| Inhibitor |
IC50 (μM) |
Ki (μM) |
Substrate used |
Cell System |
Reference |
| Abemaciclib |
0.52 |
|
Metformin1,3 |
HEK293-MATE1 |
Chappell, 2019 |
| Agmatine |
54 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Allethrin |
50.2 |
|
Tetraethylammonium1 |
HEK293 cells |
Chedik, 2017 |
| Amantadine |
7.5 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Amantadine |
37.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Amantadine |
|
111.8 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Amiloride |
2.4 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Amphetamine |
94 |
|
Metformin1,3 |
HEK293-MATE1 |
Wagner, 2017 |
| Aripiprazole |
130 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Astemizole |
26.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Atropine |
6 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Bisphenol A |
73.5 |
|
Tetraethylammonium1 |
HEK293 cells |
Bruyere, 2017 |
| Bithionol |
5.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Buspirone |
1.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Butylscopolamine |
8.2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Chen, 2017 |
| Camostat |
2.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Carvedilol |
92.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Cetirizine |
|
371.2 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Chlorhexidine |
0.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Chloroquine |
1.5 |
|
Ipratropium |
HEK293-MATE1 |
Chen, 2017 |
| Chloroquine |
2.5 |
|
Metformin1,3 |
HEK293-MATE1 |
Muller, 2011 |
| Chlorpheniramine |
|
87.6 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Cimetidine2,4 |
5.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Cimetidine2,4 |
1.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Cimetidine2,4 |
|
3.8 |
Metformin1,3 |
HEK293-MATE1 |
Ito, 2012 |
| Cimetidine2,4 |
2.56 |
|
Metformin1,3 |
HEK293-MATE1 |
Lechner, 2016 |
| Cimetidine2,4 |
|
1.1 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Clonidine |
8.09 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Clonidine |
33.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Cobicistat |
4.4 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Kikuchi, 2019 |
| Cortisone |
21.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Dabigatran |
8.1 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Dasatinib |
0.8 |
|
Metformin1,3 |
HEK293-MATE1 |
Minematsu, 2011 |
| Desipramine |
|
55.7 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Dihydroergotamine |
2.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Diltiazem |
|
12.5 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Diphenhydramine |
|
87 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Dipyridamole |
24 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Dipyridamole |
26 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Disopyramide |
66 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Disopyramide |
|
83.8 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Dolutegravir4 |
4.7 |
|
Tetraethylammonium1 |
CHO-MATE1 |
Lepist, 2014 |
| Domperidone |
2.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Donepezil |
0.78 |
|
Metformin1,3 |
CHO-MATE1 |
Martinez-Guerrero, 2016 |
| DX-619 |
|
0.82 |
Creatinine |
HEK293-MATE1 |
Imamura, 2011 |
| Epinastine |
1.1 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Erlotinib |
8 |
|
Metformin1,3 |
HEK293-MATE1 |
Minematsu, 2011 |
| Esmolol |
11 |
|
Metformin1,3 |
CHO-MATE1 |
Martinez-Guerrero, 2016 |
| Ethinyl estradiol |
21.1 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Famotidine |
2.16 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Famotidine |
0.76 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Famotidine |
|
0.6 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Gabexate |
0.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Gefitinib |
1.82 |
|
Metformin1,3 |
HEK293-MATE1 |
Minematsu, 2011 |
| Granisetron |
5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Guanfacine |
3.5 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Homatropine |
18.7 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Chen, 2017 |
| Imatinib |
0.35 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Imatinib |
0.04 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Imatinib |
0.05 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Imipramine |
10 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Imipramine |
|
42 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Imiquimod |
14 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Indinavir |
7.8 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Indinavir |
1.7 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Indinavir |
1.9 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Ipratropium |
30.5 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Chen, 2017 |
| Irinotecan |
7.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Irinotecan |
2.1 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Irinotecan |
4.3 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Ketoconazole |
1.33 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Ketotifen |
12.7 |
|
Metformin1,3 |
CHO-MATE1 |
Martinez-Guerrero, 2016 |
| Levofloxacin |
17.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Losartan |
250 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Maraviroc |
17.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Metamphetamine |
107 |
|
Metformin1,3 |
HEK293-MATE1 |
Wagner, 2017 |
| Metformin1,3 |
47 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Metformin1,3 |
250 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Metformin1,3 |
|
666.9 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Methyl ergonovine |
250 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Midodrine |
