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Structures and binding affinities of synthesized compounds
| Compound | R1 | R2 | R3 | KD’ (μM)a |
|---|---|---|---|---|
| J01-007 | -ph-4-CH3 | -ph-3-F | -i-Bu | 2.27 |
| J01-012 | -ph-4-CH3 | -ph-3-CN | -i-Bu | 1.83 |
| J01-015 | -ph-4-CH3 | -ph-5-CH3 | -i-Bu | 2.96 |
| J02-001 | -ph | -ph-3-F | -i-Bu | 7.67 |
| J02-002 | -ph | -ph-4-F | -i-Bu | 3.49 |
| J01-017a | -ph-4-CH3 | -ph-3,4-2F-5-CH3 | -i-Bu | ____b |
KD values obtained directly by NMR titration (12).
KD could not be obtained by NMR titration due to slow exchange.
