TABLE 1.
Pim1 | GSK3β | TrkA | CLK2 | |
---|---|---|---|---|
(RRu)-3 | 0.7 | 1.0 | 65 | b |
(SRu)-3 | 0.2 | 15 | 40 | b |
(RRu)-1 | 80 | 330 | 20 | c |
(SRu)-1 | 40 | 1000 | 50 | c |
(RRu)-2 | 25 | 1000 | 75 | 30 |
(SRu)-2 | 6 | 370 | 15 | 5 |
(RRu)-21 | 390 | 1200 | 6 | d |
IC50 data were obtained by phosphorylation of substrate peptides with [γ-32P]ATP or [γ-33P]ATP and 100 μM ATP in the presence different concentrations of organometallic kinase inhibitors. Each IC50 value was determined from at least two independent measurements and the average was taken. See experimental section for more details.
Racemic 3: IC50 = 35 nM at 100 μM ATP.
Racemic 1: 26% CLK2 activity at 100 nM 1 and 10 μM ATP.
50% CLK2 activity at 100 nM of (RRu)-21 at 10 μM ATP.