| Inhibitor |
IC50 (μM) |
Ki (μM) |
Substrate used |
Cell System |
Reference |
| 1-methyl-4-phenylpyridinium (MPP+) |
3.3 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Abemaciclib |
0.75 |
|
Metformin1,3 |
HEK293-MATE2K |
Chappell, 2019 |
| Agmatine |
60.8 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Amantadine |
89 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Amantadine |
|
1167 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Amiloride |
3.06 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Amphetamine |
158 |
|
Metformin1,3 |
HEK293-MATE2K |
Wagner, 2017 |
| Aripiprazole |
>500 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Atropine |
52 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Bithionol |
6.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Buspirone |
46 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Butylscopolamine |
38.2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE2K |
Chen, 2017 |
| Camostat |
12.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Cetirizine |
|
817.6 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Chlorhexidine |
0.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Chloroquine |
4 |
|
Ipratropium |
HEK293-MATE2K |
Chen, 2017 |
| Chlorpheniramine |
|
191.2 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Cimetidine2,4 |
39 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Cimetidine2,4 |
5.47 |
|
Metformin1,3 |
HEK293-MATE2K |
Lechner, 2016 |
| Cimetidine2,4 |
|
7.3 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Cimetidine2,4 |
|
2.1 |
Tetraethylammonium1 |
HEK293-MATE2K |
Ito, 2012 |
| Clonidine |
54 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Cobicistat |
3.2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE2K |
Kikuchi, 2019 |
| Dabigatran |
25.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Dasatinib |
0.8 |
|
Metformin1,3 |
HEK293-MATE2K |
Minematsu, 2011 |
| Desipramine |
|
283 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Dihydroergotamine |
12.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Diltiazem |
|
117 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Diphenhydramine |
|
266.5 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Dipyridamole |
74 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Disopyramide |
100 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Disopyramide |
|
291.6 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Domperidone |
14.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| DX-619 |
|
0.1 |
Creatinine |
HEK293-MATE2K |
Imamura, 2011 |
| Epinastine |
29.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Erlotinib |
3.45 |
|
Metformin1,3 |
HEK293-MATE2K |
Minematsu, 2011 |
| Ethinyl estradiol |
20.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Famotidine |
6.28 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Famotidine |
36.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Famotidine |
|
9.7 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Gabexate |
10.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Gefitinib |
0.194 |
|
Metformin1,3 |
HEK293-MATE2K |
Minematsu, 2011 |
| Granisetron |
311 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Guanfacine |
218 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Homatropine |
128.3 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE2K |
Chen, 2017 |
| Imatinib |
0.35 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Imatinib |
2.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Imipramine |
100 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Imipramine |
|
182.9 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Imiquimod |
19.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Indinavir |
7.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Indinavir |
>500 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ipratropium |
62.8 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE2K |
Chen, 2017 |
| Irinotecan |
7.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Irinotecan |
78.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ketoconazole |
9.33 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Maraviroc |
297 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Metamphetamine |
84.3 |
|
Metformin1,3 |
HEK293-MATE2K |
Wagner, 2017 |
| Metformin1,3 |
89.3 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Metformin1,3 |
|
6515.7 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Midodrine |
87.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Mitoxantrone |
0.53 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Mitoxantrone |
0.83 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Moxifloxacin |
7.6 |
|
Metformin1,3 |
HEK293-MATE2K |
Te, 2016 |
| N-butylpyridinium chloride (NBuPy-Cl) |
1.6 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Cheng, 2011 |
| Naloxone |
43.2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Nialamide |
236 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Nicotine |
134 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Nifekalant |
2.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Nifekalant |
6.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ondansetron |
6.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Ondansetron |
0.16 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ondansetron |
0.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Orphenadrine |
100 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Pantoprazole |
43.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Pantoprazole |
500 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Pentamidine |
2.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Pentamidine |
10.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Phentolamine |
5.3 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Pimozide |
>500 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Pramipexole |
|
24.1 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Prazosin |
38.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Procainamide |
19.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Procainamide |
|
178.1 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Proguanil |
1.39 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Propranolol |
7.71 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Pyrimethamine2 |
0.059 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Pyrimethamine2 |
0.01 |
|
Ipratropium |
HEK293-MATE2K |
Chen, 2017 |
| Quinidine |
1.47 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Quinidine |
|
23.1 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Quinine |
6.4 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Ranitidine |
10 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Ranitidine |
|
25 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Rimantadine |
288 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Risperidone |
291 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ritonavir |
4.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Ritonavir |
23.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Scopolamine |
272 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Sunitinib |
0.86 |
|
Metformin1,3 |
HEK293-MATE2K |
Minematsu, 2011 |
| Tacrine |
1.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Tacrine |
100 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Kido, 2011 |
| Talipexole |
|
119.5 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Topotecan |
8.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Tramadol |
74 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Trimethoprim4 |
2.61 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Trospium |
5.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE2K |
Chen, 2017 |
| Tubocurarine |
55.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Vecuronium bromide |
25.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
| Verapamil |
37.9 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE2K |
Astorga, 2012 |
| Verapamil |
|
32.1 |
Tetraethylammonium1 |
HEK293-MATE2 |
Tsuda, 2009 |
| Zafirlukast |
7.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE2K |
Wittwer, 2013 |
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022