. Author manuscript; available in PMC: 2018 Jun 8.

Published in final edited form as: J Med Chem. 2017 Apr 28;60(11):4680–4692. doi: 10.1021/acs.jmedchem.7b00304

Table 2.

EC₅₀ Values (μM) for Compounds 4m–4p to TRPC3/6/7 Channels

compd	TRPC3^a	TRPC7^b	TRPC6^b	TRPC6^c
4m	0.138 ± 0.023	0.213 ± 0.036	7.79 ± 0.05	2.05 ± 0.02
4n	0.019 ± 0.002	0.090 ± 0.012	1.39 ± 0.01	0.89 ± 0.01
4o	0.450 ± 0.087	0.497 ± 0.091	4.66 ± 0.03	6.28 ± 0.02
4p	0.236 ± 0.047	0.314 ± 0.059	3.91 ± 0.02	3.24 ± 0.01

Cells were loaded with the FLIPR membrane potential (FMP) blue dye; the [Ca²⁺] in the bath was 0.5 mM.

Cells were loaded with Fluo8-AM; the [Ca²⁺] in the bath was 2 mM.

Determined based on currents at +80 mV by whole-cell patch clamp recordings using a bath solution that contained 0.1 mM Ca²⁺ and a peptide solution that contained 400 nM free Ca²⁺ buffered with BAPTA.