TABLE 2.

Summary of screening sizes and hit rates of TB-WCSs

Process	Targeta	Organism	No. of compounds screened	Concn	Hit rate (%)	Agarb	Reference(s)
QS	LasR	P. aeruginosa	200,000	33 μM	0.01	N	30
	MvfR	P. aeruginosa	284,256	50 μg/mL	0.19	N	31
Pantothenate biosynthesis	PanC	M. tuberculosis	13,549		0.27	N	32
Proteome housekeeping	ClpP1P2	M. tuberculosis	503,879	10 μM	0.04	N	19
Purine biosynthesis	GuaB2	M. tuberculosis	10,000	1 and 10 μM	2.56c	N	33
Secretion	Tat	E. coli	389,481	5–20 μM	0.016–0.6	N	39
	T3SS	Y. pestis	70,966	∼17 μg/mL	0.6	N	37
		P. aeruginosa	80,000	50 μM	0.4	N	36
		S. enterica	92,000	∼160 μg/mL	0.097	N	38
	T2SS	P. aeruginosa	75,000	50 μM	0.15	N	40
		P. aeruginosa	83,986		0.17	N	41
		A. baumannii	6,400	10 μM	3c	N	43
		P. aeruginosa	40,000	10–20 μM	0.15	N	42
PG biogenesis	SAV1754	S. aureus		8 μM		N	44
	MreB	E. coli	690,000	25 μM	0.006–0.01	N	46
WTA synthesis	TarG	S. aureus	55,000	38 μM	0.08	N	20
	TarG	S. aureus	20,000	3 and 16 μM	0.02	N	48
	UppS	S. aureus	1,600	20 μM	4.25c	N	50
	DltB	S. aureus	258,000	15 μM	0.08	N	16
Oxidative protein folding	DsbB	E. coli, P. aeruginosa	342,109	16–33 μM	0.015	Y	51, 52
	VKOR	M. tuberculosis	342,109	16–33 μM	0.06–0.27	Y	51, 52
LPS biogenesis	MsbA	A. baumannii	150,000	5 μM	0.007	N	54

^aFor pathway-directed screens, a target (underlined) of the most promising inhibitor in the screen was selected. However, these screens could detect inhibitors in other steps of the pathway or its regulation.

^bAgar-based versus liquid-based screens. Y, yes; N, no.

^cHigher hit rates are likely due to the use of preselected libraries known to target M. tuberculosis (first case) or the size of the libraries tested (second and third cases).