Table 2.

In vitro metabolic stability and in vivo mouse efficacy of selected compounds.^a

Compound	Clint (µL/min/mg protein)		Efficacy in mouse modelb
	Mouse S9	Bovine S9	T. c.	T. v.
2	NTc	NTc	0/5 (2 × 10)	5/5 (4 × 10) 1/5 (1 × 10)
4	NTc	NTc	4/5 (2 × 10)	5/5 (2 × 10) 4/4 (1 × 10)
5	5.4	9.3	5/5 (2 × 10) 4/4 (1 × 10) 0/4 (1 × 5)	5/5 (2 × 10) 5/5 (1 × 10) 4/4 (1 × 10)
6	17	9.1	0/4 (1 × 10)	NTc
8	7.9	5.6	4/4 (1 × 10) 0/4 (1 × 5)	4/4 (1 × 10)
14	9.1	2.7	0/4 (1 × 10)	NTc
16	15	8.9	4/4 (2 × 10) 1/4 (1 × 10)	NTc
17	14	10	0/4 (1 × 10)	NTc
18	9.7	3.1	1/4 (1 × 10)	NTc
19	2.6	1.3	0/4 (1 × 10)	NTc
20	1.5	1.3	0/5 (4 × 10)	NTc
21	<1	<1	1/4 (2 × 10)	4/4 (2 × 10)
22	1.4	0.9	0/4 (1 × 10)	NTc
24	21	23	1/4 (2 × 10)	NTc
26	32	32	0/4 (1 × 10)	NTc
29	<1	<1	0/4 (1 × 10)	NTc
30	3.7	3.1	0/4 (1 × 10)	NTc
31	<1	<1	0/4 (1 × 10)	NTc
33	6.3	2.0	3/4 (1 × 10)	4/4 (1 × 10)
34	11.8	4.8	2/4 (1 × 10)	4/4 (1 × 10)
35	5.2	7.8	0/4 (1 × 10)	NTc
39	1.6	3.9	0/4 (1 × 10)	NTc
41	1.3	1.8	0/4 (1 × 10)	NTc
46	7.4	7.0	1/4 (1 × 10)	NTc
47	4.8	10	0/4 (1 × 10)	NTc
48	4.0	23	1/4 (1 × 10)	NTc
49	1.5	4.0	2/4 (1 × 10)	4/4 (1 × 10)
50	8.6	12.7	1/4 (1 × 10)	4/4 (1 × 10)
51	1.8	5.0	0/4 (1 × 10)	4/4 (1 × 10)
52	1.8	6.0	0/4 (1 × 10)	NTc
53	5.4	6.8	0/4 (1 × 10)	NTc
54	5.5	3.8	0/4 (1 × 10)	NTc
55	<1	3.1	0/4 (1 × 10)	NTc
62	10	20	2/4 (1 × 10)	4/4 (1 × 10)
63	0.9	1.5	1/4 (1 × 10)	4/4 (1 × 10)
69	0.7	0.6	1/4 (1 × 10)	1/4 (1 × 10)
70	1.5	0.3	1/4 (1 × 10)	4/4 (1 × 10)
71	6.4	8.1	3/4 (1 × 10)	4/4 (1 × 10)

^aMethods for testing compound efficacy in mouse models are described in the reference and note section.⁷

^bThe efficacy data in the table is presented as n/m (q × 10), where n = number of mice survived, m = total number of mice in the study group, q = how many time dosed, and 10 = 10 mg/kg.

^cNT = Not tested.