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Kainate
MW:
213.23
logP:
-0.346
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
3000 µM
EAAT2:
59 µM
EAAT3:
3000 µM
EAAT4:
 
EAAT5:
 
Kainate
MW:
213.23
logP:
-0.346
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
65 µM
EAAT1:
 
EAAT2:
 
EAAT3:
38 µM
EAAT4:
 
EAAT5:
 
Kainate
MW:
213.23
logP:
-0.346
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
7 µM
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
 
Kainate
MW:
213.23
logP:
-0.346
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
59 µM
EAAT1:
 
EAAT2:
9 µM
EAAT3:
 
EAAT4:
 
EAAT5:
 
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
4 µM
EAAT2:
4.5 µM
EAAT3:
3.7 µM
EAAT4:
 
EAAT5:
 
t-PDC
MW:
159.14
logP:
-0.985
H-acceptors:
5
H-donors:
3
Rotatable bonds:
2
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
6.2 µM
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: Although the compound is a substrate for other EAAT subtypes, it did not generate a current with a voltage dependence similar to that of glutamate.
3-Hydroxyaspartic acid
MW:
149.102
logP:
-4.061
H-acceptors:
6
H-donors:
4
Rotatable bonds:
3
EAATs:
 
EAAT1:
 
EAAT2:
 
EAAT3:
 
EAAT4:
 
EAAT5:
1 µM
Cell line:
Method: Radioactive labelling
Substrate: no
Comment: Although the compound is a substrate for other EAAT subtypes, it did not generate a current with a voltage dependence similar to that of glutamate.
3-Hydroxyaspartic acid
MW:
149.102
logP:
-4.061
H-acceptors:
6
H-donors:
4
Rotatable bonds:
3
EAATs:
 
EAAT1:
32 µM
EAAT2:
19 µM
EAAT3:
25 µM
EAAT4:
 
EAAT5:
 
Dihydrokainate
MW:
215.246
logP:
0.293
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
1000 µM
EAAT2:
196 µM
EAAT3:
1000 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: n/a
Comment: The radioactive ligand was 14C-glutamate.
The experiments were performed on COS-1 cells transiently expressing EAAT1- EAAT3.
Dihydrokainate
MW:
215.246
logP:
0.293
H-acceptors:
5
H-donors:
3
Rotatable bonds:
4
EAATs:
 
EAAT1:
 
EAAT2:
0.056 µM
EAAT3:
1000 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: n/a
Comment: The radioactive label was 14C-glutamate. The uptake assays were performed in MDCK cells stably expressing EAAT2 or EAAT3.