Table 1.

Compound 2–8 and 14–27 IC₅₀ (μM) for ChTS

Compounds	R1	R2	R3	R4	R5	ChTS IC50 (μM)	ClogP
2	COO−	H	H	H	H	20 ± 12	2.63
3	H	COO−	H	H	H	96 ± 10	2.47
4	H	H	COO−	H	H	>100	2.49
5	CH2COO−	H	H	H	H	16 ± 1	1.96
6	(CH2)2COO−	H	H	H	H	114 ± 21	2.48
7	Tetrazole	H	H	H	H	159 ± 19	1.96
8	CN	H	H	H	H	123 ± 7	2.29
14	COO−	H	H	Cl	H	28 ± 6	3.28
15	COO−	H	H	COO−	H	18 ± 2	2.51
16	COO−	H	H	OCH3	H	50 ± 8	2.66
17	COO−	H	H	CN	H	11 ± 1	2.36
18	COO−	H	H	CH2OH	H	181 ± 32	1.94
19	COO−	H	H	CH2OCH3	H	68 ± 12	2.56
20	COO−	H	H	CONH2	H	20 ± 4	1.42
21	COO−	H	H	H	CH2OCH3	>100	1.60
22	COO−	H	OCH3	H	H	222 ± 77	2.66
23	CH2COO−	H	H	OCH3	H	11 ± 1	1.99
24	CH2COO−	H	H	CN	H	9.1 ± 0.7	1.69
25	CH2COO−	H	H	COO−	H	10 ± 1	1.85
26	O(CH2)2OCH3	OCH3	~ ~	~ ~	~ ~	97 ± 44	3.42
27	COO−	OCH3	~ ~	~ ~	~ ~	>500	3.38