Table 1

Summary of properties of compounds structurally related to AR-R15896AR

AR-R	Structure		[IC₈₀] (μM) % B	% B_T	τ₂ on (s)	τ₁ on (s)	τ_off (s)
AR-R		FW (g)	[IC₈₀] (μM) % B	% B_T	τ₂ on (s)	τ₁ on (s)	τ_off (s)
Low-trapping compounds^1-a
15808 See Fig. 2(Upper)		150	8 ± 3 (8)	0.2 ± 0.0	5.8 ± 0.6	See text
	277.2	84 ± 2 (22)	See text	89 ± 1%

26952		150	40 ± 5 (6)	0.5 ± 0.3	4.9 ± 0.5	6.9 ± 1.0
	311.3	80 ± 2 (12)		70 ± 4%	High-trapping compounds^1-b
16442		20	70 ± 4 (7)	1.1 ± 0.1	5.1 ± 0.2	10.6 ± 2.2
	352.30	86 ± 2 (12)		48 ± 2%
15278		50	72 ± 2 (6)	1.0 ± 0.1	7.0 ± 1.2	7.5 ± 3.6
	281.85	86 ± 2 (8)		52 ± 8%
12859^1-c		10	72 ± 3 (6)	1.2 ± 0.2	8.0 ± 1.5	7.1 ± 1.8
	332.36	84 ± 1 (11)		49 ± 8%
15824^1-c		50	76 ± 3 (5)	1.9 ± 0.3	13.9 ± 2.3	10.5 ± 2.1
	321.98	81 ± 2 (9)		49 ± 4%
16283		50	76 ± 4 (6)	0.5 ± 0.1	2.9 ± 0.2	3.7 ± 0.6
	264.67	84 ± 1 (10)		51 ± 5%
15232		10	77 ± 5 (6)	1.3 ± 0.1	5.9 ± 0.9	10 ± 0.8
	233.74	85 ± 2 (15)		61 ± 3%
15545^1-c		100	78 ± 2 (5)	3.5 ± 0.3	18.8 ± 3.0	13.3 ± 1.1
	263.4	82 ± 2 (11)		60 ± 8%
15832		20	78 ± 6 (3)	1.3 ± 0.2	11.5 ± 0.2	15.4 ± 1.4
	339.31	76 ± 3 (6)		35 ± 6%
18526		20	80 ± 3 (8)	0.8 ± 0.1	6.4 ± 0.3	10.7 ± 1.3
	266.78	81 ± 1 (13)		49 ± 2%
15366		20	81 ± 2 (6)	1.8 ± 0.1	8.1 ± 0.1	23.8 ± 0.5
	319.3	89 ± 1 (8)		54 ± 2%
15859^1-c		20	82 ± 2 (6)	0.9 ± 0.1	7.2 ± 0.8	8.6 ± 2.4
	285.22	83 ± 2 (12)		41 ± 3%
15514^1-c		10	84 ± 3 (5)	2.4 ± 0.3	10.9 ± 1.1	45.5 ± 0.6
	253.8	84 ± 4 (10)		32 ± 6%
15844^1-c See Fig. 2(Lower)		20	84 ± 2 (8)	NA	5.3 ± 0.2	21.7 ± 1.2
	259.77	83 ± 1 (14)
15492^1-c		200	92 ± 3 (4)	2.3 ± 0.5	12.4 ± 0.2^1-e	63 ± 13
	395.5	85 ± 3 (6)		16 ± 6%
15793^1-c		20	93 ± 3 (8)	1.1 ± 0.1	7.6 ± 0.6	20.8 ± 5.3
	310.39	86 ± 1 (13)		39 ± 2%
Intermediate-trapping compounds^1-d
15896		50	54 ± 3 (9)	NA	2.4 ± 0.6	2.8 ± 0.9
	271.2	81 ± 1 (9)
15336 See Fig. 2(Middle)		100	57 ± 6 (5)	0.5 ± 0.2	4.9 ± 0.6	6.6 ± 1.1
	282.39	85 ± 3 (6)		65 ± 7%
15006		30	60 ± 4 (10)	1.2 ± 0.1	7.2 ± 0.6	15.0 ± 0.7
	444.44	83 ± 1 (15)		56 ± 2%
15614^1-c		10	60 ± 5 (5)	0.8 ± 0.1	7.8 ± 0.9	13.4 ± 0.5
	293.86	80 ± 1 (8)		56 ± 1%
15209		10	61 ± 4 (5)	0.6 ± 0.1	7.5 ± 0.6	13.1 ± 6.6
	259.78	83 ± 1 (7)		52 ± 2%
15870^1-c		10	62 ± 7 (5)	2.3 ± 0.2	11.0 ± 0.9	13.3 ± 3.3
	291.03	82 ± 1 (9)		55 ± 4%
15688		50	68 ± 3 (6)	0.5 ± 0.1	3.8 ± 0.8	3.0 ± 1.2
	450.56	82 ± 2 (11)		65 ± 3%

FW, formula weight; B_T , block trapped; NA, not applicable
↵1-a Significantly less trapping block than AR-R15896AR.
↵1-b Significantly more trapping block than AR-R15896AR.
↵1-c Fully saturated α-carbon.
↵1-d Not significantly different trapping block than AR-R15896AR.
↵1-e Not steady-state at 30 s.