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. Author manuscript; available in PMC: 2010 Dec 7.
Published in final edited form as: J Org Chem. 2009 Dec 4;74(23):8997–9009. doi: 10.1021/jo901641k

TABLE 1.

IC50 values of imide and lactam half-sandwich complexes 1–3 and (RRu)-21 against Pim1, GSK3β, TrkA, and CLK2.a

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
a

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.

b

Racemic 3: IC50 = 35 nM at 100 μM ATP.

c

Racemic 1: 26% CLK2 activity at 100 nM 1 and 10 μM ATP.

d

50% CLK2 activity at 100 nM of (RRu)-21 at 10 μM ATP.