109 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Mitoxantrone |
0.53 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Mitoxantrone |
4.4 |
|
Metformin1,3 |
HeLa-MATE1 |
Meyer, 2010 |
| Mitoxantrone |
0.19 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Mitoxantrone |
0.4 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Mitoxantrone |
5.2 |
|
Tetraethylammonium1 |
HeLa-MATE1 |
Meyer, 2010 |
| N-butylpyridinium chloride (NBuPy-Cl) |
8.5 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Cheng, 2011 |
| Naloxone |
24.1 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Nialamide |
212 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Nicotine |
167 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Nifekalant |
6.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Nifekalant |
0.65 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Nifekalant |
1.1 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Noscapine |
34.5 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Omeprazole |
16.1 |
|
Metformin1,3 |
CHO-MATE1 |
Martinez-Guerrero, 2016 |
| Ondansetron |
0.15 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Ondansetron |
0.16 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Ondansetron |
0.01 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Ondansetron |
0.03 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Orphenadrine |
65 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Pantoprazole |
43.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Pantoprazole |
2.8 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Pantoprazole |
2.8 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Pentamidine |
2.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Pentamidine |
0.41 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Pentamidine |
2 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Phentolamine |
4.64 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Pimozide |
>500 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Pramipexole |
|
141.4 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Prazosin |
1.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Procainamide |
24 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Procainamide |
|
217 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Prochlorperazine |
7.9 |
|
Metformin1,3 |
CHO-MATE1 |
Martinez-Guerrero, 2016 |
| Proguanil |
4.35 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Propranolol |
7.81 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Pyrimethamine2 |
0.07 |
|
Ipratropium |
HEK293-MATE1 |
Chen, 2017 |
| Quinidine |
1.57 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Quinidine |
11.2 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Quinidine |
|
29.2 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Quinine |
2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Ranitidine |
5.4 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Ranitidine |
8.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Ranitidine |
18.9 |
|
Metformin1,3 |
HeLa-MATE1 |
Meyer, 2010 |
| Ranitidine |
|
25.4 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Ranitidine |
17.5 |
|
Tetraethylammonium1 |
HeLa-MATE1 |
Meyer, 2010 |
| Rapamycin |
3.27 |
|
Metformin1,3 |
HeLa-MATE1 |
Meyer, 2010 |
| Rapamycin |
3.51 |
|
Tetraethylammonium1 |
HeLa-MATE1 |
Meyer, 2010 |
| Rimantadine |
7.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Risperidone |
1.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Ritonavir |
4.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Ritonavir |
15.4 |
|
Metformin1,3 |
HeLa-MATE1 |
Meyer, 2010 |
| Ritonavir |
0.08 |
|
Metformin1,3 |
HEK293-MATE1 |
Wittwer, 2013 |
| Ritonavir |
2.1 |
|
Metformin1,3 |
MDCK2- MATE1 |
Wittwer, 2013 |
| Ritonavir |
13.9 |
|
Tetraethylammonium1 |
HeLa-MATE1 |
Meyer, 2010 |
| Scopolamine |
47.6 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Scopolamine |
119.2 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Chen, 2017 |
| Spironolactone |
18.6 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Sumatriptan |
6.7 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Sunitinib |
0.275 |
|
Metformin1,3 |
HEK293-MATE1 |
Minematsu, 2011 |
| Tacrine |
0.51 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Tacrine |
1.1 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Kido, 2011 |
| Talipexole |
|
66 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Telmisartan |
17.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Tetrabromobisphenol A |
23.1 |
|
Tetraethylammonium1 |
HEK293 cells |
Bruyere, 2017 |
| Tetrabutylammonium |
18 |
|
Paraquat |
HEK293 cells |
Chen, 2007 |
| Tetraethylammonium1 |
121 |
|
Paraquat |
HEK293 cells |
Chen, 2007 |
| Tetramethrin |
47.5 |
|
Tetraethylammonium1 |
HEK293 cells |
Chedik, 2017 |
| Tetramethylammonium |
5073 |
|
Paraquat |
HEK293 cells |
Chen, 2007 |
| Tetrapropylammonium |
63 |
|
Paraquat |
HEK293 cells |
Chen, 2007 |
| Topotecan |
1.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Tramadol |
17.8 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Trichlormethiazide |
249 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Trimethoprim4 |
9.7 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Trospium |
11.6 |
|
1-methyl-4-phenylpyridinium (MPP+) |
HEK293-MATE1 |
Chen, 2017 |
| Tubocurarine |
9.4 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Vecuronium bromide |
1.9 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
Wittwer, 2013 |
| Verapamil |
42 |
|
1-methyl-4-phenylpyridinium (MPP+) |
CHO-MATE1 |
Astorga, 2012 |
| Verapamil |
|
27.5 |
Tetraethylammonium1 |
HEK293-MATE1 |
Tsuda, 2009 |
| Zafirlukast |
1.3 |
|
4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) |
HEK293-MATE1 |
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