Table 3.

Inactivation rate constants (kt) of control compounds (1-4, 8e, 9) and carboxamides 14a-p, 17g-21g for rAgAChE (WT and G119S) and rhAChE (h)

Compound	R	WT ki (mM−1 min−1)b	G119S ki (mM−1 min−1)b	h ki (mM−1 min−1)b	WT/G119S SRc
1d	NA	266 ± 9	±0.037±0.007	17.0 ± 0.4	7,200 ± 1,400
2d	NA	839 ± 22	±0.055 ± 0.007	111 ± 5	15,000 ± 2,000
3d	NA	2,620 ± 150	±0.044 ± 0.020	428 ± 12	60,000 ± 27,000
4d	NA	1,510 ± 100	0.40 ± 0.03	126 ± 3	3,800 ± 400
8ed	NA	9,140 ± 260	290 ± 7	805 ± 36	32 ± 1
9d	NA	13.3 ± 0.3	3.15± 0.08	6.5 ± 0.3	4.2 ± 0.1
14a	Me	0.46 ± 0.04	0.098 ± 0.029	1.22 ± 0.04	4.7 ± 1.4
14b	c-Pr	50.5 ± 1.4	0.20 ± 0.03	103 ± 5	250 ± 30
14c	i-Pr	500 ± 10	1.85 ± 0.09	561 ± 21	270 ± 10
14d	c-Bu	293 ± 9	0.62 ± 0.05	233 ± 13	480 ± 40
14e	s-Bu	2,290 ± 80	10.6 ± 0.5	2,170 ± 40	220 ± 10
14f	c-C5H11	1,020 ± 50	2.58 ± 0.22	677 ± 26	400 ± 40
14g	2-pentyl	5,240 ± 140	14.7 ± 0.3	3,110 ± 120	360 ± 10
14h	3-pentyl	8,530 ± 420	22.5 ± 1.1	1,990 ± 70	380 ± 30
14j	i-Bu	252 ± 4	0.55 ± 0.02	30.9 ± 2.6	450 ± 20
14k	2-methylbutyl	477 ± 7	0.99 ± 0.05	112 ± 5	480 ± 20
141	neo-pentyl	161 ± 12	0.37 ± 0.06	26.2 ± 1.1	440 ± 80
14m	3-methylbutyl	266 ± 9	0.40 ± 0.12	80.9 ± 2.0	670 ± 200
14n	CH2CH2-c-Pr	420 ± 15	1.07 ± 0.06	144 ± 7	390 ± 30
14o	CH2CH2-c-Bu	141 ± 4	0.31 ± 0.09	74.5 ± 4.4	460 ± 130
14p	CH2CH2-c-C5H9	24.3 ± 0.1	0.41 ± 0.27	92.0 ± 4.0	60 ± 4.1
17g	2-pentyl	2,240 ± 80	36.7 ± 2.7	1,860 ± 40	61 ± 5
18g	2-pentyl	156 ± 6	3.84 ± 0.20	1,080 ± 50	41 ± 3
19g	2-pentyl	7.30 ± 0.09c	1.24 ± 0.05	180 ± 3c	5.9 ± 0.3
20g	2-pentyl	134 ± 8	1.90 ± 0.11	379 ± 24	71 ± 6
21g	2-pentyl	39.0 ± 2.1	2.15 ± 0.27	26.0 ± 0.3	18 ± 3

^a NA signifies not applicable.

^bMeasured at 23 ± 1°C, pH 7.7, 0.1% (v/v) DMSO. Recombinant sources of AgAChE are rAgAChE-WT and rAgAChE-G119S.

^cEnzymatic sensitivity ratio is calculated as k_i(WT)/k_i(G119S). Standard error in the ratio is calculated according to a standard propagation of error formula.²⁰

^dData reported previously.¹²