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. 2015 Feb 20;54(16):4758–4763. doi: 10.1002/anie.201410672

Table 1.

Structures and activities of inhibitors against STAT5b and STAT5a.

Compounds Ki [μm] (STAT5b) Ki [μm] (STAT5a) Selec- tivity factor
1 Inline graphic 0.93± 0.07 34±3 37
2 Inline graphic 27±4 24±3 0.9
3 Inline graphic n.a. n.a. n.a.
4 Inline graphic 0.69± 0.04 19.2± 2.7 28
5 Inline graphic 0.82± 0.05 2.5± 0.2 3
6 Inline graphic 0.73± 0.07 21±5 30
7 Inline graphic 0.45± 0.04 16.0± 0.8 35
8 Inline graphic 0.46± 0.08 7.8± 1.0 17
9 Inline graphic 0.21± 0.04 11±2 52
10 Inline graphic n.a. n.a. n.a.
11 Inline graphic 0.24± 0.01 16.1± 1.1 67
12 Inline graphic 0.28± 0.02 9.3± 0.3 33
13 Inline graphic 0.044± 0.001 2.42± 0.05 55
14 Inline graphic n.a. n.a. n.a.
15 Inline graphic 50±3 40±2 0.80
16 QDTpYLVLDKWL 0.54± 0.08 0.41± 0.09 0.75

The selectivity factor was calculated as Ki (STAT5a)/Ki (STAT5b). Conversion of IC50 values into Ki values was carried out as described.[15] n.a.=not applicable.