Table 2.

Selected SAR related to the optimization of ML240.

		IC50 [μm]a
Compd	R1	ATPase	UbG76V–GFP
ML240	H	0.11±0.03	0.9±0.1
21	5,6-dichloro	25±8	>20
22	5,6-dimethyl	2±0.4	89±39
23	mixture of 5- and 6-chloro	0.7±0.3	31±7
24	mixture of 5- and 6-bromo	0.8±0.3	30±10
25	mixture of 5- and 6-methyl	0.24±0.06	2.5±0.5
26	mixture of 5- and 6-methoxy	0.48±0.09	0.96±0.2
27	4-fluoro	0.043±0.01	5.4±1.2
28	7-fluoro	0.5±0.1	5.4±0.8
29	4-methyl	0.045±0.006	2.6±0.3
30	mixture of 5- and 6-fluoro	0.08±0.02	6.8±1

^aMeasurements were carried out in triplicate, and results are expressed as the mean ±SD.