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. Author manuscript; available in PMC: 2020 Apr 28.
Published in final edited form as: J Med Chem. 2020 Apr 9;63(8):4315–4333. doi: 10.1021/acs.jmedchem.0c00224

Table 1.

SAR of substituents at N-1 of the imidazole ring.

graphic file with name nihms-1580926-t0002.jpg
Compound R FPA Kd(μM)* Compound R FPA Kd (μM)*
2a graphic file with name nihms-1580926-t0003.jpg 1.0 ±0.3 2i graphic file with name nihms-1580926-t0004.jpg 0.4 ±0.1
2b graphic file with name nihms-1580926-t0005.jpg 3.2 ±0.5 2j graphic file with name nihms-1580926-t0006.jpg 11 ±3
2c graphic file with name nihms-1580926-t0007.jpg 4.0 ±0.7 2k graphic file with name nihms-1580926-t0008.jpg 2.1 ±0.7
2d graphic file with name nihms-1580926-t0009.jpg 5.2 ±0.9 2l graphic file with name nihms-1580926-t0010.jpg 4.5 ±0.8
2e graphic file with name nihms-1580926-t0011.jpg 1.2 ±0.2 2m graphic file with name nihms-1580926-t0012.jpg 3.4 ±0.7
2f graphic file with name nihms-1580926-t0013.jpg 5.5 ±0.7 2n graphic file with name nihms-1580926-t0014.jpg 8 ± 2
2g graphic file with name nihms-1580926-t0015.jpg 4.0 ±0.6 2o graphic file with name nihms-1580926-t0016.jpg 38 ±3
2h graphic file with name nihms-1580926-t0017.jpg 0.4 ±0.1 2p graphic file with name nihms-1580926-t0018.jpg >40
*

Data displayed is the average of at least 3 independent replicates ± standard deviation.