Compound (Charge of Major Microspecies at pH 7.4) | Apparent Km (IC50) [µM] | ||||||
---|---|---|---|---|---|---|---|
hOCT1 | hOCT2 | hOCT3 | hOCTN1 | hOCTN2 | hMATE1 | hMATE2-K | |
ASP (+) f | 2.3–21 | 36–42 | n.t.d. | 5.8a, 34a | |||
DAPI (++) f | 8.9 | n.t.d. | n.t.d. | n.t.d. | n.t.d. | 1.1a | 3.2a |
Fluoro-L-α-methyltyrosine (+−) | n.t.d. | n.t.d. | t | ||||
Fluoromethylcholine (+) | t | 14, 1800 | t | ||||
MPP (+) | 15–32 (16) | 3–20 (3.0) | 47–83 | n.t.d. | 4.4a–100a (22a–54a) | 3.3a–111a | |
NBD-MTMA (++) f | 8.8, 9.6 (8.3, 64) | 20,a 105a (67a–112a) | |||||
N-methyl-quinindine (+) | 20 | ||||||
Rhodamine 123 (+) f | 0.54 (0.37) | 0.61 (62) | 0.79a | 10a | |||
TEA (+) | 69–229 (216) | 27–76 (110, 222) | (1240–1480) | 439 | 292, 304 | 220,a 380a (41a) | 760,a 830a (14a) |
f, fluorescent; NBD-MTMA, N,N,N-trimethyl-2-[methyl(7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)amino]ethanaminium iodide; n.t.d., no transport detected; t, transported.
↵a Uptake measurements performed in presence of an outwardly directed proton gradient; IC50 values are presented in brackets.