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CNB-TBOA
MW:
383.35
logP:
0.6
H-acceptors:
7
H-donors:
4
Rotatable bonds:
6
EAATs:
 
EAAT1:
 
EAAT2:
0.036 µM
EAAT3:
1.4 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
NO2-BzATBOA
MW:
403.24
logP:
-0.57
H-acceptors:
9
H-donors:
4
Rotatable bonds:
6
EAATs:
 
EAAT1:
 
EAAT2:
0.014 µM
EAAT3:
0.278 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
Ph-BzA-TBOA
MW:
434.44
logP:
2.25
H-acceptors:
6
H-donors:
4
Rotatable bonds:
4
EAATs:
 
EAAT1:
 
EAAT2:
0.021 µM
EAAT3:
0.034 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
niflumic acid
MW:
282.22
logP:
3.36
H-acceptors:
6
H-donors:
2
Rotatable bonds:
4
EAATs:
 
EAAT1:
666 µM
EAAT2:
666 µM
EAAT3:
 
EAAT4:
666 µM
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: n/a
Comment: Niflumic acid enhanced substrate gated currents in EAAT4, at a concentration of 300 micromolar, it induced 19% reduction of L-3H-glutamate uptake (10 microM), with no effect on DL-3H-aspartatic acid uptake.
No IC50 and Ki values given.
TAN
MW:
172.14
logP:
-1.77
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
 
EAAT1:
288 µM
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: yes
Comment: The radioactive ligand was 14C-glutamate.
The TAN is an agonist of AMPA but not the NMDA receptors.
The glucoside of TAN is present in lentil and garden pea.
PMB-TBOA
MW:
388.37
logP:
0.44
H-acceptors:
6
H-donors:
4
Rotatable bonds:
6
EAATs:
 
EAAT1:
 
EAAT2:
12 µM
EAAT3:
266 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive label was 14C-glutamate.
The assays were performed in MDCK cells stably expressing EAAT2-3.
CF3O-BzATBOA
MW:
422.37
logP:
-2.1
H-acceptors:
7
H-donors:
4
Rotatable bonds:
7
EAATs:
 
EAAT1:
 
EAAT2:
7 µM
EAAT3:
128 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
TFB-TBOA
MW:
426.34
logP:
1.49
H-acceptors:
5
H-donors:
4
Rotatable bonds:
7
EAATs:
 
EAAT1:
22 µM
EAAT2:
17 µM
EAAT3:
300 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on COS-1 cells transiently expressing EAAT2 or EAAT3.
TFB-TBOA
MW:
426.34
logP:
1.49
H-acceptors:
5
H-donors:
4
Rotatable bonds:
7
EAATs:
 
EAAT1:
 
EAAT2:
1.9 µM
EAAT3:
28 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
way-855
MW:
197.19
logP:
666
H-acceptors:
4
H-donors:
3
Rotatable bonds:
3
EAATs:
2.6 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5: