TABLE 1.

Early inhibitors found to act through aggregation^a

	IC50 (μM)
structure	Original target(s)		β-Lactamase	Chymotrypsin	cDHFR	β-Gal
	0.5 β-Lactamaseb		0.5	2.5	5	15
	5 β-Lactamaseb		5	25	35	90
	5 β-Lactamaseb		5	15	N.D.	N.D.
	8 Malarial protease		10	55	70	180
	7 pDHFR		10	50	60	300
	80 pDHFR		50	25	N.D.	600
	50 HIV Tar RNA		10	90	N.D.	600
	3 TS	30 Kinesin	3	11	20	200
	20cInsulin receptor	7.5 Kinesin	16	50	N.D.	80
	5.2 VEGF	10.0 IGF-1	6	30	30	55
	25 Farnesyltransferase		3	9	25	150
	15dGyrase		18	100	150	320
	1 Prion	30.4 TIM	3.9	40	0.4	100
	17 eNOS	24 nNOS	7	60	N.D.	N.D.
	3.8 PI3K	11.0 Integrase	4	100	N.D.	220

Abbreviations: cDHFR, chicken DHFR; β-gal, β-galactosidase; pDHFR, Pneumocystis carinii DHFR; TS, thymidylate synthase; VEGF, vascular endothelial growth factor receptor tyrosine kinase; IGF-1, insulin-like growth factor receptor tyrosine kinase; TIM, triosephosphate isomerase; eNOS, endothelial nitric oxide synthase; nNOS, neuronal nitric oxide synthase; PI3K, phosphoinositide 3-kinase; N.D., not determined.

^aTable adapted, with permission, from Ref. [8].

^bUnpublished observations.

^cKd.

^dMaximal non-effective concentration.