Table 3.
Selectivity and affinity of amino acid transporter inhibitors. Selectivity is listed against other amino acid transporters where tested. A (+) sign indicates that the compound has significant nontransporter targets where known. N.d. not determined; n.a. not available.
| Target | Inhibitor | Selectivity | Affinity (pIC50) | Reference |
|---|---|---|---|---|
| SLC1A1 | NBI-59159 | Selective for EAAT3 | 7.1 | [95] |
| DL-TBOA | All EAATs | 5.1 | [96] | |
| SLC1A2 | WAY-213613 | Selective for EAAT2 | 7.1 | [97] |
| DL-TBOA | All EAATs | 5.1 | [96] | |
| SLC1A3 | UCPH-101 | Selective for EAAT1 | 6.9 | [98] |
| DL-TBOA | All EAATs | 4.1 | [96] | |
| SLC1A4 | n.a. | |||
| SLC1A5 | Benzylserine | Also LAT1, SNAT1, SNAT2 | 3.0 | [6,99] |
| γ-glutamyl-p-nitroanilide (GPNA) | Also LAT1, SNAT1, SNAT2 | 4.0 | [6,100] | |
| V-9302 | LAT1, SNAT2, not ASCT2 | 5.0 | [42,61] | |
| Serine-biphenylmethyl carboxylate | n.d. | 4.5 | [101] | |
| (R)-γ-(4-biphenylmethyl)-l-proline | n.d. | 5.5 | [102] | |
| Proline and serine-based sulfonic acids/sulfonamides | n.d. | 5 | [103] | |
| 1,2,3 dithiazoles | n.d. | 5.5 | [104] | |
| Compound 10 | n.d. | 4.0 | [105] | |
| SLC6A5 | Org 25543 | Selective | 7.8 | [106] |
| SLC6A7 | Compound 58 | Selective | 7.7 | [107] |
| LP-403812 | Selective | 7.0 | [108] | |
| SLC6A9 | Bitopertin | Selective | 7.5 | [109] |
| R-NFPS | Selective | 8.5-9.1 | [110] | |
| SSR 103800 | Selective | 8.7 | [111] | |
| LY2365109 | Selective | 7.8 | [112] | |
| GSK931145 | Selective | 7.6 | [113] | |
| SLC6A14 | α-methyl-DL-tryptophan | n.d. | 3.6 | [114] |
| SLC6A17 | n.a. | |||
| SLC6A19 | Cinromide | Selective (+) | 6.4 | [115] |
| Nimesulide | Selective (+) | 4.6 | [116] | |
| Benztropin | Selective (+) | 4.4 | [117] | |
| E4, E18, CB3 | Selective | [118] | ||
| SLC6A20 | n.a. | |||
| SLC7A1 | n.a. | |||
| SLC7A2 | n.a. | |||
| SLC7A3 | n.a. | |||
| SLC7A4 | n.a. | |||
| SLC7A5 | JPH203 | Selective | [119] | |
| BCH | All System L transporters | [120] | ||
| KMH-233 | Selective | [121] | ||
| SKN103 | Selective | [122] | ||
| (Z)-4-chloro-N-(4-(trifluoromethoxy)phenyl)-5H-1,2,3-dithiazol-5-imine | n.d. | [123] | ||
| 2-amino-4-(3,5-Dichloro-phenyl)-butyric acid | n.d. | [124] | ||
| SLC7A6 | n.a. | |||
| SLC7A7 | n.a. | |||
| SLC7A8 | BCH | All System L transporters | [120] | |
| SLC7A9 | n.a. | |||
| SLC7A10 | BMS-466442 | Selective | 7.4 | [125] |
| (+)-amino(1-(3,5-dichlorophenyl)-3,5-dimethyl-1H-pyrazol-4-yl)acetic acid (ACPP) | 4.0 | [126] | ||
| SLC7A11 | Sulfasalazin | Selective (+) | 3.8 | [45] |
| Sorafenib | Selective (+) | 5 | [127] | |
| Erastin | Selective (+) | 6.7 | [127] | |
| SLC7A12 | n.a. | |||
| SLC7A13 | n.a. | |||
| SLC7A14 | n.a. | |||
| SLC16A10 | n.d. | |||
| SLC17A6 | n.a. | |||
| SLC17A7 | n.a. | |||
| SLC17A8 | n.a. | |||
| SLC25A2 | n.a. | |||
| SLC25A12 | n.a. | |||
| SLC25A13 | n.a. | |||
| SLC25A15 | n.a. | |||
| SLC25A18 | n.a. | |||
| SLC25A22 | n.a. | |||
| SLC32A1 | vigabatrin | 2.1 | [128] | |
| SLC36A1 | Sertraline | 2.4 | [129] | |
| SLC36A2 | None | |||
| SLC36A3 | None | |||
| SLC36A4 | None | |||
| SLC38A1 | MeAIB | SNAT1,2,4, PAT1 | 4 | [130] |
| SLC38A2 | MeAIB | SNAT1,2,4, PAT1 | 4 | [130] |
| SLC38A3 | n.a. | |||
| SLC38A4 | MeAIB | SNAT1,2,4 PAT1 | [131] | |
| SLC38A5 | n.a. | |||
| SLC38A6 | n.a. | |||
| SLC38A7 | n.a. | |||
| SLC38A8 | n.a. | |||
| SLC38A9 | n.a. | |||
| SLC38A10 | n.a. | |||
| SLC38A11 | n.a. | |||
| SLC43A1 | ESK246 | Selective | 5.0 | [132] |
| BCH | All System L transporters | [120] | ||
| SLC43A2 | BCH | All System L transporters | [120] |