Table 3.

Structure and Activities of Analogs 22^a

Compound	R	PAR4-AP PAC-1 IC50 (μM)b (pIC50±SEM)	PAR4-AP % Max PAC-1a	PARI %Maxc
7		0.18 (6.74±0.06)	0.32	98
22a		0.32 (6.49±0.03)	0.66	84
22b		2.4 (5.61±0.13)	5.1	80
22c		0.16 (6.79±0.04)	−1.2	92
22d		0.63 (6.2±0.09)	1.3	81
22e		2.1 (5.67±0.10)	11	90
		(5.67±0.10)
22f		0.24 (6.61±0.05)	0.32	92
22g		1.3 (5.88±0.13)	4.2	85
22h		1.2 (5.92±0.11)	2.84	76

^aValues indicate the percentage of max PAC-1 binding after PAR4-AP stimulation of human platelets.

^bAverage of three independent determinations.

^cValues indicate the percentage PAR1 activity in the presence of 10 μM compound.