Table 2.

Substrate-dependent IC₅₀ or K_i values for inhibition of hOCT2 by cimetidine (data from [35] and our laboratories).

Cimetidine Ki/IC50 (µM)	Substrate	Substrate concentration (µM)	Reference
14	Amil	1	[62]
36	ASP	1	[63]
23	ASP	20	[44]
26	ASP	1	[62]
27	Crea	5	[64]
1380	Et	1	[57]
510	Met	10	[65]
110	MPP	0.01	Unpublished
142	MPP	15	Unpublished
120	MPP	0.01	[58]
70.4	NBD-MTMA	10	Unpublished
70	TEA	5	[17]

Amil = Amiloride, ASP = 4-(4-(dimethylamino)styryl)-N-methylpyridinium, Crea = Creatinine, Et = ethidium, Met = metformin, MPP = 1-methyl-4-phenylpyridinium, NBD-MTMA = [2-(4-nitro-2,1,3-benzoxadiazol-7-yl)aminoethyl]trimethylammonium, TEA = tetraethylammonium. Bold = molecules highlighted to show for the same probe substrate the comparable IC₅₀ or K_i