Table 1. Inhibition of PKBβ and PKA by Substituted 4-Benzyl-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amines.

no.	Rn	PKBβ IC50 (nM)a	PKA IC50 (nM)b	selectivity for PKB against PKA (fold)c
2	4-Cl	6.0 (±1.5)d	168 (±36)d	28
3	3-Cl	46	280	6
4	2-Cl	44 (±35)e	2150 (1700, 2600)f	49
5	4-OCF3	35 (19, 50)f	660	19
6	3-OCF3	19	600	32
7	2-OCF3	84	2800	33
8	3-OMe	15	720	48
9	2-OMe	>1000	ndg	ndg
10	4-tBu	27 (±18)h	3400 (3200, 3600)f	126
11	2,3-Cl2	35	520	15
12	2,4-Cl2	8.5 (7, 10)f	1300 (1300, 1300)f	153
13	2,5-Cl2	16	770	48
14	2,6-Cl2	20	3300	165
15	3,4-Cl2	18 (9, 26)f	>300	>16
16	2-Cl, 4-F	90	1200	13
17		25	ndg	ndg
18		7.0	490	70

^aInhibition of PKBβ kinase activity in a radiometric filter binding assay,(17) single determination. Standard inhibitor N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinoline sulfonamide (H-89) gave mean IC₅₀ (±SD) = 590 (±220) nM (n = 20).

^bInhibition of PKA kinase activity in a radiometric filter binding assay,(16) single determination. Standard inhibitor N-(2-methylaminoethyl)-5-isoquinoline sulfonamide (H-8) gave mean IC₅₀ (±SD) = 5300 (±2010) nM (n = 14).

^cRatio of IC₅₀ values (PKA/PKB).

^dMean (±SD), n = 3 determinations.

^eMean (±SD), n = 4 determinations.

^fMean of two determinations, individual values in parentheses.

^gnd = not determined.

^hMean (±SD), n = 5 determinations.