Table 4.
Series of A-FABP inhibitors in development
| Structure | Compound name | X group | IC50 (μM)* | PDB code | Refs | |||
|---|---|---|---|---|---|---|---|---|
| A-FABP | H-FAPB | E-FABP | I-FABP | |||||
 |
1 | – | 0.57 | <0.6 | 6.7 | >100 | 1tow | 87 |
 |
2 | – | 1.1 | 9.9 | 9.1 | 42 | – | 87 |
 |
3a | 3-Me | 1.5 | – | – | – | – | 87 |
| 3b | 6-Me | 1.3 | – | – | – | – | 87 | |
| 3c | 5-Br | 1.3 | 9.8 | 14 | 3.9 | – | 87 | |
 |
4a |  |
1 | – | – | – | 1tou | 88 |
| 4b |  |
0.6 | 17 | – | – | – | 88 | |
| 4c |  |
3.9 | >100 | – | – | – | 88 | |
| 4d |  |
2.9 | >100 | – | – | – | 88 | |
| 4e |  |
4.0 | >100 | – | – | – | 88 | |
| 4f |  |
24 | >100 | – | – | – | 88 | |
 |
5 (BMS309403) | – | <2* | 250* | 350* | – | 2nnq | 89,90 |
*
For compound 5, values are for K, (nM). A-FABP, adipocyte fatty acid-binding protein (FABP4); E-FABP, epidermal FABP (FABP5); H-FABP, heart FABP (FABP3); I-FABP, intestinal FABP (FABP2).