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. Author manuscript; available in PMC: 2022 Nov 23.
Published in final edited form as: J Med Chem. 2022 Jan 10;65(3):2342–2360. doi: 10.1021/acs.jmedchem.1c01779

Table 4.

IC50 Values of Pyrrolidinyl Analogues 19–22 against BRD4 D1 by Fluorescence Anisotropy

graphic file with name nihms-1848605-t0011.jpg
compd stereocenter R3 BRD4 D1 IC50 by FA (μM)a
(+)-JQ1 <0.092b
19 S H 1.1 ± 0.1
20 S (CH2)2NH2 0.10 ± 0.01
21 R H 1.9 ± 0.1
22 R (CH2)2NH2 0.26 ± 0.01
a

Data represents the mean and standard deviation of three experimental replicates.

b

IC50 is less than half the concentration of bound BRD4 D1 used.