TABLE 2.
Potencies of the screened reported and potential tool compounds. Only active values are shown; the full table including literature references can be found in the Supplementary Material. a) values were published previously (Sijben et al., 2021b); b) possibly due to an indirect effect of the assay/cell model; c) as reported in Supplementary Table S2.
Compound name | ChEMBL parent ID | SLC | Assay | Activity type | Activity value | Literature median activityc |
---|---|---|---|---|---|---|
DIDS | CHEMBL1162148 | SLC1A1 | EchoMS | pIC50 | 5.2 | |
TFB-TBOA | CHEMBL1257519 | SLC1A1 | EchoMS | pIC50 | 6.4 | 6.9 |
Riluzole | CHEMBL744 | SLC1A1 | EchoMS | pIC50 | 5.1 | |
WAY-213613 | CHEMBL1628669 | SLC1A1 | EchoMS | pIC50 | 5.5 | 5.7 |
Loratadine | CHEMBL998 | SLC1A1 | EchoMS | pIC50 | 5.7 | |
KPH2f | CHEMBL5222644 | SLC1A1 | EchoMS | pIC50 | 6.0 | |
TFB-TBOA | CHEMBL1257519 | SLC1A2 | EchoMS | pIC50 | 8.1 | 7.9 |
Threo-beta-benzyloxyaspartic acid | CHEMBL475341 | SLC1A2 | EchoMS | pIC50 | 5.1 | 5.7 |
WAY-213613 | CHEMBL1628669 | SLC1A2 | EchoMS | pIC50 | 6.6 | 7.1 |
TFB-TBOA | CHEMBL1257519 | SLC1A3 | EchoMS | pIC50 | 8.1 | 8.1 |
UCPH-101 | CHEMBL474133 | SLC1A3 | EchoMS | pIC50 | 6.3 | 6.5 |
UCPH-102 | CHEMBL1259233 | SLC1A3 | EchoMS | pIC50 | 6.8 | 6.4 |
Loratadine | CHEMBL998 | SLC1A3 | EchoMS | pIC50 | 5.2 | |
WAY-213613 | CHEMBL1628669 | SLC6A2 | TRACT | pIC50 | 6 | |
Desipramine | CHEMBL72 | SLC6A2 | TRACT | pIC50 | 8.1a | 8.7 |
Vanoxerine (GBR12909) | CHEMBL281594 | SLC6A2 | TRACT | pIC50 | 6.1a | 6.9 |
KPH2f | CHEMBL5222644 | SLC6A2 | TRACT | pIC50 | 6 | |
Desipramine | CHEMBL72 | SLC6A4 | Uptake | pIC50 | 6.3 | 7.1 |
Vanoxerine (GBR12909) | CHEMBL281594 | SLC6A4 | Uptake | pIC50 | 5.7 | 6.8 |
DSP-1053 | CHEMBL4226281 | SLC6A4 | Uptake | pIC50 | 7.2 | 8.8 |
BAY-876 | CHEMBL4448899 | SLC6A4 | Uptake | pEC50 | 8.1b | |
KPH2f | CHEMBL5222644 | SLC6A4 | Uptake | pIC50 | 6 | |
DSP-1053 | CHEMBL4226281 | SLC6A12 | MP dye | Inhibition (3 µM) [%] | 36 |