Table 4. Selected SARs from the P1 Group Library^a.

					PKa % inhibition
compd	R1	R2	R3	R4	1000 nM	100 nM	PKa IC50 (nM)	LE
7a	H	H	H	H	29	0	n.d.
7b	F	H	H	H	59	13	n.d.
7c	Cl	H	H	H	67	12	n.d.
7d	CH3	H	H	H	62	12	n.d.
7e	OCH3	H	H	H	63	11	n.d.
7f	H	Cl	H	H	74	20	n.d.
7g	H	CH3	H	H	57	11	n.d.
7h	H	OCH3	H	H	83	35	90	0.31
7i	H	H	Cl	H	60	13	n.d.
7j	H	H	CH3	H	84	36	88	0.32
7k	H	H	OCH3	H	72	17	n.d.
7l	F	H	H	F	88	47	62	0.32
7m	F	H	H	Cl	92	61	31	0.33
7n	F	H	H	CF3	97	83	7.8	0.32
7o	Cl	H	H	Cl	94	56	40	0.32
7p	CH3	H	H	CH3	89	53	68	0.31

^an.d., not determined.