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o-MeO-BzA-TBOA
MW:
388.37
logP:
0.44
H-acceptors:
5
H-donors:
6
Rotatable bonds:
5
EAATs:
 
EAAT1:
 
EAAT2:
0.145 µM
EAAT3:
1 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.
m-MeO-BzA-TBOA
MW:
388.37
logP:
0.44
H-acceptors:
7
H-donors:
4
Rotatable bonds:
5
EAATs:
 
EAAT1:
 
EAAT2:
0.037 µM
EAAT3:
0.356 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.
BzA-TBOA
MW:
358.35
logP:
0.57
H-acceptors:
6
H-donors:
4
Rotatable bonds:
5
EAATs:
 
EAAT1:
 
EAAT2:
0.055 µM
EAAT3:
0.729 µM
EAAT4:
 
EAAT5:
 
Cell line:
Method: Radioactive labelling
Substrate: n/a
Comment: The radioactive ligand was 14C-glutamate. The experiments were performed on MDCK cells stably expressing EAAT2 or EAAT3.
4-(methylamino)-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
184.26
logP:
2.18
H-acceptors:
3
H-donors:
2
Rotatable bonds:
1
GATs:
>500 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-(methylamino)-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
184.26
logP:
2.18
H-acceptors:
3
H-donors:
2
Rotatable bonds:
1
GATs:
>1000 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-(methylamino)-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
184.26
logP:
2.18
H-acceptors:
3
H-donors:
2
Rotatable bonds:
1
GATs:
242 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-amino-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
170.23
logP:
1.66
H-acceptors:
3
H-donors:
2
Rotatable bonds:
0
GATs:
>500 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-amino-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
170.23
logP:
1.66
H-acceptors:
3
H-donors:
2
Rotatable bonds:
0
GATs:
>1000 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-amino-4,5,6,7-tetrahydrobenzo[d]isothiazol-3-ol
MW:
170.23
logP:
1.66
H-acceptors:
3
H-donors:
2
Rotatable bonds:
0
GATs:
290 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4:
 
4-(pyrrolidin-1-yl)-4,5,6,7-tetrahydrobenzo[d]isoxazol-3-ol
MW:
208.26
logP:
1.5
H-acceptors:
2
H-donors:
1
Rotatable bonds:
1
GATs:
>500 µM
GAT1:
 
GAT2:
 
GAT3:
 
GAT4: