Table 5.

SAR of C-6 phenyl group.

Compound	R1	R2	R3	KD (nM)
				BasE	MbtA
15	H	H	H	36.1 ± 4.9	(3.74 ± 0.41)•103
37	Me	H	H	(2.15 ± 0.11)•103	>100•103
38	H	Me	H	158 ± 24	(7.40 ± 0.90)•103
39	H	H	Me	212 ± 22	(1.44 ± 0.15)•103
40	OH	H	H	255 ± 36	(6.50 ± 0.90)•103
41	H	OH	H	124 ± 17	(7.67 ± 1.15)•103
42	H	H	OH	8.85 ± 3.16	(3.70 ± 0.50)•103
43	H	H	CH2OH	247 ± 33	(3.70 ± 0.60)•103
44	Cl	H	H	(2.48 ± 0.19)•103	>100•103
45	H	Cl	H	≤ 2.0	(4.60 ± 0.50)•103
46	H	H	Cl	153 ± 21	953 ± 90
47	H	H	Br	20.6 ± 7.0	560 ± 28
48	H	H	F	28 ± 4.7	(1.89 ± 0.21)•103
49	F	H	F	42.6 ± 8.3	(8.00 ± 0.90)•103
50	H	H	CF3	191 ± 27	887 ± 96
51	H	H	NO2	3.91 ± 2.27	202 ± 38
52	H	H	NH2	78.2 ± 13.2	(4.08 ± 0.63)•103
53	H	H	N(Me)2	628 ± 98	(1.70 ± 0.30)•103
54	H	H	NH(C=O)Me	747 ± 65	(4.20 ± 0.80)•103
55	H	H	SO2Me	13.0 ± 6.1	130 ± 23
56	H	H	CN	22.7 ± 6.2	380 ± 46
57	H	H	C(=O)NH2	288 ± 45	(1.00 ± 0.30)•103
58	H	H	COOH	776 ± 119	(6.10 ± 0.80)•103
59	H	OMe	COOH	(1.70 ± 0.15)•103	(49.9 ± 3.7)•103
60	H	OH	COOH	169 ± 13.4	495 ± 34
61	H	H	SMe	23.5 ± 5.5	178 ± 15
62	H	H	OMe	78.2 ± 13.2	(3.23 ± 0.38)•103
63	H	H	O(CH2)7CH3	191 ± 13	>50•103
64	H	H	O(CH2)11CH3	(28.4 ± 3.9)•103	>50•103
65	H	H	O(CH2)15CH3	-	-
66	H	H	OPh	32.5 ± 6.3	187 ± 28
67	H	H	OCH2Ph	2.14 ± 1.46	(5.40 ± 0.90)•103
68	H	H	OCH2(p-PhOMe)	44.5 ± 7.7	(5.80 ± 0.90)•103
69	H	H	C(=O)Me	104 ± 11	134 ± 22
70	H	H	C(=O)Ph	19.1 ± 4.9	19.1 ± 2.4
71	H	Ph	H	164 ± 20	(3.60 ± 0.38)•103
72	H	H	Ph	125 ± 9	(3.50 ± 0.30)•103
73	H	H	p-PhBr	181 ± 39	(19.7 ± 0.9)•103
74	o-PhCl	H	H	(19.7 ± 0.9)•103	>50•103