 21.3
9 2-furan 2.02 (1.18 – 3.44) 0.61 (0.46 – 0.81) 3.3
10 2-thiophene 1.77 (1.42 – 2.20) 0.83 (0.61 – 1.15) 2.1
11 2-pyrrole 1.40 (0.85 – 2.31) 1.40 (0.52 – 3.81) 1.0
12 3-furan 5.80 (3.46 – 9.74) 1.91 (1.24 – 2.94) 3.0
13 3-thiophene 5.21 (2.72 – 9.96) 1.08 (0.92 – 1.28) 4.8
14 3-pyrrole 2.48 (1.38 – 4.45) 0.41 (0.23 – 0.74) 6.0
*

Average of 3–9 replicates per compound. 95% confidence interval reported in parenthesis.