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. 2017 Jan;91(1):25–38. doi: 10.1124/mol.116.105551

TABLE 1.

Summary of the compounds investigated in this study

All the ligands have an adenosine scaffold, with substitution on the ribose 4 position (R1), N6 (R2), and/or C2 (R3). Otsuka-3 is an exception, because it does not share this structural scaffold. The individual structures of each compound are shown in Supplemental Fig. 1. References for compound disclosure; 1, (Marumoto et al., 1974); 2, (Bridges et al., 1987); 3, (Åstrand et al., 2015); 4, (Sato et al., 2010). AZ proprietary compounds are marked # and their synthesis is described in Supplemental Figs. 1–6. Inline graphic

Compound number Synonym Ref. R1 R2 R3
1aa CV1808 1 H H graphic file with name mol.116.105551fx2.jpg
2bb R-PIA 2 CH2OH CH(R-Me)CH2Ph H
2cb 2 CH2OH CH2CHPh2 H
3ab NECA CONHEt H H
3ac CGS-21680 CONHEt H graphic file with name mol.116.105551fx3.jpg
3ad # CONHEt H graphic file with name mol.116.105551fx4.jpg
3cd UK-432,097 CONHEt CH2CHPh2 graphic file with name mol.116.105551fx5.jpg
3ce # CONHEt CH2CHPh2 graphic file with name mol.116.105551fx6.jpg
3cf # CONHEt CH2CHPh2 graphic file with name mol.116.105551fx7.jpg
3ag # CONHEt H graphic file with name mol.116.105551fx8.jpg
3cg 3 CONHEt CH2CHPh2 graphic file with name mol.116.105551fx9.jpg
3dg # CONHEt CH2CH(CH3)2 graphic file with name mol.116.105551fx10.jpg
3eg # CONHEt CH(CH2CH3)2 graphic file with name mol.116.105551fx11.jpg
3ah # CONHEt H graphic file with name mol.116.105551fx12.jpg
3ch 3 CONHEt CH2CHPh2 graphic file with name mol.116.105551fx13.jpg
3dh # CONHEt CH2CH(CH3)2 graphic file with name mol.116.105551fx14.jpg
3eh # CONHEt CH(CH2CH3)2 graphic file with name mol.116.105551fx15.jpg
4 Otsuka-3 4 *