Summarised EC50 and IC50 values for Pico145 1, AM237 3, and photoaffinity probes 4–7 against TRPC1/4/5 channelsa.
| Compound | TRPC5:C5 EC50 (nM) | TRPC5:C5 IC50 (nM) | TRPC4:C4 IC50 (nM) | TRPC4-C1 IC50 (nM) | TRPC5-C1 IC50 (nM) |
|---|---|---|---|---|---|
| AM237 328 | 15 | 7c | 3d | 4c | |
| Pico145-DA 4 | 13 | 40c | 1.4c | 4.9c | |
| Pico145-DAAlk 5 | 19 | 45c | 121d | 196c | |
| Pico145 123 | 1.3b | 0.35b | 0.03b | 0.2b | |
| Pico145-DA2 6 | 18b | 16c | 1.3c | 6.1c | |
| Pico145-DAAlk2 7 | 26b | 17c | 2.0c | 6.2c |
a
EA is a negative modulator of Pico145 potency, suggesting that Pico145 is a competitive inhibitor of EA.23 Therefore, lower EA concentrations used to activate TRPC1/4/5 channels may result in lower IC50 values.
b
10 nM EA was used as activator.
c
30 nM EA was used as activator.
d
100 nM EA was used as activator.