Skip to main content
. Author manuscript; available in PMC: 2021 Mar 26.
Published in final edited form as: J Med Chem. 2020 Mar 10;63(6):2854–2876. doi: 10.1021/acs.jmedchem.9b01189

Table 5.

In vitro Activity of 4t-z

graphic file with name nihms-1577324-t0021.jpg
Compound R1 R2 R3 R4 R5 Ratio (5/50)a Fold-Signalb EC50 hPPARα (μM)c SId
4t 2-Me H H H H 0.8 1.2 1.45±0.06
4u 3-Me H H H H 1.4 1.2 0.037±0.01 >2700
4v H Me H H H 0.2 0.3
4w H H Me H H 0.8 1.7 0.90±0.08
4x H H H Me H 0.1 0.6 25.6±3.5
4y H H H H Me 0.2 1.6
4z H H H Me Me 0.2 0.8 8.52±1.83
4a (A91) 0.5 1.4 4.43 ± 0.01 >20
4b 0.8 1.3 0.77 ± 0.03 >125
GW590735 1.0 1.0 0.015±0.002
a

Ratio of relative light unit (RLU) signal at 5 μM and 50 μM compound concentrations.

b

Ratio of signal maximal signal (RLU) strength observed for the compound of interest to that obtained with GW590735.

c

EC50 values represent the mean ± SEM of atleast two separate experiments performed in triplicate.

d

EC50 (PPARγ or PPARδ) / EC50 (PPARα). Blank cells indicate compound was not selected for testing in the corresponding assay.