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. Author manuscript; available in PMC: 2020 May 1.
Published in final edited form as: Pharmacol Ther. 2020 Jan 28;209:107497. doi: 10.1016/j.pharmthera.2020.107497

Table 4.

Small molecule TRPC1, C4, C5 antagonists.

Namea Structure Target Concentration or IC50 Reference
ML204 graphic file with name nihms-1563237-t0049.jpg TRPC4
TRPC5
IC50, 0.96 μM Miller et al., 2011
M084 graphic file with name nihms-1563237-t0050.jpg TRPC4
TRPC5
IC50, 10.3 μM
IC50, 8.2 μM
Zhu et al., 2015
HC-070 graphic file with name nihms-1563237-t0051.jpg TRPC4
TRPC5
TRPC4–C1
TRPC5–C1
IC50, 46 nM
IC50, 9.3 nM
Just et al., 2018
HC-608 (Pico145) graphic file with name nihms-1563237-t0052.jpg TRPC4
TRPC5
TRPC4–C1
TRPC5–C1
IC50, 32.5 nM
IC50, 6.2 nM
9 – 1,300 pM
Just et al., 2018; Rubaiy et al., 2017
AC1903 graphic file with name nihms-1563237-t0053.jpg TRPC5 IC50, 14.7 μM Zhou et al., 2017
Clemizole graphic file with name nihms-1563237-t0054.jpg TRPC4β
TRPC5
IC50, 6.4 μM
IC50, 1.0–1.3 μM
Richter et al., 2014a
GFB-887 Not disclosed TRPC5 IC50, 11 nM Mundel et al., 2019
A54 graphic file with name nihms-1563237-t0055.jpg A498 cells
TRPC1–C4
IC50, 62 nM Rubaiy et al., 2018b
[6]-shogaol graphic file with name nihms-1563237-t0056.jpg TRPC5 IC50, 18.3 μM Kim et al., 2016
Galangin graphic file with name nihms-1563237-t0057.jpg TRPC5 IC50, 0.45 μM Naylor et al., 2016
Kaempferol graphic file with name nihms-1563237-t0058.jpg TRPC5 IC50, 3.9 μM Naylor et al., 2016
Quercetin graphic file with name nihms-1563237-t0059.jpg TRPC5 IC50, 6.5 μM Naylor et al., 2016
AM12 graphic file with name nihms-1563237-t0060.jpg TRPC5
TRPC4
IC50, 0.28 μM Naylor et al., 2016
Chlorogenic acid (CGA) graphic file with name nihms-1563237-t0061.jpg Suppressed TRPC1 expression 300 μM Jung et al., 2017
Spironolactone graphic file with name nihms-1563237-t0062.jpg Suppressed TRPC1, C6 expression 3 mg/kg body weight/day (in vivo) Li et al., 2017
Topotecan (TPT), graphic file with name nihms-1563237-t0063.jpg Suppressed expression of TRPC1, C4 IC50, 1–10 nM Jiang et al., 2018
Rosiglitazone (RSG) graphic file with name nihms-1563237-t0064.jpg Reduced TRPC1 activation IC50, 10 μM Wei et al., 2017
Apigenin graphic file with name nihms-1563237-t0065.jpg TRPC5 IC50 >>10 μM Naylor et al., 2016
a

Compounds with selectivity information and likelihood of direct interaction with the channel are highlighted in bold letters and shaded rows.