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. Author manuscript; available in PMC: 2016 Jan 1.
Published in final edited form as: ChemMedChem. 2014 Sep 10;10(1):57–61. doi: 10.1002/cmdc.201402277

Table 2.

Evaluation of the right-hand phenyl group.

graphic file with name nihms637838u1.jpg
Cmpd R R1 R2 MrgX1 EC50, μMa Emax (%)a
4a Me H graphic file with name nihms637838t6.jpg 0.531 ± 0.16 238 ± 63
4b Me H graphic file with name nihms637838t7.jpg 3.06± 1.50 188 ± 7
4c Me H graphic file with name nihms637838t8.jpg 0.42 ± 0.33 130 ± 28
4d Me H graphic file with name nihms637838t9.jpg Inactive ND
4e Me H graphic file with name nihms637838t10.jpg 1.01± 0.19 180 ± 9
4f Me H graphic file with name nihms637838t11.jpg 2.34± 1.30 241 ± 25
4g Me Me graphic file with name nihms637838t12.jpg 0.50± 0.12 184 ± 14
4h Me Me graphic file with name nihms637838t13.jpg Inactive ND
4i Me Me graphic file with name nihms637838t14.jpg 0.55±0.17 149 ± 19
4j Ph H graphic file with name nihms637838t15.jpg Inactive ND
4k Ph H graphic file with name nihms637838t16.jpg Inactive ND
a

Assay was run in the presence of 10 nM of BAM8-22; n = 2, N.D.: not determined since Emax is too low.