Table 2. External validation set of nipecotic acid derivatives of hGAT1 inhibitors.
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Validation set compound # (VSC) | n | R1 | R2 | IC50 µM | −log IC50 | Predicted −log IC50 | Residual value |
VSC_1 | 1 | H | H | 0.10 | 1.00 | 0.24 | 0.75 |
VSC_2 | 1 | F | H | 0.07 | 1.12 | 0.33 | 0.78 |
VSC_3 | 1 | CH3 | CH3 | 0.20 | 0.68 | −0.06 | 0.74 |
VSC_4 | 1 | CH3 | Cl | 0.15 | 0.80 | 0.49 | 0.30 |
VSC_5 | 2 | Cl | H | 1.58 | −0.20 | 0.33 | −0.53 |
VSC_6 | 2 | F | H | 2.75 | −0.44 | 0.26 | −0.70 |
VSC_7 | 2 | CH3 | H | 1.28 | −0.11 | 0.13 | −0.24 |
VSC_8 | 2 | H | Cl | 3.38 | −0.53 | −0.04 | −0.48 |
VSC_9 | 2 | Cl | Cl | 0.93 | 0.03 | −0.19 | 0.22 |
VSC_10 | 2 | F | F | 1.99 | −0.30 | −0.38 | 0.08 |
VSC_11 | 2 | Cl | F | 0.97 | 0.01 | −0.06 | 0.07 |
VSC_12 | 2 | CH3 | Cl | 0.97 | 0.01 | 0.20 | −0.19 |
VSC_13 | 2 | CH3 | F | 1.31 | −0.12 | 0.19 | −0.31 |
VSC_14 | 2 | H | H | 3.80 | −0.58 | 0.37 | −0.95 |
VSC_15 | 2 | CH3 | CH3 | 3.46 | −0.54 | 0.40 | −0.94 |