Table 4.

Compilation of further characterization experiments on promising p97 inhibitor analogues.

			IC50 [μm]a			Cytotoxicity GI50 [μm]a
						HCT15		SW403
Compd	R1	R2	ATPase	UbG76V–GFP	ODD-Luc	24 h	72 h	24 h	72 h
DBeQ	see Figure 1		1.6	2.3	56±14	3.2±1.0	1.8±0.7	2.2±0.6	1.4±0.5
11c	see Table 1		0.4	7.8	NMb	5±1	2.5±0.6	5.4±2	4.1±1.7
14c	see Table 1		0.6	10	6.5±1.1	1.1±0.3	0.8±0.3	0.8±0.3	0.5±0.2
44c	H	3-fluorophenyl	1.6	2.7	NMb	5.8±1.6	3.1±0.9	5.6±2.4	4.3±1.8
45c	H	4-methylbenzyl	3	1.5	16±5	3.6±1.2	3.5±1.2	3.3±1.1	2±0.7
46c	H	4-trifluoromethylbenzyl	2.6	2.5	15±3	3.4±1.1	2±1	3.0±1	1.6±0.7
47c	H	3-methoxybenzyl	4.5	1.7	>20	4.4±1.6	3.9±1.5	4.7±2.2	3±0.9
48c	H	3-fluorobenzyl	3.1	1.1	11±3	3.4±1	3.5±1.2	4.6±2	2.6±0.7
49c	H	3-bromobenzyl	3.7	1.3	12±3	3.4±1.2	3.5±1.2	4.3±1.9	2.8±0.7
50c	methoxy	3-chlorophenyl	0.5	5.4	18±4	29±6	19±4	12±5	11±5
51c	methoxy	3-fluorophenyl	0.5	4.8	22±4	8.0±2.7	3.7±1.3	4.9±2.0	4±1.6
52c	methoxy	thiophen-2-ylmethyl	1.7	1.8	4±1	0.82±0.17	0.7±0.3	0.5±0.1	0.35±0.1
ML240	see Figure 3		0.1	0.9	28±7	0.76±0.14	0.54±0.19	0.5±0.07	0.5±0.1
19d	see Figure 3		0.3	7.8	10±2	1.7±0.8	1.4±0.5	1.7±0.7	1.4±0.5
ML241	see Figure 3		0.1	3.5	46±8	53±5	13±4	33±7	12±3
15e	see Figure 3		0.6	7	>20	24±3	10±3	21±5	13±4
17e	see Figure 3		0.4	6.4	17±2	37±7	16±5	18±10	9.7±3.7
33e	see Table 3		0.1	3.8	>20	28±3	17±5	42±9	9.4±2.9
34e	see Table 3		0.6	6.5	27±5	12±4	9±3	15±7	7.9±2.7
35e	see Table 3		0.4	5.3	61±6	13±5	7.1±2.5	11±5	3.9±1
38e	see Table 3		0.2	3.3	>20	25±5	12±3	43±11	13±4
40e	see Table 3		1.9	3.7	>20	27±4	8.9±2.3	21±6	9.4±2.6

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

^bNot measured due to interference with luciferase assay.

^cAnalogue of DBeQ.

^dAnalogue of ML240.

^eAnalogue of ML241.